IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
JANUARY 2014
1

DEVELOPMENT AND VALIDATION OF UV SPETROSCOPIC METHOD FOR ESTIMATION OF METAXALONE IN BULK AND MICROEMULSION AT DIFFERENT PHYSIOLOGICAL PH

Nitesh Waman1*, Rohit Ajage1, Prakash Kendre1, Veena Kasture1

1Department of Quality Assurance Techniques, Sanjivani College of Pharmaceutical Education and Research, Kopargaon, Maharashtra

Abstract

Metaxalone, a muscle relaxant and pain reliever caused due to strain, sprains. It is considered as a strong muscle relaxant and with relatively low side effects. The UV spectroscopic method is simple, precise, accurate, rugged, robust and economic for estimation of the drug in microemulsion form. The present study explores a method to analyze Metaxalone in different solvents like 0.1N HCl (gastric fluid), phosphate buffer (pH 6.8) and phosphate buffer saline (pH 7.4) as per ICH guidelines. The objective of the study was to determine the effect of different pH on absorbance and to develop validated method for estimation of Metaxalone in different simulated body fluids since it is oral dosage form. The spectrophotometric analysis was done at λmax 270.8 nm. Calibration curve showed a linear relationship between the absorbance and concentration. The Beer’s law was obeyed in the concentration range 30-180 μg/ml for different simulated body fluids. The method was validated as per ICH guidelines, the SD and %RSD for metaxalone in 0.1N HCl, Phosphate buffer pH 6.8 and phosphate buffer pH 7.4 was 0.00339 and 0.729, 0.00254 and 0.573, 0.00304 and 0.66 respectively. The simple sensitive and cost effective UV Spectrophotometric method was developed for estimation of metaxalone at different pH. The method is also applicable for bioavailability studies.

2

PHYTOCHEMICAL, ANTIOXIDANT AND ANTIMICROBIAL EVALUATION OF ACONITUM KASHMIRICUM Stapf ex Coventry, A CRITICALLY ENDANGERED MEDICINAL HERB

Rameashkannan M.V, Riyaz A.Pala*, Mudasir. A.Mir.

Sharmila Institute of Medicinal Products Research Academy in affiliation with SIRO/DSIR/Bharathidasan University, Thanjavur-613007, Tamil Nadu, India.

Abstract

Aconitum Kashmiricum Stapf ex Coventry is a critically endangered important medicinal herb of J&K state, India. The current research was undertaken with the aim of phytochemical analysis along with antioxidant and anti-microbial evaluation of rhizomic portion of this plant species. The powdered sample was successively subjected to various solvent extractions using Soxhlets apparatus and aqueous extraction using maceration method. The extracts were subjected to phytochemical analysis using various standard procedures and anti-microbial activities were performed using agar well diffusion method, also ethanolic extract was subjected to anti-oxidant activity using DPPH method. The extracts revealed presence of various important phytoconstituents & all extracts were analyzed for In-vitro anti-microbial activities, also ethanolic extract was subjected to anti-oxidant activity. The Petroleum ether extract showed strongest anti-bacterial activity against Serratia Marcescens (MTCC-7298, SP110) with zone of inhibition as 15mm, followed by aqueous extract with zone of inhibition as 14mm while as methanolic extract showed strongest antifungal activity against Candida albicans (MTCC-1637) with zone of inhibition as 18mm followed by 13mm against Trichophyton rubrum (MTCC-7859),Gentamycin and Ketoconazole were used as  positive controls for bacterial and fungal cultures respectively. The Ethanolic extract showed less antioxidant activity as compared to Rutin having IC50 value I,e at >1000 ug/ml & 3.91 ug /ml respectively. The findings of our study indicates strong anti-microbial activities and also showed antioxidant potential of root extracts of A.Kashmiricum. In summary, the significant biological activities indicates that it could be used a source of anti-microbial agents and also as an anti-oxidant source.

3

COMPARATIVE IN-VITRO AND EX-VIVO STUDIES OF GLICLAZIDE MUCOADHESIVE TABLETS BY USING NATURAL AND SEMISYNTHETIC POLYMERS

Saravanakumar K1, Sasi Deepthi K1, Nagaveni P2, Lohita M1, Ashok Kumar CK1, Jayachandra Reddy P2, Anitha K1

1Department of Pharmaceutical Sciences, Sree Vidyanikethan College of Pharmacy, A Rangampet, Tirupati, Andhra Pradesh

517 102, India.

2Department of Pharmaceutical Sciences, Krishna Teja Pharmacy College, Renigunta Road, Tirupati, Andhra Pradesh 517520, India.

Abstract

The main objective of using oral mucoadhesive tablet is to achieve prolong stay of drug in GIT. Stability problem in intestinal fluids can be overcome through this delivery. The different compositions of Gliclazide mucoadhesive tablets were prepared (S1-S4, D1-D4) by wet granulation method using natural polymer like Momordica charantia fruit extract powder and semisynthetic polymer like sodium carboxy methyl cellulose as mucoadhesive agents. The DSC and FTIR studies revealed that there is no interaction between drug and excipients used. Among the 8 formulations, D3 has considered as best formulation for optimum release in 12 hr and also had good optimum swelling index, residence time and ex-vivo permeation through the stomach mucosa of sheep. From the obtained in-vitro dissolution profile, the drug release data were fitted into various kinetic models, which were suggested that all formulations follows first order release with Higuchi kinetics except S1 and S4 shows zero order release with Higuchi kinetics.

4

HEPATOPROTECTIVE ACTIVITY OF LEAVES OF CRATAEVA MAGNA (LOUR.) DC IN DIFFERENT TYPES OF HEPATOTOXIC RAT MODELS

Amaresh Panda1*, Seemanchala Rath2*, Debashis Pradhan1, Arpan Mahanty2, Bijan Kumar Gupta2, Nripendra Nath Bala2

1 University Department of Pharmaceutical Sciences, Utkal University, Vani Vihar, Bhubaneswar - 751 004, Odisha, India.

2 BCDA College of Pharmacy and Technology, 78 Jessore Road (south), Hridaypur, Barasat, Kolkata – 700127, West Bengal, India.

Abstract

Crataeva magna (Lour.) DC belonging to family Capparaceae is a high-value medium sized deciduous medicinal tree of tropical climate found in tropical regions of the world and also grows almost all over India, especially in the semiarid regions. The present investigation is designed to conduct phytochemical screening of Crataeva magna leaves after each successive extraction with petroleum ether, chloroform, methanol and water followed by its hepatoprotective activity study. Three different types of models used to examine the in vivo hepatoprotective activity of the above said extract were carbon tetrachloride, ethanol and paracetamol induced hepatotoxicity in rats and compared with silymarin (20 mg/kg) as reference standard. Phytochemical screening revealed the presence of carbohydrates, phenolic compounds, tannins, flavonoids, saponins and fixed oils in the aqueous extract of the Crataeva magna leaves. Two way analysis of variance study of the estimated biochemical parameters to illustrate, aspartate aminotransferase, alanine amino transferase and alkaline phosphatase were revealed that there is significant difference (p-value < 0.001) exists between the different treatment groups. Severe hepatic lesions induced by carbon tetrachloride, ethanol and paracetamol were significantly lowered after the administration of CM 200 mg/kg to the respective control groups (carbon tetrachloride > paracetamol > ethanol) which was also evident from the histopathological study of liver sections.

5

ANTI-INFLAMMATORY ACTIVITY OF Cycas beddomei Dyer. MALE CONE EXTRACTS

C. Alekhya*, N. Yasodamma, D. Chaithra

Department of Botany, Sri Venkateswara University, Tirupati- 517502.

Abstract

Cycas beddomei (Cycadaceae) is an important medicinal plant towards rheumatoid arthritis, atherosclerosis and asthma. Local herbalists of Seshachalam hill ranges used the male cones to cure rheumatoid arthritis, swellings, muscle pains, burning sensation and also increase male sexual potency (aphrodisiac). Hence scientific evaluation of the male cone aqueous, alcohol and methanol extracts were tested for their acute toxicity studies as per the OECD guidelines 428 and find that there is no toxicity up to 5000mg/kg. b.wt and further screened for anti-inflammatory activity in carrageenan induced rat hind paw oedema. The results proved that alcohol, aqueous and methanol extracts were effective at 100 mg /kg.b.w with 61.05; 53.68 and 52.89% of inhibition respectively when compared with standard drug diclofenac. Hence the herbal drug may be recommended for isolation of bioactive compounds against arthritis and the drug designing.

 

6

FORMULATION AND EVALUATION OF SWELLABLE DRUG DELIVERY SYSTEM FOR PREGABALIN

SANTOSH G. SHEP*, S.R.LAHOTI.

Department of Pharmaceutical Sciences, Bhagwant University, Sikar Road, Ajmer (Raj),India 305001

Abstract

Present investigation deals with the preparation and characterization of swellable drug delivery system (SDDS) of Pregabalin containing Psyllium Husk, HPMC K4M, Crosspovidone and Polyvinylpyrolidone, as the polymers. The SDDS tablets were prepared by wet granulation method. Nine formulations were developed which differed in the ratio of polymers. Formulations.PF-1, PF-2, PF-3, PF-4, PF-5, PF-6, PF-7, PF-8 and PF-9were composed of Psyllium Husk, HPMC K4M, Crosspovidone and Polyvinylpyrolidone respectively. All the formulations were evaluated for hardness, friability, weight variation, drug content uniformity, swelling index and in vitro drug release study. Estimation of pregabalin in the prepared SDDS was carried out by extracting drug in double distilled water and HCL by measuring the absorbance at 210 nm. In vitro drug release study was performed using United State Pharmacopoeia (USP) type 2 dissolution test apparatus employing paddle stirrer at 50 rpm using 900 ml of 0.1N HCl maintained at 37ºC ± 0.5ºC as the dissolution medium. On the basis of evaluation parameter formulation PF-5 was selected as developed formulation. Therefore, it can be concluded that the SDDS may be exploited successfully for the delivery of drugs such as pregabalin.

7

ANALGESIC EFFECT OF THE METHANOL ROOT EXTRACT OF HOLARRHENA FLORIBUNDA IN ALBINO MICE

Udoh A.E1., Nwafor P.A1., Udobre A.S2.

1Department of Pharmacology and Toxicology, Faculty of Pharmacy, University of  Uyo, Nigeria.

2Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmacy, University of  Uyo, Nigeria. 

Abstract

The Analgesic effect of the methanol root extract of Holarrhena floribunda in mice was investigated. Thermally-induced pains, Acetic acid induced writhing and Formalin-induced hind paw licking in mice were evaluated. The phytochemical analysis showed that the extract contained alkaloids, tannins, saponins, flavonoids, steroids and cardiac glycosides. The LD50 of the methanol extract was 367.42mg/kg. The extract produced analgesic effect in the three models evaluated. The extract decreased the latency responses in the thermally-induced pain significantly (p<0.001- 0.01) relative to control. The extract also decreased the abdominal constriction and hind paw stretching in the Acetic acid writhing test significantly ( p<0.001- 0.05) relative to control. The hind paw licking also decreased significantly (p<0.001- 0.05) in the Formalin test relative to control. The bioactive constituents may be responsible for the analgesic property.

