IAJPR

Indo American Journal of Pharmaceutical Research

ISSN NO.: 2231-6876
  • INDEXING
  • PUBLICATION CERTIFICATE
  • Impact Factor Journal
MAY 2014
1

SYNTHESIS, CHARACTERIZATION AND ANTI-INFLAMMATORY ACTIVITY OF SOME SUBSTITUTED PYRIMIDINE DERIVATIVES

Osman Ahmed*1, Syed Azeemuddin Razvi1, T K Md Rayees1, M A Nafay Shoeb1, Md. Salahuddin2

1Department of Pharmaceutical Chemistry, Deccan School of Pharmacy, Hyderabad, A.P. India.

2Department of Pharmaceutical Chemistry, Farooqia College of Pharmacy, Mysore, Karnataka, India.

Abstract

The main objective was to synthesize and characterize novel pyrimidine derivatives and screen them for anti-inflammatory activity. A series of four 6, 7-dihydro-3-aceto substituted pentaleno [2, 1-d] pyrimidin-4-one derivatives (PM1-PM4) were synthesized from 2-amino-3, 4, 5, 6-tetra hydro pentalene-1-carboxamide. The synthesized compound, characterized on the basis of satisfactory analytical and spectral (H1NMR, C13Mass) and elemental data. Studies were carried out for the synthesized compounds which were also evaluated for anti-inflammatory activity by Carrageenan induced rat paw edema method. Indomethacin was used as standard anti-inflammatory agents. The synthesized compounds showed good anti-inflammatory activity, compared to standard drugs. Two of the compounds PM2 and PM4 exhibited significant anti-inflammatory activity, as compared to standard drug Indomethacin. We reported the successful synthesis of novel pyrimidine derivative, as well as their spectral characterization.

2

SIMPLE SPECTROPHOTOMETRIC METHOD VALIDATION OF NIFEDIPINE SOLID DOSAGE FORM

Patitapabana Parida1*, Subash Chandra Mishra2, Subha Prakash Tripathy3

1*Department of Biotechnology and Medical Engineering, National Institute of Technology,  Rourkela, Odisha-769008, India.

2Department of Metallurgical and Materials Engineering, National Institute of Technology, Rourkela, Odisha-769008, India.

3Torrent Pharmaceuticals Limited, Ahmadabad, Gujarat – 380009, India.

Abstract

Simple, sensitive and specific spectrophotometric method was developed for the validation of nifedipine  in tablet dosage form in two different brands. Active ingradient showed  the absorption maximum in ethanol and chloroform at 235.5 nm and 235 nm respectively. The linearity was established in the concentration range of 2-10 μg/ml for nifedipine in different solvent with correlation coefficient (r2) of 0.997 - 0.999 respectively. The mean % recoveries were found to be in the range of 99.57 - 99.81 % for nifedipine in different brands. Statistically potency of two marketed brands were determined that there were no significant difference between the two brands where ANOVA at f (5,3) =196.0143 and significant level of p-value observed at 0.004. Hence the proposed method can be applied for  the routine analysis of active molecule from the formulations.

3

EFFECT OF MERCURIC CHLORIDE ON PROTEIN CONTENT OF MUSCLES AND HEPATOPANCREAS OF FRESH WATER PRAWN Macrobrachium lamarrei lamarrei

Siddhant Bhardwaj, K. Borana, Nahila Sujad and Susan Manohhar

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

Abstract

Mercury is considered to be one of the most lethal heavy metals present in the aquatic environment and  Macrobrachium lamarrei lamarrei (H. Milne-Edward, 1837), being the inhabitant of freshwater encounters mercury in one way or the other and get affected. In the present investigation, Macrobrachium lamarrei lamarrei (H. Milne-Edward, 1837) were exposed to 0.002 mg/l mercuric chloride for a period of 60 days to check its impact on the protein content in muscles and hepatopancreas. A drastic decrease was observed in protein content in prawn muscles and hepatopancreas.

4

THE TOXIC EFFECT OF CYPERMETHRIN ON ZEBRAFISH EMBRYO- AN ALTERNATIVE MODEL FOR ASSESSING THE EMBRYO TOXICITY OF ENVIRONMENTAL CHEMICALS

K.Sathya¹, M.Thiripurasundari¹, A.Uma2*, M.R.Srinivasan3, M.Subas Chandra bose¹

¹Rajalakshmi Engineering College, Thandalam, Chennai 602105

2Fisheries Research and Extension Centre, Tamilnadu Fisheries university, Madhavaram Milk Colony, Chennai 600051

3Tamilnadu Veterinary and Animal sciences university, Madhavaram Milk Colony, Chennai 600051

