IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
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MARCH 2018
1

“A STUDY ON PRESCRIBING PATTERN OF ANTIMICROBIAL AGENTS IN PATIENTS SUFFERING FROM PELVIC INFLAMMATORY DISEASE IN A TERTIARY CARE TEACHING HOSPITAL”

Anju Paulose*, Bharathi D.R.1, B. Shankar Reddy1, Anju Arpana2, Anto John1, Anu Rajan1, Rahul Jose1, Y Satyakrishna1
1Department of Pharmacy Practice, SJMCP, Chitradurga, Karnataka, India.
2Department of OBG, BMCH & RC, Chitradurga, Karnataka, India.

Pelvic inflammatory disease (PID) constitute the Upper reproductive tract infection in women and a major health concern leading to profound gynaecological morbidity among women in reproductive age group with impact on individual women, their families and communities. These infections entail a heavy toll on women, if untreated they can cause long-term complications, such as tubal infertility, ectopic pregnancy, chronic pelvic pain and abortions. Objectives: To analyze and evaluate the rationality of prescribing pattern of AMAs in PID and to monitor the ADRs & drug interactions, if any, with AMAs & concomitant drugs. Materials and Methods: A six months prospective observational study was carried out at OBG In-Patient department of Basaveshwara Medical College Hospital & Research Centre, Chitradurga. Results: A total of 85 patients were enrolled in the study aged above 18 years from the OBG In-Patient department. Coming to the prescription pattern of antibiotics Nitroimidazoles & Cephalosporin’s were majority of 36.36% & latter with 29.54. Coming to the concomitant drugs, NSAIDs & antacids were major in proportions (7.24% & 44.15%). Coming to the combination of antibiotics mostly prescribed drugs were Nitroimidazoles + Cephalosporins (37.34%) & Nitroimidazoles + Fluoroquinolones(13.29%). Conclusion: This study concludes that Nitroimidazoles & Cephalosporins were the first line choice of antibiotics in PID either alone or combination of same. NSAIDs with the combination of Aceclofenac/Diclofenac with Camylofin were mostly preferred for relieving pain & antacids were co-prescribed with NSAIDs to avoid NSAID induced gastric irritation.

2

A COMPREHENSIVE PHYTOPHARMACOLOGICAL REVIEW OF STEVIA REBAUDIANA

Pankaj Khuspe1*, Kishori Kokate1, Trushali Mandhare1, Ajay Kharche2, Prashant Kumar Katiyar2
1Navsahyadri Institute of Pharmacy, Naigoan, Nasrapur, Pune-412213.
2Ideal College of Pharmacy & Research, Bhal, Kalyan-421306.

Stevia rebaudiana is known for not only its nutritional values but also for medicinal benefits. Stevia rebaudiana is one of member of the genus Stevia. In the era of synthetic medicine and excipients natural plants and their products can be used as sources of medicine & exciepients. Stevia rebaudiana is belongs to family Astaraceae. With varieties of chemical constituents stevia rebaudiana consist of antioxidants like flavonoids and various phenolics, essential oils, tannins, etc. It is a natural source of steviol glycosides, like rebaudioside A and a potential source of prebiotics, with promising beneficial immunomodulating activity. Stevia rebaudiana is natural sweetener & is about 300 times sweeter than table sugar. Nutritional value of Stevia rebaudiana is beneficial for both the geriatrics & pediatrics ones. Stevia shows antiseptic, antiglycemic, antimicrobial, antibacterial, anticancer activity & also be used in indigesion, stomach upset, heart burn, weight loss, etc. It is expected hope for diabetic people who have craze to eat sweet. The aim of this review article is to describe systematic information with detailed exploration of pharmacological properties of stevia rebaudiana which will provide a direction for further research.

3

EVOLUTION OF CRUDE EXTRACT AND FRACTIONS OF Camellia sinensis LEAVES AGAINST HUMAN PATHOGENIC BACTERIALSTRAINS

Ganesan S*, Rajakumar R
Department of Biotechnology, MarudhuPandiyar College, Thanjavur-613 403, Tamil Nadu, India.

