IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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JANUARY 2016
1

EVALUATION OF ANTICHOLINERGIC PROPERTY OF AMITRIPTYLINE AND PROMETHAZINE ON SALIVARY FLOW SECRETION IN NORMAL HEALTHY HUMAN VOLUNTEERS

B.V.S. Lakshmi1*, U. Shoba Jagdish Chandra2, M. Sudhakar1, S.Shruthi1
1Malla Reddy College of Pharmacy, Dhulapally, Maisammaguda, Secunderabad 500014, Telangana, India (Affiliated to Osmania University).
2Malla Reddy Institute of Medical Sciences, Suraram, Secunderabad 500014, Telangana, India.

Abstract

Objective: Human saliva mirrors the body’s health and can be collected non-invasively, does not require specialized skill. The Aims were twofold: to evaluate the Anticholinergic Property of Amitriptyline and Promethazine on salivary flow secretion in normal healthy Human Volunteers and to evaluate Anticholinergic property between antidepressant and antihistamine. Method: Salivary samples were collected from 12 non-smoking healthy human volunteers aged between 18 – 45 years, weight more than 50kgs.Baseline evaluation of salivary flow was done by placing four sterile absorbent cotton balls onto the vestibule of the mouth for 5 min which were pre-weighed. The weight of the saliva was determined by subtracting pre weight from post weight, in (ml). The volunteers were crossed over after wash out period of 7 days to the other formulation as per randomisation. Results: Effect of Promethazine (25mg), Amitriptyline (10mg), Amitriptyline (25mg) on saliva secretion in ml at different time interval values are expressed as Mean±SD. Promethazine (25mg), Amitriptyline (10mg), Amitriptyline (25mg), have shown significant anticholinergic activity at 5h (p**< 0.01), 6h (p**<0.01) and at 4h (p***<0.001) respectively when compared to baseline using one way ANOVA followed by student’s’ test. Conclusion: Amitriptyline (25mg) showed most significant decrease in salivary secretion levels (ml) at different time intervals when compared with the corresponding levels after administration of Promethazine (25mg), Amitriptyline (10mg). By this study it is proved that Tricyclic Antidepressants and Antihistamines have significant anticholinergic property.

2

BIOCHEMICAL ANALYSIS AND ANTIPROLIFERATION ACTION OF Centratherum anthelminticum (L) Kuntze SEED EXTRACT ON CANCER CELL LINES LIKE DALTON’S LYMPHOMA ASCITES (DLA) AND EHRLICH ASCITES CARCINOMA (EAC)

K. M. Thara1, K. F. Zuhara2
1Department of Biotechnology, University of Calicut,Thenjippalam,Malappuram District,Kerala,India.Pin-673635.
2Professor, Department of Life Sciences, University of Calicut.

Abstract

Centratherum anthelminticum (L) Kuntze., (Purple flebane). Traditionally the plant used for treating thread worm infections and gastric troubles. The methanol extract from the seeds of the plant Centratherium anthelminticum was biochemically analyzed for different bioactive components by HPLC and other biochemical tests. Antioxidant activity of the extract was evaluated by DPPH and reducing power method. The anticancer activity of this plant extract was studied using Dalton’s Lymphoma Ascites (DLA) and Ehrlich Ascites Carcinoma (EAC) cell lines. The extract showed significant (p<0.02) anticancer activity against DLA and EAC cell lines with 63.5 and 65% of inhibition of growth of these cell lines respectively. On testing the cytotoxicity on normal cell lines, the extract was found to less toxic to normal cell lines while it shows anti proliferation effect on cancer lines like EAC and DLA.

3

GREEN TEA TABLETS- A REVIEW

V. Hema Suma Sree*, CH. SRC Hemanth Kumar*, Dr. A. Seetha Devi
Hindu College of Pharmacy, Guntur.

Abstract

Now-a-days many people are using green tea in various ways like for decreasing the body weight, for improving mental alertness, in the treatment of various diseases like Osteoporosis, Crohns disease, prevent skin cancers. It also treats stomach disorders, diarrhea and vomiting. Tablets are the most convenient dosage forms containing a unit dose of one or more medicament. Green tea extract can be prepared from the green tea leaves. With the green tea extract by the use of excipients such as disintegrating agents, binders, glidants, lubricants, Organoleptic additives such as sweeteners, flavoring agents green tea tablets can be prepared for easy intake and effective action. Green tea can also be formulated as both effervescent and dispersible tablets.

4

INVESTIGATION OF CNS DEPRESSANT, ANTI-DIARRHEAL AND CYTOTOXIC ACTIVITIES OF CRUDE METHANOLIC EXTRACTS OF ACACIA NILOTICA AND JUSTICIA ADHATODA ROOT

Fahad Hussain, Saikat Kumar Poddar, Amlan Ganguly, S.M. Abdur Rahman
Department of Clinical Pharmacy & Pharmacology, Faculty of Pharmacy, University of Dhaka.

Abstract

A long tradition of indigenous herbal medicinal systems, based on rich local plant diversity, is considered as an important component of primary health care system in Bangladesh. The main purpose of this study is screening of methanolic extracts of Acacia nilotica and Justicia adhatoda roots for possible CNS depressant, Anti-diarrheal and Cytotoxic activities in experimental swiss albino mice. After collection, plants were dried, powdered and extracted by methanol, followed by n-hexane, ethyl acetate, and chloroform fraction for getting the sample root extracts. Swiss-albino mice were used for CNS depressant, Anti-diarrheal effect assay whereas Artemia salina leach was for the cytotoxic activity screening. Sodium-phenobarbitone induced sleeping time, castor oil induced diarrhea and brine shrimp lethality bioassay were followed for CNS depressant, Anti-diarrheal and cytotoxic activity assay. Dunnett t-test analysis was done by SPSS version 19 on windows. The methanolic extract of A. nilotica root at the doses of 200 mg/kg and 400 mg/kg body weight showed highly significant (P<0.001) CNS depressant activity. In case of anti-diarrheal activity assay, A. nilotica at the dose of 400 mg/kg showed 41.37% inhibition of defecation which is comparable to the value obtained by standard Loperamide (58.62%). In cytotoxicity testing, methanolic extract of J. adhatoda root showed mild cytotoxicity (LC50 58.61μg/ml) while for the A. nilotica, it appeared as 42.55 μg/ml compared to the value obtained by standard Vincristine Sulfate (0.544 μg/ml).These current findings confirm that the methanolic extracts of A. nilotica and J. adhatoda root exhibited prominent CNS depressant, anti-diarrheal potential and less cytoxicity.

 

5

MICROBALLOONS: A NOVEL APPROACH FOR GASTRORETENTION

Dhyani Archana, Thakur Sujata*, Juyal Divya
Himalayan Institute of Pharmacy and Research, Rajawala, Dehradun, Uttarakhand.

Abstract

The purpose of this review is to accumulate the recent study on floating drug delivery system with special emphasis on microballoons as drug delivery. Microballoons are emerging as the most promising drug delivery as it overcome many limitations of conventional drug delivery system. As microballoons delivery system provides longer retention in gastric pH, hence longer is the residence time and therefore enhance the solubility of drugs that are less soluble in high pH environment. The formation of cavity inside the microsphere depends upon the preparation temperature and the surface smoothness determines the floatability and the drug release rate of the microballoons.The review includes the classification, advantages, disadvantages, method of preparation and future aspects of microballoons. Basic anatomy and physiology of stomach is also studied.

6

A STUDY TO EVALUATE RATIONALITY BEHIND PRESCRIPTION PATTERNS USING WORLD HEALTH ORGANIZATION PRESCRIBING INDICATORS

Pratap Devi Shankar Sai Prakash1*, Dr. Vinay Umesh Rao1, Dr. Prashanth R Kokiwar2, Sunkari Sowmya1, Gyara Vishweshwaran1
1Malla Reddy College of Pharmacy, Osmania University, Hyderabad, Telangana.
2Malla Reddy Institute of Medical Sciences, Dr NTR University of Health Sciences, Hyderabad, India.