Abstract

Cypermethrin is a synthetic pyrethriod which has been used widely as pesticides. Contaminations of the aquatic environment with organic pesticides have been reported to cause lethal and sub lethal effects in the organisms inhabiting the aquatic environment.  Zebrafish embryo toxicity test (ZFET) was used to determine the toxic effects of cypermethrin in the present study. The LC50 value obtained for cypermethrin in the ZFET was 0.05µg/l. Zebrafish embryos were exposed to various concentration of cypermethrin (0.001, 0.003, 0.01, 0.03and 0.05 µg/l) and the observations on the lethal, sub lethal and sublethal continuous endpoints were recorded. The results showed that the sub lethal and lethal effects of the zebra fish embryos increased with respect to an increase in the concentration of the cypermethrin. It is evident from this study that even low levels of cypermethrin contamination in the aquatic environment would affect the developmental stages of fishes inhabiting the aquatic systems.

5

MOLECULAR MODELING, SYNTHESIS, ANTIBACTERIAL AND ANTITUBERCULAR ACTIVITIES OF SOME NOVEL PYRROLYL 1,2,4-TRIAZOLE DERIVATIVES

Shrinivas D. Joshi*, Sheshagiri R. Dixit, Uttam A. More, Shweta Rai, Venkatrao H. Kulkarni.

Novel Drug Design and Discovery Laboratory, Department of Pharmaceutical Chemistry, S.E.T.’s College of Pharmacy, Sangolli Rayanna Nagar, Dharwad 580 002, Karnataka, India.

Abstract

Tuberculosis treatment remains a challenge that requires new antitubercular agents due to the emergence of multidrug-resistant Mycobacterium strains. This paper describes the molecular modeling, synthesis, antitubercular activity and spectral analysis of Schiff bases of pyrrolyl 1,2,4-triazoles. The  binding  mode  of  the  compounds  at  the  active  site  of  enoyl-ACP reductase was explored using surflex-docking method, compound 5i and 5f have shown a good docking score of 7.06 and 7.05 respectively. An evaluation of antibacterial and antitubercular activities of the prepared compounds has indicated that the compounds 5i and 5f have shown MIC value of 3.125µg/ml, respectively as compared to standard drugs pyrazinamide and isoniazid and selectively screened molecules for cytotoxicity found non-cytotoxic at 62.5 µg/ml concentration. A series of Schiff base containing pyrrolyl 1,2,4-triazole were synthesized based on their molecular docking studies, it revealed that most of the compounds could have a prospective to become a lead molecule and may act as a good enoyl ACP reductase inhibitors. From the antitubercular screening we can say that the compounds having electron donating groups like -OH, -CH3, -OCH3 showed good in vitro biological activity then those compounds having electron withdrawing groups like -Cl,-Br, -F which showed moderate activity.

6

SYNTHESIS AND ANTI-CONVULSANT EVALUATION OF NEW BENZOTRIAZOLE DERIVATIVES

N.Karthik Rao1, J.Prathyusha Reddy2, B.Srujana1, M.Ravali1, K.Navaneetha2, B.Venkateswara Reddy2, T.Divya1, V.Varun Kumar1, K.Venkata Ramana Reddy3

1Rosory College of Pharmacy, Hanasparthy, Warangal.

2St.Pauls College of Pharmacy, Turkayamjal, Hayathnagar, R.R.Dist.

3Sree Dattha Institute of Pharmacy, R.R.District. Andhra Pradesh.

Abstract

A new series of benzotriazole aldehyde and ketone  derivatives were prepared starting from ortho-phenyl di amine (OPDA) in five steps which includes dehydration, cyclization, acetylation, reaction with hydrazine hydrate and finally reacting with aromatic aldehydes or aromatic ketones groups. All these synthesized compounds were evaluated for anti-convulsant activity. The benzotriazole derivatives may show significant reduction in the hind limb tonic extensor phase, which is similar to Grand-mal epilepsy in humans; this may be due to the inhibition of voltage dependent Na+ channels. The Benzotriazole aldehyde derivatives showed better activity than benzotriazole ketone derivatives

7

PHYTOCHEMICAL SCREENING AND ANTI-INFLAMMATORY POTENTIAL OF DREGEA VOLUBILIS IN DIFFERENT SOLVENTS

Ravi P1*, K E Pravallika1, P. Raghuveer1 and Ganga Rao B2

1University College of Pharmaceutical Sciences, Acharya Nagarjuna University, Nagarjuna nagar, Guntur, A.P-522510, India

2Department of Pharmacognosy, University College of Pharmaceutical Sciences, Andhra University, Visakhapatnam, A.P-530003, India.