8

A SIMPLE METHOD FOR DETERMINATION OF GLICLAZIDE IN SERUM BY HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY

Abedulla Khan K*1, Satyanarayana S2 and Eswar Kumar K3

1Sultan-ul-uloom College of pharmacy, Banjara hills, Hyderabad-34, A.P.

2Avanti Institute of Pharmaceutical Sciences, cherukapally (V), Vizianagaram (Dt), A.P.

3A.U. College of Pharmaceutical Sciences, Andhra University, Visakhapatnam, A.P.

Abstract

A simple, rapid, uncomplicated and specific method for determination of gliclazide in serum by high performance liquid chromatography. This method enables the determination of gliclazide even at ng/ml concentrations in serum. A simple method employs thermo column (100mm length X 4.6 mm diameter), Phosphate buffer and acetonitrile (50:50) adjust to pH 2.5 with orthophosphoric acid as mobile phase and the elute was monitored at 229 nm wavelength UV detector. Acetonitrile was added to precipitate proteins and extract gliclazide. The limit of quantitation (LOQ) for gliclazide in serum was 50 ng/ml at 229nm. The method was linear over the range of 50 ng/ml - 1µg/ml with r2 of 0.998. Mean recovery for gliclazide was 99.48%.The retention time was 5.419 mints. This method was found to be precise, accurate and suitable for pharmacokinetic study of orally administered gliclazide.

9

APPLICATION OF BIORELEVANT DISSOLUTION TESTS TO THE PREDICTION OF IN VIVO PERFORMANCE OF CLOPIDOGREL EXTENDED RELEASE MINI TABLET FILLED IN CAPSULES

RAJA SUBBURAYALU1,  Dr. JANAKIRAMAN KUNCHITHAPATHAM1, DEVI.T2

1Department of Pharmacy, Annamalai University, Annamalai Nagar, Chidambaram, Tamil Nadu, India.

2Jaya college of Pharmacy, Thirunindravur, Chennai, Tamil Nadu, India.

Abstract

The main objective of the present study is to enable the prediction of in vivo performance of clopidogrel extended release mini-tablets in capsule by simulated In vitro bio relevant dissolution testing method. The optimized formulation evaluated for dissolution at different agitation speed  shown, no significant difference in dissolution profile and the F2 value observed was 96 & 88 at  75 RPM & 125RRPM respectively in comparison to 100RPM. The formulation evaluated for dissolution under simulated pre-prandial condition and post-prandial conditions using USP dissolution apparatus -3, resulted the extent of dissolution of  82.3% and 91.5% respectively at 12 hours. A pharmacokinetic study conducted with clopidogrel extended release mini tablets, on rabbits under pre-prandial condition was deconvulted to fraction of drug absorbed, and compared for IVIV–level A correlation. The result reveals good correlations between in-vitro drug release and in-vivo drug absorption in pre-prandial state, and the F2 value observed was 73. 

10

ANTIDIARRHOEAL ACTIVITY OF Pterolobium hexapetalum (Roth.) Sant. and Wagh. LEAF AND FRUIT EXTRACTS ON CASTOR OIL INDUCED DIARRHOEA

B. Kavitha, N.Yasodamma, C. Alekhya

Department of Botany, S.V.University, Tirupati-517201

Abstract

The herbal drug Pterolobium hexapetalum leaf and fruit paste is used in the treatment of diarrhoea by the Chenchu tribes of Nallamalai Hills. Hence aqueous and methanol leaf and fruit extracts at 50 and 100 mg/kg b.wt were tested on castor oil induced diarrhoeal wistar albino rats and the intestinal fluid content was compared with the standard drug Atropine at 3mg/kg b.wt. Leaf methanol extracts at 100 mg/kg b.wt showed 6.4 dry and 2.4 wet defecations after 4 hours of Castor oil induced diarrhoea with 60% of diarrhoeal inhibition, whereas with fruit aqueous extracts 6.4 wet and 1.8 dry defecation with 70% of inhibition to that of the standard as 6.4 and 2.4 dry and wet defecations with 60% of diarrhoeal inhibition. Enteropooling activity also very effectively reduced with fruit aqueous extracts as 1.40 ml and 60.45% of inhibition than 1.64ml and 53.67% with leaf methanol extracts to that of the standard with 1.68ml and 52.54% of intestinal fluid inhibition. Hence the leaf and fruit extracts are proved the herbal use against diarrhoeal activity and it is recommended as antidiarrhoeal drug further to isolate the bioactive compound and drug designing. 

11

A SURVEY ON PERCEPTION OF COMPLICATIONS AMONG PREGNANT WOMEN

M.Santhosh Aruna*, Sk. Shafiya Begum*, J.Lakshmi Prasanna, M.Surya Prabha, N.Rama Rao

Chalapathi Institute of Pharmaceutical Sciences Lam, Guntur.

Abstract

Back ground: Giving birth to an off-spring is the most beautiful experience for a woman. Yet in most of the world, pregnancy and childbirth is a tough journey. Every pregnant woman faces the risk of sudden, unpredictable complications that could end in death or injury to herself or to her infant. Aim: To determine the awareness of pregnancy related complications among pregnant women in Govt. Hospital in Narasaraopet, Guntur, SouthIndia. Method: A prospective, observational, cross sectional study was conducted by collecting the data in a structured questionnaire and also by interviewing the patients for a period of 4 months. Results:  Only 46% were having knowledge about the high risk pregnancy. Anemia was seen in 68% of the selected subjects. Swelling over feet was noted in one fourth of respondents and blood pressure of more than 140/90mmHg was seen in 36% of the subjects. Conclusion: Lack of awareness about obstetric danger signs was related to low level of education about the danger signs of pregnancy.

12

SYNTHESIS, CHARACTERIZATION AND DETERMINATION OF PROCESS-RELATED IMPURITY IN DARUNAVIR HYDRATE BULK AND FORMULATION

Vaishali Shinde1, Seema Gosavi1, Deepak Musmade1, Sarita Pawar1, Veena Kasture1*

1SRES’s, Sanjivani College of Pharmaceutical Education and Research – Kopargaon Dist –Ahmednagar- 423603, India

Abstract

The plethora subscribed in this research is directed towards the development and validation of RP-HPLC method for the estimation of process related impurities from bulk and formulation. The study of impurity profile of a drug is the thrust area of research in pharmaceutical industry. It is useful in identifying the impurities of drug and thus providing scope for a better product with higher purity and better quality. It can be predicted that the intermediate(s) formed during synthesis, can act as an impurity by accompanying the desired final synthesized drug or drug product, thereby creating hazardous health and safety issues. Thus impurity profiling can act as quality control tool. The process related impurity of darunavir was synthesized, purified and characterized by UV, IR, NMR, and GC - MS spectrometry.  The HPLC method was developed for quantification of synthesized impurity.  The method was validated according to ICH guidelines with respect to linearity, accuracy, precision and specificity. Based on HPLC data of the Darunavir sample after spiking with the impurity we conclude that impurity is present in Darunavir. Finally 4-amino-N-(2-methyl propyl) benzene sulphonamide (impurity) was quantified from bulk Darunavir hydrate and its marketed tablet formulation. The amount of impurity in tablet and bulk was found to be 0.46 % and 0.98% respectively. 

13

DISCOVERY OF PHARMACOGNOSTICAL CHARACTERS FROM ROOTS OF STEREOSPERMUM COLAIS BUCH.

Rashid Akhtar 1*, Mohib Khan2

1Department of Pharmaceutical Sciences, JJT University, (Rajasthan) India.

2Oriental college of Pharmacy, Sanpada, New Mumbai, (M.S.) India.

Abstract

The objective of present studies deals with the macroscopically and microscopically studies of roots of Stereospermum colais. Some distinct and different characters were observed with section of young thin roots. Physiochemical parameters of the roots powder were also carried out. The present study on Pharmacognostical investigation of Stereospermum colais. roots might be useful to supplement information in regard to its identification parameters assumed significantly in the way of acceptability of herbal drugs in present scenario lacking regulatory laws to control quality of herbal drugs. Result: Discovery of Pharmacognostical characters of root of stereospermum colais revealed presence of various identifying characters which may act as identification standards for pharmacognocist, botanist and other related authorities of medicinal and aromatic plants. The important characters which have been revealed from the root  showed a cork consisting of 15 to 20 rows of lignified  cubical cells; secondary cortex narrow consisting of 2 to 5 rows of thin-walled parenchymatous cells with cortical fibers and occasional stone cells etc.

14

NEW VISIBLE SPECTROPHOTOMETRIC METHODS FOR THE DETERMINATION OF ATENOLOL IN PURE AND DOSAGE FORMS VIA COMPLEX FORMATION

Kumble Divya and  Badiadka Narayana*

Department of Post Graduate Studies and Research in Chemistry, Mangalore University, Mangalagangothri 574199, India.

Abstract

Simple, new and direct visible spectrophotometric methods are developed for the determination of atenolol (ATN) in pure form and in pharmaceutical formulations. The methods are based on the formation of a colored complex between the drug and metal ions like Fe(III) chloride  and Cr(III) sulphate.  The maximum absorption wavelength is 454 nm for Fe(III)-ATN complex and 594 nm for Cr(III)-ATN complex. The conditions for complex formation are studied and optimized to obtain highest absorbance. Statistical comparison of the results is performed with regard to accuracy and precision using student’s t-test at 95% confidence level. Thus developed methods are successfully applied for the analysis of ATN in pure form and in commercial tablets.

15

TASTE MASKING: OVERVIEW OF TASTE ASSESSMENT APPROACHES IN THE DEVELOPMENT OF ORAL PHARMACEUTICAL FORMULATIONS

Malode Sarika S, Gudsoorkar Vilas R

Department of Pharmaceutics, MVP Samaj’s College of Pharmacy, Gangapur Road, Nashik, Maharashtra, India.

Abstract

Taste has an important role in the development of oral pharmaceutical formulation, with respect to patient compliance. Hence, pharmaceutical companies invest time, money and resources in developing palatable and pleasant tasting products and adopt various taste masking techniques to develop an appropriate formulation. Taste assessment is one of the important quality-control parameter for evaluating taste-masked formulations. To date, several innovative in vivo approaches, in vitro drug release studies utilizing taste sensors, specially designed apparatus and drug release by modified pharmacopoeial methods have been reported in the literature for assessing the taste of drugs or drug products. The most widely used method is psychophysical evaluation by a human taste panel. It may be suitable for product development, but not typically acceptable for product quality control.  In vitro methods, direct or indirect, must be developed at some point to support commercial production. More recently, Biomimetic taste sensing systems (BMTSSs) with combined use of multivariate data analysis (MVDA) has been demonstrated to be a powerful tool in taste measurement technology. BMTSSs have been marketed as taste sensors, or electronic tongues or e-tongues. An e-tongue, was first proposed and patented by Toko’s group in 1989, and subsequently abundant research has been performed on the application of e-tongues to the valuation of taste and quality of foods or medicines. The taste-sensing systems SA401 and SA402B, the Alpha MOS electronic tongue Astree2 and the Insent taste sensing system TS-5000Z have been developed for high-throughput taste screening and quality control. These instruments employ electrochemical sensors coupled with chemometric methodologies to perform qualitative and quantitative analyses of organoleptic and chemical properties of substances and products. The instrument, however, is very heavy and expensive. Some research groups have proposed portable-type, miniaturized or disposable taste sensor systems. However, practical implementations of these types of taste sensor, which might address the limitations of conventional laboratory analyses, have not yet been reported. BMTSSs have been shown to be globally selective for detecting and quantifying specific classes of chemical compounds. As we discuss here, the latest trends in the taste assessment of pharmaceuticals will result in a decreased reliance on human panel tests.

