IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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JULY 2014
1

STRESS DEGRADATION BEHAVIOR OF SAPROPTERIN DI HYDROCHLORIDE AND DEVELOPMENT OF SUITABLE STABILITY-INDICATING RP-HPLC METHOD FOR THE DETERMINATION OF SAPROPTERIN DI HYDROCHLORIDE IN TABLET DOSAGE FORM

Bhavani Vukkum 1*, Siva rao T valluria 1, Jamelunnisa Begumb 2

1Dept of Inorganic and Analytical Chemistry, Andhra University, Visakhapatnam (AP),  India.

2Department of Chemistry, St. Theresas College, Eluru, Andhra Pradesh, India.

Abstract

A novel stability-indicating reversed phase high performance liquid chromatographic  method was developed for the quantitative determination of  Sapropterin dihydrochloride in Tablet dosage form. The chromatographic separation was achieved on a Waters HPLC , with phenomenex Luna SCX  C18, 250 mm × 4.6 mm, 5 μm particle size column with mobile phase containing a isocratic solution ( 30Mm KH2PO4 -PH adjusted to 3.0 with orthophosphoric acid ) .The flow rate was set as 1.2 mL/min and the run time was 15.0 min. The drug substance was subjected to stress studies of  acid, base, humidity, Photolytic, oxidation, UVlight, and thermal degradation. Sapropterin dihydrochloride was found to degrade significantly in basic and oxidative stress conditions. The formed degradation products were well resolved from Sapropterin. Degradation products were identified by mass spectrometry, Nuclear magnetic resonance spectroscopy and proposed structures were reported. The formed degradation products. The mass balance was found to be satisfactory in all stress conditions, thus proving the stability indicating capability of the method. The developed RP-HPLC method was validated in agreement with ICH requirements and found to be simple, accurate, precise, linear, specific and suitable for the quantitative determination of Sapropterin dihydrochloride in bulk drug and in its pharmaceutical dosage form. 

2

IN-VIVO NEPHROPROTECTIVE ACTIVITY OF KALANCHOE PINNATA LEAVES ON ETHYLENE GLYCOL INDUCED UROLITHIASIS IN ALBINO RATS

K. Ramesh*, E. Paari and S. Rajeshkumar*

Research Department of Biochemistry, Adhiparasakthi College of Arts and Science, Kalavai – 632506, Vellore District, TN, India.

Abstract

In this present investigation, Nephroprotective activity of Ethanolic extract of Kalanchoe pinnata leaves on Ethylene glycol induced Urolithiasis in albino rats was analyzed. For that adult male albino rats weighing 150-200g were selected and divided into Six groups of six animals each, a single dose of Ethylene glycol 75mg/kg was given to Group-II, Group-III and Group-IV rats.  After two hours, Group-III was treated with ethanolic extract 75mg/kg body weight of Kalanchoe pinnata leaves 100mg/kg of body weight orally and Cystone was given to Group-IV rats at 75mg/kg of body weight. After 10 days, all the rats were sacrificed blood was drawn from the external jugular vein serum separated by centrifugation and used for the analysis of biochemical markers like Creatinine, Urea, SGOT, SGPT, Uric acid and Total Protein. Administration of K. pinnata Leaves significantly reduced the elevation of Urea (36.16), Uric acid (6.12), Creatinine (1.26), ALP (75.70), SGOT (25.42), SGPT (22.73) and Total Protein (7.7) in serum comparing with standard drug Cystone. The miracle medicinal plant Kalanchoe pinnata played a good role on nephroprotective activity in albino rats and it is an effective method for knowing medicinal values of the plant. The results show that the level of the biomarkers and enzymes levels were near to the normal levels as found in standard drug.

3

METHOD DEVELOPMENT AND VALIDATION FOR THE SIMULTANEOUS ESTIMATION OF CEFTRIAXONE AND SULBACTAM BY RP-HPLC IN FINISHED DOSAGE FORM

Mohammed Azeem Husain, P.Sunil Kumar Chaitanya*, P.Kishore2 Sheena M Raj, G.Rohini Reddy

Dept of Pharmaceutical Analysis & Quality Assurance, St.Pauls College of Pharmacy, Turkhyamzal, Hyderabad

Abstract

In the present work a simple, sensitive and specific Reverse Phase-High Performance Liquid Chromatography (RP-HPLC) method has been developed and validated for the estimation of Ceftriaxone and Sulbactam in Bulk and Pharmaceutical dosage form to create an affordable and reliable method than the previous ones. The elution was carried with Intersil ODS C18 column (250*4.6mm and 5 µm) in isocratic mode, using a mobile phase containing Acetonitrile: phosphate buffer (pH5.6) in the ratio of 45:55 at a   flow rate of 1.0ml / min. The analytes were detected at 210 nm. The retention times were found to be 2.817 & 4.297 for Sulbactam & Ceftriaxone respectively. The method was validated for system suitability, linearity, precision, accuracy specificity, robustness, LOD and LOQ. The method was found to be linear with r2 values 0.999 & 0.998 for Sulbactam and Ceftriaxone respectively. The accuracy of the present method was evaluated at 100,120&140% and recovery for Ceftriaxone and Sulbactam is found to be in the range 100.72-98.49. Inter-day & intra-day precision studies were carried out and the % RSD values were less than two. Sensitivity was estimated by determination of LOD & LOQ and the values were found to be 3.03 & 9.18 for ceftriaxone and 0.47 & 1.42 for sulbactam. Proposed method can be successfully applied for the quantitative determination of ceftriaxone and sulbactam in Bulk drug and Pharmaceutical dosage form.

4

SCREENING OF STRESS RELATED DETERMINANTS IN URBAN ADOLESCENT POPULATION

Praveen.D*, Ranadheer Chowdary.P, J. Divya Maria, G. Thanmayi, Sajel.S Shanmuga Priya.J, S.Yeswanthi, G.Poojitha

School Of Pharmaceutical Sciences,Vels University.

Abstract

This study is a continuation of the study done by Praveen.D et.al [1].There is a high prevalence of Hypertension which is one of the major health problem across the globe. Hypertension has its roots in adolescent age but goes undetected unless it is properly diagnosed. Hence we conducted this study in anurban setup in Chennai; Tamil Nadu among adolescents about their sleep time, diet, obesity etc. A study was conducted at Chennai, Tamil Nadu during June 2014. The study was conducted among school going adolescent children between the age group of 13 to 17. Blood pressure readings were analysed as per guidelines of JNC-7 as well as with inputs from JNC-8.657 participants has participated in the study. 312 participants have a normal BP, while 12.94% participants have hypotension7.30% population had stage 2 secondary hypertension while 11.11%persons fall with stage1 hypertension. The incidence of hypertension is higher among the adolescents in urban area than those in rural area. Proper care should be shown to children with hypertension as this may virtually be a tougher aspect to deal with.

5

DEVELOPMENT AND VALIDATION OF ANALYTICAL METHOD FOR ESTIMATION OF TINIDAZOLE BY USING DERIVATIVE SPECTROSCOPY

Solanke S.B*.,  Mohammad Zameeruddin., Kalyankar S.S., Jadhav S.B., Kadam V.S., Bharkad V.B.

Department of Quality Assurance, SSS Indira College of Pharmacy, Vishnupuri  Nanded.

Abstract

Tinidazole is used in the treatment of protozoal infections. Two simple, sensitive, accurate and economical spectrophotometric methods have been developed for the estimation of Tinidazole in bulk drug and pharmaceutical formulation. Methods are based on measurements of first order and second order derivative spectroscopy adopted to eliminate spectral interference, in which derivative amplitude was measured at 295nm and 213nm respectively. The drug obeys Beer’s law in the concentrations range of 4 - 40μg/ml. The results of analysis were validated for accuracy, precision, and ruggedness, limit of detection (LOD) and limit of quantification (LOQ). These results were found to be satisfactory. The proposed methods are simple, sensitive, rapid, economical and suitable for routine quality control applications in pharmaceutical formulation. This method is found to be useful in the method development of tinidazole.

6

CHANDRAKANTHI CHOORNAM: SIDDHA MEDICINE INDICATED FOR OLIGOSPERMIA – A REVIEW

Akila B*, Manickavasakam K

Department of Maruthuvam, National Institute of Siddha, Tambaram sanatorium, Chennai -600047.