Abstract

In this present research work roots of Dregea volubilis of family Asclepiadaceae was selected to isolate the phytoconstituents and to evaluate the anti-inflammatory effect of hexane (HE), ethyl acetate (EA) and ethanolic (EE) extracts in either sex of wister albino rats. The method of extraction was carried out with soxhlet apparatus and the process of column chromatography was used to isolate the chemical constituents. The anti-inflammatory effects of hexane, ethyl acetate and ethanolic root extracts of the Dregea volubilis (100, 200 & 400 mg/kg p.o.) were examined on rat paw oedema induced by subplantar injections of carrageenan (0.5 ml/kg). Indomethacin (50 mg/kg p.o.) was used as the reference anti-inflammatory agent for comparison. Both the ethyl acetate and ethanolic extracts of D. volubilis roots (200 and 400 mg/kg p.o.) significantly reduced rat paw oedema induced by subplantar injections of carrageenan. However, the ethyl acetate and ethanol extracts of the plant produced relatively greater and more pronounced anti-inflammatory effect than hexane extract counterpart in the experimental animal model used. The ethyl acetate and ethanol extracts were potent as indomethacin but hexane extract of root of D. volubilis was found to be markedly less potent than indomethacin as anti-inflammatory agent. The results of this experimental animal study indicate that all the extracts of roots of D. volubilis possess anti-inflammatory activity, and thus lend credence to the suggested folkloric use of the plant in the management and control of inflammatory conditions in India.

8

FORMULATION AND EVALUATION OF BILAYER TABLETS OF VALSARTAN FOR THE EFFECTIVE TREATMENT OF HYPERTENSION

S.K. Uma Devi1, M. Arjun Kumar1, P. Naga Haritha1, G. Rohini Reddy2, E.Himabindu1, K. Navaneetha1 , P.Sunil Kumar Chaitanya2

1Department of Pharmaceutics, St. Pauls College of Pharmacy,

2Department of Pharmaceutical Analysis, St. Pauls College of Pharmacy, Turkayamjal (V), R. R Dist-501510, A.P, India.

Abstract

The aim of the present study is to develop bilayered tablets of Valsartan which was containing an immediate release layer and a sustained release layer of Valsartan for the effective treatment of hypertension.  Sodium starch glycolate, Croscarmellose sodium, and Crospovidone were used as super disintegrants in the immediate release layer and HPMC, Xanthan gum, Guar gum were used as release retardants in the sustained release layer. The compatibility between the drug  and polymers were depicted by the results of FTIR. The pre compression parameters such as bulk density, tapped density, carr’s index and hausner’s ratio and angle of repose were evaluated separately for the granules of both the layers which were within the limits of USP.  The results of evaluation of immediate release layer tablets  for  thickness (mm) of the layer was found to be in the range of 2.46±0.21 (F6) to 2.65±0.21 (F7), the hardness (kg/cm2) was observed between the range of 4.53±0.30 (F4) to 5.5±0.4 (F6). The friability was found to be 0.48±0.070 (F3) to 0.826±0.04 (F5) and weight variation was found to be 179.1±1.72 (F8) to 180.4±1.94 (F4) and the drug content was observed to be from 99.35±0.449 (F5) to 99.74±0.115 (F6). The results of evaluation of sustained release layer tablets were found and  the thickness (mm) of the layer was found to be in the range of 4.08±0.070 (F6) to 4.77±0.083 (F2), the hardness (kg/cm2) was observed between the range of 6.82±0.174 (F3) to 7.71±0.27 (F6). The friability (%) was found to be 0.31±0.048 (F9) to 0.653±0.080 (F2) and weight variation (mg) was found to be 599.18±1.21 (F6) to 601.2±1.27 (F2) and the drug content (%) was observed to be from 99.35±0.37 (F1) to 101.37±0.54 (F2). All the evaluation parameters were found to be within the satisfactory limits (USP).The percentage drug release for the optimized formulation F5containing 7.5% of SSG was 99.44% in 20 mins. The sustained release layer containing drug and HPMC in the ratio of (1:2) (F3) released 98.70% of drug at the end of 10 hrs. Drug release followed zero order kinetics. The percentage  drug release from the bilayer tablets were 101.2% for immediate release layer at 20 min in pH1.2 HCl  and 96.35% for sustained release layer at the end of 10 hrs pH 6.8 phosphate buffer which depicts that the bilayered tablets of Valsartan will be useful in case of Hypertension.

9

ANTIMICROBIAL ACTIVITY OF SWIETENIA MAHAGONI (SEED) AGAINST VARIOUS PATHOGENIC MICROBES

Md. Khasrul Alam1, Fariha Jasin Mansur2, Mohammad Minnatul Karim1 and Md. Anwarul Haque1*

1Department of Biotechnology and Genetic Engineering, Islamic University, Kushtia-7003, Bangladesh.