Abstract

Title: A study to evaluate the rationality behind the prescription pattern using World Health Organization Prescribing indicators. Objectives: To obtain prescribing patterns in study sites of Ranga reddy district. To evaluate the rationality behind the prescription patterns. Study design, Study period and Study site: A cross sectional evaluation study conducted from March – August 2014 in randomly selected study sites in Ranga reddy district. Methodology: There are a total of 516 pharmacies in Ranga reddy district out of these 20% of the pharmacies i.e., a total of 106 pharmacies were visited in morning hours and prescriptions coming to that pharmacy were studied at the day. Results: A total of 4000 prescriptions were collected and evaluated. The average number of drugs prescribed was 2.31 per patient visit. The Antibiotics or injections during an encounter prescribed were determined to be 30.3% and 5.7%, respectively. In addition, the total percentage of drugs prescribed by both generic name essential drug list were less than 0.5%% and 53%, respectively. The commonly prescribed drug classes in highly accounted diseases respective of their each physiological disease system. Conclusions: On evaluation of the study, over prescription of the drugs has been resulted. Antibiotics prescribed were shown over the standard recommended range by World Health Organization. On the other, generic prescribing and prescribing from EDL were found to be a key problem in this study. Prescribing patterns of drugs were highly deprived from the standard value recommended.

7

PRESCRIBING PATTERN OF DIFFERENT ANTIBIOTICS AND ANALGESICS USED IN PATIENT WITH DIABETIC FOOT ULCER

Elahe Elhami1*, Kiran Nagaraju2
1Pharm D, In Visveswarapura Institute of Pharmaceutical Sciences, Bangalore.
2Assistant Professor, Department of Pharmacy Practice, Visveswarapura Institute of Pharmaceutical Sciences, Bangalore.

Abstract

The present study was to investigate the antimicrobial susceptibility pattern of microbes in DFIs. We used the patient database to conduct a retrospective observational study of hospitalized patients with diabetic foot infections. Patient record system, which contains patient demographics, diagnoses, diagnostic studies, treatments received and patient outcomes. Diabetes mellitus with foot ulcer was observed to be higher in patients with the age group of 40-50 years, affecting (59.33%) male and (40.66%) females. The most common comorbid conditions observed by us were Nephropathy. In our study antibiotic drugs were prescribed as monotherapy in 26 (17.33%) patients. Two drug combinations were prescribed to 46 (30.66%) patients and 3 drug combinations were prescribed to 100 (66.66%) patients. In the present study S.aureus 39(26%) was predominantly isolated. As regards the aerobic Gram negative bacilli, 56(37.33%) were E.coli, 21(14%) were Ps.aeruginosa, 12(8%) were k.pneumoniae, 10(6.66%) were c.koseri, 7(4.66%) were Citrobacter spp, 5 (3.33%) was p.vulgaris. Out of 396 antibiotic drugs prescribe the most commonly used antibiotic drugs are amino glycoside (21.46%), Quinolones (20.2%) and cephalosporin’s (19.44%).In our study analgesic drugs were prescribed as monotherapy in 45 (30%) patients. Two drug combinations were prescribed to 79 (52.66%) patients and 3 drug combinations were prescribed to 26 (17.33%) patients. Out of 281 analgesic drugs the most common drugs were, 17.79% lidocaine Hcl and Tramadol follow by 17.08% Aceclofenac and14.23% Paracetamol. The percentage of generics prescribed in our study (9.33%) is very low.

8

DEVELOPMENT AND VALIDATION OF HPLC-UV METHOD FOR THE ESTIMATION OF STAVUDINE IN HUMAN PLASMA

Rama Mohan Reddy Thummaluru*, Srikanth Gurrala
Department of Pharmaceutical Chemistry, CMR College of Pharmacy, Kandlakoya (v), Medchal, Hyderabad, Telangana.

Abstract

The present work aimed to develop a simple, rapid, selective and sensitive validated HPLC method for the determination of stavudine in human plasma by liquid-liquid extraction technique. Stavudine was measured using a validated HPLC method with UV detector at 265nm chromatographic peaks were separated on Hypercil, C18 column (250 mm x 4.6 mm x3.5μ) using 90.9: 8: 1: 0.1 v/v 10mM ammonium acetate pH 3.5, methanol, acetonitrile and glacial acetic acid as mobile phase at a flow rate of 1 ml/min. The maximum recovery was obtained by extracting the drug with tertiary butyl methyl ether from human plasma. The chromatograms showed good resolution and no interference from plasma. The retention time of stavudine and internal standard (4μg/ml) (Hydrochlorothiazide) were approximately 8.44±0.05min and 6.25±0.03min respectively. The mean recovery from human plasma was found to be above 62%. The method was linear over the concentration range of 0.05to 2μg/ml with coefficient of correlation (r2) 0.988. The intraday and interday precision and Accuracy of the method was found to be 0.76 to 3.22% and 99.78 to 102.83 respectively. The low % RSD values (≤ 2) indicated that the method was precise, accurate and successfully applied to forced degradation studies and can be adopted for routine estimation of stavudine in quality control laboratories. This method was successfully applied to pharmacokinetics studies.

9

FORMULATION AND EVALUATION OF TIME DEPENDANT RELEASE OF MONTELUKAST TABLET USING MINI TABLET TECHNOLOGY

Talath Fatima*1, 2, Anas Rasheed2, Amer Mahboob1, 2, Afiya Ansari1, 2, Amatullah Fathimah1, 2, Humeera Rafeeq1, 2.
1Deccan School of Pharmacy. Hyderabad-01, Telangana.
2Spectrum Pharma Research Labs. Hyderabad, Telangana.

Abstract

Asthma is a very common disorder in many countries all over the world, resulting in hyper responsiveness of airways exhibiting chronic inflammation and obstruction of the respiratory tract. Montelukast is a Leukotriene Receptor Antagonist (LTRA) probably used for the management of asthma. This drug acts by limiting the activity of substances that trigger the attack of asthma. The aim of this formulation and evaluation of time dependant release of Montelukast tablet using mini tablet is to enhance and prolong the bioavailability of Montelukast via, first pass mechanism. It shows plasma or biological half-life 2.5 to 5.5 hrs, thereby decreasing bioavailability up to 64%. The present work describes such delivery system, which will improve the biological half-life as well as bioavailability of Montelukast. This makes Montelukast a suitable candidate for incorporation in sustained-release dosage form and was used as a model drug. In the present work an attempt has been made to prepare Coated Mini-Tablets-In-Capsule System (CMTICS) containing both Immediate-Release (IRCMT) and Sustained-Release Coated Mini-Tablets (SRCMT) of Montelukast which may lead to increased bioavailability. The aim was to specifically target the nocturnal peak symptoms of asthma. The core mini-tablets were prepared using wet granulation method. The mini-tablets prepared were evaluated for various parameters like weight variation, hardness, friability, drug-polymer interaction, drug content, in-vitro disintegration time and in-vitro drug release. The compatibility of drug with other ingredients was checked by FTIR and DSC studies. The core mini-tablets of both IRCMT and SRCMT prepared possess a weight variation of 80.4±0.69 mg and 79.5±1.58 mg respectively, which is below 10 %, hardness of 3.5±0.2 kg/cm2 and 4.03±0.057 kg/cm2 respectively, percentage friability of 0.23±0.05 and 0.18±0.08 respectively, drug content uniformity was 98.51±0.44 % and 97.04±0.76 % respectively. The core mini-tablets of IRCMT was found to disintegrate within 16±0.17 min. In-vitro drug release showed 26.47 % and 25.99 % of Montelukast sodium release in an hour as an immediate-release phase and 97.07% and 98.74% of Montelukast sodium was sustained for a period of 24 hrs. Release of Montelukast from all the formulations was First-order and mechanism was Quasi-Fickanian diffusion. This helps in advancement of medication or dosages for geriatrics.

10

SYNTHESIS OF 1-(-4-METHYL PHENYL)-2-(3-BROMO PHENYL) -4-(4-SUBSTITUTED BENZYLIDENE ) -5-IMIDAZOLONES

R. M. Kedar, S. A. Deshmukh
P.G.Deptt of Chemistry, Shri Shivaji Science College, Amravati.

Abstract

In this work some new imidzolones have been reported from bromo substituted oxazolones in presence of zeolite as a catalyst. The bromo substituted oxazolones in turn were obtained from bromo benzoyl glycine and variedly substituted aromatic aldehydes in presence of acetic anhydride and anhydrous sodium acetate. The ten variedly substituted compounds were prepared by this method. Reflux time in the synthesis of 5-imidazolones was significantly reduced by employing Zeolite as a catalyst. The characterisation of these compounds was made by chemical properties, elemental analysis as well as spectral analysis (like IR,1H-NMR).Most of the synthetic methods required longer reflux time and tedious work out of the product formed but use of zeolite as a catalyst afforded us shorter reflux time ,easy to work out procedure and increased percent yield of the products.