16

ANTIULCER ACTIVITY OF Pterolobium hexapetalum (Roth.) Sant. and Wagh. LEAF AND FRUIT EXTRACTS ON PYLORIC LIGATED RATS

              B. Kavitha*, N. Yasodamma, D. Chaithra

              Department of Botany, Sri Venkateswara University, Tirupati – 517501.

Abstract

Pterolobium hexapetalum (Roth.) Sant. and Wagh. (Caesalpiniaceae) is a gregarious straggling spiny shrub distributed along the dry deciduous forests of Andhra Pradesh. The plant parts are having a wide range of herbal uses by the Chenchu tribes of Nallamalai forests. Phytochemical screening, antibacterial and antifungal activities of P.hexapetalum proved its efficacy in controlling the human pathogenic bacteria and fungi. Traditional uses against ulcerous activity showed interest for the biological assaying in Wistar Albino rats to prove its effectiveness. Results revealed in the decrease of the gastric fluid content at 100 mg/kg b.wt of fruit aqueous and leaf methanol extracts to that of the standard drug Omeprazole with the ulcer protection 80.38; 81.33 and 82.45% respectively. And also maintain in the PH of gastric juices and acidity values in the pyloric ligated ulcer rats equally to that of the standard drug. Hence aqueous fruit extracts and methanol leaf extracts has to be subjected for the isolation of respective bioactive compounds against the ulcerous activity and also recommended for the drug designing in future studies.

17

MUR-A: A CRITICAL TARGET BEHIND NEW ANTIBACTERIAL DRUG DISCOVERY

Deepak S. Musmade*, Patil Poonam P., Aher Sunil J. and Ware Agasti L.

Dept. of Pharmaceutical chemistry, SRES’s Sanjivani College of Pharmaceutical Education and Research, Kopargaon, MS, India-423603.

Abstract

The bacterial cell wall represents an attractive target site for antibiotic research as it is a fundamental structure for bacterial survival.  The enzyme MurA (UDP-Nacetylglucosamine enolpyruvyl transferase, accomplishes an initial step in the cytoplasmic biosynthesis of peptidoglycan precursor molecules. It catalyzes the transfer reaction of phosphoenolypyruvate (PEP) to the 3‘hydroxyl group of UDP-N-acetyl glucosamine (UNAG) generating enolpyruvyl-UDPN-acetyl glucosamine (EP-UNAG) and inorganic phosphate. The broad-spectrum antibiotic fosfomycin – to date still the only known MurA inhibitor with clinical relevance - acts as an analogue of the substrate PEP by irreversible alkylation of the Cys115 thiol group .The MurA-dependent metabolites are of vital importance for bacteria, and the enzyme is  therefore in the focus of anti bacterial drug discovery.

18

SYNTHESIS, CHARACTERIZATION AND DEVELOPMENT OF VALIDATED RP-HPLC METHOD FOR THE ESTIMATION OF PROCESS-RELATED IMPURITIES INNICARDIPINE FORMULATION

Veena S. Kasture*1, Sarita S. Pawar 2 , Deepak S. Musmade 2, Poonam P. Patil 2 and Swapnil R. Gaware 1

1Department of Quality Assurance Techniques, S.R.E.S.’s, Sanjivani College of Pharmaceutical Education andResearch,Kopargaon, MS, India- 423603.

2Department of Pharmaceutical chemistry, S.R.E.S.’s,  Sanjivani College of Pharmaceutical Education and Research, Kopargaon, MS, India- 423603.

Abstract

The plethora subscribed in this research is directed towards the synthesis and characterization of Some possible intermediates of nicardipine which can be further evaluated as an impurity in nicardipine bulk as well as dosage form. The synthesis of diethyl, 1, 4-dihyro-2, 6- dimethylpyridine-3,5-dicarboxylate and diethyl, 1, 4-dihyro-2, 6-dimethyl-4-(3-nitrophenyl)  pyridine-3, 5-dicarboxylate as an intermediates and the attempt has been made in view of identification, characterization, development and validation of an analytical method for the  estimation of these intermediates as probable impurities in the bulk and formulation in   nicardipine.

19

EFFECTS OF ROSA DAMASCENA MILL FLOWERS, CICHORIUM INTYBUS LINN ROOTS AND THEIR MIXTURES ON SERUM ELECTROLYTES AND HEMATOLOGICAL PARAMETERS AGAINST GENTAMICIN INDUCED TOXICITY IN ALBINO RABBITS

Faiza Mumtaz¹, Tanweer Khaliq¹, Zia-ur-Rahman¹, Ijaz Javed¹, Arslan Iftikhar¹, Bilal Aslam¹, Asghar Ali¹, Zubair Ahmad²

¹ Department of Physiology and Pharmacology, University of Agriculture, Faisalabad, Pakistan.

² Department of Bioinformatics and Biotechnology, Government College University, Faisalabad, Pakistan.

Abstract

The herbal plants can be used alone or in combination with other plants to treat different ailments and are relatively safer, less expensive and have fewer side effects. Gentamicin (GM) induced tubular damage, vascular and glomerular dysfunction and altered tubular reabsorption leads to hematological and electrolyte disturbances. The effects of aqueous extracts of Rosa damascena (250mg/kg and 500mg/kg), Cichorium intybus (250mg/kg and 500mg/kg) and their mixture (250mg/kg and 500mg/kg) on serum electrolytes and hematological parameters was evaluated against gentamicin (80mg/kg) induced toxicity in albino rabbits by using the standard drug silymarin (200mg/kg). The study period was from 0-21 days and blood samples were collected at 0, 7th, 14th and 21st day. Analysis was done by using the standard protocols and results were subjected to two way analysis of variance and duncan multiple range test as applicable. Statistically significant (p≤0.01) increase in levels of potassium, erythrocytes count (RBC), hemoglobin (Hb), hematocrit (Hct) and platelet count and statistically significant (p≤0.01) decrease in levels of sodium, chloride, total leukocyte count (TLC) and erythrocyte sedimentation rate (ESR) was accessed for both plants and their mixture in dose dependent manner as compared to control groups. In conclusion, the overall results of study suggest that mixture of extracts of R. damascena flowers and C. intybus roots better improves the level of serum electrolytes and hematological derangements associated with the toxicity by repeated dose of gentamicin than the extract of individual plant in dose dependent manner.

20

FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF ZIDOVUDINE

Pamu. Sandhya*1, 2, Md. Afreen1, Afreen Jahan1, Aliya Sultana Sadia1

1Department of Pharmaceutics, Shadan Women’s College of Pharmacy, Khairatabad, Hyderabad, 500 004, India

2University College of Technology, Osmania University, Hyderabad, 500 007, India

Abstract

In the present investigation, an attempt was made to formulate the oral sustained release matrix tablets of zidovudine in order to improve efficacy, reduce the frequency of administration, and better patient compliance.  Tablets were prepared by direct compression method using various hydrophilic polymers viz; HPMC E15LV and HPMC E50LV alone or in combination with hydrophobic polymer like ethyl cellulose. The formulated granules showed satisfactory flow properties. All the tablets formulation showed acceptable pharmaco technical properties and complied with pharmacopoeial standards. The in-vitro release profiles from tablets of drug anddifferent polymer ratio were applied on various kinetic models. Based on t90% values the formulation F4 was found to show good initial release (12% in 2 hrs) and may extend the release (90% in 12 hrs) and can overcome the disadvantages of conventional tablets of Zidovudine. The n value obtained from korsmeyer – peppas model confirmed that the drug release was non- fickian diffusion mechanism. The drug release from the tablets was sufficiently sustained and anomalous diffusion mechanism of the drug from tablets was confirmed. Based on the in- vitro drug release data the formulation F4 was concluded as best formulation.

21

FORMULATION AND DEVELOPMENT OF TASTE MASKED ORALLY DISINTEGRATING TABLETS (ODTS) OF CEFPODOXIME PROXETIL USING ION EXCHANGE RESINS

Raichur Vinay*, Khanum Aisha, Pandit Vinay, Patel Mithil, Rahman Abdul

Dept. of Pharmaceutics, Al-Ameen College of Pharmacy, Bangalore, India.

 Abstract

Urinary and respiratory tract infections are common incidences in children for which Cefpodoxime proxetil is a choice of drug .However the bitter taste of the drug limits its use, due to which conventional oral formulations suffer the drawback of rejection by pediatric population. Hence to improve patient compliance, Orally Disintegrating Tablet (ODT) containing taste masked cefpodoxime was formulated. The first step of taste masking was achieved by complexation of the drug with various ion exchange resins like Kyron T-104, T-114, T-134 and T-154. After optimization of process and formulation parameters, the final complex was evaluated for in-vitro drug release, swelling studies DSC, XRD, NMR studies and was selected to be formulated into ODT. The concentrations of the tabletting excipients were optimized by 32 full factorial design. The formulation with Kyron T-314 at concentration of 5% and diluent blend of Pharmaburst: MCC in the ratio of 1:2 was selected as optimum with a disintegration time of 11 seconds which was a major outcome in designing elegant ODTs with a rapid disintegrating nature. The SEM of the tablet cross section showed presence of hollow spaces. The negligible release of drug in salivary pH helped to conclude that ion exchange is an effective approach of taste masking. Optimized formulations were found to be stable after 3 months accelerated stability studies. 

22

EVALUATION OF ANTIUROLITHIATIC ACTIVITY OF Cuminum cyminum IN ETHYLENE INDUCED UROLITHIASIS RATS

1Purnachandar. M, 2Saritha. Ch,2Shankaraiah. P*

1SRR Collge of Phamraceutical Sciences, Valbhapur, Elkathurthy, Karimnagar, A.P., India.

2Chaitanya College of Pharmacy Education and Research,Kishanpura,  Hanamkonda, Kakatiya University,Warangal -506 001, A.P, India.

Abstract

The fruit of Cuminum cyminum Linn (Apiaceae) used in traditional medicine for the treatment of urinary stones. The present study was undertaken to evaluate the antiurolithatic effects of the methanolic extract of the fruit of C. cyminum on ethylene glycol (EG) induced urolithiatic rats. EG administration resulted in hypercalciurea as well as increased renal excretion of phosphate and development of Kidney stones. Treatment with methanolic extracts of C. cyminum fruit significantly reduced the elevated urinary calcium and phosphate and the increased deposition of stone forming constituents in the kidneys by ethylene glycol, was also significantly lowered by curative and preventive treatment groups by using methanolic extracts of the fruits of C. cyminum.  Conclusions were made that results indicates the fruit of C. cyminum is antiurolithiatic activity and scientifically valid and traditional use in the treatment of urinary calculi.