2Department of Biological Chemistry, Yamaguchi University, Japan.

Abstract

Various medicinal plants are used to prevent or cure infectious diseases as an alternative solution to antibiotics. In this study, Swietenia mahagoni (Seed) was selected and antibacterial activity of extracts with various solvents (Petroleum Ether, Ethyl Acetate, Dichloromethane, and Methanol) was studied in laboratory test. The antibacterial activity of these extracts was assessed against Bacillus subtillis, Sarcina lutea, Xanthomonas campestris, Klebsiella pneumoniae, Escherichia coli and unidentified kidney infectious bacteria based on the zone of inhibition using Agar disc diffusion method. The antibacterial activity among extracts was broad against both gram positive and gram negative microorganisms. Among the various solvents extract, both ethyl acetate and methanol extract was more active against tested organisms. The results suggested that Swietenia mahagoni (Seed) has phytochemicals which are active against broad spectrum bacteria and both methanol and ethyl acetate could be used for extraction of active phytochemicals from Swietenia mahagoni (Seed). 

10

OSMOTIC PUMP: A NOVEL APPROACH TO CONTROL DRUG DELIVERY

Smitapadma Mohanty *, Manoranjan Sahu, A. Sirisha

School of Pharmaceutical Education and Research, Berhampur University, Bhanja Bihar, Odisha, India, PIN-760007

Abstract

Controlled release dosage forms are designed to complement the pharmaceutical activity of the medicament in order to achieve constant plasma level over a longer time period. Among various approaches of drug delivery, osmotically controlled drug delivery system is one of the promising technologies. It is one of the novel drug delivery system which can control release of drug from the dosage form. It provides a better control of plasma drug level which helps in increased efficacy and constant delivery. These systems utilize osmotic pressure as major driving force for delivery of drug. Osmotic pump consists of inner core consists of drug and osmogen. This inner core coated with a semi-permeable membrane.  When this system exposed to gastro intestinal fluids, water flows through the semi-permeable membrane into the system due to osmotic pressure difference which dissolves the drug and pumps it out through the orifice by the osmotic force. Drug release from the osmotic pump in a controlled manner which is independent of chemical properties of the drug, patient’s physiological factors or concomitant food intake; this is the primary advantage of osmotic drug delivery system. In this article, various types of osmotic pump, the basic components of osmotic pump and evaluation of osmotic tablets have been discussed briefly.

11

PLANT SOURCES FOR THE HEALING OF OPHTHALMIC DISEASES BY THE TRIBALS OF DISTRICT RAISEN ( M.P.), INDIA.

1Zahoor Ahmad Lone, 2Shaukat Saeed Khan and 3Fatima Khan

1Department of Botany Saifia Science College Bhopal ( M.P.) INDIA.

2Department of Microbiology Saifia Science College Bhopal ( M.P.) INDIA.

3Govt. Science and Commerce , Benazeer  College Bhopal ( M.P.) INDIA

Abstrac

Our eyes are very delicate organs that require constant care to keep them in good health . Apart from the disease of the eyes, the body has a lot of diseases that reflect themselves in the health of the eyes. Among the many diseases that can affect the eyes include the metabolic diseases, stomach disorders, infections, kidney disorders and allergic reactions etc. The Raisen district in the central India is the home of numerous herb species. The agro climatic conditions prevailing in the region provide an ideal habitat for the natural growth of a variety of plants and herbs, which provide raw material for pharmaceutical, phytochemical , food , flavouring and cosmetic industries . The present paper provides information on 6 medicinal plants belonging to 6 different families and used by the Gond, Bhill and Baiga tribes of Raisen district of Madhya Pradesh , India for the  ophthalmic disorders . Information was collected from local tribals pertaining to the use  of various species of plants employed by them in ophthalmic disorders. Herbalists, herb sellers and traditionalists living within the area of study were interviewed by the administration of questionnaires. A need for further scientific research based on the findings of this survey is indeed very necessary and recommended so that adequate records of indigenous methods for the management of ophthalmic diseases can be kept for posterity especially in the study area . A need for analytical work on the plants identified as useful for the treatment of ophthalmic diseases is also necessary in order to determine the actual dosage applicable so that the medicinal values of these plants could be made available to humanity and hence reduce the ophthalmic disorders in tribal people of district Raisen . More attempts should be made to authenticate and evaluate the efficacy of these herbs and products used by tribals.