Abstract

Oligozoospermia,Teratozoospermia and Asthenozoospermia are the main basis of lnfertility in men.Siddha sastric preparation Chandrakanthi Choornam, a herbomineral formulation from Chikicha rathna deepam-part-II is indicated in Oligospermia,Poly urea,Vaginal disease, Venereal disease and all biliousness. It comprises of 25 ingredients such as Curculigo orchioides, Madhuca longifolia, Cinnamomum verum, Cinnamomum tamala, Syzygium aromaticum, Coscinium fenestratum, Mesua ferrea, Maerua arenaria, Adhatoda vasica, Moringa oleifera, Lawsonia inermis, Vitis vinifera, Bombax ceiba, Bambusa aurundinaceae,  Phoenix dactylifera, Illicium verum, Mucuna pruriens, Cyperus rotundus, Glycyrrhiza glabra, Tribulus terrestris,Cuminum cyminum,  Costus speciosus, Myristica fragrans, Alternanthera sessilis and Asphaltum punjabinum.This review article has been presented to document  the therapeutic potential, preclinical and clinical studies of the herbs and mineral of chandrakanthi choornam in regard to the treatment of oligospermia. Phytochemicals like amino acids, steroids, flavonoids, phenols, tannins, saponins and nutritional elements like calcium, magnesium, iron, zinc and copper were identified to defend the spermatogenic activity. Traditional uses of the ingredients claims its indication in treating spermatorrhoea, male infertility, impotency, premature ejaculation, oligospermia and nocturnal emission. Shilajith act as the synergistic enhancer of other drugs. Some drug has aphrodisiac action and antioxidative properties. The review validates its effectiveness in treating oligospermia and claim its support  in clinical application.

7

TO EVALUATE THE ANTIOXIDANT STATUS IN TYPE 2 DIABETIC PATIENTS WITH OR WITHOUT NEPHROPATHY

Dr. Harnam Kaur1, Mrs. Sonia Gupta2, Dr.Rumana Farooq Mir3, Dr. Sheikh Afaq4, Dr. Sheikh Ishaq5*.

1ESIC Medical College Faridabad Haryana [Current Affiliation].

2Department of  Biochemistry, M.M.Institute of Medical Sciences and Research, Mullana, Ambala, Haryana.

3Demonstrator, Department of Microbiology. SKIMS Medical College, Bemina, Srinagar, Jammu and Kashmir.

4 Assistant Consultant, Department of Emergency Medicine, King Abdullah Medical City, Holy Makkah Kingdom of Saudi Arabia.

5Medical Officer, Jawaharlal Nehru Memorial Hospital, Srinagar, Jammu and Kashmir.

Abstract

Oxidative stress is a condition in which the cellular production of reactive oxygen species (ROS) exceeds the physiological capacity of the antioxidant defense system to render ROS inactivate. Objective: To estimate the levels of Vitamin C and GSH in type 2 diabetic patients. To find out the correlation, if any, between glycemic control and the levels of Vitamin C and GSH. Method: The study was conducted on patients attending rural medical college hospital of India The sample was analysed for estimation of fasting blood glucose, glycated Hb, Vitamin C and GSH. Statistical analysis: Data obtained were analyzed as per standard statistical methods. Results: Out of 150 subjects, Fasting blood glucose (FBG) and glycated hemoglobin was higher in diabetic patients with microalbuminuria than in those without microalbuminuria. Highly significant increase in FBG and HbA1c in non-complicated and complicated cases as compared to healthy controls. Vitamin C level and GSH were significantly decreased in non-complicated and complicated cases. Conclusion: Anti-oxidant levels decrease in diabetic patients,more so with complications. Combinations of antioxidants given as dietary supplements seem to offer the most promising for achieving clinical breakthroughs.

8

INFLUENZA IMMUNIZATION: A REVIEW FOR PHARMACISTS

Sappa Dilip Kumar*, Nasara Reddy Nakka, A. Avinash, V. Bhavan Kumar

R.M Medical College & Hospital, Annamalai University India 608002.

 

Abstract

Influenza infection is associated with significant morbidity and mortality. Two types of influenza vaccines are available, including the trivalent inactivated influenza vaccine (TIV) and the live, attenuated influenza vaccine (LAIV). The prevalence of influenza A (H3N2) viruses has increased in recent years. Both types of vaccines contain 3 virus antigens that are matched to the main circulating strains of influenza each year. The LAIV is available as an intranasal spray and is only indicated for use in select patients. After vaccine administration, the patient should be monitored for signs and symptoms of acute reactions; The medications involved in the treatment influenza are classified as antiviral medications, of which there are 4 different agents: oseltamivir, zanamivir, amantadine, and rimantadine. According to current guidelines from the Centers for Disease Control and Prevention (CDC), 2 FDA-approved antiviral medications have been recommended for use in the United States during the 2012-2013 influenza season: oseltamivir (Tamiflu) and zanamivir (Relenza).Specific groups of high-risk individuals include children younger than 5 years (but especially those younger than 2 years), adults 65 years and older, and pregnant woman. Pharmacists play an important role in disease prevention by advocating and administering immunizations. This present study has attempted to review the importance of pharmacist role in the influenza immunization.

9

SYNTHESIS AND ANTIOXIDANT, ANGIOTENSIN CONVERTING ENZYME INHIBITORYACTIVITIES OF BOTH N-BUTYL-2-(QUINOLIN-8-YLOXY)ACETAMIDE AND N-BUTYL-2-[5-(QUINOLIN-8-YLOXY)METHYL)-1,3,4-OXADIAZOLE-2-YLTHIO)ACETAMIDE DERIVATIVES

Ravikumar N. Naik1, Shilpa C. Patil1, Pramod. H2Satish Sreedharamurthy2, Sudha. B. Satyanarayan1*

1Department of Chemistry, Yuvaraja’s College, University of Mysore, Mysore- 570 005, Karnataka, Indi

2Department of Studies in Microbiology, Manasagangotri, University of Mysore, Mysore - 570006 Karnataka, India.

Abstract

A new series of N-butyl-2-(quinolin-8-yloxy)acetamide (2a-e) and N-butyl-2-(5-((quinolin-8-yloxy)methyl)-1,3,4-oxadiazol-2-ylthio)acetamide(5a-e) were synthesized and characterized by FTIR, 1H NMR, 13C NMR and LC-MS. The antioxidant properties by DPPH, hydroxyl radical scavenging activity and superoxide radical scavenging activities against standard ascorbic acid, mannitol and butylated hydroxyl anisole were evaluated respectively. Further angiotensin converting enzyme inhibition activity (ACE-I) inhibition of the newly synthesized compounds (2a-e) and (5a-e) were described. From the results obtained it was revealed that the compounds 2e, 5a and 5e possess better antioxidant property and the compound 2d as active ACE-I inhibitor against standard lisnopril. Docking simulation further supported the probable binding conformation of ACE-I active site by N-butyl-2-(quinolin-8-yloxy)acetamide derivatives 2a-e. From the antioxidant screening it was explored that the compounds having electron donating groups like -CH3 and a parent compound showed good in vitro biological activity than those compounds having electron withdrawing groups like -Cl which showed moderate activity. The compound having both –Cl and –CH3 showed good in-vitro ACE-I inhibitor activity. Analysis of the docking study gave details on the fine relationship linking structure and activity, and also offer clues for structural modifications would improve the activity.

10

ANGIOTENSIN-I-CONVERTING ENZYME INHIBITION AND ANTIOXIDANT ACTIVITY OF BENZAMIDE APPENDED OXADIAZOLE DERIVATIVES

Shilpa C. Patil1, Ravikumar N. Naik1Satish Sreedharamurthy2, Pramod H2, Sudha B. Satyanarayana1*.

1Department of Chemistry, Yuvaraja’s College, University of Mysore, Mysore- 570 005, Karnataka, India

2Department of Studies in Microbiology, Manasagangotri, University of Mysore, Mysore - 570 006, Karnataka, India

Abstract

In continuation of our research on the synthesis of benzamide appended heterocyclic compounds, here in some new benzamide appended oxadiazole derivatives (2a-i) were prepared and structures were confirmed by their spectral studies. ACE-I inhibition activity was investigated, Compounds 2a and 2i proved to be potent ACE-I inhibitors with IC50 value of 27.50 μg/μl and the compounds 2b-e showed moderate ACE-I inhibition with IC50 value in the range of 34-36 μg/μl when compared to standard lisinopril (IC50=30.83 μg/μl).. Compounds 2g-h exhibit least ACE inhibition activity with IC50 values of 41.66 μg/μl  and 43.33 μg/μl . Antioxidant activities was probed by DPPH assay, lipid peroxidation assay and super radical scavenging activity. DPPH assay revealed that compounds 2a-e were moderate radical scavengers with IC50 value in the range of 16-20 μg/μl when compared to standard Ascorbic acid (IC50 value = 9.73μg/μl). The compounds 2a-f showed moderate anti-lipid peroxidation activity when compared to standard α-tocopherol (IC50 value = 30.47 mg/ml). By Superoxide radical scavenging assay, compounds 2a-g were found to be moderate superoxide radical scavengers with activity in the range of 35-29% when compared to standard Butylated hydroxyanisole (39.93%). By antioxidant assay it was proved that the compound 2h was potent radical scavenger.