11

PHARMACEUTICAL ‘GOOD MANUFACTURING PRACTICES’ AND ‘GOOD DISTRIBUTION PRACTICES’- A COMPARATIVE REVIEW OF DILIGENCE IN REGULATORY STANDARDS

Nirmal Kumar*, Dr (Prof) Ajeya Jha
Department of Management Studies, Sikkim Manipal Institute of Technology, Majhitar, Sikkim, India-737132.
 

Abstract

The objective of the study is to compare the persistence of provisions of quality systems prescribed for pharmaceutical manufacturing and distribution i.e Good Manufacturing Practices (GMP) and Good Distribution Practices (GDP). Method: The approach shall be exploratory studies, based on regulatory standards on ‘Good Manufacturing Practices’ and ‘Good Distribution Practices’. These practices are regarded as quality system during pharmaceutical manufacturing and distribution operations respectively. The quality system guidance have been issued by various agencies like, USFDA, EMEA and WHO. Result: There is more emphasis on maintaining quality system during product manufacturing process, whereas that during distribution process is not elaborative. The global pharmaceutical regulators have invoked adequate provisions to ensure quality system during manufacturing process which is more rigorous as compared to that during distribution process. Conclusion: Each pharmaceutical manufacturer should design suitable quality system that shall take care of product quality during their plant operation as well as distribution operation.

12

SWIFT ELECTROCHEMICAL DETECTION OF ANTI-ESTROGENIC DRUG CLOMIPHENE AT BI2O3 – MWCNTS FILM SENSOR

Jahangir Ahmad Rather1*, Vikas2, Dhanjai3, Palanisamy Kannand4
1Department of Chemistry, Sultan Qaboos University, Box 36, Al-Khod 123, Oman.
2Department of Chemistry, Shrimant Madhavrao Scindia P.G.College Shivpuri (M.P).
3School of Studies in Chemistry, Jiwaji University, Gwalior-474011, India.
4Singapore Centre for Environmental Life Sciences Engineering (SCELSE) Nanyang Technological University, 60 Nanyang Drive, Singapore – 637551.

Abstract

A sensitive electrochemical sensor for swift detection of clomiphene was developed based on the enhanced electrochemical response at glassy carbon electrode modified with film of nanoparticles of bismuth (III) oxide (Bi2O3) and multi-walled carbon nanotubes (MWCNTs). The developed sensor Bi2O3-MWCNTs/GCE was characterized by scanning electron microscopy (SEM) and electrochemical methods. Cyclic voltammetric studies of clomiphene indicated that the oxidation process is irreversible and diffusion-controlled. The proposed squarewave voltammetric method was linear over the concentration range of 50 ng mL-1 to 800 ng mL-1 with detection limit (LOD) and quantification limit (LOQ) of 18.68 ng mL-1 and 55.45 ng mL-1, respectively. The results indicate that the present sensing platform (Bi2O3-MWCNTs/GCE) shows good sensitivity, good accuracy, and reproducibility for the swift detection of clomiphene in pharmaceutical dosages.

13

DEVELOPMENT OF A STABILITY INDICATING RP-HPLC METHOD FOR RELATED SUBSTANCES OF BENZOYL PEROXIDE AND CLINDAMYCIN PHOSPHATE UNDER COMMON CHROMATOGRAPHIC CONDITIONS

Prakashkumar B. Modi12*, Nehal J. Shah2,3
1Analytical Research & Development, IPDO, Dr. Reddy’s Laboratories, Bachupally, Hyderabad-500072, Andhra Pradesh, India.
2School of Pharmacy, RK University, Kasturbadham, Rajkot-360020, Gujarat, India.
3Pharmaceutical Chemistry, Indubhai Patel College of Pharmacy and Research Centre, Dharmaj-388430, Gujarat, India.

Abstract

A stability indicating RP-HPLC method is developed for the estimation of related substances of Benzoyl peroxide and Clindamycin phosphate. Being a complex combination, where clindamycin phosphate can be oxidized in the presence of benzoyl peroxide, if both are in solution state. Method established with common chromatographic conditions for the estimation of benzoyl peroxide (BPO), benzoic acid (BA), benzaldehyde (BENZ), ethyl benzoate (ETHB), clindamycin phosphate (CP), lincomycin hydrochloride (LINCO) and clindamycin hydrochloride (CLINDA). Unique diluent system was established for BPO and CP to avoid interaction while chromatographic conditions are common. Separation of all analytes was achieved with Xbridge C18 (50 × 4.6 mm, 3.5 μm) as stationary phase using variable mixture of pH 3.80 triethyl amine buffer and organic solution (acetonitrile: methanol, 90: 10, v/v) as mobile phase with gradient elution. UV detection of BPO and CP related impurities was carried out at 272 nm and 210 nm respectively. The proposed method was successfully validated as per ICH guideline and utilized for the related substances estimation in marketed gel formulations of BPO and CP. The proposed method could be used in pharmaceutical industries to monitor the related substances of BPO and CP in pharmaceutical dosage forms.

14

ROLE OF POLYMERS AND THEIR ROLE IN FUNCTIONAL ASPECTS OF SWELLABLE MUCOADHESIVE HYDROGEL BEADS - A REVIEW

K. V. Ramana Redddy*1 , M. V. Nagabhushanam2, P. Srikanth Chowdary3
1KVK College of Pharmacy, Himayath Nagar.Lashkar Guda, Ranga Reddy Dt.Telangana State. India-501512.
2Hindu College of Pharmacy, Guntur, Andhra Pradesh .India-522 002.
3Vision College of Pharmaceutical Science and Research, Uppal, Hyderabad. Ranga Reddy Dt. Telangana State. India-500 039.

Abstract

Hydrogel structures having three dimensional networks which imbibe water or biological fluids in large amount at least 15-20 times their molecular weight, thus become swollen. The most important representatives of this group of polymers are cellulose ethers such as hydroxypropylmethyl cellulose, methyl cellulose, and hydroxy ethyl cellulose. Upon water contact, these polymers swell and undergo a transition from the glassy to the more permeable rubbery state resulting in the formation of a gel layer. Drug release from a swellable matrix is mainly controlled by the rate of swelling of the polymer and the drug diffusion through the gel. The gel layer thickness is time dependent, which is important for the drug release kinetics. After the entire polymer has been subjected to hydrate then gel layer thickness becomes decrease.

15

A NOVEL SYNTHESIS ROUTE TO INDOLOPYRIDOQUINAZOLINE ALKALOID ANALOGUES FROM CONDENSED PYRIMIDINE SCAFFOLDS

Rahul H. Khiste*1,2, Ashok G. Peepliwal1, Hemant Kumar Jain3
1NIMS University, Jaipur 303121, Rajasthan, India.
2Marathwada Mitra Mandal’s, College of Pharmacy, Thergaon, (Kalewadi) Pune 411033, Maharashtra, India.
3Sinhgad College of Pharmacy, Vadgaon (Bk), Pune 411041, Maharashtra, India.

Abstract

Development of new, elegant synthetic routes to bioactive quinazolinocarboline alkaloids Rutaecarpine, Euxylophoricine and their analogues is a challenging task of current interest. The present work focuses on a novel synthetic approach to Indolopyridoquinazoline and it’s derivatives. The pentacyclic compounds were synthesized efficiently by using various condensed 2-chloromethyl pyrimidine scaffolds as important heterocyclic building blocks. This approach has been extended to the synthesis and diversification of compounds based on cyclization of a variety of nitriles with o-aminoesters of benzene, dimethoxybenzene under acidic conditions for pyrimidine scaffolds. Starting from condensed pyrimidine scaffolds, we have demonstrated an elegant five step practical synthesis of bioactive natural Indolopyridoquinazoline alkaloid analogues. This novel synthetic approach is amenable for the generation of library of bioactive Indolopyridoquinazoline analogues.