12

SCREENING FOR ANTIBACTERIAL PROTEINS FROM CERTAIN SELECTIVE TISSUES OF INDIAN MAJOR CARP, CATLA CATLA AGAINST HUMAN PATHOGENIC BACTERIA

Sundaramoorthy M1, Kannaki S1 and Saravanan T.S2

1PG & Research Department of Zoology, AVC College (Autonomous), Mannampandal, Tamilnadu, India, Pin- 609 305.

2Department of Biotechnology, Dr. M.G.R  Educational and Research Institute University,  Chennai,  Tamilnadu,  India, Pin-600 095. 

Abstract

The pharmaceutical use of antimicrobial proteins/peptides (AMPs) as natural antibiotics is fascinating in the current scenario as they overcome the bacterial resistance by their direct cytolytic mode of action.  The AMPs have been well documented as part of innate immune system of plants and animals.  Herein we demonstrate the partial purification of antibacterial proteins (ABPs) from liver, kidney, heart and gills of Catla catla and their antibacterial and haemolytic properties.  The ABPs were semi purified by following the procedures of acid extraction, 30% ammonium sulphate precipitation and dialysis.  The tissues yielded 14.8, 16.0, 22.6 and 6.0 mgs of protein / g.wet.wt. respectively.  Of these, the heart tissue yielded the highest amount of protein i,e 22.6 mg/g wet .wt.  The proteins were also characterized for TLC patterns and absorption spectra. The absorption spectrum (λ-max) was found to be 280 nm for all the proteins invariably.  The post TLC of each protein sample showed a single spot with Rf values in a narrow range of 0.305 to 0.385.  Following this, the ABPs purified from all the four organs were tested for MICs and they exhibited potential bactericidal activities on all test organisms (Escherichia coli, Proteus mirabilis, Staphylococcus aureus, Klebsiella pneumonia, Salmonella typhi, Salmonella paratyphi 'A', Salmonella typhimurium and Pseudomonas aeruginosa) in the range of 3-25 µg concentrations.  The growth of most of the test bacteria was inhibited by the lowest concentration of the proteins subjected (MIC = 3 µg).  To check their cytotoxicity, haemolytic assays were also performed and none of the proteins caused haemolysis on ABO hRBCs.  The results reveal that the ABPs semi-purified from different parts of the fish have all the major qualities of AMPs such as natural occurrence, low molecular weight, antibacterial and non haemolytic properties to act as natural antibiotics for the treatment of infectious diseases.

13

IN VITRO EVALUATION OF THE ANTIMICROBIAL ACTIVITY OF DIFFERENT SOLVENT EXTRACTS OF ROOTS OF VANDA TESSELLATA (ROXB.)HOOK.EX G.DON

Chhavi Gupta 1,  S.S.Katewa 2

Laboratory of Ethnobotany and Agrostology.Department of Botany, University College of Science,M.L. Sukhadia University, Udaipur (Rajasthan), India.

Abstract

Bioassay (petroleum ether, chloroform, ethyl acetate, acetone, methanol and hexane) of various root extract of Vanda tessellata (Roxb.)Hook.ex G.Don were investigated for an in vitro antimicrobial activity by agar-well diffusion method .These were  tested against six bacteria: Escherichia coli, Staphylococcus aureus, Klebsiella pneumoniae, Proteus mirabilis and Bacillus subtilis and two fungi Candida albicans and Aspergillus niger. Ethyl acetate extract produced definite antibacterial activity against the human pathogens such as Escherichia coli and Staphylococcus aureus with the zone of inhibition ranging from 11-16 mm and 11-13 at various concentrations respectively. But only the ethyl acetate extract showed significant antifungal activity against the Candida albicans with the zone of inhibition ranging from 11‐16 mm at various concentrations. The susceptibility of the microorganisms to the extracts of these plants was compared with each other and with selected antibiotics. The present investigation showed the effectiveness of crude extract of this plant against tested bacterial strains. This study further imparts the use of whole plant extract in treating disease caused by tested microbial organisms.

14

LIQUISOLID TECHNIQUE BASED TABLETS FOR ENHANCEMENT OF DISSOLUTION RATE OF NATEGLINIDE

Iizhar Ahmed Syed and Bhavani.G

Dept of Pharmaceutics, SR College of Pharmacy, Ananthsagar, Hasanparthy- Warangal-506371

 