The main purpose of this study was to find out the antibacterial activity of individual crude extract and fraction and mixture active fraction of Camellia sinensis. For antibacterial test, disc diffusion technique was used against human pathogenic bacterial strains. The noteworthy inhibition of ethanol mixed methanol active fraction was inhibit 7 mm zone against Streptococcus pneumoniae, and 8 mm zone against Staphylococcus aureus, it was higher activity than allindividual fractions and crude extract. In the GC-MS analysis, 20 bioactive phytochemical compounds were identified in the ethanolic fraction of Camellia sinensis. Further work needs to be done in these materials including fractionation to isolate active constituents and subsequent pharmacological evaluation.

4

SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF NOVEL PYRROLYL PYRAZOLINE METHANONE DERIVATIVES

C. S. Hallikeri*, Poul Rubeza, Sheshagiri R. Dixit, Venkatarao H. Kulkarni, Shrinivas D. Joshi
Novel Drug Design and Discovery Laboratory, Department of Pharmaceutical chemistry, S.E.T’s College of Pharmacy, Sangolli Rayanna Nagar, Dharwad 580 002, India.

Novel pyrrolyl-pyrazoline methanone derivatives (5a-j) were synthesized by reacting mixture of substituted quinoline chalcones (3a-j) and 4-pyrrol-1yl benzoic acid hydrazide (4) in ethanol. The reaction mixture was heated under reflux for 16 h on a water bath followed by addition of ice cold water at room temperature and mixture was kept overnight resulting in the formations of substituted pyrrolyl-pyrazoline methanone derivatives. Purity of newly synthesized compounds were confirmed by TLC and melting point. The structure of the all newly synthesized compounds were confirmed by spectral study such as IR, 1H NMR and Mass spectroscopy. The title compounds were screened for their antibacterial and antitubercular activities.

5

AN OVERVIEW OF THE SIDDHA POLYHERBAL FORMULATION - ATHIMADHURA CHOORANAM FOR MIGRAINE HEADACHE

Mathipriya T1, Kasirajan N2, Maanickha Chelvi KS2
1Siddha physician, Sankarankovil, Tamilnadu.
2Siddha Regional Research Institute, Thiruvananthapuram.

The Siddha system of medicine is one of the ancient and primitive medical systems. The major strength of this Siddha system is its ease handiest, wide accessibility, naturalness of the products and cost effective. Siddha medicine has specialized therapeutic procedures for rejuvenation, health promotion and prevention. “Siddha Materia Medica” (Medicinal Plants Division) illustrates a safer and more potent poly herbal formulation “Athimadhura Chooranam” (AMC) comprised of three herbal ingredients such as Glycyrrhiza glabra, Pimpinella anisum and root bark of Plumbago zeylanica. This formulation is very effective an anti-inflammatory and analgesic. The aim of this systematic review of the literature was to summarize the literature on the safety and anti inflammatory and analgesic activity of the above herbs. Textbooks on medicinal plants, research papers and their bibliographies were also searched. These included studies on the anti-pyretic, anti-allergic, anti-bacterial, anti-viral, anti-hepatotoxic, anti-tussive & expectorant, antioxidant activity, etc, and also phyto compounds were identified. Conclusion of this review validates that all ingredients of AMC have anti inflammatory and analgesic activity based on research papers and Siddha literature.

6

SIDDHA THERAPEUTICS FOR THE MANAGEMENT OF PCOS - A REVIEW

A. Faridha*, Gayathri Gunalan, A. Rajendra Kumar
Siddha Regional Research Institute (CCRS), Kuyavarpalayam, Puducherry – 605013.