11

REAL-TIME PCR FOR RAPID DETECTION OF MYCOBACTERIUM TUBERCULOSIS IN PULMONARY SPECIMENS

Dr. Harnam Kaur1, Dr.Rumana Farooq Mir2 , Dr.Sheikh Ishaq3*,Dr.Jasbir Singh4, Dr.Neeru Bhaskar5, Dr.Arshad Rashid6, Dr.Shikhaa Mahajan7.

1Professor & Head, ESIC Medical College Faridabad Haryana.

2Demonstrator, Department of Microbiology. SKIMS Medical College, Bemina, Srinagar, Jammu and Kashmir.

3*Medical Officer, Jawaharlal Nehru Memorial Hospital, Srinagar, Jammu and Kashmir.

4Professor & Head, Department of Biochemistry. M.M.I M.S.R, Mullana, Ambala, Haryana

5Associate Professor, Department of Biochemistry. M.M.I M.S.R, Mullana, Ambala, Haryana

6Assistant Professor, Department of Surgery. M.M.I M.S.R, Mullana, Ambala, Haryana

7Assistant Professor, Department of Biochemistry, M.M. Medical College and Hospital, Kumarhatti, Solan, Himachal Pradesh.

Abstract

To compare the sensitivity and specificity of real time polymerase chain reaction (Q-PCR) with standard conventional methods for diagnosing tuberculosis (TB) and to establish Q-PCR as a diagnostic tool for tuberculosis. Method: This was a prospective study conducted on 162 sputum specimens from TB suspects, attending rural medical college hospital of India. A Löwenstein-Jensen medium culture and clinical diagnosis were used as gold standard. Results: Of the 162 sputum samples, 91 were culture positive, 89 were Q-PCR positive and 77 were smear positive for acid-fast bacillus (AFB). The sensitivity, specificity and accuracy of the Q-PCR were 87.25%, 98.34% and 91.36% respectively which was significantly better than that of smear AFB (p=0.0479) and comparable to that of culture (p=0.8280). Conclusion: Q-PCR performed on sputum smears demonstrated satisfactory sensitivity, specificity and accuracy, and may therefore be recommended as a method for diagnosing TB.

12

PRESCRIBING PATTERN AND USE OF ANTIBIOTICS AND COMBINATION OF ANTIBIOTICS IN A TERTIARY CARE TEACHING HOSPITAL

Syed Zahed pasha*, B.Devi Prasad1, L.Shalem, T.Bhanu chand, G.Veeramani

Department of Pharmacy Practice, Annamalai University, Tamilnadu

Abstract

Antibiotics are most extensively used drugs in hospitals. The approach of the study is to decrease the adverse drug reactions,compare cost effectiveness of the drugs,to decrease drug resistance of the drugs and to reduce the medication errors in the prescriptions.The major antibiotic group which were used to treat the antibiotics are mentioned.Wide ranges of antibiotics are available to treat various types of infections. Though the choice of antibiotics prescribed depends upon the clinical interest, culture sensitivity, age and gender, their extensive use, may lead to the poor therapeutic outcome in terms both health and economic conditions. The present study was conducted over a period of 8 months i.e. from July 2013 to February 2014 in tertiary care teaching hospital. The research summarized a total of 250 cases were reviewed to evaluate the prescribing pattern of antibiotics in the treatment of various types of infection. The result was found that majority of the patients were treated with Quinolones (36.55%), the major route of drug administration employed was oral route. Excessive and inappropriate use of antibiotics contributes to the development of bacterial resistance. This study was carried out to collect relevant demographic information and antibiotics prescribing patterns.250 patients were prescribed antibiotics; 128 were male (51.2%) and 122 were females (48.8%). Median duration of hospitalization was 10 days. 390 antibiotics were prescribed. The most common were ciprofloxacin, amoxicillin, metronidazole, ampicillin, aminoglycosides, macrolide antibiotics, cephalosporin and sulphonamides. Antibiotic resistance is becoming a problem in the general medicine ward. The strategies required to prevent antibiotic resistance are as follows ;Formulation of a policy for hospital antibiotic use, educational  programmes should be conducted for patients and  health care providers. Patient counseling is required for proper use of antibiotics, culture sensitivity tests should be conducted before prescribing antibiotics.

13

SYNTHESIS, CHARACTERIZATION AND EVALUATION OF NOVEL AROMATIC SULFONYLHYDRAZIDE DERIVATIVES AS ANTI-FUNGAL AND ANTI-MYCOBACTERIAL AGENTS

Ashwini A. Kulkarni, Dr. Vilasrao Kadam, Dr. Mrunmayee P. Toraskar*

Department of Pharmaceutical Chemistry, Bharati Vidyapeeth’s College of Pharmacy, Sector-8, CBD Belapur, Navi Mumbai, Postal code-400 614, Maharashtra, India.

Abstract

New class of sufonylhydrazide derivatives was prepared from aromatic carboxylic acid hydrazide on treatment with various benzenesulfonyl chlorides in presence of pyridine as a catalyst. The structures of these compounds have been elucidated by FT-IR, 1H- NMR and Mass Spectroscopy. Furthermore the compounds were screened for in-vitro anti-fungal activity against C. albicans by tube dilution method. Micro plate Alamar Blue Assay (MABA) method was used for anti-mycobacterial activity against M.tb H37Rv. Amonst all compounds IIIf and VIe had shown excellent anti-fungal activity C. albicans at MIC 1.6 µg/ml which is less than the standard used. Also compounds IIIg and VIf were displayed equal activity as Streptomycin against M. tuberculosis H37Rv at 6.25 µg/ml.

14

SYNTHESIS OF THIOPHENE-2-CARBOXYLIC ACID N-(3-ARYL/SUBSTITUTED ARYL/HETEROARYL-ACRYLOYL)-HYDRAZIDE DERIVATIVES AS ANTI-CANCER AGENTS

Suvarna M. Patil, Nikhil K. Tadge, Priya S. Hargunani, Dr. Vilasrao J. Kadam and Dr. Mrunmayee P. Toraskar*

Department of Pharmaceutical Chemistry, Bharati Vidyapeeth’s College of Pharmacy, Sector-8, C.B.D. Belapur, Navi Mumbai-400614, Maharashtra, India.

Abstract

In the present work, an attempt was made to synthesize derivatives of thiophene-2-carboxylic acid N'-(3-aryl/substituted aryl/heteroaryl-acryloyl)-hydrazide by reaction of aryl/substituted aryl/heteroaryl aldehydes with thiophene-2-carboxylic acid N'-acetyl-hydrazide under basic conditions. The structures of newly synthesized chalcone derivatives were characterized and confirmed by FTIR and 1H-NMR. The newly synthesized compounds were evaluated   for their in vitro anticancer activity against human tumor breast cell line (MCF7) using Adriamycin as a reference drug at Tata Memorial’s Advanced Center for Treatment, Research and Education in Cancer (ACTREC), India. Sulforhodamine B (SRB) protein assay was used to estimate cell stability or growth. All the compounds showed varying degrees of cytotoxicity in the tested cell line, most marked effect was observed by compound IIa.

15

IN SILICO MOLECULAR DOCKING STUDIES OF LICHEN METABOLITES AGAINST VARIOUS CANCER PROTEINS

E. Susithra1, S. Meena2, D. Chamundeeswari3

1Jawaharlal Nehru Technological University Hyderabad, Kukatpally, Hyderabad-500 085, Telangana, India

2Acharya and B.M Reddy College of Pharmacy, Bengaluru-560 107, India.

3Faculty of Pharmacy, Sri Ramachandra University, Porur, Chennai-600 116, India.

Abstract

The architecture of lichen compounds offers a large area for developing scaffolds for combinatorial libraries towards discovery of lead compounds. The present study emphasizes the significance of lichen metabolites namely the depsides, depsidones and dibenzofuran derivatives well known for their anti-proliferative and cytotoxic activities. In this regard, molecular docking simulations were carried out for the lichen metabolites likely atranorin, lecanoric acid, salazinic acid & dibenzofuran derivatives (usnic acid) with various cancer proteins like, JNK1, MMP-9, Caspase-3, PARP-1, ERK2, AIF, FGFR2, AKT1, CDK2, CDK6 & PI3K, and the docked results were compared with the standard reference ligands (methotrexate & 5-fluorouracil). Among all the docked ligands, the depside - atranorin has shown satisfactory H-bond interactions with JNK1, MMP-9, CDK2, CDK6 & PI3K proteins and with highest glide score -9.83, -8.98, -10.25, -7.84 & -10.16, respectively; lecanoric acid has shown acceptable H-bond interactions with PARP-1, ERK2, CDK2 & CDK6 proteins with glide score -9.29, -8.28, -9.64, -7.53, respectively. The depsidone molecule salazinic acid has shown meaningful hydrogen bond interactions and binding energy with Caspase-3, AIF, FGFR2 & AKT1 and with glide score -7.71, -8.49, -11.26, -6.04, respectively. Of the dibenzofuran derivatives, usnic acid has shown adequate docking score with all the target proteins but amongst all the S1-S7 ligands, S3 & S4 have shown favorable H-bond interactions with the target cancer proteins. These docking results reveal that the lichen metabolites might have inhibitory activity against several cancer proteins, and are expected to be useful in conducting in vitro studies on the target specified cancer proteins and for further structural elucidation of lichen metabolites in the development of effective potent newer chemical entities with anti-cancer properties.