Abstract

It is suggested here that liquisolid technique has the potential to enhance solubility and dissolution rate of BCS class II. This technique shows delivering of drugs, which is suitable mostly for liphophilic drugs. However, an apparent limitation of this technique is the formulation of a high dose because a large amount of liquid vehicle is needed, which finally results in a low-dose liquid solid formulation.The aim of the present work is to improve the solubility and dissolution rate of poorly water-insoluble drug nateglinide (NTG), by using this technique. NTG was dispersed in PEG-400 as a liquid vehicle. Then a binary mixture of carrier–coating materials (MCC- Aerosol) was added to the liquid medication under continuous mixing. Precompression studies, such as flow properties were also carried out. The formed mixture was compressed to get tablets matrices by using the tableting machine. The prepared liquisolid tablets were evaluated by hardness, friability, disintegration test and in vitro dissolution studies. The dissolution property of a water-insoluble drug nateglinide (NTG) was investigated. The dissolution profile of the prepared liquisolid tablets was also compared to that of a marketed formulation (MR). The results indicate that liquisolid based tablets (F3) showed greater disintegration and dissolution rate. It might be due to the presence of PEG-400 as it showed the enhancement in the solubility of NTG. FT-IR results showed compatibility of nateglinide with excipients used. The investigation suggest that liquisolid compacts of NTG with increasing the amount of carrier to coating ratio along with super disintegrating agent also resulted in higher dissolution rate, which are directly proportional to the amount of drug released. In conclusion, the results showed that the liquisolid technique could be a promising alternative technique to increase dissolution of water-insoluble drugs nateglinide.

15

ISOLATION AND CHARACTERIZATION OF BIOACTIVE COMPOUNDS FROM TABERNAEMONTANA DIVARICATA AND A STUDY OF ITS ANTIOXIDANT AND ANTIBACTERIAL ACTIVITY

S. Venkatachalapathi, C. Saranya and S. Ravi

Department of Chemistry, Karpagam University, Coimbatore-640 021, Tamilnadu, India.

Abstract

Three novel compounds ethyl-4-n-octyl benzoate 1 and ethyl-4- n-decyl benzoate 2 from the flowers of Tabernaemontana divaricata   and digalactosyl deconate 3 from the latex of T.  divaricata have been isolated and characterized by spectroscopic analysis. Further compounds 1–3 were evaluated for their antibacterial and antioxidant activities. For antibacterial activity Three gram positive (Staphylococcus aureus, Streptococcus farcalis, Bacillus species) and two gram negative (E.coli and Proteus mirabilis) bacteria were used. The zone of inhibition (ZOI) of the compounds 1-3 was determined. All the compounds showed significant antibacterial activity. The antiradical activity evaluated by DPPH method. Compound 1 and 2 showed better radical scavenging activity, with IC50 value of 1.67µg/ml and 1.20µg/ml, respectively against standard BHA with IC50 valu of 28µg/ml.

16

IDENTIFICATION AND QUANTIFICATION OF MAJOR CAROTENOIDS IN COLEUS FORSKOHLII

K. Sunitha, K. Bhaskara Chary, and D. Manohar Rao*1

1Dept. of Genetics, Osmania University, Hyderabad - 500 007, India.

2National Institute of Nutrition, Hyderabad - 500 007, India.

Abstract

Coleus forskohlii, (lamiaceae) an ancient medicinal plant. It is mostly used in ayurvedic medicine in the treatment of heart ailments, asthma, bronchitis, insomnia, epilepsy, anaemia, inflammation. Qualitative analysis of this plant showed the presence of terpenoids, tannins, flavonoids, phlobatannins, saponins and cardiac glycosides. The present study was initiated to induce callus and use it as raw material, along with the leaves, for identification and quantification of carotenoids. Callus was induced by sixteen different concentrations and combinations of NAA + BAP and NAA + KN in leaves of the field grown Coleus forskohlii plants.  Among the treatments, 0.5mg / l NAA + 1.5mg / l BAP was found to be the most efficient (98.8%), while 1.0 mg / l NAA+ 1.0 mg /l BAP, (42.3 %) was the lowest in inducing callus. In view of this, RP- HPLC analysis was carried out for identification and quantification of different carotenoids in both the extracts. Analysis revealed the presence of β –carotene, lutein, zeaxanthin and β – cryptoxanthin in both the extracts. Higher amounts of β-carotene (3.63 mg /100g) and lutein (2.85 mg /100g) were recorded in leaf extracts compared to meager amounts noticed in the callus extracts. Since β-carotene and lutein were found to be more than 2.0 mg /100g in leaf extracts, these are considered to be the principal carotenoids.  Further, highest amounts of total carotenoids (8.60 mg /100g) were also recorded in the leaf extracts compared to very meager amounts (0.99mg/100g) noticed in the callus extract.

17

FORMULATION AND EVALUATION OF RANOLAZINE EXTENDED RELEASE TABLETS

B.D.Swapna1*, G. Sailaja2, Ashok, B.P.Malavika1, Sruthi2

1Annamalai University,Chidambaram,Tamil Nadu,India.