Siddha system of medicine is the renowned indigenous traditional system, provided for all the lives of earth by the scientific sages, Siddhars. The therapeutic methodology in Siddha is based mainly on three humors viz, vatham, pittham and kabam, which are when altered from its equilibrium, results in various ailments. In Siddha, etiology of a disease is mainly depicted with alterations in lifestyle, diet and environmental conditions. As a part of such modifications, PCOS is a major troublesome complication among female population in recent days. In Siddha literatures, Pararasasegaram, Yugimuni vaithiya kaaviyam, Gnanavettiyan -1500, PCOS and its associated complications may be related to sinaipai neer kattigal, soothagavaayu, soothaga kattigal, soothaga thadai, karparogam, karpa vaayu. PCOS, being a major restraint for healthy life, results in arising health issues such as hyperandrogenism, anovulatory menstrual cycle, sub-fertility, obesity, amenorrhoea and dysmenorrhoea along with insulin resistance. To overcome the adverse effects of available modern treatment, we are in need of implying the better methodology for the treatment of PCOS to sustain the growing female population of reproductive age. The objective of this review is to emphasize various Siddha formulations and available herbal-polyherbal practices for PCOS, which are depicted in the literatures possessing potential therapeutic values, are discussed with scientific validations. The management protocol ensures not only the treatment but also for the prevention and recurrence of the disease condition. The medicines practiced may be adopted for scientific validation in future for further clinical and research purposes.

7

CLUSTER HEADACHES- A REVIEW

Nakka Varshitha*, D.Sai Aravind, Dr.G.Susmitha, Dr.G.Ramesh, Dr.V.Tejaswi, Dr.P.Srinivasa Babu
Department of Pharmacy Practice, Vignan Pharmacy College, vadlamudi, GunturS-A.P.

Cluster headache is a neurological disorder characterized by recurrent, severe headaches on one side of the head, typically around the eye. This condition usually first occurs between 20 and 40 years of age. Men are affected about four times more often than women. Based on the duration cluster headaches can be classified in to acute or episodic cluster headache and chronic cluster headache. The exact cause of cluster headache is unknown. The activation of trigeminovascular,cranial parasympathetic and Internal carotid artery dilation may lead to painful vascular changes within the cavernous sinus, secondary involvement of the sympathetic plexus overlying the cavernous ceratoid artery, and stimulation of secretory function of the lacrimal and other mucosal glands. Common signs and symptoms during a headache include Excruciating pain, generally situated in or around one eye, but may radiate to other areas of your face, head, neck and shoulders ,One-sided pain. Differential diagnosis is necessary. Triptans and supplemental oxygen are first-line abortive therapies for cluster headache. Verapamil and lithium are the mainstays of treatment for chronic cluster headache. Prophylactic therapy is intended to shorten the duration of episodic cluster attacks, in addition to reducing the frequency and severity of attacks in both episodic and chronic cluster headache.

8

DETERMENATION OF SIMULTANEOUS ESTIMATION HPLC METHOD FOR ELITRAGRAVIR, TENOFOVIR DISPROXIL FUMARATE, EMTRICITABINE AND COBICISTAT ITS BULK AND TABLET DOSAGE FORM.

S. K. Godasu, S. A. Sreenivas
Mewar University, Chittorgarh, Rajasthan.

A New method was established for simultaneous estimation of Elvitegravir, Tenofovir, Emtricitabine and Cobicistat by RP-HPLC method. Chromatographic separations were carried using Inertsil ODS (4.6 x 250 mm, 5?m) column with a mobile phase composition of 0.1% OPA buffer and Acetonitrile(30:70) have been delivered at a flow rate of 1ml/min and the detection was carried out using waters HPLC auto sampler, separation module 2695 with PDA detector 2996 at wavelength 252 nm.The retention time for Elvitegravir, Tenofovir, Emtricitabine and Cobicistat were 2.287, 2.957, 5.652 and 9.801 minute respectively. The correlation coefficient values in linearity were found to be 0.999 and concentration range 75-225 ?g/ml for Elvitegravir, 150-450 ?g/ml for Tenofovir, 100-300 ?g/ml for Emtricitabine and 75-225?g/ml for Cobicistat respectively. For accuracy the total recovery was found to be 100.11%, 100.26, 100.64 and 100.08% for Elvitegravir, Tenofovir, Emtricitabine and Cobicistat respectively. The LOD and LOQ for Elvitegravir was found to be 2.98 and 9.98, LOD and LOQ for Tenofovir was found to be 3.02 and 10.02, LOD and LOQ for Emtricitabine was found to be 3.00 and 10.00 and LOD and LOQ for Cobicistat was found to be 3.00 and 10.02. The force degradation studies were performed for the dosage form and the results are within the limits. The results of study showed that the proposed RP?HPLC method is a simple, accurate, precise, rugged, robust, fast and reproducible, which may be useful for the routine estimation of Elvitegravir, Tenofovir, Emtricitabine and Cobicistat in pharmaceutical dosage form.