23

ISONIAZID INDUCED PSYCHOSIS: A CASE REPORT

Shazia Yousuf*, Sana fatima, Faiq unnisa, syeda Sanober ghazaal, Azhar uddin sultan, Ayesha kouser,    

Deccan school of pharmacy (DSOP), JNTUH, Hyderabad-500024, Andhra Pradesh, INDIA.

Abstract

Isonicotinic acid hydrazide (INH) or otherwise called Isoniazid is one of the primary drugs used in the treatment of Mycobacterium tuberculosis infection. The common side effects of INH are peripheral neuropathy, hepatitis, and rash. Rarely, psychosis, convulsions, and even death have been reported on conventional doses of this drug. We present a case of patient in whom a 3 months of anti-Tubercular therapy with appropriate dose of INH, evolved to Psychosis. Isoniazid (INH) is included in all drug regimens used for the treatment of tuberculosis because of its potency, safety and low cost. We reported a case of 36 year-old female patient who developed psychotic symptoms on later phase of her treatment for tuberculosis. She was prescribed short-course antituberculous treatment as per WHO guidelines, with an initial 2 months of rifampicin, isoniazid, ethambutol, and pyrazinamide followed by 4 months of rifampicin and isoniazid. Patient on INH/Rifampin -300mg/450mg capsule, approached with complaints of twitching of cheeks and eyelids, restlessness, Agitation and sleep deprivation.. The symptoms resolved within 6 days of discontinuing the isoniazid and use of antipsychotics and suitable sedatives. Patient had a history of seizures few months back and was hospitalized for 3 days. Physicians should be aware of the potential for INH toxicity and should assess their patient’s current mental and psychosocial status when prescribing it. Rare incidence of this adverse effect of INH prompted us to publish it as for the awareness of INH poisoning may prevent severe morbidity and mortality.

24

AN EFFICIENT SYNTHESIS OF ISOXAZOLO[3,4-D]PYRIMIDINE-4,6-DIONE DERIVATIVES AND THEIR ANTIMICROBIAL ACTIVITY

Shrikant V. Hese, Rahul D. Kamble, Pratima P. Mogle, Ashok P. Acharya, Milind V. Gaikwad, Shiddhodan N. Kadam,  Bhaskar S. Dawane*

School of Chemical Sciences, Swami Ramanand Teerth Marathawada University, Nanded (MS). India-431606.

Abstract

An efficient single step, environmentally benign synthesis of new series of isoxazolo[3,4-d]pyrimidine-4,6-dione derivatives were synthesized by the reaction of α, β-unsaturated ketones with hydroxyl amines hydrochlorides in presence of catalytic amount of bleaching earth clay pH 12.5 using polyethylene glycol 400 (PEG-400), the advantage of the present methodology are mild reaction condition and  excellent yield. The synthesized derivatives were evaluated for their antimicrobial activity. The results of antimicrobial screening reveal that most of the synthesized isoxazole analogues can be considered as a scaffold for the development of novel and effective antibacterial and antifungal agents.

25

PHARMACOLOGICAL INVESTIGATIONS OF ECLIPTA ALBA EXTRACT FRACTIONS (WHOLE PLANT)

Taj Ur Rahman1*, GhiasUddin2 Wajiha Liaqat2, M. Iqbal Choudhary3, Abdul Wadood4, Ghulam Mohammad5 and Ayaz Ahmed6

1Department of chemistry, Abdul Wali khan, University, Mardan, KPK, Mardan, Pakistan.

2Institute of Chemical Sciences University of   Peshawar, Peshawar 25120, Pakistan.

3H.E.J. Research Institutes of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi -

 75270, Pakistan.

4Department of Biochemistry, Abdul Wali khan, University, Mardan, KPK, Mardan, Pakistan.

5Veternary health officer, Incharge civil veterinary hospital Hayaseri, Dir (L) KPK, Pakistan.

6Department of Biotechnology, Abdul Wali khan, University, Mardan, KPK, Mardan, Pakistan.

 

Abstract

In the current study the various fractions of extract of medicinal plant Eclipta alba was subjected to pharmacological investigation. The results obtained showed that all the fractions displayed no antibacterial activity against all bacterial strains used for antibacterial activity. These fractions showed no bioactivity against selected fungal strains except water fraction (F4) and residue fraction (F5) which exhibited 35 % activities against M.cannies. In case of insecticidal activity all the tested fractions shows no activity against the insects Castaneum, Rhyzopertha dominica and Callosbruchuanalis, except residue fraction (F5) which revealed 20 % activity against each insect and 20 % against Rhyzopertha dominica. On the other hand in case of phytotoxicity, n-Hexane fraction (F1), Ethyl acetate fraction (F2) Chloroform fraction (F3) water fraction (F4) Residue fraction (F5) showed good phytotoxicity activity at 1000 μg/ml concentration and moderate to low activity at 100 μg/ml concentration. However, the n-Hexane fraction showed moderate activity at 10 μg/ml and the rest of the fraction showed low activities at 10 μg/ml respectively. From the results above it is clear that this plant has significant potential of phytotoxicity activities, which in turn supports the conclusion that extensive research should be conducted on the basis of biological activity (Phytotoxicity) to explore its phytochemicals

26

A REVIEW ON NOVEL APPROACHS IN GASTRORETENTIVE MICROSPHERES

Muttepawar Supriya S.1, Jadhav S.B.1, Kankudate A.D.2, Kadam V.S.1, Motarwar S.S.1,Bharkad V.B.1

1Department of Pharmaceutics, Indira college of pharmacy, Vishnupuri, Nanded, Maharashtra, India

2Department of Pharmaceutics, School of Pharmacy, S.R.T.M.U. Nanded, Maharashtra, India

Abstract

Gastroretentive drug delivery system offers several advantages besides providing better bioavailability to poorly absorbed drugs and a required release profile thus attracting interest of pharmaceutical formulation scientists. Different approaches for Gastroretentive dosage form include floating system, Mucoadhesion or bioadhesion, sedimentation or high density, expansion, modified shape systems etc. These systems are useful to overcome the several problems encountered during the development of a pharmaceutical dosage forms. Microsphere should be primarily aimed to achieving more predictable and increased bioavailability of drugs. Prolonged gastric retention improves bioavailability, reduces drug waste, useful for drugs acting locally in the GIT, drugs which are poorly soluble and unstable in intestinal fluids and also  microspheric drug delivery system has gained enormous attention due to its wide range of application as it covers targeting the drug to particular site to imaging and helping the diagnostic features. The purpose of this review is to focus on the recent advances in the field of formulation, characterization, evaluation and applications of Gastroretentive dosage forms. The review also highlights briefly about the floating microspheres, polymeric microspheres which provide a variety of application in life sciences, mucoadhesive microspheres which is one of the most useful drug delivery system with its various advantages, magnetic microspheres which provide drug disease site durg release and different types of radioactive microspheres.

27

ANTIBACTERIAL ACTIVITY AND GC-MS ANALYSIS OF METHANOLIC EXTRACT FROM STEM BARK AND LEAVES OF MITRAGYNA PARVIFOLIA (ROXB.) KORTH

Pashupat Vasmatkar1*, Ashutosh Dubey1, Bhawna Tyagi1, Pratibha Baral1, Shishir Tandon2, Amar Kadam3

1Department of Biochemistry,

2Department of Chemistry, College of Basic Sciences and Humanities, G. B. Pant University of Agriculture and Technology, Uttarakhand, India.

3Centre for plant Biotechnology and molecular Biology, College of Horticulture, Kerala Agriculture University, Kerala, India.

Mitragyna parvifolia is important medicinal tree belongs to family Rubiaceae. It is traditionally mainly known for its antimicrobial and anti-inflamatory properties. The antibacterial activity with its Minimum Inhibitory Concentration (MIC) were determined by disk diffusion testing against Escherichia coli, Pseudomonas aeruginosa and Bacillus subtilis, the investigation was also carried out to determine the possible bioactive components of leaf and bark methanolic extract using Gas Chromatograph and mass spectrometer (GCMS). The highest antibacterial potential demonstrated against E. coli with 31±1.4 mm and 31.5±2.12 mm zone of inhibition by leaves and bark extract respectively and interestingly which is found to be more than Chloramphenicol. The MIC for both extracts was 12 mg/ml for the same bacterial strain. The lowest MIC of both extract was seen against B. subtilis. The major compounds identified in the extracts of leaf and bark of were isobutanoic acid, 2-ethylhexyl ester (19.36%), 4 methyl mannose (53.13%), mitraphylline (21.59%), isomitraphylline (3.37%) and 1, 2 Hydrazine dicarboxylic acid, diethyl ester (3.50%), α, α-dimethyl mucconic acid (22.97%), isobutanoic acid, 2-ethylhexyl ester (43.83%), α-D-glucopyranoside, α-D-glucopyranosyl (27.21%) respectively. Among these compounds found in the leaf of M. parvifolia, a pentacyclic oxindole alkaloid mitraphylline is known for its anti-inflammatory, antiproliferative activities. Our investigation conducted on different parts of this plant validate the traditional usage of this plant as antimicrobial and several compounds identified by GC-MS analysis are principal factors for significant antibacterial activities.

28

ESTIMATION OF DAPSONE IN BULK & DOSAGE FORM BY UV SPECTROSCOPIC METHOD

Anjan De1*, Suddhasattya Dey1, Prasanna Kumar Pradhan2, Falguni Chaudhari2, Madhavi Patel2

1Dr. B.C. Roy College of Pharmacy And Allied Health Sciences, Bidhan Nagar, Durgapur-713 206, India.

2Sigma Institute of Pharmacy,  Bakrol, Vadodara-390 019, Gujarat, India.

Abstract

The present study describes development and validation of UV-spectrophotometric method for estimation of Dapsone in bulk & dosage form. During development of analytical method water, phosphate buffer, methanol were tried but drug was found to be soluble in 60% methanol. Standard stock solution was prepared in methanol: water (60:40).  λ max was found to be 293nm &310nm for zero order &first order. Calibration curves were prepared. The proposed method obeys Beer’s law in the range of 2-6μg/ml. Absorption maxima was determined with 4μg/ml by scanning in the range of 200-400nm. % Recovery studies were in the range of 98.88%-100.25% &101.13%-102.75% for zero order & first order respectively. The method was validated in terms of Linearity, Precision,  Accuracy, Annova & F-test. Results of analysis were validated statistically and by recovery studies. From that it was observed that there was no interference of impurities or excipients during the estimation of drug in formulation. Further, this method utilizes no additional chemical reagent for development of any coloring species with dapsone as observed in some studies in literature and hence this method is very accurate, simple & less time consuming. This shows the adaptability of the method for routine estimation of dapsone in bulk & dosage form. This study thus exploits the possibility for determining Pharmacokinetic profiles of dapsone in rat plasma which may be required in clinical study in near future.

29

FORMUALATION AND EVALUATION OF DICLOFENAC DIETHYLAMINE GELS PREPARED USING HYALURONIC ACID: INFLUENCE OF VARIOUS PERMEATION ENHANCERS ON RAT SKIN PENETRATION

Bhargavi Chinta1, Satyadev TNVSS2, Tata Santosh3, Madhavi Nannapaneni*

1Lecturer Dept of Chemistry, Andhra Loyola College , Vijayawada, A.P, India

2Lecturer, PG Centre, P.B.Siddhartha College of Arts and Science,Vijayawada, A.P.