2Malla Reddy college of Pharmacy, Dhulapally post,Secunderabad,Andhra Pradesh,India.

Abstract

In the present work an attempt has been made to prepare Ranolazine extended release tablets where polymers were blended with the drug and excipients. The compatibility determined by FTIR and about nine different formulations were developed by wet granulation method. Formulation F9 containing 500mg of drug contains Micro Crystalline Cellulose, Carbopol  940, Hydroxyl Propyl Methyl Cellulose and opadry orange as the film coater  released  99% of drug  at 24hrs of time intervals under different media like 0.1HCl and phosphate buffer(7.4) and release followed zero order kinetics. All tablets were good fit for Higuchi plot (R2=0.99) therefore diffusion mechanism was found and superimposable with the market product RANEXA. Accelerated stability studies conducted at 400c/75%RH for three months as per ICH guidelines.

18

1-OXOISOINDOLINE-4-CARBOXAMIDES: DESIGN, SYNTHESIS, MOLECULAR DOCKING AND THEIR ANTIOXIDANT ACTIVITY STUDIES

C. Kishore Kumar1, Giriyapura R. Vijayakumar2*

1Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore-570 006, Karnataka, India

2Department of Chemistry, University College of Science, Tumkur University, Tumkur-572103, Karnataka, India.

Abstract

Series of 1-oxoisoindoline-4-carboxamides were synthesized from the 1-oxoisoindoline-4-carboxylic acid. Antioxidant properties were evaluated for the synthesized compounds using DPPH free radical assay and inhibition of human low-density lipoprotein (LDL) oxidation assay. The results confirmed that all the synthesized 1-oxoisoindoline-4-carboxamides exhibit significant antioxidant activity. Molecular docking study revealed the binding orientations of 1-oxoisoindoline-4-carboxamides in the active sites of KDR kinase enzyme. Among the synthesized analogous compounds N-(2-hydroxyphenyl)-1-oxo-N-phenylisoindoline-4-carboxamide, 6c showed very good antioxidant activity which is almost same as that of comparing standard BHA.

19

RELATION BETWEEN LIPID PROFILE CHANGES AND HELICOBACTER PYLORI INFECTION

Kumaran C1, Mohana Rupa L2

1Department of pathology, Shridevi Institute of Medical Sciences & Research Hospital, Sera road, Tumkur, Karnataka. India.

2Department of Pharmacology, Sri Sathya Sai Medical College & Research Institute, Tiruporur, Guduvancherry, Ammapettai, Sembakkam, Tamilnadu, India.

Abstract

Helicobacter pylori infection is one of the most common diseases among the developing countries. The present study was undertaken to investigate the changes in lipid profile in patients with a H. pylori infection. We analyzed the Total cholesterol, LDL-cholesterol, Triglyceride and Lipoprotein (a) of 24 male patients suffering with H. pylori infection confirmed by urease breath test (UBT). The results were compared with 24 healthy controls included in the study. In the present study, we found a significant increase in lipid profile in patient with H. pylori infection. The finding supports the hypothesis that, there is a relation between the lipid profile change and H. pylori infection.

20

DESIGN AND DEVELOPMENT OF HOLLOW-TYPE FAST AND SUSTAIND RELEASE OF CHLOROQUINE PHOSPHATE SUPPOSITORIES

CHALAKANTI. SURYAKUMARI*, A.ANIL KUMAR*, A.ANUSHA, P.ANITHA

Vikas college of pharmacy, Vissannapeta, Krishna dist, Andhra Pradesh.

 

Abstract

Chloroquine phosphate is a useful drug for the treatment prophylaxis is of un complicated plasmodium falciferum malaria in spite of prevalence of the drug resistance of malaria. Chloroquine phosphate treatment of severe malaria must be rapidly effective. The Suppositories may be valuable for childhood malaria when circumstances prevent oral or parenteral therapy(1,3,6). The aim of this study was to prepare fast and sustained release hollow type of Chloroquine phosphate suppositories to design. The main scope of my project work rectal suppositories is given following benefits. It improves therapeutic efficacy of treatment of Malaria, To reduces side effects like gastric irritation,To improve the bioavailability,It improve patience acceptance especially for children's,To reduce drug interactions, To improve the stability of the drug, Onset of action is very fast, To take one suppository in once a day.In first part of this study the natural bases cow Ghee and vanaspathi were compared with synthetic bases.  The inner layer were developed by using hydrophobic base with hydrophilic polymers. The investigations of developed formulations contains both fast and sustained release of Chloroquine phosphate from the same device was obtained using hollow type suppositories for effective treatment of malaria  in children's.