16

ISOLATION AND CHARACTERISATION OF CUCUMIS ANGURIA SEEDS FOR THEIR THERAPEUTIC POTENTIAL

N.S Gill*, Anish Mahajan, Rashmi Arora

Rayat Institute of Pharmacy, Ropar, Punjab, India.

Abstract

Cucumis anguria L. also known as Burr gherkin and West Indian gherkin is a vegetable crop with a nutritional value same as that of Cucumber and belongs to Cucurbitaceae family.  Seeds extract of this plant is used for carrying out Phytochemical Screening as well as for checking its Antioxidant Activity. Beside this total phenolic content and total flavonoids content are also estimated from its seeds extract. For estimation of Antioxidant activity both DPPH and H2O2 Methods are used. At the last isolation of the compound using TLC and Column Chromatography is done and its characterization using H NMR and IR spectra. From the Research carried out it is showed to posses Antioxidant activity and various constituents such as Flavonoids, Alkaloids, Triterpenoids, Carbohydrates, Tannins, Sterols, Anthraquinone glycosides and Saponins are present in it. The compound isolated from its seeds extract is found to contain a steroid or triterpenoid nucleous. The hypothetical structure of the isolated compound is drawn from the two spectra.

17

COMPARATIVE ANTI-DIABETIC EFFECT OF METHANOLIC EXTRACT OF INSULIN PLANT (Costus pictus) LEAVES AND ITS SILVER NANOPARTICLE

Ajithadas Aruna*, Ramraj Nandhini, Venkatachalam Karthikeyan, Pandi Bose, Kannappan Vijayalakshmi

College of Pharmacy, Madurai Medical College, Madurai-20, Tamil Nadu, India.

Abstract

To compare anti diabetic effect of Methanolic extract of Insulin plant (Costus pictus) leaves (MECP) and its silver nanoparticle (MECPAgNPs) by various in vitro screening methods. Preliminary phytochemical screening, Vitamin C, total phenolic and flavonoid content were determined by standard procedure. TLC and HPTLC (quantitative) analysis of MECP was done by using Quercetin as a standard. Screening of in vitro anti diabetic activity was done by Inhibition of α-amylase & α-glucosidase enzyme assay, Glucose uptake in yeast cells and Non-enzymatic glycosylation of Hemoglobin assay. Preliminary phytochemical screening showed the presence of carbohydrates, triterpenoids, proteins, alkaloids, tannins, saponins, flavonoids, sterols and volatile oil. Phenolic, Flavonoid content and Vitamin C of MECPAgNPs was higher than MECP. TLC analysis of MECP confirmed the presence of Quercetin and its amount was found to be 115.41mg/g by HPTLC. Non-enzymatic glycosylation of Hemoglobin assay, MECPAgNPs exhibited higher inhibition of glycosylation as compared with the MECP at a concentration of 200-1000µg/ml. In α-amylase and α-glucosidase enzyme inhibition assay, the results showed MECPAgNPs had efficiently inhibit both enzymes, in vitro in dose dependent manner than MECP at a concentration of 200-1000µg/ml. It can be concluded that the leaves of C.pictus D. Don can be a good source for synthesis of silver nanoparticle which shows potent anti oxidant and anti diabetic activity than the MECP. The important outcome of the study will be the development of value added product from medicinal plant Costus pictus D. Don for biomedical and nanotechnology based industries. Furthermore, in vivo studies are required for providing scientific information on the plant.

18

MUTATIONAL ANALYSIS OF ANDROGEN INSENSITIVITY SYNDROME

Tapan Behl*1, Ishneet Kaur2, Heena Goel3, Rajesh K. Pandey4

1Department of Pharmacology, Vallabhbhai Patel Chest Institute,University of Delhi, Delhi.

2Department of Pharmacy, Chandigarh College of Pharmacy, Mohali, Punjab.

3Department of Animal Husbandry, Junga, Shimla, Himachal Pradesh.

4All Excel Inc, 135 Wood St. West Haven CT 06410 USA. 

Abstract

Androgen Insensitivity syndrome is a rare disorder specifically affecting the male gender during their development stages, viz., the period after their birth and most commonly seen during the puberty age. This condition is characterized by the incompetence of the cells of a male human to respond to the stimulus of the male sex hormone (collectively termed as androgens) normally. As a consequence of this, the male person affected by this syndrome might possess some features which are characteristic to females besides having some features of males as well. This condition predominantly affects male homosapiens (i.e., the humans whose genetic makeup comprises of the possession of one X chromosome and one Y chromosome), whose abnormal inheritance is cited as the reason behind this syndrome. Furthermore studies revealed that this abnormality, perceived exclusively in X chromosome only, is owed to certain mutations in an explicit gene known as AR (androgen receptor) gene. The results of the inheritance of such abnormal or mutated genes is inability of the male to accomplish the complete process of masculinization during the puberty age which may lead to the development of mixed gender features, which sometimes becomes a source of embarrassment and might create some really awkward situations for the affected person, especially in such insensitive stereotyped society, such as India, where non-conventional gender system has not yet found respectable acceptance. The various researches conducted for exploring this disorder in detail revealed numerous mutations in the concerned gene which are held responsible for its pathophysiology. These discovered mutations could lead to the evolvement of future aspects which could potentially be utilized for the better understanding of this disorder and probably finding a way for its management.

19

USAGE OF ONLINE TOC ANALYZER- PROCESS ANALYTICAL TECHNOLOGY INITIATIVE

Saravana Kumar .V*1, Dr.P.Shanmugasundaram2

1Quality Assurance, Hospira Healthcare India Private Limited, Chennai, India.

2Professor & Head, Department of Pharmaceutics, School of Pharmaceutics, VELs University ,Chennai ,India.

Abstract

Process Analytical Technology (PAT) has been introduced as an advent of new tool which has given an opportunity for all the pharmaceutical manufacturers to improve upon their quality and compliance. The application of this technology in pharmaceutical manufacturing ensures the quality of raw material attributes that too at-line, in-line or on-line, which was difficult earlier, thereby decreasing the chances of error and significant savings in time required for testing.. In this article, Process Analytical Technology has been introduced briefly and explained its different tool in order to illustrate how application of this technology ensures quality of pharmaceutical products by implementing Online measurement in existing pharmaceutical utility system (eg.Online TOC analyzer) and through this implementation, significant amount of process loss has been minimized and it also enhances delivering quality products at right time first time. In Total, Process Analytical Technology lays a way for producing a standard product which is in line with Quality and thus creating a satisfaction with customer needs and making a good brand image for the organization.

20

ANTICLASTOGENIC ACTIVITY OF HYDROALCOHOLIC EXTRACT OF MANGIFERA INDICA LINN. USING MAMMALIAN CHROMOSOMAL ABERRATION TEST IN BONE MARROW OF MICE

Sindhu Priya E.S*1, Dipak Patel1, Venkata Krishna K1, Nagashree K.S1, Shyam Prasad K2, Lingaraju H.B3

1Department of Preclinical Research Lab, Vidya Herbs Pvt. Ltd, #101, Jigani II phase, Bangalore-560078, Karnataka, India.

2Managing Director, Vidya Herbs Pvt. Ltd, #101, Jigani II phase, Bangalore-560078, Karnataka, India.

3Department of Phytochemistry Research, Vidya Herbs Pvt. Ltd, #101, Jigani II phase, Bangalore-560078, Karnataka, India.

Abstract

It is to determine the anticlastogenic activity of Hydroalcoholic Extract of Mangifera indica Linn. leaves, stem bark and fruit skin (HEMI) on chromosomal damage induced by Cyclophosphamide (CP) by in vivo mammalian Chromosomal aberration test in mice. In the present investigation, eight groups of swiss albino mice six in each group were used. Except the first group all the remaining groups were treated with CP (40 mg/kg). Group I serve as control.  Group II was treated with CP. Mice of III, IV and V groups were treated with HEMI at 50,100 and 150 mg/kg doses respectively along with CP. Mice of VI, VII and VIII groups were treated with HEMI at 50,100 and 150 mg/kg doses respectively without CP.  Metaphase of bone marrow cells of all animals were analyzed for structural and numerical chromosomal aberrations. Break, gap, fragment, association, deletion, polyploidy, pulverization, ring, other multiple aberrations, total aberrations, total aberrated cells and mitotic index were observed. Groups III and IV showed significant (P<0.001) decrease in chromosomal aberrations when compared to CP group. Groups III, IV and V showed 66.77%, 60.04% and 50.26 % protection against CP induced chromosomal aberrations respectively. Total chromosomal aberrations were found to be 431, 367 and 524 in III, IV and V groups respectively. From the present study it can be observed that HEMI possess significant anticlastogenic activity against CP induced chromosomal aberrations.