9

PROTEOMIC STUDIES OF CHEMICAL CONSTITUENTS OF EUPHORBIA HIRTA

Nagavalli Dhandapani*, Saranya sundaralingam, Anu Baskaran, Aruna Muthusamy, Brindha Vasudevan, Dhivya Murugan, Divya Gopalakrishnan, Sujaritha jayaraj.
Adhiparasakthi College of Pharmacy, Melmaruvathur.

The present research work was aimed to discover anti-viral and anti-dengue activity of the phytochemicals present in Euphorbia hirta using Molecular docking studies. In this research work, we have screened anti-dengue and anti-viral activity of 10 chemical constituents from Euphorbia hirta through docking studies, the target enzymes were chosen for the study is 3P54, 2V33, 5B1C, 4M9K and 5FC8 using Argus lab 4.0.1 software. Among the 10 screened compounds of Euphorbia hirta, shows best to moderate (-9.49194kcal/mol to –5.61913kcal/mol) binding energy and various bonding interactions against the targeted proteins. On the basis of docking study results, it can be concluded that chemical constituents of Euphorbia hirta, serve as promising chemical probes to design therapeutic agents with anti-dengue and antiviral properties.

10

“IN VITRO EVALUATION OF ANTHELMINTIC ACTIVITY OF JUICE OF EUPHORBIA LIGULARIA ROXB.”

Akshay M Baheti*1, Shikha A. Baheti2, Suvarna Ingale3, Chinmay Deshmukh1, Manish S.Wani1
1MAEER’s Maharashtra Institute of Pharmacy, Paud Road, Pune, India- 411038.
2Sohit Pharmacy, Bavdhan, Pune.
3SCES, Indira College of Pharmacy, Wakad.

The aim of present study was to evaluate anthelmintic potential of the juice of Euphorbia ligularia using Pheretima posthuma and Ascardia galli as test worms. Various concentrations (10 – 100 mg/ml) of juice were tested in the bioassay, which involved determination of time of paralysis (P) and time of death (D) of the worms. Piperazine citrate (10 mg/ml) was included as standard reference and distilled water as control. The results of present study indicated that juice significantly demonstrated paralysis, and also caused death of worms especially at higher concentration of 100 mg/ml, as compared to standard reference Piperazine citrate. In conclusion, the E. ligularia juice as an anthelmintic have been confirmed.

11

EVALUATION OF ANTI-CANCER ACTIVITY IN METHANOLIC EXTRACT OF ENICOSTEMMA LITTORALE ON DEN INDUCED HEPATOCARCINOGENESIS IN RATS

Abarnadevika Alagiri, Thanga kokila Mookiah, Ariharasivakumar Ganesan, Manisenthil Kumar Thigarajan, Rajasekaran Aiyalu, Arivukkarasu Ramasamy*
KMCH College of Pharmacy, Coimbatore, Tamilnadu, India-641048.

The present study is aimed at evaluating the chemoprotective effect of Enicostemma littorale in DEN induced hepato-carcinogenesis in Sprague Dawley rats. The preliminary steps involved extraction, phytochemical investigation, HPTLC study and In vitro antioxidant activity using DPPH, ABTS. and Initiation of HCC was done by single i.p injection of DEN at a dose of 200mg/kg. The MEEL received treatment for 90 days after 14 days of development of HCC and continued for entire study period, whereas the other two group given normal saline, 5-flurouracil (20mg/kg ) i.p. The results showed that the injection DEN lead to the development of liver tumors in rats. Significant effect of serum biochemical parameter like SGOT, SGPT, ALP, UREA, TOTAL PROTEIN and tumor marker was observed with depletion of endogenous antioxidants SOD, CAT, GSH, there by leading to higher LPO. The result exhibited that MEEL treatment (Preventive) group offered excellent shielding against HCC and displayed all the parameter in near normal range with a maintained antioxidant enzyme system. The result obtained showed that extracts were found to containing phenols at a concentration of 70.25 mg/g and flavonoids 26.03mg/g. HPTLC Analysis showed presence of Quercetin, Mangiferin, Gallic acid, Catechin and sweroside. In the DPPH, ABTS, FRAP, TRAP radical scavenging assay MEEL has displayed the highest antiradical activity in both assays and was also comparable with the standard qucertein The present study reveal the efficacy of the MEEL to prevent malignancy induced by chemical carcinogen and the phytoconstituents responsible for activity.