3Corpuscle Research Solutions, Visakhapatnam, A.P.

Abstract

Hyaluronic acid is a polymer of disaccharide, themselves composed of D-Glucuronic acid and D-N- acetyl D-glucosamine, linked via alternating β-1,4 and β-1,3 glycosidic bonds. In the Present work an attempt is made to prepare HA gels containing Diclofenacdiethylamine, the gels prepared are subjected to extensive rheological evaluation, drug content estimation, pH measurement, stability study and drug release study across hairless albino skin rat. The influence of various permeation enhancers on rat skin permeation are also studied. The major outcomes of the research are as follows. Gels prepared using HA revealed a pH of 6.45.Since HA is a component of the human skin no hypersensitivity reactions can be expected when used as a carrier in preparation of topical gels. Rheological evaluation studies indicated that there is no significant change in the viscosity of the formulation. The prepared HA gels had a greater initial rate of permeation as compared with the marketed formulations. From the results of the experiment we can expect a superior onset of therapeutic action as compared with the marketed formulation. Since HA is an endogenous component involved in cellular signaling, wound repair, morphogenesis and matrix organization these gels do not cause skin irritation and hypersensitive reactions. The rate of skin permeation of the drug increased with increasing concentration of the permeation enhancer (PEGs) until a certain threshold value. At very high concentrations of the permeation enhancer, the rate of permeation has decreased suggesting intramolecular attraction of the PEGs thus limiting the rate of permeation.

30

INDIA –VICTIM OF BIO-PIRACY

Madhu Verma1, Iti Chauhan1, Raj Kumari2, Meenakshi Sharma2

1 Department of Pharmaceutics, ITS Paramedical (Pharmacy) College,UPTU,India.

2Department of Pharmacognosy, ITS Paramedical (Pharmacy) College,UPTU,India.

Abstract

Since the last two decades multinational corporations are profiting by patenting the indigenous knowledge and resources of Indian hotspots and associated communities. Bio-piracy is hampering the livelihoods of communities and farmers who have invested their time, care, hard work and knowledge in restoring their heritage. An account of  various medicinal plants like turmeric, neem, basmati rice, ashwagandha, pudina, kalmegh, aloe-vera, karela, jamun and brinjal have been given, which are  victimized  by bio-piracy and where India have successfully put forward its perspective in the international courts and came forth as a winner. This is the ripe time where genuine efforts are required from government, Non Government Organization (NGO)’s, scientists and publishers to restrict highly ambitious pharmaceutical and biotechnological firms to escort our national wealth. There is a dire need of modification or amendments in international and national rules in order to safeguard national interests and to negate the privatization of international knowledge and resources. So far, the best solution provided by India has been the construction of databases and traditional knowledge archives -Traditional Knowledge Digital  Library (TKDL) to endorse the preservation, promotion, dissemination and exercising  suitable use of traditional knowledge as 'Prior art'. This article will bestow limelight on the loot practice of western world under the guise of Intellectual Property Rights (IPRs) and some possible suggestions to forbid such practices.

31

SYNTHESIS AND BIOLOGICAL EVALUATION OF (6-CHLORO-3-OXO-2,3-DIHYDRO-1H-INDEN-1-YL)ACETIC ACID ESTERS AS ANTI-INFLAMMATORY AGENTS DEVOID OF ULCEROGENIC POTENTIAL AT THE TESTED DOSE LEVEL

Sudip Kumar Mandal1 and Saumendra Mohan Ray2,*

1 Dr. B. C. Roy College of Pharmacy & Allied Health Sciences, Dr. Meghnad Saha Sarani, Bidhannagar, Durgapur - 713206, West Bengal, India.

 2,* Guru Nanak Institute of Pharmaceutical Science &Technology, 157/F, Nilgunj Road,  Panihati, Sodepur, Kolkata - 700114, West Bengal, India. 

Abstract

A series of ester derivatives of (6-chloro-3-oxo-2,3-dihydro-1H-inden-l-yl)acetic acid were synthesized and screened for their analgesic and anti-inflammatory activities. These were designed to serve as possible potential nonsteroidal anti-inflammatory agents free from gastrointestinal toxicity and sulphur sensitivity. The synthesized compounds exhibited useful analgesic activity but low anti-inflammatory activity. Few selected compounds were also screened for their antipyretic and ulcerogenic potential. The compounds showed no ulcer formation at the dose level of 100 mg/kg p.o. Aspirin was used as the standard nonsteroidal anti-inflammatory agent. Experimental results indicate that compound 5d holds promise to serve as a novel lead for designing better (less toxic) analgesic antipyretics.

32

A REVIEW ON: ANALYTICAL METHODOLOGY AND INSTRUMENTATION

K. R. Patil1, T. A. Deshmukh2

1SES, Arunamai College of  Pharmacy, Mamurabad, Jalgaon, Maharashtra, India.

2TVES’S Hon’ble L.M.C. College of Pharmacy, Faizpur, Jalgaon, Maharashtra, India.

Abstract

Analytical chemistry is very important for the development of any new drug in market. Every chemist used various methods and instruments for the data interpretation of particular drugs in following article. We will discuss various instruments, their relative principals, methods and instrumentation part along with their pharmaceutical and non pharmaceutical application. The following article describes spectroscopic instrument i.e. Ultraviolet spectroscopy (UV), the recent and most usable instruments i.e. HPLC and HPTLC. These are sophisticated instrumental technique based on the full capabilities of thin layer chromatography. The advantages of automation, scanning, full optimization, selective detection principle, minimum sample preparation, hyphenation, better interpretation etc. enable it to be a powerful analytical tool for chromatographic information of complex mixtures of inorganic, organic, and bio molecules.

33

CARDIOVASCULAR DRUG LOADING: A WURSTER BASED DRUG DELIVERY TECHNOLOGY

Patil Atul1, 3, Ganga Srinivasan2

1Department of Pharmaceutical Science, JJT University, Jhunjhunu, Rajasthan;

2 VES College of Pharmacy, Chembur, Mumbai University, Maharashtra;

3VerGo Pharma Research Laboratories Pvt Ltd, Verna, Goa.

Abstract

Background: Cardiovascular drugs delivery mechanism has significant impact on theraputic effect and benifit, actives such as Dipyridamole, Aspirin and Carvedilol phosphate are currently available in the market but there are no generic formulations available due to complexity involved in developing these formulations. These actives can be mixed as per requirement to get synergistic therapeutic effect. There are no commercial formulations available for Aspirin in pellet dosage form; Drug layering is critical aspect in the Pelletisation to achieve desired drug release it is must to have uniform, highly porous, high potency drug loading. Due to insoluble, crystalline nature, loading of aspirin, Carvedilol & dipyridamole on different substrates is extremely difficult.  Objective: of this research was to develop drug loaded pellet formulations for Aspirin, Dipyridamole and Carvedilol phosphate. In this research work a pellet based drug delivery system by Wurster technolgy was envisaged, Hence basic objective was to establish drug loading on selected substrate to get high potency drug loaded pellets  Investigation: of drug loading was carried out in GPCG 1.1 and Pam Glatt 125Lts. Drug loading has direct impact on formulation performance. A significant impact of manufacturing process, binder, solvent was investigated, a significantly improved drug layered pellet system was developed for crystaline drugs such as Dipyridamole, Carvedilol Phosphate & Aspirin. Observations and conclusion: Excellant drug layereing effeciency was obtianed by slecting suitable solvent and binder. A suitable HPLC method was developed to detect active content in the beads, SEM analysis of these pellets confirmed controlled porocity of drug layered pellets confirming uniformity,and suitability for their application from commercial manufacturing point of view. DSC study also confirmed the polymorphic form of the active in the formulaiton. In overall drug layered pellets such developed were sucessfully scaled up from GPCG1.1 to Pam Glatt 125lts, and thus confirmed comercial feasibility of the work done. These pellets thus can be in future coated with rate modulating polymers & can be mixed synergestically to acheive required theraputic benifit.

34

EFFECT OF AGEING ON STORAGE IN BIOCHEMICAL AND ANTIOXIDANT CHARACTERIZATION OF SESAME (SESAMUM INDICUM L.) SEEDS

Chitra Bhattacharya1, Bhagyashree Deshpande2, Bhawana Pandey2, Seema Paroha1

1Project Coordination unit, All India Coordination Project (Sesame and Niger),Jawaharlal Nehru Krishi Vishwa Vidyalaya, Jabalpur, M.P.

2Bhiali Mahila Mahavidyalaya, Bhilai, C.G.

Abstract

Sesamum indicum is the widely spread the world and is cultivated for its edible seed and oil. It was made to determine the differences in biochemical and antioxidant properties of sesame varieties with different seed coat colours viz white, black and brown and to assess the possible biochemical changes after one year of storage. Identify the suitable cultivars for maximum desirable biochemical traits after storage to assess the biochemical traits with maximum deterioration during storage using different methods. Some of the important biochemical and antioxidant characters were taken in the present study viz. biochemical like Oil, Carbohydrate, Protein, Fibre and Ash content and Antioxidant (Sesamol) value. These samples were stored for one year in the seed storage and were subjected to estimation of oil content in the year 2010. The results revealed the same pattern of variation in oil content within the varieties of different seed colour i.e. reduction from white to brown seeded varieties (45.96% in white, 40.30% in black and 36.50% in brown), protein content was found approximately 19.8% to 18.5%, almost unchanged values were observed in carbohydrate, ash, crude fibre and antioxidant (Sesamol) content due to storage. These data indicates that the biochemical and antioxidant characteristics of sesame seeds changes due to after one year storage.

35

SOLID DISPERSION– STRATEGY TO ENHANCE SOLUBILITY AND DISSOLUTION RATE OF POORLY AQUEOUS SOLUBLE DRUG-AN UPDATED REVIEW

Sameer H. Lakade1*,  Bhalekar.M.R2

1 Department of Pharmaceutics, Karpagam University, Coimbatore (T.N) India and

2 Department of Pharmaceutics, AISSMS College of Pharmacy Kennedy road Pune 411001.

Abstract

Now a days majority of drug manufactured by synthetic process, so large volume of drug produce which are highly water in soluble drugs but having no issue on permeability, means BCS class II category drugs. To improve the status of such major problem many approaches have been introduced for the solubility enhancement of such drugs. SD is usually one of the most widely and adopted technology used for this purpose.. Poor water solubility is the major drawback for the various types of drugs and various approaches have been introduced so far for the solubility enhancement of such drugs. Solid dispersion is one of unique technique adopted for the formulation of such drugs and various novel methods were used for the preparation of solid dispersion. Solid dispersion techniques have attracted majority because of low cost & due to improving the dissolution rate of highly lipophilic drugs and hence their bioavailability. This article reviews on classification, various preparation methods, advantages and disadvantages of solid dispersion.

36

PREPARATION AND EVALUATION OF NANOSUSPENSIONS FOR ENHANCING THE DISSOLUTION OF LORNOXICAM BY ANTISOLVENT PRECIPITATION TECHNIQUE

Shinde Sunita S*1, Hosmani Avinash H2

1Research Scholar, JJT University, Jhunjhunu, Rajasthan, India.

2Dept. of Pharmaceutics, Tatyasaheb Kore College of Pharmacy, Warananagar, Kolhapur, MS. India. 416113.