16

UV SPECTROPHOTOMETRIC ANALYSIS FOR THE DETERMINATION OF TRAMADOL HYDROCHLORIDE IN PHARMACEUTICAL FORMULATION

Bhagyashree R. Dhumal1, Kishore P. Bhusari1, Mahavir H. Ghante, Nishant S. Jain*2
1Sharad Pawar College of Pharmacy, Hingna Road, Wanadongari, Nagpur-441110, India.
2Institute of Pharmaceutical Sciences, Guru Ghasidas University (A Central University), Bilaspur-495009 (C.G.), India.

Abstract

The proposed UV spectrophotometric method for the determination of tramadol hydrochloride in the pharmaceutical formulations was found to be specific, precise and validated as per ICH guidelines. The methods are carried out for tramadol hydrochloride at 271.0 nm in distilled water with linearity in the concentration range of 5-25 μg/ml. The validation for specificity, precision, robustness and recovery of the method was also performed. The present methods were found to be simple, linear, precise, accurate and sensitive and can be used for routine quality control analysis for the estimation of Tramadol Hydrochloride in bulk and capsule dosage form.

17

BIOISOSTERES OF BRASSININ: SYNTHESIS, MOLECULAR DOCKING AND CHEMOTHERAPEUTIC ACTIVITY

O. Navneetha1, S. Anuradha Bai1, M. S. N. Sandhya1, Sree Kanth Sivan2, Vijjulatha Manga2, Saritha Jyostna Tangeda1,
1Department of Pharmaceutical Chemistry, Sarojini Naidu Vanitha Pharmacy MahaVidhyalaya, Tarnaka, Secunderabad, 500017, India.
2MMMC Group, Department of Chemistry, University College of Science, Osmania University, Hyderabad – 500007, India.

Abstract

A series of benzimidazoledithiocarbamate derivatives (5a-l) were synthesized by using key intermediate 2-(α-chloroethyl) benzimidazole following the addition of carbon disulfide and various amines. All the synthesized compounds were characterized by modern analytical tools. The present study deals with evaluation of dithiocarbamate derivatives for antibacterial, antifungal and antioxidant activities and to perform the docking studies inorder to know the binding affinities of derivatives with receptor active site. Furthur docking studies revealed that the molecules are more selective for anticancer activity than antimicrobial activity.

18

DEVELOPMENT AND VALIDATION OF STABILITY INDICATING RP-HPLC METHOD FOR SIMULTANEOUS ESTIMATION OF ATORVASTATIN AND TELMISARTAN IN BULK AND PHARMACEUTICAL FORMULATIONS

Pasala Mounika, Bonthu Mohan Gandhi*, Vatchavai Bhaskara Raju, Kamatham Srinivas Sumanth, Venkata Koteswaramma Kagitapurapu, Kolli Srinivas, Meesala Santhi Neelima
Sri Vasavi Institute of Pharmaceutical Sciences, Pedatadepalli, Tadepalligudem-534101, Andhra Pradesh.

Abstract

The main objective of the present work was to develop and validate a simple, fast, precise, selective and accurate RP-HPLC method for the simultaneous determination of Atorvastatin and Telmisartan in Pharmaceutical formulations & to perform forced degradation studies. Different Columns and mobiles phases were tried for the development of this method. Finally, the separation of these two drugs was achieved on a SHISHEDO C18, 250×4.6mm, 5 micron size column with a mobile phase consisting of acetonitrile and phosphate buffer (45:55 v/v) at pH 2.5 with flow rate of 1.2 ml/min and UV detection at 254nm. The retention times were observed to be 3.150 and 5.660 minutes for Atorvastatin and Telmisartan respectively. Linearity was found to be 25-125 μg/ml and 50-250 μg/ml for Atorvastatin and Telmisartan respectively. The method was statistically validated for linearity, recovery, limit of detection, limit of quantification, accuracy and precision. The forced degradation studies were performed by subjecting the drugs individually and in their mixture under different conditions like acidic, alkaline, peroxide, photo-degradation and thermal degradation conditions, their degradation products are well resolved from the analyte peaks. The method was successfully validated for accuracy, precision, linearity, limit of detection, limit of quantification & robustness. Forced degradation studies were also performed successfully for HPLC method. This method can be successfully employed for the simultaneous estimation of atorvastatin & telmisartan in bulk and pharmaceutical dosage forms.

19

BILAYER RELEASE TABLET: CLINICAL OUTCOME AND EVALUATION

Duve Amol Baburao*, Pentewar R.S, Sayyed Sarfaraz Ali, Kamble Santosh, Patil Kishore
Department of Pharmaceutics, Channabasweshwar Pharmacy College, Latur, Maharashtra.

Abstract

Bilayer tablet is new era for the successful development of controlled release formulation along with various features to provide a way of successful drug delivery system. Bi-layer tablet is suitable for sequential release of two drugs in combination, separate two incompatible substances and also for sustained release tablet in which one layer is immediate release as initial dose and second layer is maintenance dose. Novel technologies with improved performance, patient compliance and enhanced quality have emerged in the recent past. Multilayer tableting is getting increasing attention for a variety of reasons like patent extension, therapeutic effect, marketing to name. The goal in designing the bilayer tablets are suitable for the sequential release of two drugs in which one layer is immediate release as loading dose and second layer as maintenance dose. The Fixed Dose Combination (FDC) of two or more drugs in single dosage form, which is more safe and effective for single or different diseases. The bimodal release of formulation is mainly used to achieve rapid and extended release in a single dosage form. For good quality bilayer tablet, the machinery should be constructed as per GMP. The present study focuses the dual release tablets on different types of press, technology and the process used.

20

HEPATO– AND NEPHRO – PROTECTIVE EFFECT OF TINOSPORA CORDIFOLIA AGAINST SODIUM NITRITE – INDUCED OXIDATIVE STRESS

Manju Bala1 , Girdhari Lal Gupta2*
1Jaypee University of Information Technology, Waknaghat, Solan, Himachal Pradesh, India.
2School of Pharmacy and Technology Management, SVKM’s NMIMS University, Mumbai, Maharashtra, India.

Abstract

Sodium nitrite (NaNO2) is widely used as a bacteriostatic and preservative for meats and fish. Meanwhile, NaNO2 is also associated with detrimental health effects on liver and kidney. Moreover, no scientific validation is available for traditionally used Tinospora cordifolia (Willd.) Hook. f. and Thoms. (Guduchi) in NaNO2 induced oxidative stress. The objective of the present investigation was to evaluate the effects of ethanolic extract of stems of Tinospora cordifolia (Willd.) (ETC) in NaNO2 induced oxidative stress, hepatic and renal dysfunction. Twenty–four adult male Sprague–Drawly rats were daily treated with sodium nitrite (80 mg/kg) in the presence or absence of ETC (200 mg/kg) for three months. Biochemical and morphological changes were assessed in liver and kidney sections. ETC significantly restored SOD, catalase and glutathione level compared with sodium nitrite. ETC also reduced serum SGOT, SGPT, urea, creatinine, malondialdehyde and nitric oxide level as compared to sodium nitrite treated group. Therefore, It is suggested that ETC has hepato– and nephro–protective effect against sodium nitrite–induced oxidative stress.

21

FORMULATION DEVELOPMENT OF RIVAROXABAN LIPID SOLID DISPERSION USING DIFFERENT TECHNIQUES FOR THE DISSOLUTION ENHANCEMENT

M. Ganesh1, Dr. B. Chandra Shekar2, Prof (Dr). Y. Madhusudan3 

1Jawaharlal Nehru Technological University, Kukatpally, Hyderabad-72, Telangana. 

2Bomma Institute of Pharmacy, Allipuram, Khammam -507318, Telangana. 

3Vagdevi College of Pharmacy, Hanmakonda, Warangal, Telangana.