21

FORMULATION AND EVALUATION OF ORAL DISPERSIBLE TABLETS OF CLOPIDOGREL BI SULFATE BY SOLID DISPERSION METHOD

R. Redya Naik1*, Aishwarya Madikanti1, T.Sunitha2, NusrathYasmeen2, P.S. Malathi 1, D. Vijay kumar 1 Gummadi  Sridharbabu 1 , Sujatha  Ramavath 1. S.Srinu Naik 3.

1Department of Pharmaceutics, Pragathi Pharmacy college,Jangoan, Warangal, Telangana, India.

2Department of Pharmacology, University College of Pharmaceutical sciences, KU, Warangal,Telangana, India.

3Department of Chemical Engineering,University College of Technology,Osmania University,Hyderabad,Telangana,India.

Abstract

Oral route is presently the gold standard in the pharmaceutical industry where it is regarded as the safest, most economical and most convenient method of drug delivery.  Oro dispersible tablets are the fast growing and highly accepted drug delivery system now a day’s mainly to improve patient compliance. In recent years superdisintegrants have been employed to develop effectual mouth dissolving tablets & to overcome limitation of conventional tablets, which is because of their convenience in administration and suitability for patients having dysphagia. It is suited for tablets undergoing high first pass metabolism and is used for improving bioavailability with reducing dosing frequency to minimize side effect and make it more cost effective. Clopidogrel Bisulphate is an oral, thienopyridine class antiplatelet agent used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease. The objective of the present investigation was to prepare Oro dispersible tablets of Clopidogrel Bisulphate by using Solid Dispersion technique; sodium starch glycolate, Croscarmellose sodium and CrosspovidoneXL-10 were used as superdisintegrants in combinations to achieve optimum release profile, disintegration time and hardness. The tablets were formulated by Solid Dispersion technique and the fabricated tablets were evaluated for various micromeritic properties like bulk density, tapped density, compressibility index, Hausner’s ratio, angle of repose and post compression characteristics like thickness, hardness, friability, disintegration time, drug release, drug content, water absorption ratio, wetting time, in-vitro drug release. The drug and excipients compatibility study was performed by FTIR to study the interaction between drug and excipients FTIR studies and short term stability studies. The tablets prepared by solid dispersion technique posses a weight variation in the range 290 to 310mg which is below ±7.5%, hardness of 2.00 kg/cm2to 4.5kg/cm2, disintegration time 10 to 20sec in-vitro drug release showed 98.42% within 10mins.Hence the above said formulation can be upgraded for further research studies and can be made available to common man after all the clinical trials.

22

SYNTHESIS AND IN-VITRO ANTIOXIDANT ACTIVITY SCREENING OF SOME NOVEL SERIES OF THIADIAZOLIDINONE/ IMIDAZO (2.1-b) 1,3,4-THIADIAZOLE DERIVATIVES

M.R. Pradeep Kumar*1, S.S. Honnalli2

1Department of Pharmaceutical Chemistry, SET’s College of Pharmacy, Dharwad- 580002, Karnataka.

2Department of Pharmaceutical Chemistry, KLE’s College of Pharmacy, Hubli-580031, Karnataka.

 

Abstract

Along with the globalization and improper nutrition supply many new diseases are emerging in the world. Oxidative decomposition of cellular components leads to some diseases, which are life threatening one. As anti-oxidants are developing as drug candidates for treating these diseases by preventing the oxidative decomposition of cellular components, there is a need for developing some potent anti-oxidant agents. In this research we have synthesized some novel series of thiadiazolidinone and imidazo(2,1-b)-1,3,4-thiadiazole derivatives. The title compounds, thiadiazolidinone 5(a-b) and imidazo(2,1-b)-1,3,4-thiadiazoles 6(a-j) were synthesized by the reaction between Schiff bases of 1,3,4-thiadiazoles with thioglycollic acid in the presence of ethanol and 2-amino-5-(substituted phenyl)-1,3,4-thiadiazoles with different substituted aryl/heteroaryl a-bromoketones in dry ethanol respectively. Structure of the synthesized compounds was confirmed on the bases of spectral data (IR, 1H NMR and Mass). These compounds were screened for anti-oxidant activity using Nitric oxide scavenging and DPPH method. Ascorbic acid was used as standard drug. The results showed that compounds 6c, 6d, 6g, 6f, 6h and 6j exhibited good anti-oxidant activity. The presence of coumarin moiety in the synthesized drugs potentiates the anti-oxidant activity.

23

IMMUNE MEDIATED THROMBOCYTOPENIA, DIAGNOSIS ANDRECENT ADVANCEMENT IN ITS TREATMENTIN DOGS - A REVIEW

Muhammad Ahsan Naeem*, Bilal Aslam, Ahmad Raza, Tanweer Kaliq,Ijaz Javed Hasan, Junaid Ali Khan, Asghar Ali, Shamshad ul Hassan and Zainab Kaleem

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

Abstract

Mononuclear phagocytic system causes the elimination of platelets with the help of antibodies and as result immune mediated thrombocytopenia (IMT), which there is activation of auto- or allo-antiglobulins against thrombocytes leads to its premature destruction by macrophagic engulfment in dogs. Immune system due to presence of other disorder my cause the destruction of platelets so by confirming the absence of secondary disorder is an evidence that immune system is responsible for causing destruction of platelets and this type of thrombocytopenia is primary immune mediated thrombocytopenia and it can be treated by suppressing immune system with the help of immune suppressive therapy while the thrombocytopenia caused by presence of any other disorder is secondary immune mediated thrombocytopenia which can be treated by removing that disorder which is responsible or due to which this type of immune mediated thrombocytopenia has been occurred or we can also give immune suppressive drug.If dogs suffering from immune mediated thrombocytopenia do not show any response to the therapy then additional immunotherapy can be given and in some cases the examination is repeated again in order to find out any other cause involved which may be left to be identified.

24

SEIZURE RELAPSE BASED UPON WITHDRAWAL PERIOD OF ANTI-EPILEPTIC DRUGS IN PEDIATRIC EPILEPSY PATIENTS

Rajat Rana1,  Soumadip Das2, S Ramesh3, S Chidambaramnathan4, Aravinda Swami5 , Ajit Singh6

1,2 R.M Medical College & Hospital, Annamalai University, India 608002.  

3 R.M Medical College & Hospital, Annamalai University, India.

4 Department of Pediatrics4, RM Medical College, Annamalai University, India.

5 R.M Medical College & Hospital, Annamalai University, India.

6 Manipal College of Pharmaceutical Sciences (MCOPS), Manipal University, India. 

Abstract

This study was done to quantify risk of seizure recurrence after discontinuation of AEDs after varying duration of seizure remission in children with epilepsy and to assess the variables modifying the risk of seizure recurrence. Randomized controlled trials that evaluate withdrawal of AEDs after varying periods of seizure remission in pediatric epilepsy patients which could be unblinded, single blind or double blind. The database searching included Cochrane Epilepsy Group Specialised Register, MEDLINE, EMBASE, CINAHL, WHO Clinical trial register and the Cochrane Central Register of Controlled Trials. Two independent authors extracted the data and assessed trials for quality. The pooled relative risk ratio for early AEDs withdrawal and late AEDs withdrawal was assessed as 1.22(95% CI 0.94 to 1.57), for type of epilepsy pooled relative risk was 1.52(95% CI 0.96 to 2.41), EEG relative risk was assessed as 1.65(95% CI 1.08 to 2.51) and the underlying etiology relative risk ratio was assessed as 1.65(95% CI 1.08 to 2.51).The high grade evidence of this study supports that discontinuing AED medication prior to at least 2 seizure free years is associated with higher seizure recurrence risk than waiting for two or more seizure free years in children.

 

25

PHYTOCONSTITUENTS FROM THE FLOWER OF AGERATINA ADENOPHORA (SPRENG)

Subban Vasanthi1, Velliyur Kanniappan Gopalakrishnan2*

1Department of Biotechnology, Karpagam University, India.

2*Department of Biochemistry and Bioinformatics, Karpagam University, Coimbatore- 641 021, Tamil Nadu, India.