Abstract

The aim of this study was to prepare and characterize lornoxicam nanosuspensions to enhance the dissolution rate of this drug. Nanosuspensions were prepared by the precipitation–ultrasonication method.. The particle size and zeta potential of nanospray dried powder were 213nm  and −20mV, respectively. The morphology of nanocrystals was found to be spherical in shape by scanning electron microscopy (SEM) observation. The X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC) analysis indicated that there was no substantial crystalline change in the nanocrystals compared with pure drug. The in vitro dissolution rate of lornoxicam was significantly increased by reducing the particle size. . The amorphous LOR nanoparticles showed dramatic improvement in rate as well as extent of in-vitro drug dissolution. The improvement can be attributed to amorphization and surface area, reduced particle size and decreased diffusion layer thickness. Spray drying process produced dry nanosuspension with high stability compared to liquid formulation.

37

ANXIOLYTIC EFFECT OF MEDICAGO SATIVA SEEDS EXTRACT ON RODENTS

A.Tamil Selvan, S.Prithvi, R.Suthakaran, R.Ravali, G.M. Kumar and R.Ravali

Department of Pharmacology, Teegala Ram Reddy College of Pharmacy Meerpet, Hyderabad, Andhra Pradesh, India

Abstract

Central nervous system disorders are of great concern in the present day world due to increasing stress and changing living conditions. Herbs and plants are used as a remedy and curative regimens for such kind of disorders from time immemorial. Medicago sativa (Leguminosae) is used to improve to kidney pain, antioxidant, antimicrobial and CNS disorders. The present study has been designed to evaluate the anxiolytic activity from ethyl acetate fraction of bioactive methanolic extract of the seeds of Medicago sativa using elevated plus maze model, hole board test, open field test, stair case test, light/dark exploration, social interaction and locomotor performance in experimental animal models. A trail has been done to separate the bioactive compound by fractionation method. Fractionation of bioactive ethyl acetate of the seeds showed significant anxiolytic action at a dose of 100mg/kg per oral when compared with the standard drug diazepam (1mg/kg, p.o). TLC profile of the fraction contains the spots indicating the presence of flavonoids. Hence the present study preclinically validates the anxiolytic action of Medicago sativa seed extract fraction. From the above study it was concluded that Medicago sativa can be safely used in the anxiety and other CNS disorders.

38

A NEW RP-HPLC ANALYTICAL METHOD DEVELOPMENT & VALIDATION FOR ESTIMATION OF LORNOXICAM IN BULK AS WELL AS IN PHARMACEUTICAL FORMULATION BY USING PDA DETECTOR

S. Ashutosh Kumar*1, Manidipa Debnath2, J. V. L. N. Seshagiri Rao3, B. Chaitanya1­, B. Balatripura Sundari1, D. Balaji1, G. Nagendra Ratna1, M. Anjani Ramya Krishna1, T. Vijay Shankar1

1Department of Pharmaceutical Analysis & Quality Assurance, A.K.R.G College of Pharmacy, Nallajerla, West Godavari, 534112, A.P, India

2Department of Pharmaceutics, A.K.R.G College of Pharmacy, Nallajerla, West Godavari, 534112, A.P, India

3 Department of Pharmaceutical Analysis, Yalamarty College of Pharmacy, Visakhapatnam, A.P, India.

Abstract

A simple, rapid, and precise method was developed for quantitative analysis of Lornoxicam (LXM) in bulk as well as in pharmaceutical dosage forms. SUMMARY:  The chromatographic separation of LXM was achieved on a Hypercil BDS C18 (4.6 x 150mm, 5 mm) analytical column with Potassium Dihydrogen Phosphate Buffer & Acetonitrile [HPLC Grade] in the ratio of 40:60 (v/v), as mobile phase at ambient temperature. The flow rate was 1.0 ml/min and detection was by absorption at 382 nm using a PDA detector. The number of theoretical plates and tailing factor for LXM were found to be 1483.4 and 1.5 respectively. The linearity of the method was excellent over the range 10–50 µg/ ml LXM. The correlation coefficient was 0.9999. The relative standard deviations of peak areas from five measurements were always less than 2%. The proposed method was found to be suitable and accurate for quantitative analysis of LXM. CONCLUSION: The present work was undertaken with the aim to develop and validate a rapid and consistent RP-HPLC method development in which the peaks will be appear with short period of time as per ICH Guidelines. The proposed method was adequate sensitive, reproducible and specific for the determination of Lornoxicam bulk as well as in its Pharmaceutical dosage form. The validation of method was carried out utilizing ICH-guidelines. The described RP-HPLC method was successfully employed for the analysis of pharmaceutical formulations containing the dosage form. The proposed method was simple, fast, Accurate and precise method for the Quantification of drug in the dosage form, bulk drug as well as for routine analysis in Quality control. Overall the proposed method was found to be suitable and Accurate for the Quantitative determination and stability study of the drug in Pharmaceutical dosage form.

39

PREDICTION OF BINDING ENERGIES/INTERACTIONS BETWEEN DIOSPYRIN AND DIFFERENT TARGET PROTEINS OF Mycobacterium tuberculosis BY IN SILICO MOLECULAR DOCKING STUDIES

A.Jerad Suresh*, R. Devi, K. M. Noorulla, P.R.Surya

Department of Pharmaceutical Chemistry, College of Pharmacy, Madras Medical College, Chennai -600003, Tamil Nadu, India.

Abstract

Diospyrin, the compound under research binds to a novel site on well known enzyme DNA Gyrase of Mycobacterium tuberculosis and inhibits the enzyme. The aim of the present study was to predict the binding energies/interactions between Diospyrin compound and different target proteins of Mycobacterium tuberculosis. The following target proteins with their Protein Data Bank (PDB) ID were selected, NADH-dependent enoyl- ACP reductase  (InhA) - 2NSD, Adenosine kinase (Adok) - 2PKK, Mycolic acid synthase (PcaA) - 1L1E, Lysine N-acetyltransferase (MbtK) - 1YK3, Thymidylate synthase X (ThyX) - 3GWC, Thymidylate kinase (TmK) – 1G3U, Serine/threonine-protein kinase (PknG) – 2PZI, beta-ketoacyl-ACP synthase III (FabH) – 1HZP, Arabinosyl indolyl acetyl inositol synthase (EmbC) – 3PTY, dTDP-rhamnose synthase (RmlD) – 1KC3, Cyclopropane fatty acid synthase (CmaA2) – 3HEM, Diaminopimelate decarboxylase (LysA) – 1HKV, L,D-Transpeptidase type 2 _ 3VAE, Gyrase type IIA topoisomerase C-terminal domain _ 3UC1 and Topoisomerase IV (E.coli) _ 3FV5 to study their susceptibility to Diospyrin compound. The 3D and 2D structures of target proteins are downloaded from PDB database. The extent of binding positions and affinity of the Diospyrin with the selected target proteins were predicted based upon the scoring functions - Glide score (G Score) of Glide software.  The Cyclopropane fatty acid synthase (CmaA2) was identified as potential target enzyme through our molecular docking studies. Structure-based drug design is now becoming the effective tool with the potential to identify the lead molecule to the development of new anti-tubercular agents, effective against persistent and resistant Mycobacterium tuberculosis infections.

40

EFFECTS OF PARTICLE SIZE AND SOME FORMULATION ADDITIVES ON THE DISSOLUTION PROFILE OF IBUPROFEN FROM COMPRESSED TABLETS.

Umeh O.N.C.*,Orji I.E,Ofoefule S.I.

Department of Pharmaceutical Technology and Industrial Pharmacy,University of Nigeria, Nsukka

Abstract

Drugs of low aqueous solubility provide a major challenge in the design of modern oral dosage form due to dissolution and bioavailabilty difficulties. The present study was undertaken to investigate the effect of particle size and some formulation additives (sodium laurylsulphate (SLS), Primogel R and Ac-Di-Sol) on the release profile of poorly soluble drug, ibuprofen from compressed tablets. Six batches (A - F) of Ibuprofen granules and tablets were prepared by the wet granulation method. Batches A, B and C contained granules that were fractionated from three sieve fractions (0.42, 0.25 and 0.15 mm respectively) in ascending order of particle size. D, E and F contained 2 % Primogel R, 1 % Ac-Di-Sol and 0.2 % SLS respectively. Tablet properties evaluated as a function of particle size and formulation additives include: hardness, friability and dissolution efficiency at 60 min. Results obtained indicated a decrease in the dissolution rate of the batches as the particle size increased. All the Ibuprofen tablet batches produced exhibited better drug release (in terms of rate and extent of release) than a commercially available sample, Multifen®. The overall and expected in vivo bioavailability in the batches on the basis of dissolution efficiency parameter (DE60) is in the order of E (98.3 %) > D (98.0 %) > A (97.7 %) > F (96.9 %) > B (95.3 %) > C (93.8 %) > Multifen® (26.0%). Statistical comparison of the DE60 parameter indicated a significant difference (p ˂ 0.05)  in the results from the formulated batches and the commercially available sample, Multifen®. The results indicated that particle size reduction of granules and the inclusion of formulation additives like SLS, Ac-Di-SOL and Primogel R can be utilized in improving the release profile of Ibuprofen from compressed tablets.

41

IN-VITRO AND EX-VIVO EVALUATION OF MUCOADHESIVE TABLETS USING NATURAL POLYMERS BY GASTRO RETENTIVE DRUG DELIVERY SYSTEM

D.Krishnarajan*1, 2, N.Senthil Kumar1, 2, Sasikanth Kanikanti1

1Department of pharmacy, JKK Munirajah Medical Research Foundation College of Pharmacy, Ethirmedu, B.Komarapalaym, Namakkal – 638183, Tamilnadu, India.

2Department of pharmacy, Sunrise University, Alwar, Rajasthan – 301030, India.

Abstract

The aim of the present study was to determine the comparative mucoadhesive strength , mucoadhesive force and mucoadhesive retention time of some natural polymerts by simple invitro method. Various natural polymers were selected in the current study. The tablets were prepared by wet granulation method and the following evaluation methods were used such as swelling index, mucoadhesive strength, mucoadhesive force, ex-vivo mucoadhesive time and in-vitro mucoadhesive retention time was determined. And all these in-vitro evaluations were done by using goat intestinal mucous memberane. The study reveals that the ascending order of natural polymers for formulating a gastro retentive mucoadhesive system was found to be gum Arabic(1.53) < neem gum(1.55) < locust bean gum(1.60) < tragacanth(1.64) < chitosan(1.71) < guar gum(1.82) < xanthan gum(1.87) < karaya gum(1.92) < carbopal 934(2.27).

42

HEPATOPROTECTIVE ACTIVITY OF HERBAL FORMULATION AGAINST PARACETAMOL-INDUCED HEPATOTOXICITY IN RATS

Sanjay Arote*, Shravan K. Gupta, Paresh Lodha, Pravin Yadav, Mangesh Lodha

SRES’s Sanjivani College of Pharmaceutical Education & Research, Kopargaon, Maharashtra State, 423603.