Abstract

Rivaroxaban drug used in acute coronary syndrome (ACS), Prevention of cardiovascular death, myocardial infarction and stent thrombosis. Rivaroxaban is a potent selective oral direct factor Xa inhibitor, Rivaroxaban BCS Class II. Depending on the choice of excipient(s) and formulation techniques, it is possible to obtain a variety of systems including physical mixtures, liquid/solid solutions, solid dispersions, and Self-Micro or Self-Nano Emulsifying Drug Delivery Systems (SMEDDS/SNEDDS).Lipid based formulations including lipid solid dispersion formulations offer the potential for enhancing the dissolution and absorption of poorly soluble and/or poorly permeable compounds. Lipid solid dispersions are prepared by three different techniques Solvent evaporation, Hot melt granulation and Spray drying method and evaluated by drug content, saturation solubility, particle size analysis and in-vitro dissolution. Comparative evaluation of three different techniques studied and Spray drying method (SDRD8) shows better dissolution profile as comparative to the other two techniques and marketed market product. Spray dried formulation was stable at accelerated condition.

22

TO INVESTIGATE ANTI-ARTHRITIC ACTIVITY OF PSORALEA CORYLIFOLEA EXTRACT AND CLOZAPINE IN RATS

Dimple N. Thakkar
L.J. Institute of Pharmacy, Ahmedabad, Gujarat, India.

Abstract

In the Arthritis, immune system of the body will target its own tissues and results in Inflammation. Furthermore, Signalling Pathway like Akt phosphorylation, PI3 kinase activation and jak-stat pathway also plays a major role. This study was carried out to Investigate Anti-Arthritic activity of Psoralea Corylifolea and Clozapine in rats. Psoralidin which is one of constituent of Psoralea Corylifolea inhibits above mentioned Signalling pathway which involves in arthritis. [1] Clozapine shows immunosuppressant effect which proved beneficial role in Rheumatoid Arthritis. In this study, Carrageenan Induced Paw Edema and Complete Freund’s adjuvant (CFA) Induced Arthritis Methods were used to evaluate anti-Inflammatory and anti-arthritic effect of study drugs respectively. In both the methods, selected rats were randomly grouped as per their body weight into normal control, arthritic rats and treated rats (Includes Standard and Test Treatment). The effects of drugs were evaluated by change in paw volume, body weight and arthritis index, change in erythrocyte sedimentation rate (ESR), detection of serum rheumatoid factor (RF), blood cell count, SGOT, SGPT and by histopathology of knee joint before and after treatment. For both the drugs, results showed that % Inhibition in Paw volume was observed 84.53 in Psoralea corylifolea (P) and 60.89 in clozapine(C). Arthritic Index was decrease up to 0.033 in both the test groups. RA factor was not significantly decreased in P extract (50 mg/kg) treated group as compared with Disease control group. But it was significantly decreased in P extract 50 mg/kg+ C 1.25 mg/kg, Methotrexate (1 mg/kg) treated groups. Hb increased 2.25 gm/dl in P, 2.30gm/dl in C. RBCs were significantly increase by 1.36cmm in P, 0.83cmm in C. WBCs were significantly decreased by 0.44 cmm in P while 1.413 cmm in C. SGPT was decreased by 7.08 U/L in P while increased by 13.16 U/L in C. SGOT was decreased by 35.28 U/L in P while increased by 16.88 U/L in C. Combined treatment of P and C (P+C) showed Synergistic effect.

23

ENHANCEMENT OF SOLUBILITY BY USING HYDROXYPROPYL B-CYCLODEXTRINS OF LIPOPHILIC DRUG AND FORMULATION OF FAST DISSOLVING TABLET

Pentewar R. S*, Kshirsagar Nilesh, Sayyed Sarfaraz Ali, Nasheer Shaikh, Gapat Sandeep
Department of Pharmaceutics, Channabasweshwar Pharmacy College, Latur, Maharashtra, India.

Abstract

The main aim of the present study was to evaluate Azithromycin and Chloroquine drug in combination therapy used in the treatment of Chloroquine resistant malaria by increasing the solubility and dissolution rate of Azithromycin and Chloroquine phosphate by complexation techniques using hydroxypropyl β-Cyclodextrins with varying concentrations and after selection of proper ratio with carriers an attempt was made to develop and evaluate fast dissolving tablet of Azithromycin Chloroquine phosphate using synthetic super disintegrates. The main objective of the present investigation is to explore the possibility of improving low solubility and hence dissolution profile of Azithromycin and Chloroquine phosphate with fewer side effects and reduce dosage regimen with less toxicity for treatment for many acute and chronic disease. Evaluation of solubility profile, the pre and post compression parameters of the tablets, drug content, % drug release formulation containing hydroxypropyl β-Cyclodextrins from Azithromycin FDT shows 71.25 to 86.0% at the end of 45 min and Chloroquine phosphate shows 76.33 to 86.4% drug release at the end of 45 min., drug content of all the formulations were with its range and the disintegration time 19-29 Sec. Hence HPβCD technology can open up new perspectives for both existing and future drugs as new dosage forms, new administration routes and new formulations become available.

24

FORMULATION AND EVALUATION OF CONTROLLED RELEASE GASTRO-RETENTIVE MUCO-ADHESIVE MICROSPHERES FOR DILTIAZEM HYDROCHLORIDE

Nishan N. Bobade*, Pritesh V. Ambalkar, Shubham P. Malviya, Aashish V. Makdeja, Shrikant D. Pande
Department of Pharmaceutics, Vidya-Bharati College of Pharmacy, C. K. Naidu Road, Camp Amravati, Dist. Amravati, State Maharashtra. India 444602.

Abstract

In present study is to develop Controlled release muco-adhesive microspheres using natural and synthetic polymers. Controlled release microspheres are one of the multi-particulate delivery systems and are prepared to obtain prolonged or controlled drug delivery, to improve bioavailability, stability, reducing side effects. Controlled release muco-adhesive a microsphere of Diltiazem Hydrochloride was successfully prepared using sodium alginate, Chitosan and HPMC K4M as polymer by the emulsification-internal gelation technique. The prepared formulations were subjected to particle size and shape analysis, % drug entrapment efficiency, swelling rate, in vitro muco-adhesion and in vitro drug release studies. The prepared microspheres were discrete, aprrox spherical with a mean particle size in the range of 513.39 ± 1.21 μm to 839.32 ± 2.24 μm. Entrapment efficiency was found to be in the range of 79.71± 1.134% to 86.13 ±1.065%. Optimized Formulation contains 180 mg Diltiazem Hydrochloride, 600 mg sodium alginate, 225 mg HPMC K4M, 225 mg Chitosan, 74 mg Barium carbonate. The result of optimized formulation for Percent yield, Particle size, Drug Entrapment Efficiency, % Cumulative Drug Release are 91.48 %, 801.789 μm, 2.64, 91.23 %, 83.57 % respectively. Formulated muco-adhesive microspheres were stable at the selected temperature and humidity in storage for 3 month. From the stability studies it was found that there was no significant change in the drug content and release characteristics. It was concluded that the prepared Controlled release muco-adhesive microspheres of Diltiazem Hydrochloride may prove to be potential candidate for safe and effective Controlled drug delivery for extended period of time.

25

EFFECT OF SUPERDISINTEGRANTS ON IN-VITRO DRUG RELEASE OF ACECLOFENAC AND PARACETAMOL TABLET

Mr. Samir Patil, Miss. Sayali Lokhande, Mr. Tejas Mahajan, Dr. Tushar Deshmukh
Department of Pharmaceutics S.E.S. Arunamai College of Pharmacy, Mamurabad, Jalgaon, Maharashtra, India.425002.

Abstract

Aceclofenac is the potent phenyl acetic acid derivatives having effective anti-inflammatory and analgesic properties. Paracetamol is the major metabolite of Phenacetin and has similar analgesic-antipyretic action but it does not possess anti-inflammatory or anti rheumatic activity. Aceclofenac and Paracetamol are practically insoluble and for poorly soluble orally administered drug, the rate of absorption is often controlled by the rate of dissolution. Faster disintegration of tablets delivers a fine suspension of drug particles resulting in higher surface area and faster dissolution. Formulation of fast dispersible tablet of aceclofenac and paracetamol using wet granulation technique and their evaluation has been attempted in the present study. The behavior of superdisintegrants likes Croscarmellose sodium, Crospovidone and sodium starch glycolate in the formulation has also been studied. Said tablets were evaluated for different parameter like Disintegration, Drug Content Uniformity and In- vitro drug release studies etc. Results show that Croscarmellose sodium is having good disintegrant property with increasing concentration. But in combination with Crospovidone and sodium starch glycolate it showed better disintegrant property. Results also revealed that if the concentration of sodium starch glycolate increases, disintegration time increases. From the behavior of superdisintegrants, it can be concluded that superdisintegrants can work better in combination with each other than single. Hence, it was worthwhile to formulate and evaluate dispersible tablets of aceclofenac and paracetamol using this disintegrants.