Abstract

Ageratina adenophora Spreng belongs to the Family Asteraceae is a very common weed and reported to possess diverse medicinal properties.  Three compounds 1, 2 and 3 kaempherol diglycoside derivative (1), quercetin-3-O-beta-d-glucopyranoside (2) and  quercetin-3-O-rutinoside (3) were isolated by column chromatography from the methanol extract of the flower part of A. adenophora Spreng   and chemical structures identified by means of their spectral data. This is the first report for the presence of the flavanoids 1, 2 and 3 from the flowers of A. adenophora Spreng.  Further this investigation enhances the chances for the possible utilization of  A. adenophora Spreng as a medicinal herb.

26

HPTLC FINGERPRINTING AND ANTIOXIDANT ACTIVITY OF BARLERIA GRANDIFLORA LEAVES

Nishant M1*, Shilpa V1, Hemant S2, Dhamodaran P1

1JSS College of Pharmacy Ooty,Tamilnadu India- 643001.

2 Shri Rawatpura Sarkar Institute of Pharmacy Durg Chhattisgarh- 490042.

Abstract

The objective of the study was to evaluate the antioxidant potential of the plant Barleria grandiflora Dalz (Acanthacae) (B.G). Phytochemical screening had shown the presence of carbohydrates, proteins, glycosides, phenolic compounds and flavanoids in ethanolic and aqueous extracts of leaves of the plant. HPTLC finger printing revealed the presence of thirteen and four different constituents in ethanolic and aqueous extacts respectively. Column chromatography on ethanolic extracts resulted in to eight fractions. The total phenolic content was determined by Folin-ciocalteu method. The total phenolic content in ethanolic and aqueous extract was found to be 42.32 and 33.43 GAE/ mG respectively. Using lipid peroxidation inhibition, hydrogen peroxide radical scavenging, nitric oxide radical inhibition, ABTS radical scavenging activity, antioxidant potential of ethanolic extract, aqueous extract and fractions resulted from column chromatography were compared using standard antioxidants like ascorbic acid, tocopherol and rutin by calculating IC50 values. Both ethanolic and aqueous extract had shown antioxidant potential. Ethanolic extract and among the fractions resulted out of it, fraction IV and fraction V had shown greater and comparable antioxidant potential to that of standards used. The anti oxidant property of fraction IV and V for various methods was found to be 80.4±1.693 µg/ml and71.3±0.448 µg/ml (LPO), 42.4±0.088 µg/ml and 43.6 ± 0.659 µg/ml (H2O2), 74.9±0.68 µg/ml and 79.1±0.523 µg/ml (NO), 6.2±0.088 and 7.1 ± 0.145µg/ml (ABTS).The total antioxidant capacity of the ethanolic, aqueous, and isolated fractions from column of Barleria grandiflora was measured spectrophotometrically using phosphomolybdenum method. Among ethanolic extract, aqueous extract and the fractions, fraction IV had shown high TAC value 12.1±1.68 mM equivalent to ascorbic acid. This antioxidant potential of the plant may be the reason behind the use of the plant in treatment of oral ulcers.

27

Artesunate-Amodiaquine and Ciprofloxacin Combination Improves Biochemical and Histological Markers of Renal Function of Malaria Infected Mice

Anthony Fidelis Uwah1, Jessie Idongesit Ndem1 , Aniekan Imo Peter2

 1Department of  Biochemistry, Faculty of Basic Medical Sciences, University of Uyo, Akwa Ibom State, Nigeria

 2Department of  Human Anatomy, Faculty of Basic Medical Sciences, University of Uyo, Akwa Ibom State, Nigeria

Abstract

The effects of combining artesunate-amodiaquine (ACT) and ciprofloxacin (quinolone) on some biochemical and histological indices of renal status of adult mice infected with Plasmodium were investigated. This triple regimen is a very common management modality for febrile illness, suspected malaria and malaria-typhoid co-infection in Nigeria. Adult mice were passaged with Plasmodium berghei berghei and observed till parasitemia was achieved. Calculated amount of the drugs were orally administered to both the parasitized mice and the control, based on the standard dosages of 4mg/kg body weight of Artesunate, 10mg/kg body weight of amodiaquine and 9mg/Kg body weight of ciprofloxacin. The drugs were administered for 3 and 5 days for ACT and ciprofloxacin respectively. The results obtained showed a general derangement in serum electrolytes of the group exposed to Plasmodium berghei berghei compared to the normal control. Animals treated with combination of ACT (artesunate- amodiaquine) and ciprofloxacin had chloride, bicarbonate and sodium levels nearer to the normal control group than the groups treated with either ACT or ciprofloxacin only. Treatment of P. berghei berghei infected mice with a combination of ACT and ciprofloxacin yielded a higher serum albumin and total protein levels. The results showed that combining ciprofloxacin with artesunate-amodiaquine had significant restorative effects on the plasmodium-induced renal function derangements in mice.

28

INVESTIGATION OF IN VITRO ANTHELMINTIC ACTIVITY OF PROSOPIS SPICIGERA L.

Siddabathuni Aneela ⃰ 1, Akalanka Dey, 2 A.M.S.Sudhakar Babu3, Somnath De 1

1 Dr. Samuel George Institute of Pharmaceutical Sciences, Markapur- 523316, Andhra Pradesh.

2Annamalai University, Department of Pharmacy, Annamalai Nagar-600 802, Tamil Nadu, India.

3A.M.Reddy Memorial Colleges of Pharmacy, Narasaraopet, Guntur-522601, AndhraPradesh.

Abstract

The methanolic extract of Prosopis spicigera Leaves was investigated for anthelmintic activity using earthworms (Pheretima posthuma). The concentrations (25, 50, and 100mg/ml) of plant extract were tested in this study. Piperazine citrate (10 mg/ml) was used as reference standard drug whereas distilled water as control. Determination of paralysis time and death time of the worms were recorded. Extract exhibited significant anthelmintic activity at the concentration 100mg/ml. The result shows that methanolic extract possesses vermicidal activity and found to be effective as an anthelmintic. Therefore, the anthelmintic activity of the methanolic extract of Prosopis spicigera Leaves has been reported.

29

A STUDY ON PRESCRIPTION PATTERNS AND RATIONALITY OF ANTIMICROBIALS IN GYNECOLOGY DEPARTMENT IN A HOSPITAL

Sana Afreen1, Sidhra Fatima1, Muniba Suad1, Mohd Nasir Mohiuddin1, Dr.Ayesha Jehan2

1Deccan school of Pharmacy, Dar-us-salam, Aghapura, Hyderabad-01. A.P. India.

2Department of gynecology and obstetrics, Princess Esra Hospital.

Abstract

Background: Prescriptions should be assessed to know the attitude of the physicians towards their prescribing, their therapeutic knowledge upgrading need/requirement and to ensure rationality in the prescription. There is no clear indication of antimicrobials given to approximately half of the hospitalized patients, for its use, choice and duration of therapy. The systematic assessment and feedback on usage patterns and rationality of antimicrobials may greatly help physicians in prescribing rationally. Objective: To assess the prescribing patterns and rationality of antimicrobial agents in the patients of gynecology department.Methods: Drug data of all the antimicrobial drugs prescribed, dose frequency, route of administration and dose were recorded. Results: A total of 220 patients were admitted to the in-patient and out-patient department during the study period. 47% were in-patients and 53% were out-patients. 46 patients were on Monotherapy, 77 patients on two drug therapy, 48 patients were on combination therapy of three drugs. A total of 61 prescriptions were irrational and 159 prescriptions were found to be rational out of 220 prescriptions. Conclusions: Antimicrobials are over used, particularly for minor infections, misused for viral infections and underused due to financial concerns. Our finding indicates an urgent need for the establishment of proper guidelines and supervision of antibiotic usage.

30

INTESTINAL PERMEABILITY STUDIES EMPLOYING CELL CULTURE MODELS - CRITICAL ISSUES INVOLVED

Ramesh KVRNS*, Shahnaz Usman, Omar Sarheed and Fasiha Shah

RAK College of Pharmaceutical Sciences, RAK Medical & Health Sciences University, PB No. 11172, Ras Al Khaimah, UAE

Abstract

Intestinal permeability is an important prerequisite for drug compounds which show promising pharmacological and therapeutic properties.  Several medicinally useful substances get rejected for not showing sufficient gastrointestinal absorption features. So to optimally characterize a lead compound’s intestinal permeability – it is essential that the investigators employ models which can reliably predict the permeability. Of the various models that were developed over the years – cell culture models have gained in importance because of the ease and rapidity with which the screening of drugs can be performed. However the cell culture models themselves have inherent limitations which if the investigators overlook can lead to unreliable and under or over prediction of permeability. The biochemical and physical properties of cultured cells can vary depending on the cultural and other conditions which entail that the intestinal permeability studies are carried out following standardized protocols and addressing the critical issues involved in employing the cultured cells. The outcomes of the research studies of various investigators are summarized in this review article. The findings of the literature survey and a study of the investigations indicate that permeability studies – are influenced by a number of factors and the studies are to be performed addressing various critical issues. It may be concluded from the various research studies that reliable and reproducible cell lines need to be employed to enable smooth and early regulatory acceptance. The research studies of various investigators suggest that Caco-2 cells possess a variety of advantages and are widely employed in permeability assessment of drugs.