Abstract

The present research work is directed towards the study of hepatoprotective activities of herbal formulation against paracetamol-induced hepatotoxicity in rats. The study was designed to evaluate the hepatoprotective activity of herbal formulation in acute experimental liver injury induced by paracetamol (750mg/kg) in Wistar albino rats. The effect of formulation was also studied on serum glutamate oxalate transaminase (SGOT), serum glutamate pyruvate transaminase (SGPT), serum alkaline phosphatase (SALP), total bilirubin, and total protein.   The histological study exhibited reduced signs of paracetamol-induced hepatotoxicity. The hepatoprotective activity of formulation (100mg/kg and 200mg/kg) was also substantiated by significant (p<0.05) decrease in levels of SGOT, SGPT, SALP, and Total bilirubin. The effects of formulation were comparable to that of standard drug, Silymarin. From the study, it can be concluded that the herbal formulation has hepatoprotective activity.

43

PHYTOCHEMICAL AND HPTLC FINGERPRINT ANALYSIS OF TERMINALIA ARJUNA (ROXB) WIGHT & ARN. IN DIFFERENT SOLVENT EXTRACTS

N.M.A. Rasheed1, M.A. Shareef1, Atiya Rehana1, M.A. Waheed1, S. Arfin2 & Aminuddin2

1Central Research Institute of Unani Medicine, Opp. E.S.I. Hospital, A. G. Colony Road, Erragadda, Hyderabad, 500038

2Central Council for Research in Unani Medicine, 61-65, Institutional area, Janakpuri, New Delhi, 110058

Abstract

Terminalia arjuna (Roxb) Wight & Arn belongs to the family combretaceae known as potent cardiotonic since ancient times. Herbal drug aid with technology is utilized for converting botanicals into medicines, where there is an importance of standardization and quality control studies with appropriate integration of modern techniques and traditional knowledge. The qualitative and quantitative aspects which are widely accepted in the quality assessment of herbal drugs such as TLC and HPTLC studies. In the present study Terminalia arjuna fingerprint of different solvent extracts has been studied by HPTLC along with phytochemical screening in different solvent extracts. Thin layer chromatography was carried with mobile phase Chloroform: Methanol (9.2:0.8) (v/v) on Precoated aluminium Silica gel plates (Merck) and a densitometric determination was done at 580 nm. Other parameters studied such as morphology, heavy metals, aflatoxin contamination and fluorescence behaviour to lay down the standard for the genuine drug.

44

CNS DEPRESSANT, OPIOID TYPE OF ANALGESIC & ANTI-HISTAMINE ACTIVITIES OF BASELLA ALBA VAR RUBRA (LINN) STEWART

Kavya.K*1, Veera Vijay.B2, Pandu Ranga Reddy.B3, Thanga Thirupathi.A3

1C.M College of Pharmacy, Maisammaguda, Dhulapally, Secunderabad - 500014.

2NIPER, Bhangagarh, Guwahati - 781006.

3Sankaralingam Bhuvaneswari College of Pharmacy, 3/77-C, Anaikuttam Road, Anaikuttam, Sivakasi -  626130.

Abstract

The objective of this research work is to evaluate in detail CNS depressant, Analgesic and Anti-histamine activities of different lead extracts of Basella alba. The plant leaves and twigs were shade dried, size reduced and soxhlet extracted with Petroleum ether, Ethanol, Chloroform and Aqueous solvents. The potency of these various extracts were compared in every category with standard drugs like Chlorpromazine, Pheniramine maleate and Pentazocine for CNS depressant, Anti-histamine & Opioid analgesic activities respectively. The therapeutic values of these various extracts of Basella alba were found to be equally comparable with respective standard drugs.

45

A REVIEW ON LOZENGES

Satish G Shinde*, Vaishali Kadam,  G.R. Kapse, S.B. Jadhav, Md. Zameeruddin, V.B. Bharkad

Department of Pharmaceutics, Indira College Of pharmacy, Nanded, Maharashtra India.

Abstract

Lozenges are tablets that dissolve slowly in the mouth and so release the drug in the saliva. Lozenges are used for the local medication dissolving in the mouth or throat, e.g. it will produce local anaesthesia, antiseptic and antibiotic action of drugs. There are different types of lozenges such as Chewable Lozenges, Hard Lozenges, and Soft Lozenges. Chewable lozenges are popular with the paediatric population. Hard-candy lozenges are mixtures of sucrose and other sugars and/or carbohydrates in an amorphous state. Soft lozenges have become popular because of the ease of extemporaneous preparation and applicability to a wide variety of drugs. The lozenges are prepared by direct compression and Wet granulation method. Ordered mixing, Drug adsorption, Drug excipient hybrid mixing by spray drying these are methods by which compressed tablet lozenges are prepared. There are some evaluation parameters by which lozenges will be evaluated such as diameter, weight variation, friability, hardness, In-vitro drug dissolution studies, Stability studies etc.

46

SYNTHESIS OF PLANT-MEDIATED SILVER NANOPARTICLES USING AERVA LANATA LEAF AQUEOUS EXTRACT AND EVALUATION OF ITS ANTI BACTERIAL

.P. Balashanmugam1*, S. Santhosh 1, D.J Mukesh kumar1, S. Anbazhakan2,P.T. Kalaichelvan1

1Centre for Advanced Studies in Botany, University of Madras, Chennai 600025, India.

2PG and Research dept.of Botany, Government Arts College, Tiruvannamalai, 606603, India.

Abstract

In the present study the synthesis of silver nanoparticles has been carried out from the Aerva lanata aqueous Leaf extract. The reduction of silver nitrate led to the formation of Silvernanoparticles within one day at room temperature. The size, shape and elemental analysis were carried out using TEM with EDX, FT-IR and visible absorption spectroscopy. The prepared AgNPs showed surface Plasmon resonance center at 425 nm with average particle size of 15-20 nm. Crystalline nature of the nanoparticles is confirmed from the XRD patterns. From the FTIR spectra it is found that the biomolecules are responsible for capping in silver nanoparticles. The synthesized silver nanoparticles have been investigated against human pathogenic bacteria.

47

STABILITY INDICATING HPTLC METHOD FOR DETERMINATION OF EPROSARTAN MESYLATE FROM BULK DRUG AND PHARMACEUTICAL FORMULATIONS

Vineeta Khanvilkar, Vinayak Dalvi, Atmaram Tambe, Daksha Parmar, Vilasrao Kadam

Department of Pharmaceutical Analysis, Bharati Vidyapeeth’s College of Pharmacy, Navi Mumbai- 400614.

Abstract

A simple, selective, precise and stability-indicating high-performance thin-layer chromatographic (HPTLC) method for analysis of eprosartan mesylate both as a bulk drug and in formulations was developed and validated. The method employed TLC aluminium plates precoated with silica gel 60F254 as the stationary phase. The solvent system consisted of ethyl acetate: acetonitrile: glacial acetic acid (5: 5: 0.7, v/v/v). This system was found to give compact spots for eprosartan mesylate (Rf value of 0.48 ± 0.02). Densitometric analysis of eprosartan mesylate was carried out in the absorbance mode at 238 nm. The linear regression analysis data for the calibration plots showed good linear relationship with r2 = 0.996 in the concentration range 100-700 ng per spot. The method was validated for specificity, precision, accuracy, limit of detection, limit of quantification and robustness. Statistical analysis proved that the method is specific, precise and accurate for the estimation of said drug. Eprosartan mesylate was subjected to acidic, alkaline, hydrolytic, oxidative and photolytic degradation. As the method could effectively separate the drug from its degradation product, it can be employed as a stability-indicating one.

48

A REVIEW ON HEALTH BENEFITS OF SCALAR ENERGY

Sagar Sanghai1,Vaishal Kadam2, Satish Shinde

Department of Pharmaceutics, Indira college of pharmacy, Vishnupuri, Nanded, Maharashtra, India.

Abstract

Scalar energy was First discovered by James Clerk Maxwell in the 19th century, and proven by Nikola Tesla, the existence Scalar energy is also acknowledged by Nobel Prize winner, Albert Einstein. Researchers at the Max Planck Institute, Germany, found that scalar energy unclumps and activates living cells. Cellular energy and body energy level increases by use of scalar energy. For every cell to function normally it require energy of 70-90 milivolt and we can verify this by using spectrogram. Scalar energy can protect our DNA from damage, improve cell wall permeability, helpful in cancer treatment. Scalar waves prevents the uptake of nor-adrenaline by PC 12 nerve cells, Reduces inflammation, promotes un-clumping of cells, improves circulation, improves immune and endocrine systems. They also has the ability to kill viruses and bacteria, enhances cellular nutrition and detoxification. Scalar energy has great importance in human health, and wide scope for establishing a new era in the pharmaceutical life.

49

SYNTHESIS, EVALUATION AND MOLECULAR DOCKING OF NOVEL SERIES OF N-[5-(ARYL)-3-PHENYL-4,5-DIHYDRO-PYRAZOLE-1-CARBOTHIOYL]-ACETAMIDE DERIVATIVES

Mitul V Patel1,Deepali M Jagdale1*,Sharad H Bhosale2, Vilasrao J Kadam1

1BharatiVidyapeeth’s College of Pharmacy, Navi Mumbai.

2Poona college of Pharmacy, Pune

Abstract

The Aim of the research work was to synthesis aseries of novel N-[5-(Aryl)-3-phenyl-4,5-dihydropyrazole-1-carbothioyl]-acetamide derivatives and evaluated it . The structural elucidations of newly synthesized compounds were characterized by spectroscopic data such as IR and1H NMR. The synthesized compounds were screened for their anti-cancer activity against Human breast cancer cell line MCF7. All compounds were found to be moderately active, with compound 3jhaving substitution at 3rd position with bromine possessed activity comparable with standard drug Adriyamycin having log GI50< -7.0.

50

ISOLATION AND IDENTIFICATION OF PHENOLIC COMPOUNDS FROM LEAF EXTRACTS OF COCHLOSPERMUM RELIGIOSUM (L.) ALSTON BY ELECTROSPRAY IONIZATION MASS SPECTROMETRY

Sasikala A, Linga Rao M* and Savithramma N

Department of Botany, Sri Venkateswara University, Tirupati - 517502, Andhra Pradesh, India.

Abstract

The present study intended to isolate phenolic compounds from the leaf of Cochlospermum religiosum by using 70% acetone and poly vinyl pyrrolidane; and characterized by UV-visible spectrometry, high performance liquid chromatography/ electrospray ionization mass spectrometry.  The results showed that totally 87 phenolic compounds were obtained at both positive and negative ion modes of LCMS. Among the isolated phenols, 11 phenolic compounds have been identified based on their retention time and m/z values namely, Gallic acid, 2,3-Dihydroxybenzoic acid, Ascorbic acid, Quercetin, Cynarine, 1,2,3,4,6-Pentagalloyl glucose, Syringaldehyde, Thymol, Ellagic acid, Isorhamnetin and Benzoic acid.  This study illustrates the rich array of phenolic compounds of leaves of Cochlospermum religiosum could be utility as health beneficial bioactive compounds.

51

EFFECT OF SUB LETHAL DOSES OF COPPER SULPHATE ON CERTAIN BIOCHEMICAL PARAMETERS OF COMMON CARP, CYPRINUS CARPIO

Zahoor Ahmad Dar and K. Borana

Department of Zoology and Applied Aquaculture, Barkatullah University, Bhopal (MP)India.