26

RED ALGAE DIVERSITY FROM THOOTHUKUDI AND ITS THERAPEUTIC POTENTIALS: A SEARCH

Sumayya S S, Bosco Lawarence, Manoj G S & Murugan K*
Plant Biochemistry and Molecular Biology Laboratory, Department of Botany, University College, Thiruvananthapuram 695 034, India.

Abstract

Red algae are one of the ancient and largest groups of eukaryotic algae. Most of them are multicellular seaweeds. They provide habitat for near-shore benthic floras and are also considered ecologically unique as they contribute substantially to primary production. Most of the red algae are economically important in pharmaceutical and cosmetic industries. Increasing concern on destruction of seaweed resources is noticed due to anthropogenic and climatic disturbances demand to study their diversity and species richness. Seaweeds include all the macroscopic algae occurring in the marine and brackish water habitats and are considered as one of the primary producers of the marine ecosystem. In the present study, the status of red algae variation along Thoothukudi coastal region was investigated. The sampling was conducted for six months from June to November 2015 to document the seaweed diversity of the coast. Total of 36 species belonging to 7 order, 11 family and 20 genera are documented. Gracilariaceae was the dominant family with 9 species, followed by Corallinaceae and Rhodomelaceae with 6 and 5 species each. The maximum species richness was found to be in the month of July in comparison to other months. Thus, the field exploration presents the current status of seaweed wealth of different beach fronts of Thoothukudi. Further, the present study showed the potential algal marine resources of this coast especially Kappahycus alvarezii and Hypnea musciformis. Future studies are designed to analyze the major lead molecule present in the selected red algae such as Kappahycus alvarezii and Hypnea musciformis and their therapeutical potentialities.

27

FORMULATION AND EVALUATION OF OXYBUTYNIN CHLORIDE EXTENDED RELEASE MATRIX TABLETS

S.B. Thirumalesh Naik*, Kambham Venkateswarlu, K. B. Chandrasekhar
Oil Technological Research Institute, Jawaharlal Nehru Technological University Anantapur, Ananthapuramu-515001, Andhra Pradesh, India.

Abstract

Formulation of Oxybutynin Chloride (OBC) matrix tablets offers good controlled release and less anticholinergic adverse effects in the treatment of overactive bladder (OAB) besides this it also reduces the dosage frequency. Matrix tablets were formulated by using HPMC K4M, HPMC K100M, Carbopol, Polyvinyl pyrrolidine (PVP), Ethylcellulose (EC) and Sodium alginate (SA) as release controlling polymers for 24 h by using direct compression method. For confirmation of compatibility, the pure drug and its physical mixtures were subjected to FTIR studies. All the formulations have shown acceptable limits in all precompression and post compression parameters. Dissolution studies of all the formulation were studied for 24 h, first 2h using 0.1N HCl and 6.8phosphate buffer for the remaining duration and found that formulation F8 with HPMC K4M has shown good controlled release for 24 h with cumulative release of 95.59% of drug release. From the kinetic studies, it was observed that formulation F8 showed first order drug release with the mechanism of drug release of non fickian diffusion.

28

PRODUCTION AND OPTIMIZATION OF PECTINASE BY BACILLUS SP. ISOLATED FROM VEGETABLE WASTE SOIL

Sukhvir Kaur*, Harjot Pal Kaur, Bhairav Prasad, Tejaswani Bharti
Assistant Professor, Shaheed Udham Singh College of Research and Technology, Tangori, Mohali.

Abstract

Microbial enzymes have shown tremendous potential for different applications. Over the years due to their remarkable features enzymes have occupied the centre stage of all the biochemical and industrial processes. Pectinases are a group of enzymes responsible for the hydrolysis of pectic materials found in plants and are important industrial enzymes. In the present study, pectinase is produced from Bacillus sp. that was isolated from vegetable waste dump soil samples. A total of five isolates showed pectinase production and designated as PPB1 to PPB5. The screened isolates were used as a source of pectinase production using cassava waste as a substrate. Isolate PPB5 showed maximum enzyme activity of 0.641 IU/ml. Pectinase activity was optimized for various parameters like incubation time, temperature, pH, different carbon and nitrogen sources. Enzyme activity was observed maximum at 96 hr of incubation, 35°C temperature and at pH 6. The best carbon was found to be glucose. Among organic and inorganic nitrogen sources yeast extract and ammonium nitrate was founded to be better than other nitrogen sources. Among the five isolates, the isolate PPB5 showed maximum activity at all optimum conditions. This isolate is best producer and can be used in future for further pectinase production.

29

STABILITY-INDICATING STRESS DEGRADATION STUDIES OF RILPIVIRINE HYDROCHLORIDE USING UV SPECTROPHOTOMETRIC METHOD

K. Vijaya Sri*, G. Vinay Jain, M. Madhuri
Department of Pharmaceutical Analysis, Malla Reddy College of Pharmacy, Maisammaguda, Secunderabad-500 014, TS, India.

Abstract

To develop a simple, precise, accurate, and stability indicating a UV-method for estimation of rilpivirine hydrochloride. Method A involves the method development and solvent was used as a methanol and water (8:2). Linearity in the concentration range of 0.5–3.5 μg/ml and absorbance was measured at 305 nm. Method B involves forced degradation studies of rilpivirine hydrochloride were carried out under hydrolytic, oxidation and photolytic as per stability indicating assay methods at different time intervals 0.5, 1, 2, 3,4,6, 12 and 24 hr and different temperature like room temp, 600 and 90.0 The low % RSD values are indicates the accuracy and precise of the method. The proposed methods can be successfully applied for method development, validation and stability study of rilpivirine hydrochloride. Degradation of rilpivirine hydrochloride was found to occur in alkaline, oxidation and neutral conditions whereas it was found to be stable in acidic and photolytic condition. The kinetic parameters (rate constant, t1/2, and t90) of the degradation of rilpivirine hydrochloride were calculated.

30

SYNTHESIS AND CHARACTERIZATION OF SILVER NANOPARTICLES USING ALLIUM CEPA AND ITS ANTI-INFLAMMATORY ACTIVITY AGAINST HUMAN BLOOD CELLS

P. Anitha1, P. Sakthivel2*
1Assistant Professor, Department of Physics, Roever College of Engineering and Technology, Perambalur, Tamilnadu, India.
2*Associate Professor, Department of Physics, Urumu Dhanalakshmi College, Trichy, Tamilnadu, India.

Abstract

In this paper, we report for the first time the use of onion leaf (Allium cepa) in the biosynthesis of silver nanoparticles (AgNPs) under microwave irradiation. Influence of various reaction parameters such as microwave irradiation power and microwave irradiation time was analyzed. The synthesized nanomaterial was characterized by UV-visible absorption spectroscopy and Fourier transforms infrared spectrum analysis. X-ray diffraction (XRD) and transmission electron microscopy (TEM) analysis confirms the formation and the crystalline nature of the synthesized nanomaterial. The average size of particle is found to be 22.62nm and 22.2nm by XRD and TEM analysis respectively. Further, these nanoparticles were found to exhibit AgNPs which may also be efficiently employed in Anti-inflammatory activity of Pharmaceutical research to obtain better result of plant as shown by our study. The anti-inflammatory activity of silver nanoparticles was tested and confirmed against human blood cells. The leaf of Allium cepa has good anti-inflammatory activity. Hence, the present research aims to open new avenues for the improvement of medicinal uses with the synthesis of silver nanoparticles by using Allium cepa extract for various ailments and to bring the anti-inflammatory medicinal plant to the scientist’s notice, to educate awareness and add values to the resources.

31

CHALCONES -VERSATILE AND EMERGING LEAD MOLECULES: SYNTHESIS, STRUCTURE DIVERSITY: A REVIEW

Dr. Srinivasa Rao .D1, Pavan Kumar G. V1*, Harika G2, Pooja B2, Anil Kumar Y3, Sadasiva Rao G3
1K C Reddy Institute of Pharmaceutical Sciences, Jangamguntapalem, Medikonduru (Md), Guntur (Dt), A.P, India.
2Sims College of Pharmacy, Mangaldas Nagar, Guntur (Dt) A.P, India.
3Hindu College of Pharmacy, Amaravathi Road, Guntur (Dt), A.P, India.