12

ESTIMATION OF PHYTOCONSTITUENTS AND COMPARATIVE EVALUATION OF ANTI-OBESITY ACTIVITY OF AYURVEDIC AND HOMEOPATHIC MEDICINES IN HIGH FAT DIET ANIMAL MODEL

Saravanan Jayaram, Sangeetha Govindaraj, Ariharasivakumar Ganesan, Ramasamy Muthu, Jeevanantham Appusamy, Rajasekaran Aiyalu, Arivukkarasu Ramasamy
KMCH College of Pharmacy, Coimbatore, Tamilnadu, INDIA-641048.

The objective of the study is to assess the anti-obesity activity of ayurvedic and homeopathic formulations namely Stholyantak churna and Phytolacca berry in high fat cafeteria diet induced obesity (HFCD). Obesity was induced by administration of HFCD for a period of 42 days and both the formulations were given for 42 days. Administration of HFCD significantly increased the body weight and organ weights. Hepatic marker enzymes such as ALT, ALP and AST levels were increased and HDL level was decreased in HFCD control group compared to normal group. Treatment with formulations showed a significant reduction in the body weight gain, organ weight of the liver, kidney, spleen. Levels of hepatic enzymes and lipid profile were restored. The total phenolic content of the Phytolacca berry and Stholyantak churna was found to be 31.16?g/g and 70.39 ?g/g. The total flavonoid content of the Phytolacca berry and Stholyantak churna was found to be 12.28?g/g and 41.36?g/g. Chemical investigation of Phytolacca berry and Stholyantak churna led to identify the flavonoids quercetin and phenols gallic acid were present in formulations by HPTLC technique along with standard markers. The HPTLC fingerprinting of formulations revealed the presence of the 0.04% of gallic acid in Phytolacca berry, Stholyantak churna in aqueous showed 0.47% of gallic acid and Stholyantak churna in methanol showed 0.08% of quercetin and 0.03% of gallic acid. Based on the above results, it was concluded that the ayurvedic and homeopathic formulations, Stholyantak churna and Phytolacca berry possess significant anti-obesity activity in HFCD induced obesity model. Stholyantak churna possess higher anti-obesity activity than Phytolacca berry.

13

SYNTHESIS OF 1-SUBSTITUTED-2-THIO-4-AMINO-6-ETHYLFORMAMIDINO,1,3,5-TRIAZINES

D. T. Tayade* S. P. Ingole
Department of Chemistry, Government Vidarbha Institute of Science and Humanities, Amravati 444606.

Recently in this laboratory 1-substituted-2-thio-4-amino-6-ethylformamidino 1,3,5-triazines (XIIIa-r) were synthesised by isomerisation of 2-substituted imino-4-amino-6-formamidino-1,3,5-thiadiazines (XIIa-r) successfully by refluxing with 10% aqueous ethanolic sodium bicarbonate medium. The structure of all the synthesized compounds was justified on the basis of chemical characteristics, elemental analysis and spectral studies.

14

SKELETAL MUSCLE RELAXANT ACTIVITY OF BOUGAINVILLEA GLABRA LEAVES IN SWISS ALBINO MICE

Sudheer K Dokuparthi1*, Suresh Kandagatla2, Yesubabu Maddala2, Shiva Shankar P2
1Department of Pharmacognosy, Vijaya College of Pharmacy, Munaganoor – 501511, Hyderabad, Telangana, India.
2Doer Innovations, LB Nagar, Telangana, India.