31

A REVIEW ON PHYTOCHEMICAL ANALYSIS BY USING CALLUS EXTRACTS OF IMPORTANT MEDICINAL PLANTS

Dr. Sirigiri Chandra kala*

Department of Botany and Microbiology, Acharya Nagarjuna University, Nagarjunanagar, Guntur – 522510, Andhra Pradesh, India.

Abstract

A large number of medicinal plants are explored from the natural flora for the production of commercial drugs. The past few decades have seen increasing scientific interest in both growth of plant tissue culture and the commercial development of this technology as means of producing valuable phytochemicals. The most important of these bioactive constituents of plants are alkaloids, tannins, terpenoids, saponins, quinones, flavonoids, steroids, cardiac glycosides, oils and phenolic compounds.  This review also covers the different methods of qualitative phytochemical analysis and revealed the phytochemicals used with different phytohormone combinations of tissue culture medium in some medicinal plants calli.  Phyto pharmacological screening of medicinal plants and their extracts will reveal their presence of valuable compounds and provide insight into new ways of treatment with new drugs.  Phytochemical constituents are the basic source for the establishment of several pharmaceutical industries.

32

STABILITY INDICATING METHOD FOR THE DETERMINATION OF KETOROLAC TROMETHAMINE IN PHARMACEUTICAL FORMULATIONS BY HPLC

Bhagyashree R. Dhumal1*, Madhukar R. Tajne2, Kishore P. Bhusari1, Mahavir H. Ghante1, Nishant S. Jain3.

1Sharad Pawar College of Pharmacy, Hingna Raod, Wanadongari, Nagpur-441110, India

2Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur-440033, India

3Institute of Pharmaceutical Sciences, Guru Ghasidas Central University, Bilaspur

Abstract

RP-HPLC stability indicating method was developed for determining Ketorolac in pharmaceutical formulations and its degradation products using C8 column with the mobile phase containing mixture of buffer (water [45] + glacial acetic acid [10 ml]: Methanol in the ratio of 35:65 v/v/v at a flow rate of 1.0 ml/min was found to yield satisfactory retention time of about 5.321 min with sharp symmetrical peak at a detection wavelength of 254 nm. The method was validated using ICH guidelines and was found to be  linear in the range 0.1-0.5 µg/ mL. The methos proposed shows good separation of Ketorolac and its degradation products. The developed method can be applied successfully for the determination of Ketorolac.

33

SYNTHESIS AND CHARACTERIZATION OF CERTAIN THERMOTROPIC LIQUID CRYSTALLINE RANDOM COPOLYESTERS AND THE STUDY OF THEIR BLEND NANOFIBERS

P Sathish1, D Reuben Jonathan2, M Mayavathi1 and D Roopsingh 1

1PG and Research Department of Chemistry, Presidency College, Chennai – 600 005, Tamilnadu, India.

2Department of Chemistry, Madras Christian College, Chennai – 600 059, Tamilnadu, India.

Abstract

A new set of two thermotropic liquid crystalline  random copolyesters were generated by utilizing 4,4’-oxybis(benzoic acid), 2,6-napthalene dicarboxylic acid with  a common diol, namely, 2,7-bis(4-hydroxy-3-methoxybenylidene)cycloheptanone and  hydroquinone bis(2-hydroxyethyl)ether by direct polycondensation in dry pyridine solvent  with diphenylchlorophosphate (DPCP) as the condensation agent. These copolyesters had inherent viscosity values of 1.15 dl/g and1.65 dl/g. The structural aspects were resolved by making use of FT-IR, 1H and 13C NMR spectroscopy. Differential scanning calorimetry was involved in deducing the thermal transition behavior of the copolyester. Composite nanofibers were produced by electrospinning by blending the copolyester PNVH with polyvinylchloride (PVC) in tetrahydrafuran (THF) and then with PVC and nanoclay in THF. The surface morphology of the polymer composite nanofibers was investigated by scanning electron microscopy (SEM). These composite nanofibers may emerge as suitable materials for drug delivery system.

34

FAST DISSOLVING TABLETs (FDTs): RECENT TRENDS AND NEW MARKET OPPORTUNITIES

Sanket Kumar*, Shiv Kr. Garg, Ajay Anseri, Pradeep Luhani

Research Scholar, Dept. of Pharmaceutics, Maharishi Arvind College of Pharmacy, Ambabari, Jaipur, Rajasthan, India.

Abstract

Fast dissolving tablets are those intended to dissolve on a patients tongue rather than swallowed. This is becoming an increasingly popular dosage form as typically no water is required. This doses form has received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical industry. Oral drug delivery remains the preferred route for administration of various drugs. Recent developments in the technology have prompted scientists to develop FDTs with improved patient compliance and convenience. The popularity and usefulness of the formulation resulted in development of several FDT technologies. FDTs are solid unit dosage forms, which disintegrate or dissolve rapidly in the mouth without chewing and water. FDTs or orally disintegrating tablets provide an advantage particularly for pediatric and geriatric populations who have difficulty in swallowing conventional tablets and capsules. Developing FDTs can be challenging since the tablet must dissolve fast along with having a pleasant taste and mouth feel. Typically, the tablet should dissolve in less than 30 seconds according to the USP disintegration test method. While designing FDTs, it is mandatory to consider the physiochemical and pharmaceutical aspects of the drug as well as the biopharmaceutical aspects. Methods of preparation include freeze drying, cotton candy, molding, spray drying, compaction and mass extrusion. In the evaluation process, although many parameters are of that of the tablets, the standard pass range varies so as to meet the requirement of fast disintegrating properties of the formulation.

35

QUALITATIVE AND QUANTITATIVE CHARACTERIZATION OF PHYTOCONSTITUENTS FROM FRUITS OF STEREOSPERMUM COLAIS (BUCH.-HAM. EX DILLWYN) MABB

MD. Imran 1*, Mohib Khan2

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

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

Abstract

In qualitative analysis, the phytochemical compounds such as steroids, carbohydrates, triterpenoids, coumarines, phenolic compounds, flavonoids, saponins, anthroquinones, Proteins and lipids were screened in fruit of S.  colais. Quantitative analysis of phenols, flavonoids and Triterpenoids was further performed. Thin layer chromatography was used to analyze the active Phytoconstituents.  Preliminary phytochemical screening of fruit methanolic extracts identified 11 major functional groups, amongst them flavonoid, phytosterols, saponins and coumarins. Additionally total ash analysis of identified three inorganic elements, iron, chloride and sulphate. The same extract was used for quantitative determination of total phenolic content (72.5 mg/g), total flavonoid content (70.53 mg/g) and total triterpenoids content (12.68 mg/g). For further purification of identified chemical constituents, TLC was performed and it showed remarkable results. The methanolic extract of S.  colais fruit contains beta sitesterol and lupeol which are very useful therapeutically.

36

FORMULATION AND IN-VITRO EVALUATION STUDIES ON EFFERVESCENT FLOATING MATRIX TABLETS OF CEFACLOR BY DIRECT COMPRESSION TECHNIQUE

S.Chandra1, D.Kilimozhi2

1Department of Pharmaceutics, J.K.K.Munirajah foundation college of Pharmacy, B.Komarapalayam,Tamilnadu,India-638183

2 Department of Pharmacology, Annamalai university, Chidambaram, India

Abstract

The main aim of the study is to formulate the floating tablets of cefaclor drug by using the polymers such as HPMC K15M,K100M and Carbopol 934P  which were prepared by direct compression technique.The tablets were prepared by varying the concentrations of polymers. The drug polymer compatibility was studied by FTIR studies.The tablets were evaluated by weight variation, hardness, Friability,drug content, In Vitro buoyancy studies, Swelling studies & In vitro dissolution studies. No significant drug polymer interactions were observed in FTIR studies. In vitro drug release profile of cefaclor tablets was examined in pH 0.1N HCl for the 12 hrs and the percentage drug release was found to be 94.91%.The formulated tablets had shown higher percentage drug release by the optimized formulation F11,better swelling and buoyancy.By the stability studies there are no significant difference in formulations F11 and the kinetic studies such as Zero order Plot, First order plot, Higuchi’s Plot and Korsemeyer Peppa’s plot .By the applying kinetic studies to the In vitro drug release which follows korsemeyer Peppa’s and showss anomalous type or non Fickian diffusion.

37

EVALUATION OF CITRULLUS LANATUS SEEDS GUM AS A BINDER IN TABLET FORMULATION

Shilpa P. Chaudhari, Ganesh K. Akuskar, Jitendra V. Bangar, M. P. Ratnaparkhi .