Abstract

Chalcones are 1,3-diphenyl-2-propene-1-one, in which two aromatic rings are linked by a three carbon α, β-unsaturated carbonyl system. These are abundant in edible plants and are considered to be precursors of flavonoids and isoflavonoids.In the development, chalcones do not only comprise derivatives of trans-1,3-diaryl-2-propen-1-ones, but also their analogs. Chalcones isolated from nature show exotic structure, which is sometime unrecognizable directly. The aim of this review to give summary of methods for synthesis of Chalcones, its chemical modifications to flavonoids, flavanone,oxazoles.Furthermore the bi-electrophile character of chalcone makes them more attractive to be used as synthon in the synthesis of heterocyclic compounds, such as pyrazoline, pyrimidinone, and benzazepine, through cyclo-condensation reaction with a bi-nucleophilic species. This article highlights the structure diversity of chalcone whether from nature or synthetic origin and various synthetic methods of chalcone are discussed.

32

COMPREHENSIVE ADVERSE DRUG REACTION MONITORING IN DERMATOLOGY DEPARTMENT

C. Pandu Varaprasad*, Nrithya S. Kumar, Anakha Thyag, H. Sreehari, M. Javeed Baig, E. Sam Jeeva kumar.
Department of Pharmacy Practice, P. Rami Reddy College of Pharmacy, Kadapa - 516003, AP, India.

Abstract

BACKGROUND: Dermatological Adverse drug reactions are one of the most common leading causes of morbidity and mortality. The increasing cause of ADR may diminished quality of life, increased physician visit, hospitalization and even death. Pharmacovigilence service is needed to increase the ADR reporting system MATERIALS AND METHODS: A prospective observational study carried out at Department of Dermatology at RIMS, kadapa over a period of six months. The inclusion criteria of the study were patients of all age groups with both genders, presenting in department of dermatology. Pregnant women were excluded in the study. Causality of ADRs was evaluated assessment scale such as Naranjo’s scale, WHO scale etc. RESULT: A total of 1963 study population, 169 patients with Drug related problem were screened. Among 8 drug related class, Adverse drug reaction 83(49.11%)is highly occurred in our study. out of 169 DRP’s ,83 ADR cases were found. The most suspected ADR were Skin rashes/lesions/eruption. There were four different intervention done against the suspected drug which were drug discontinuation15 (8.87%), Antidote given 107 (63.31%),time gap (30min to 1hr) between one drug to other36(21.0%), dose tapered 11(6.51%). CONCLUSION: Clinical pharmacist should be responsible to provide awareness to the health care system for the importance of ADR monitoring and reporting thereby improving the quality of life public health.

33

URSANE’S FROM SALVIA SPECIES

Dilip Gorai1, Shyamal K. Jash2, Rajiv Roy3*
1Department of Chemistry, Bolpur College, Bolpur, Birbhum-731204, West Bengal, India.
2Department of Chemistry, Saldiha College, Saldiha, Bankura-722173, West Bengal, India.
3*Independent researcher, Ph. D, Bhatgonna (Dignagar), Burdwan-713128, West Bengal, India.

Abstract

This review article focuses on ursane triterpenoids, the main group of triterpenoids found in Salvia species among which ursolic acid is most abundant, which can be obtained readily during the isolation procedures of salvia plant extracts. This review article compiled almost 83 ursane triterpenoids from about 80 species of salvia which were reported from literature survey till date.

34

FORMULATION OF DOXORUBICIN LOADED SOLID LIPID NANOPARTICLES IN ORDER TO IMPROVE ORAL BIOAVAILABILITY

Pragna Shelat*, Vinod K. Mandowara, Deepak G. Gupta, Shetul V. Patel
K. B. Institute of Pharmaceutical Education and Research, Kadi Sarva Vishwavidyalaya, Sector-15, KH-5, Gandhinagar-382015 GUJARAT (INDIA).

Abstract

Doxorubicin is an antitumor antibiotic first isolated in 1969 from a fungi Streptomyces peucetius var caesius. Present study focuses on formulation and characterization of solid lipid nanoparticles of Doxorubicin. Fatty acid coacervation method was adopted to formulate solid lipid nanoparticles of Doxorubicin. Compritol 888 ATO and Precirol ATO 5 were explored as solid lipids with LIPOID S 75 being used as surfactant. Freeze dried solid lipid nanoparticles were compared with raw Doxorubicin in rat plasma using High Pressure Liquid Chromatography (HPLC) method using ultraviolet (UV) detector. Particle size measurements performed on Solid lipid nanoparticles of Doxorubicin revealed mean particle size of 200-300nm for optimized formulations and entrapment efficiency of close to 70%. Sucrose and Dextrose were suitable cryoprotectants to prepare freeze dried solid lipid nanoparticles. Doxorubicin loaded solid lipid nanoparticles exhibited sustained release pattern during in vitro release kinetics. In vivo pharmacokinetics study in Swiss albino rats revealed that encapsulation of Doxorubicin into solid lipid nanoparticles increased oral bioavailability of Doxorubicin by 3.6 folds when compared with raw Doxorubicin.

35

EVALUATION OF IN VITRO ANTI-INFLAMMATORY AND IN VIVO ANTIARTHRITIC ACTIVITY OF CLINACANTHUS SIAMENSIS

Sreena K*, Sujith S Nair
Crescent College of Pharmaceutical Sciences, Payangadi R.S, Kannur, Kerala.

Abstract

Clinacanthus siamensis is a medium sized perennial shrub grows up to 2m in height belonging to the family Acanthaceae. It is distributed throughout the Western Ghats growing as an under shrub. The Leaves, roots and stem are used traditionally as Poison bites, inflammation, traumatic edema and swelling due to poison stings. The present study aimed at the evaluation of the anti-inflammatory, anti-arthritic and cox1 and cox2 inhibitory activity of the methanolic extract of Clinacanthus siamensis. Invitro method was estimated by human red blood cell membrane stabilization (HRBC) method and cox1 and cox2 inhibitory activity and invivo method was estimated on the formalin induced arthritic inflammation. Both the methods showed significant anti-inflammatory property of the methanolic extract. The MECS at a concentration of 400μg/ml showed potent activity on comparing with the standard drug.

36

HERB-DRUG INTERACTION BETWEEN ETHANOLIC EXTRACT OF ALOE VERA WITH GLIPIZIDE IN STREPTOZOTACIN INDUCED DIABETIC RATS

P. Naveen, J. Padma, Dr. B. Vasudha, Dr. T. Shivaraj Gouda*
Department of Pharmacology, School of Pharmacy, Anurag group of institutions Hyderabad.
*NET College of Pharmacy, Raichur, Karnataka.

Abstract

Objective: To evaluate herb drug interaction between ethanolic extract of Aloe vera with glipizide in streptozotacin induced diabetic rats. Methods: The streptozotacin induced diabetic rats were treated with ethanolic extract of Aloe vera at selective doses (20, 40 and 80 mg/200g, p.o), glipizide (0.18mg/200g, p.o) and combination of high dose (80 mg/200g, p.o) of ethanolic extract of Aloe vera and glipizide. The Blood glucose level was estimated at 0, 7, 14, 21 and 28 days. Body weight of the rats of all the groups was recorded before and after the study period of 28 days. Results: Significant hypoglycemic effect observed in ethanolic extract of Aloe vera and glipizide treated groups. The decreased blood glucose levels were observed higher in combination of drug treatment group than single administration groups, and body weight also improved significantly in streptozotocin induced diabetic rats. Conclusion: The results clearly revealed ethanolic extract of Aloe vera augments the hypoglycemic effect of glipizide in streptozotacin induced diabetic rats. Further studies are recommended for clinical benefits in humans to reduce the glipizide dose and avoid the adverse effect of glipizide.

37

MICROEMULSION BASED GEL DRUG DELIVERY SYSTEM

Yuga Satish Sonegaonkar*, Sushma Singh, Dr. Nilesh Khutle
Department of Pharmaceutics, Dr L.H. Hiranandani College of Pharmacy, Ulhasnagar.