The current work is carried out to investigate the skeletal muscle relaxant property of Bougainvillea glabra (400mg/kg, p.o). Rota rod model was constructed to evaluate the activity in Swiss albino mice. The animals were randomly devided into test, standard and control. The control group received distilled water, standard group received diazepam 4mg/kg and the test group received the methanol extract. The methanol extract of Bougainvillea glabra significantly reduced the fall off time (5.63 secs) compared to the fall off time of diazepam treated animals (2.55 secs). The reduced fall off time observed in Bougainvillea glabra methanol extract treated mice indicates the motor incordination on rotarod apparatus. Moreover, the preliminary phytochemical screening of the extract indicates that it possess various bioactive components like alkaloids, glycosides, flavonoids, saponins and tannins. In conclusion, the above results indicates that there is a need of identification and isolation of active constituents of methanolic extract of Bougainvillea glabra which might be responsible for the skeletal muscle relaxant activity.

15

“A STUDY TO ASSESS DRUG UTILIZATION ON TYPE 2 D/M PATIENTS WITH OR WITHOUT COMPLICATIONS IN GENERAL WARD OF TERTIARY CARE TEACHING HOSPITAL AT VIJAYANAGAR INSTITUTE OF MEDICAL SCIENCES, BALLARI, KARNATAKA”

Mr. Arun J1*, Sharad Chand2, B. Nagaraju2 , Mukul Acharya2 , R. Anusha2.
1Assistant Professor, Department of Pharmacy Practice, TVM College of Pharmacy, Ballari, Karnataka.
2Department of Pharmacy Practice, TVM College of Pharmacy, Ballari, Karnataka.

A Prospective observational study was carried out for the period of six months in inpatient Department of General Medicine at Vijayanagar Institute of Medical Sciences, Ballari. Objective: To study the antidiabetic drug utilization pattern in hospitalized patient with type II diabetes mellitus with or without complications. Results: A total of 200 patients were chosen for the study, 54% of the patients were males and 46% of the patients were females. Most of the patients were in the age group of 51-65 years (49.5%). The major co morbidities identified were 76 patients (38%) with cardiac complications, followed by 41 (20.5%) patients had other concurrent illness & 25 (12.5%) had nephritic complications. Antidiabetic drugs accounted for 338 of the total drugs prescribed. Among the antidiabetic, Insulin was prescribed in 159 patients, accounted for 47.04%, followed by Biguanides (Metformin) were prescribed in 114 patients, accounted for 33.73%, Sulfonylureas were prescribed in 60 patients, accounted for 17.75%, , ?- Glucosidase Inhibitor were prescribed in 02 (0.591%) patients and Meglitinide were prescribed in 03 (0.888%) patients. Antibiotics were widely used 170 (25.56%) of all prescribed drugs (n=665) followed by PPI/H2RA in 139 (20.90%) prescriptions. Conclusion: The prescribing pattern of drugs should be based on severity of disease condition, associated co morbid conditions and currently available evidences. The prescribing trend has been monotherapy with insulin followed by antidiabetic drugs in the form of Insulin and Metformin Combination.

16

ROLE OF VARIOUS NATURAL AND SYNTHETIC POLYMERS IN DEVELOPMENT AND IN-VITRO CHARACTERIZATION OF ORAL CONTROLLED DRUG DELIVERY SYSTEM OF FEXOFENADINE

Muthadi Radhika Reddy*, Sajal Kumar Jha, Kondapuram Parameshwar
Dept. of Pharmaceutics, School of Pharmacy Guru Nanak Institutions Technical Campus, Ibrahimpatnam, Hyderabad-501506, India.