Abstract

The effect of sub- lethal concentrations of copper sulphate (2 mg/1 and 5 mg/1) on various biochemical parameters during different time periods i.e. 30, 60 and 90 days on Cyprinus carpio were studied. Serum albumin, serum globulin and serum total protein showed an overall decrease in all the copper sulphate treated groups throughout the experimental investigations with marked significant values.

52

ENHANCED ANTIMICROBIAL ACTIVITY OF HONEY WITH GREEN SYNTHESIZED AGNPS BY USING TABERNAEMONTANA CORONARIA (JACQ.) WILD FLOWER EXTRACT

Durgam Heemasagar, Kannan Jeeva, Muthusamy Sureshkumar

Department of Biotechnology, Muthayammal College of Arts & Science, Rasipuram, Namakkal Dist–637408, Tamilnadu, India. 

Abstract

An eco-friendly procedure for the synthesis of silver nanoparticles using the flower extract of Tabernaemontana coronaria (jacq.) wild. as a reducing and stabilizing agent. The synthesised AgNps by using fresh and dry flower extract (aqueous extract) were characterized using UV-Visible spectroscopy, FTIR analysis, XRD and SEM and EDAX. The synthesized metal is face centered cubic (fcc) Ag nanocrystals and the AgNps obtained from both fresh and dry flower extract were spherical in shape with size of 16-56 nm and 14-39 nm  respectively. The synthesised AgNps had significant antibacterial activity and also the particles showed the moderate antibacterial activity when it was mixed with honey towards Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumonia, and Salmonella typhi; compared with standard antibiotics. The green synthesized AgNps showed moderate antibacterial activity in combination with honey. This antibacterial activity of green synthesized silver nanoparticles with honey is the novel approach and can be easily improved to handle the development of antibiotic resistance in bacterias.

53

PRESCRIBING PATTERNS OF ANTIBIOTICS IN POST OPERATIVE PATIENTS IN A TEACHING HOSPITAL

Ayesha Parveen*1, Khudeeja Shaheen1,Mahnoor Qamer shaik1, Sofia Wajid Ali1,Dr.S.Mumtaz Hussain2, Syed Amir Ali3,Dr. Arshad Hussain Mohd1, Mohammed Mohiuddin3.

1Pharm.D, Department Of Pharmacy Practice, Deccan School Of Pharmacy, Hyderabad, A.P, India.

2MS, Department of General Surgery, Owaisi Hospital and Research Centre, Hyderabad, AP, India.

3M.Pharm, Department Of Pharmacy Practice, Deccan School OfPharmacy, Hyderabad, A.P, India.

Abstract

The use of antibiotics to prevent infections at the surgical site is known as the surgical prophylaxis. Appropriate antibiotic prophylaxis can reduce the risk of wound infections after surgery, but additional antibiotic use also increases the selective pressure favoring the emergence of antimicrobial resistance. A prospective and observational study was carried out on 200 post-operative inpatients for a period of 6 months. A total of 200 patients were included in the study in which 83(59%) male and 117(41%) female. The total numbers of antibiotics used were 420 in which 37.1% of third generation cephalosporin and 31.4% of metronidazole were used. In the study five different combinations of antibiotics were prescribed. The most common surgery performed was appendectomy. The number of antibiotics per prescription on average basis was found to be 3.92 and the mean duration of days the antibiotics given to the patients was found to be 3.16 days during their stay in the hospital. The study concludes that most common use of cephalosporins and metronidazole seems to be effective in reducing the surgical site infection and other complications. Patients in surgical wards develop infections post-surgery; many of the infections are caused by bacteria that are highly virulent. As a result there is a need for prophylactic or empirical treatment with antibiotics that can cover broad spectrum of pathogens.

54

SYNTHESIS, CHARACTERISATION AND BIOLOGICAL EVALUTION OF SOME NOVEL 6-FLUORO BENZOTHIAZOLE SUBSTITUTED THIAZOLIDINONES AS ANTI-OXIDANT AND ANTIMICROBIAL AGENTS

Ravi Sankar Reddy.D*, D.Sudhakar

Department of Pharmaceutical Chemistry, University College of Pharmaceutical Sciences, Acharya Nagarjuna University, Guntur-522510(India).

Abstract

Some 3-(7-Chloro-6-Fluoro benzo [d] thiazol-2-yl)-2-(4-Chlorophenyl) thiazol 1,3 lidin-4-one have been synthesized by the reaction of substituted -2-aminobenzothiazole with aromatic amines (para amino benzoicacid, diphenylamine, Morpholine, Dimethylamine and Diethylamine) followed by condensation with Mercaptoacetic acid. All the synthesized compounds were characterized by elemental analysis, IR Spectra, 1H NMR and Mass Spectral studies. These were screened for anti-oxidantand and anti-microbial activity

55

DEVELOPMENT AND VALIDATION OF CHEMOMETRIC ASSISTED UV SPECTROPHOTOMETRIC AND RPLC-PDA METHODS FOR THE SIMULTANEOUS IN VITRO ANALYSIS OF ISONIAZID, RIFAMPICIN AND PIPERINE IN THEIR PHARMACEUTICAL FORMULATION

Shakeel S Mansuri, Abhishek Pathak, Sadhana J Rajput*

Pharmaceutical Quality Assurance Laboratory, Centre of Relevance and Excellence in Novel Drug Delivery System,

Shri G H Patel Pharmacy Building, Pharmacy Department, The Maharaja Sayajirao University of Baroda, Fatehgunj, Vadodara-390 002, Gujarat, INDIA.

Abstract

Two chemometric assisted UV spectrophotometric and one RPLC-PDA (Reversed Phase Liquid Chromatography with Photo Diode Array Detector) methods were developed and validated for the simultaneous in vitro analysis of Isoniazid (INH), Rifampicin (RIFA) and Piperine (PIP) in their ternary mixture and pharmaceutical formulation. The two chemometric methods applied were inverse least square (ILS) and classical least square (CLS). These approaches were successfully applied to quantify each drug in their mixture using the information included in the UV absorption spectra of appropriate solutions in the wavelength range 220-360nm with the intervals of 10nm (Δλ=10nm) at 15 wavelength points. For the chemometric calibration, 20 ternary solutions were prepared as training set and 10 ternary solutions were prepared as validation set. The chemometric methods do not require any separation step. The chromatographic separation was achieved on a reversed-phase, Phenomenex Luna C18 column (250X4.6 mm, 5 m particle size). Gradient elution was carried out with a mobile phase of 0.05M Disodium hydrogen phosphate buffer pH -7.0 (solution-A) and Acetonitrile (solution-B). The total run time was 12 min.  Quantitation was achieved with PDA detection at 290nm for INH, RIF and PIP based on peak area. Linearity was observed over concentration range of 30-270 µg mL-1 for INH, 20-180 µg mL-1 for RIFA and 1-9 µg mL-1 for PIP. The developed methods were successfully applied for laboratory prepared mixtures as well as commercial capsule formulation for INH, RIFA and PIP concentration. The results obtained for pharmaceutical formulation by ILS and CLS methods were compared with gradient RPLC-PDA method and a good agreement was found.

56

DEVELOPMENT AND VALDIATION OF UV SPECTROPHOTOMETRIC METHOD FOR THE ESTIMATION OFEBERCONAZOLE IN BULK AND PHARMACEUTICAL FORMULATIONS

K. Vijaya Sri*, V.Pavali, M.L.V. Setti

Department of Pharmaceutical Analysis Malla Reddy College of Pharmacy, Maisammaguda, Secunderabad-500 014, Andhra Pradesh, India.

Abstract

The main objective was to develop and validate the UV-spectrophotometric method for the estimation of eberconozole nitrate in bulk and pharmaceutical formulations as per ICH guidelines. A simple, sensitive and accurate UV-spectrophotometric method has been developed using   methanol a solvent for the estimation of eberconozole nitrate  from bulk and pharmaceutical formulation. The λmax of eberconozole nitrate   was found to be 220 nm  it was proved  linearity in the concentration range 1–15 μg/ml with a correlation coefficient value of 0.999. The % recovery was found to be in the range of 98.54– 99.98%. The limit of detection (LOD) and limit of quantification (LOQ) were found to be 0.188and 0.626 µg/ml, respectively. The % RSD low values   are indicates the accuracy and precise of the method. The above method was a rapid tool for routine analysis of eberconozole nitrate in the bulk and in the pharmaceutical dosage form

57

ANALYTICAL METHOD DEVELOPMENT AND VALIDATION FOR THE ESTIMATION OF SUNITINIB MALATE IN BULK AND ITS PHARMACEUTICAL DOSAGE FORM USING RP-HPLC

Iffath Rizwana1, Dr. K. Vanitha Prakash2*, Dr. G. Krishna Mohan3

1 Research Scholar, School of Pharmaceutical Sciences, JNTU-K, Kakinada & DeccanSchool of Pharmacy, Hyderabad, A.P. India

2Department of Pharmaceutical Analysis, SSJ College of Pharmacy, Gandipet,Hyderabad, A.P. India.

3Centre for Pharmaceutical Sciences, IST, JNTU Hyderabad, A.P. India.

Abstract

A simple, specific and accurate RP-HPLC method was developed for the determination of Sunitinib malate in bulk and its pharmaceutical dosage form. Hypersil ODS C18 (4.6 x 150mm, 5 m,) column was used in isocratic mode with mobile phase containing Acetonitrile : phosphate buffer pH 3.0 (pH adjusted with orthophosphoric acid) in the ratio of 50:50 v/v. The flow rate was 1.0 mL/ min and eluents was monitored at 248nm. The retention time Sunitinib malate was found to be 2.567 min, respectively. The linearity for Sunitinib malate was in the range of 10-50 μg/ml respectively. The mean recovery of Sunitinib malate was found to be 99.5%, respectively. The proposed method was validated according to ICH guidelines and successfully applied to the estimation of Sunitinib malate in capsule dosage form. The developed method was very simple, economic, accurate and precise and can be used for routine quality control examination of capsules of Sunitinib malate.

58

HISTAMINE RECEPTORS IN CENTRAL NERVOUS SYSTEM

Nishant S. Jain*

Institute of Pharmaceutical Sciences, Guru Ghasidas University (A Central University), Bilaspur-495009 (C.G.), India

Histamine is a slow-acting neurotransmitter and affects the central nervous system (CNS) activity. The central actions of histamine are mediated through its four distinct G-protein coupled, i.e. H1, H2 or H3 receptors, which are widely expressed in distinct patterns in the mammalian brain and also through H4 mainly thought to be restricted to hematopoietic cells and is suggested to mediate functions of the immune system and chemotaxis, have also been found to modulate CNS actions. The central presence of histaminergic system was ascertained immunohistochemically with the origin in the tuberomammillary (TM) nucleus, a part of the posterior hypothalamus, with wide distribution of histaminergic projections to the rest of the CNS. The histamine actions are regulated by histamine H3 receptor, which is an inhibitory autoreceptor or heteroceptor that controls histamine synthesis and release of histamine and other neurotransmitters in the brain, such as acetylcholine, norepinephrine, serotonin, dopamine or GABA located on the somata and axon terminals of histamine neurons. The present report is the compilation of the central role of histamine via its receptors.