Abstract

The present study was conducted to investigate the microemulsion based topical drug delivery system of anti-inflammatory drug triamcinolone acetonide for psoriasis in order to bypass its gastrointestinal adverse effects and to improve patient compliance. The pseudo ternary phase diagrams were developed for combinations of Capmul MCM EP oil phase, Cremophor EL as surfactant and Transcutol P as cosurfactant using water titration method. The developed microemulsion was characterized for globule size and polydispersibility index. The average globule size of the microemulsion was found be less than 100nm. Centrifugation studies were carried out to confirm the stability of the developed formulation. The formulation was thickened with a gelling agent carbopol 940, to yield a gel with desirable properties facilitating the topical application. The developed microemulsion based gel was characterized for pH, spreadability, refractive index and viscosity. Optimized formulation was then subjected to In vitro drug release. Optimized microemulsion based gel formulation was found to exhibit significant prolonged release as compared to drug suspension. Optimized gel obtained was analysed for transdermal permeability by using franz diffusion cell diffusion cell through an excised rat skin. Thus the present study indicates that microemulsion can be a promising vehicle for the topical delivery of triamcinolone acetonide as it increases the solubility of the drug thus in turn loading capacity of the drug as well.

38

A OVERVIEW ON EPILEPSY AND ANTI-EPILEPTIC THERAPY

M. N. L. Aishwarya*, Prasanna Kumar Kar, K. Sakhira, P. C. Jayanth, M. Niranjan Babu
Department of Pharmacology, Seven Hills College of Pharmacy, Venkataramapuramu, Tirupati-517561.

Abstract

The brain is susceptible to many different disorders that strike at every stage of life. Developmental disorders such as autism and dyslexia first appear in early childhood. Psychiatric diseases such as depression and schizophrenia are typically diagnosed in teens or early adulthood. Epilepsy is the fourth most common neurological disorder and affects people of all ages. Epilepsy is a group of related disorders characterized by a tendency for recurrent seizures. There are different types of epilepsy and seizures. Epilepsy drugs are prescribed to control seizures, and rarely surgery is necessary if medications are ineffective. Epilepsy is a spectrum condition with a wide range of seizure types and control varying from person-to-person. This Article aims towards the types of Epilepsy, Its Diagnosis, Its Treatment and The Phytotherapy towards the Epilepsy.

39

SPECTROPHOTOMETRIC METHOD DEVELOPMENT AND VALIDATION OF POORLY WATER SOLUBLE DRUG BY USING UREA AS HYDROTROPIC AGENT

Bhaskar O. Aher*1, Sachin S. Gaikwad2
1Department of Pharmaceutical Chemistry, J.E.S. College of Pharmacy, Nandurbar. (MS) India.
2Department of Pharmaceutics, Amruthvahini College of Pharmacy, Sangamner.(MS) India.

Abstract

Several techniques are used to increase the aqueous solubility of poorly water soluble drugs. Hydrotropic solubilisation technique is one of them. In the present investigation hydrotropic solution of urea (5M) has been employed as solubilizing agent to solubilization poorly water soluble drug Simvastatin by spectrophotometric determination in ultraviolet region. Simvastatin shows maximum absorbance at 250 nm. Beer’s law was obeyed in the concentration range of 50-200 μg/ml. Results of analysis were validated statistically and by recovery studies. From this we concluded that proposed method is new, simple, environment friendly, accurate and cost effective and can be successfully employed in routine analysis of Simvastatin in tablets. Hydrotropic agent urea did not interfere in spectrophotometric estimation.

40

REDISCOVERY OF IGF-1R TARGETED INHIBITORS FROM AN APPROVED DRUGS DATABASE THROUGH RECEPTOR-BASED PHARMACOPHORE MODELLING AND DOCKING

Anup S. Ramdhave, Mukesh Nandave*
SPP School of Pharmacy & Technology Management, SVKM’s NMIMS, Mumbai, INDIA.

Abstract

Involvement of Insulin-like growth factor-1 receptor (IGF-1R) in carcinogenesis has led to the development of new cancer therapies. But due to the very high degree of homology among IGF-1R and insulin receptor, these drugs are known to inhibit insulin receptor to a significant degree, leading to hyperglycemia and the concomitant diabetic complications. Thus, our aim was to explore safe IGF-1R targeting agent with lesser side effects by means of structure-based pharmacophore modelling and docking approach. High affinity compounds for IGF-1R were searched among a database of chemical structures comprising 9,127 approved drugs, chemical isolates from traditional medicinal herbs, and regulated chemicals, termed SWEETLEAD. Seven different pharmacophore models and a merged pharmacophore model were generated using seven different inactive crystal structures of IGF-1R. Pharmacophore-based screening yielded overall 5,842 hits. Afterwards, all these hit compounds were docked to the inactive form of IGF-1R using docking and scoring protocols. The best pose was further evaluated based on the existence of key residues for antagonist binding in its vicinity which retrieved 28 hits. After final evaluations based on S-score, 9 hits were revealed. Although the experimental validation of these compounds are lacking, computational methods predicts them as strong binders. Further experimental validation of these compounds will confirm this in silico study results and their potential role in treatment of cancer with high IGF-1R expression.

41

PHYTOCHEMICAL STUDIES AND ANTIOXIDANT ACTIVITY OF BACOPA MONNIERI PLANT LEAVES PROTEINS

Dr. Dinesha Ramadas*, Dr. Ravishankar M, Dr. Shwetha S, Dr. Chikkanna D
AIMS – Central Research Laboratory, AIMS, B. G. Nagara.

Abstract

The proteins from aqueous extract of Bacopa monnieri plant leaves were studied to evaluate its antioxidant activity by in vitro methods. The phytochemical analysis and antioxidant activity of Bacopa monnieri plant leaves proteins was evaluated. The quantitative phytochemical study was done for the dialyzed ammonium suphate precipitated proteins. The crude extract had more sugars (150.63mg/g), proteins (10.54mg/g) and the dialyzed protein precipitate contains more proteins (8.82mg/g) and negligible amount of other phytochemicals. Free radical scavenging activity was evaluated using 1, 1-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay and nitric oxide scavenging assay. The study reveals that, the Bacopa monnieri plant leaves proteins showed potent antioxidant activity in comparison with standard antioxidants like Ascorbic acid and BHA at a lower dose of 10μg. The above result shows that, the proteins from Bacopa monnieri plant leaves has significant antioxidant activity.

42

A NEW METHOD DEVELOPMENT AND VALIDATION OF DUAL WAVELENGTH UV SPECTRO- PHOTOMETRIC METHOD FOR SIMULTANEOUS ESTIMATION OF METAXOLONE AND DICLOFENAC POTASSIUM IN COMBINED DOSAGE FORM

Vijaya Jyothi Mallela1*, Praneeth Kumar Reddy Kovvuru2, Amulya B3, Latha Sree P4
1Department of Pharmaceutical Chemistry, RIPER, Anantapuramu-515721.
2Department of Pharmaceutical Analysis and Quality Assurance, RIPER, Anantapuramu-515721.

Abstract

A simple, accurate, and precise dual wavelength UV spectrophotometric method was developed for simultaneous determination of Metaxolone and Diclofenac potassium in combined pharmaceutical dosage forms. The literature review reveals that there is no dual wavelength method development for this combination of drugs, hence this method was developed. The wavelengths selected for determination of Metaxolone were 270 nm and 280 nm, whereas, the wavelengths selected for determination of Diclofenac potassium were 265 nm and 278 nm. Methanol and distilled water were used as solvents. Regression analysis of Beer’s plots showed good correlation in concentration range of 15-90 μg/ml for Metaxolone and 2-12 μg/ml for Diclofenac potassium. Accuracy of method was found between 98.0-102.0%. The intra-day and inter-day precision studies of the method were found to be within limits. Limit of Detection was found to be 0.780μg and 0.0456 μg for Metaxolone and Diclofenac potassium respectively and Limit of Quantitation was found to be 2.36μg and 0.1382 μg for Metaxolone and Diclofenac potassium respectively. The developed method is validated as per ICH guidelines and the results were found to be within the results. Hence, the proposed method can be successfully applied for determination of these drugs in commercial tablets.