The objective of the present work was to formulate and to characterize controlled release matrix tablets of Fexofenadine in order to improve bioavailability and to minimize the frequency of administration and increase the patient compliance. A matrix tablets was developed that releases Fexofenadine over a 12-hour period and the influence of the polymer type and concentration on the release rate of the drug was evaluated. Fexofenadine tablets were prepared by direct compression technique by the use of different natural, synthetic polymers such as gum acacia, hydroxypropyl methyl cellulose K15, xanthum gum and guar gum individually and also in combination. Studies were carried out to study the influence of type of polymer on drug release rate, and in vitro release kinetics were examined. All the formulations were subjected to physicochemical characterization such as weight variation, hardness, thickness, friability, drug content. In vitro dissolution studies were carried out simulated gastric fluid (pH 1.2) for first 2 h and followed by simulated intestinal fluid (pH 6.8) up to 12 h, and obtained dissolution data were fitted to in vitro release kinetic equations in order to know the order of kinetics and mechanism of drug release. Formulated tablets were found to be within acceptable limits for physical and chemical parameters. Formulation containing HPMC K15 obtained the desired drug release profile up to 1h followed zero order kinetics. The release kinetics of the HPMC k15 formulation showed the best linearity (r2 =0.947) in fitting zero-order kinetics, suggesting the release rate was time independent release. Based on the results, fexofenadine controlled release matrix tablets prepared by utilizing HPMC k15 can attain the desired drug release up to 12 h. Which results in maintaining steady state concentration and improving bioavailability.

17

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF ARTEMETHER AND LUMEFANTRINE

R. Margret Chandira*, B. S. Venkateshwarlu, A. Pasupathi, P. Palanisamy, K. Somu
Vinayaka Mission’s College of Pharmacy, Vinayaka Mission’s University, Salem (D.T), Tamil Nadu (State), India.

Artemether and lumefantrine are anitmalarial drugs used in the management of malaria. The objective of the proposed research work is to prepare and evaluate the fast dissolving tablets (FDTs) of artemether and lumefantrine, which avoid the first-pass metabolism, improved the dissolution rate and enhance the bioavailability. Fast dissolving tablets (FDTs) were prepared by direct compression method by using combination of superdisintegrant like, Crosspovidone and sodium starch glycolate(5%,10%,&15%) and evaluated for physico-chemical evaluation parameter such as hardness, friability, weight variation, drug content uniformity, water absorption ratio, wetting time, in-vitro andisintegration time, in-vitro dissolution studies. The control tablet (without superdisintegrant) was formulated and evaluated. The 12 formulations, F1to F6 were formulated and among these formulations, F3 (crosspovidine) was optimized. The hardness, friability, weight variation and drug content were found to be within pharmacopeias limits. The water absorption ratio, wetting time, in-vitro disintegration time of optimized formulation, F3 was found to be 62.87%, 12secs and 15secs respectively. The formulation, F3 was considered to best formulation, which released up to 99.49% (artemether) & 99.15% (lumefantrine)in 25 minutes. The comparison of dissolution rate profile of formulation and controlled formulation of artemether and lumefantrine tablet with best formulation, F3 was conducted. The result showed that the formulation, F3showed complete drug release within 25 minutes and controlled formulation showed 26.50% (artemether) &24.50%(lumefantrine) drug release in 25 minutes. The stability study was also conducted the best formulation, F3 and it indicates that there was no significant change in any parameters. Hence the formulation F3 was considered to be highly stable.

18

PRELIMINARY PHYTOCHEMICAL AND GC MS STUDY OF ONE MEDICINAL PLANT CARISSASPINARUM

Mudiganti Ram Krishna Rao1*, Anisha G1

Bharath Institute of Higher Eduction and Research, Bharath University, Chennai, 600 073, India.

The knowledge of scientific validation of the efficacy of medicinal plants in the light of modern research parameters is of great importance in understanding the plant’s role as medicine. To understand the presence of different phytocompounds present in a medicinal plant a number of techniques are available. The present study is one step in this direction which deals with the preliminary phytochemical and Gas Chromatography Mass Spectroscopy analysis of different leaf extracts of one medicinal Carissa spinarum. This plant has wide medicinal and edible properties. It was observed that flavonids, tannins, saponins and steroids were present in Methanolic extract. Flavonids, alkaloids, saponins and steroids were present in hexene fraction where as alkaloids, saponins, proteins and triterpenoids were present in aqueous extract. The GC MS analysis of hexane and aqueous leaf extracts indicated the presence of some important biomolecules such as Hexadecanal, 2-(1-Cyclohexenyl) cyclohexanone, Phytol, Squalene, Vitamin E, Octasiloxane, 1, 1, 3, 3, 5, 5, 7, 7, 9, 9, 11, 11, 13, 13, 15, 15-hexadecamethylz, 1-Monolinoleoylglycerol trimethylsilyl ether, .beta.-Sitosterol, .alpha.-Amyrin, Lupeol, 1-Monolinoleoylglycerol trimethylsilyl ether and Lup-20(29)-en-3-ol, acetate, (3.beta.)-, Catechol, N-Benzyl-2-phenethylamine, Resorcinol, 2-Methyl-9-.beta.-d-ribofuranosylhypoxanthine, Paromomycin and 3-O-Methyl-d-glucose etc. correspond well with the reported medicinal roles of C. spinarum. Further work is in progress towards understanding this plant’s role as a medicine.