Marathwada Mitra Mandal’s College of Pharmacy, Thergaon, Pune-33, University of Pune, Maharashtra, India.

The aim of current study was to extract the gum from Watermelon (Citrullus lanatus) seeds and to investigate the compressional behavior of gum in tablet formulation in comparison with standard binders such as starch using Heckel and kawakita plot. Using paracetamol as model drug granules were prepared with different concentration (1%, 1.5, 2%, 2.5, and 5%) of the gum and binder by wet granulation method. The granules and tablets were evaluated for their flow properties, hardness, weight variation, thickness etc., and found to have hardness and disintegration time slightly more compared to starch as binder and hence satisfactory for preparing compressed tablets. The study revealed that the Citrullus lanatus seed gum compared favourably with the standard starch as a binder but plasticity of starch is more than Citrullus lanatus seed gum as binder. The Citrullus lanatus seed gum has a potential for formulating sustained release formulations due to prolong drug release.

38

EFFECT OF AT1 BLOCKER LOSARTAN ON LOCOMOTION AND NEUROBEHAVIOURAL ASSESSMENT

Ch.Maheswara Reddy, P.Padmabhushanam, K.F.H.Nazeer Ahmed, A.Tamil Selvan

Department of Pharmacology, Teegala Krishna Reddy College of Pharmacy, Medbowli, Meerpet, Hyderabad, Andhra Pradesh, India.

Cerebral ischemic injury caused by bilateral common carotid artery occlusion (BCCAo) shows impaired neurological deficit and sensory motor dysfunction. Enhanced production of oxidative stress markers (TBARS) and depletion of superoxide dismutase (SOD) and catalase (CAT) is involved in the development of apoptosis in brain. Chronic administration of AT1 blocker losartan prevents brain injury caused by ischemia and reperfusion. The present study is aimed to test the chronic oral administration of Losartan AT1 blocker in mice with cerebral ischemia/reperfusion induced stroke. The two different doses of Losartan (1mg & 10mg) were used in the present experimental model of stroke. The data from sensory and neurobehavioral of ischemic mice treated with losartan suggests an improvement in the sensory motor and neurological deficit due to chronic blockade of AT1 receptor in the brain. In addition Losartan treatment reduced the lipid per oxidation and influences Bcl-2 and attenuates Caspase-3 in the cerebral cortex and hippocampus of the ischemic mouse brain. This is the first kind of reports suggests that long term oral administration after 40 day of reperfusion influences the anti-apoptotic markers of the mouse brain. The anti-apoptotic effect of losartan in this study may have the potential for stroke prevention.

39

FAST DISINTEGRATING TABLETS OF METOCLOPRAMIDE HCL PREPARED BY WET GRANULATION METHOD USING PLANTAGO OVATA MUCILAGE

Shahidulla S M*1, Mohib khan2, Jayaveera K N3

1Dr. Samuel George Institute of Pharmaceutical Sciences, Markapur.

2Oriental College of Pharmacy, Mumbai.

3Jawaharlal Nehru Technological University, Anantapur.

Metoclopramide HCl is a potent dopamine receptor antagonist used for its anti emetic and prokinetic properties. Thus it is primarly used to treat nausea and vomiting, and to facilitate gastric emptying in patients with gastroparesis. In the presence study, fast disintegrating tablets of Metoclopramide HCl were prepared for to enhance patient compliance by wet granulation method. In the presence study, to prepare fast disintegrating tablets of the drug using, plantago ovata mucilage and crospovidone were used as superdisintegrants (2.5 to 10 % w/w) along with starch paste as a binder. The disintegrant incorporated during the wet granulation process as extra granular incorporation. The prepared tablets were evaluated for hardness, friability, drug content uniformity, wetting time, water absorption ratio and in vitro dispersion time. Based on in vitro dispersion time ( approximately 13 s), the two formulations were tested for the in vitro drug release, short term stability (at 400/75% RH for 3 months) and drug excipient interaction (IR spectroscopy). Among the two promising formulations, the formulations prepared by using 10% w/w of plantago ovata mucilage and 32% w/w of starch paste as emerged as the overall best formulation (t50% 2.50 min) compared to conventional commercial tablets formulation (t50% 6.20 min). Short-term stability studies on the formulations indicated that there are no significant changes in drug content and in vitro dispersion time (p<0.05). The results concluded that natural super disintegrants like Plantago ovata mucilage showed better disintegrating property than the most widely used synthetic super disintegrant like cross povidone in the formulations of Fast disintegrating tablets.

40

PHARMACOGNOSTIC STUDIES AND PRELIMINARY PHYTOCHEMICAL SCREENING ON THE ROOT OF GLYCOSMIS PENTAPHYLLA (Retz.,) DC., (RUTACEAE)

M. Sivakumar*, D. Chamundeeswari

Department of Pharmacognosy, Faculty of Pharmacy, Sri Ramachandra University, Porur, Chennai, India.

Glycosmis pentaphylla (Retz.,)DC (Rutaceae) is an important traditional medicinal plant being used for treatment of cough, rheumatism, anemia, antioxidant and jaundice. Systematic pharmacognostical evaluation of the root of the plant has been carried out with respect to macroscopy, microscopy, physicochemical parameters and estimation of different standards. TLC profiles were developed for petroleum ether, chloroform, ethyl acetate and ethanol extracts. The preliminary phytochemical investigations indicated presences of alkaloids, terpenoids, flavanoids, tannins, sugar, glycoside and phenolic compounds. The results obtained are useful for standardization of the root established the macro, micro, powder microscopy and physiochemical parameters to characterize the genuine plant drug. This parameter can be utilized for quick identification of the drug and are particularly useful in the case of powdered forms and also contribute towards establishing pharmacopoeial standards for the specified plant. Glycosmis pentaphylla possesses medicinally important secondary metabolites; these can be employed in the treatment of various diseases.

41

SYNTHESIS AND BIOLOGICAL ACTIVITIES OF SCHIFF BASES OF 2, 5 – DIMERCAPTO 1, 3, 4-THIADIAZOLE DERIVATIVES

Kanakasabai Sundaram and Ravi Subban*

Department of Chemistry, Karpagam University, Coimbatore-641 021, Tamilnadu, India.

The biological activities of 1, 3, 4-thiadiazole have been reviewed in the last few years. 2,5-di (Mercapto-aceticester)-1.3.4-thidiazole (2) prepared from 2, 5 – Dimercapto -1, 3, 4-thiadiazole was treated with hydrazine hydrate in methanol to yield 2,5-di (Mercapto-acetic hydrazide)-1.3.4-thidiazole (3).The condensation of compound 3 with various aromatic aldehyde yielded the corresponding Schiff bases of substituted 2,5 – Dimercapto -1,3,4-thiadiazoles(4a-j). The structures of the Schiff bases were elucidated by IR, 1H- and 13C -NMR spectral measurements. The target compounds 4a-j was screened for their in vitro antimicrobial activity and the Minimum Inhibitory concentration of each compound was determined by liquid broth method. From newly synthesized series of compounds 4f and 4j exhibited significant antimicrobial potential against Staphylococcus aureus and Bacillus substilis (gram-positive), Escherichia coli and Salmonella enteritidis (gram-negative) bacteria. The compounds also showed significant antifungal activity against Candida albicans, Trichophyton rubrum, Trichoderma viride and Aspergillus flavus.

42

SPECTROFLUORIMETRIC QUANTIFICATION OF ETHAMBUTOL HYDROCHLORIDE IN BULK AND ORAL DOSAGE FORM

A.M.Sekar*, S.Anbazhagan, A.Baskar, N.Saranya, D.Rajakumari

Department of pharmaceutical chemistry, Surya School of Pharmacy,Surya group of Institutions, Vikravandi-605652, Tamil Nadu, India.

Two new, simple and sensitive spectrofluorimetric methods have been developed for the estimation of ethambutol hydrochloride in bulk and oral dosage form. Method A involves the determination of ethambutol hydrochloride by direct spectrofluorimetric method the relative fluorescence intensity was measured an emission wave length ( λem ) of 521nm with an excitation wave length ( λex ) at 385nm; the fluorescence concentration range was found to be 0.2-1.0μg/mL; Method B involves the determination of ethambutol hydrochloride by oxidative spectrofluorimetric method using potassium permanganatethe relative fluorescence intensity was measured an emission wave length ( λem ) of 469nm with an excitation wave length ( λex ) at 405nm; the fluorescence concentration range was found to be 0.2-1.0μg/mL. The correlation coefficients for the methods were found to be 0.998 & 0.999. The methods showed good reproducibility and recovery. So the proposed methods were found to be simple, precise and accurate. The results of analysis have been validated statistically by ANOVA method and by recovery studies.