19

STANDARDIZATION AND PHYSICOCHEMICAL INVESTIGATION OF TRIPHALA CHURNA

Sweta Kulkarni*, Deepika Bairagee, Neetu Choudhary
School of Pharmacy, Dr. A. P. J. Abdul Kalam University, Indore-452001, M.P.

Standardization is an essential measurement for ensuring the quality control of the herbal drugs and to have a good coordination between the quality of raw materials, in process materials and the final products. The present paper reports the standardization of Triphala Churna which is mainly used for constipation, indigestion and other abdominal problems. Triphala is an ayurvedic herbal formulation containing three fruits (also known as three myrobalans) in equal proportions. The Churna have been standardized on the basis of various physicochemical parameters. The tests parameters were found to be satisfactory and within the standard limits. Triphala churna and can be used as reference standards for the quality control/ quality assurance study mostly on plant drugs for their primary healthcare needs. The results obtained may be considered as tools for assistance to the regulatory authorities, scientific organization and manufacturers for developing standard formulations of great efficacy.

20

FORMULATION AND EVALUATION OF MOUTH DISSOLVING TABLETS OF MONTELUKAST SODIUM

Chamanpreet Kaur*, Sandeep Kumar
A.S.B.A.S.J.S. Memorial College of Pharmacy, Affiliated to I.K Gujral Punjab Technical University, Bela (Ropar), Punjab, India. Pin- 140111.

Convenience of administration and patient compliance are gaining significant importance in the design of dosage forms. Despite of tremendous innovations in drug delivery, the oral route remains the preferred route for administration of therapeutic agents because of accurate dosage, low cost therapy, self medication, non invasive method and ease of administration leading to high level of patient compliance. US-FDA: United States Food and Drug Administration defined orally disintegrating tablets as “A solid dosage form containing medicinal substance or active ingredients which disintegrate rapidly usually within a matter of seconds when placed upon the tongue”. These results to a rapid onset of action and greater bioavailability of the drug than those observed from conventional tablet dosage forms. These are novel types of tablets that disintegrate/dissolve/disperse in saliva .They are also suitable for the mentally ill and bed ridden patients who do not have easy access to water. The benefit in terms of patient compliance, rapid onset of action, increased bioavailability and good stability makes these tablets popular as a dosage form of choice in the current market.

21

SYNTHESIS AND CHARACTERIZATION OF SOME NOVEL INDOLIZINE DERIVATIVES

Basavaraj M1*, Giles D2, Das AK2, Sakharam AG2
1Vivekananda college of Pharmacy, Rajajinagar, Bengaluru-55.
2Acharya and BM Reddy College of Pharmacy, Bengaluru-107.

A novel approach has been adopted for the synthesis of Indolizine nucleus. Pyridinium-N-methylides (1a, b) were synthesized by reacting pyridine with different haloacetic acids. Further, the indolizine nucleus were synthesized through 1,3-cycloaddition of pyridinium-N-methylides with electron deficient alkynes or alkenes in presence of MnO2 to give indolizine carboxylates (2a, b). Later on, derivatives of indolizine (4a-d) were prepared by treating 2a and 2b with hydralazine and metformin. Synthesis of indolizine 2-carboxylic acid was achieved, by reacting 2- methyl pyridine with ethylbromopyruvate. The resulting acid was treated with hydralazine and metformin to form corresponding indolizine derivatives (5a, b). Synthesized compounds were characterized by IR and NMR spectroscopic techniques.