21

DETERMINATION OF ARISTOLOCHIC ACID I CONCENTRATION IN THE FOUR SPECIES OF ARISTOLOCHIA USING HPLC

Soumya Murali*, M.S. Francis and Rashmi, T.R.

Department of Botany, Centre for Post Graduate Studies and Research, Sacred Heart College, Thevara, Kerala, India– 682013.

Abstract

Aristolochic acids are nitrophenanthrene carboxylic acids reported to have various functions, both adverse and beneficial. They act as an oviposition stimulant and are involved in chemical defense. The study of aristolochic acid I composition in the four species A.indica, A.tagala, A.krisagathra and A.ringens all reported as medicinally useful is significant and was carried out using standard HPLC procedure with reverse phase phenomenex C18 column. The standardization was done using standard aristolochic acid I. The identification of the plant samples were carried out by comparing with the retention time and absorption spectra of standard references. The analyses showed the highest concentration of aristolochic acid I in A.krisagathra followed by A.ringens. Different seasons were also found to influence the concentration of the species. The highest concentration was found in winter (9.9070± 0.0989µg/g) for A.krisagathra among all the species studied and all the seasons compared. In A.ringens no significant variation was observed in aristolochic acid I composition. Some species showed a linear trend of decrease or increase in the content of aristolochic acid I with the seasons. The study thus shows that the aristolochic acid I composition in the plant is determined by many factors and is variable depending on seasons and species.

22

Synthesis, characterization and antimicrobial & antioxidant activity of 2-Isonicotinoyl-5-methyl-2,4-dihydro-3H-pyrazolone derivatives

Sujit Kumar Mohanty*, Anuradha Ahuntia, M.Ramesh, T.Siva Shankar, M.Harish, M.Shaikshavali, S.Shadab Hussain, S.Mahaboob Basha

Department of Pharmaceutical Chemistry, CES college of Pharmacy, Chinnatekur, Kurnool

Abstract

Isoniazid reacted with ethylacetoacetate in absolute ethanol to give 2-isonicotinoyl-5-methyl-2,4-dihydro-3H-pyrazol-3-one (P1). This compound when treated with aliphatic aldehyde in presence of 20% sodium hydroxide yielded 4-ethylidene-2-isonicotinoyl-5-methyl-2,4-dihydro-3H-pyrazol-3-one (P2) which further treatment with hydrazine hydrochloride produced 1-isonicotinoyl-3,4-dimethyl-1,3a,4,5-tetrahydropyrazolo[3,4-c]pyrazole (P3). In another set of oxidation reaction was carried out where the compound (P1) is treated with silver oxide to get N'-[(4E)-1-isonicotinoyl-3-methyl-5-oxo-1,5-dihydro-4H-pyrazol-4-ylidene]benzohydrazide (P4). The compound (P1) were further treated with isoniazide in presence of sulphuric acid undergoes cyclization to yield Synthesis of 2-isonicotinoyl-6-phenyl-2,5-dihydro-3H-pyrazolo[4,3-c]pyridazin-3-one (P5). Mild oxidizing agents such as iron (III) chloride in limited amounts are used for oxidation of the compound (P1) to convert into Synthesis of 2,2'-diisonicotinoyl-5,5'-dimethyl-2,2',4,4'-tetrahydro-3H,3'H-4,4' bipyrazole-3,3'-dione (P6). The intensity of the oxidation reaction depends on the oxidizing-reducing potential of the material involved.  This research summarizes results from the literature concerning on tautomerism, synthetic approaches and chemical properties of title compounds as well as their chemical reactions since the pyrazolone chemistry began in 1883 by Ludwig Knorr to date are reported. Emphasis is placed on pinpoining old literature reports that need reinspection in light of modern techniques. The synthesized novel compounds were characterized and carried out for the antimicrobial activity like antibacterial and antifungal activity and Invitro antioxidant activity. The results showed that synthesized compounds have good antibacterial activity and moderate antifungal and Invitro antioxidant activity.

23

ANTICANCER ACTIVITY OF MENTHA ARVENSIS

Kumar Chandan, Subash Vishwakarma, R. Caroline Jeba* Sheikh Khushbu,

Department of Industrial Biotechnology, Dr. MGR Educational and Research Institute, University, Maduravoyal, Chennai-600 095

Abstract

The comparative study of antioxidant activity, total flavonoids and phenol content of these three plants species (Mentha arvensis, Elettaria cardamomum and Allium porrum)   were studied.  Mentha arvensis was found to contain more antioxidant,total flavonoids and phenol content when compared to others. Ethanolic extracts of Mentha arvensis was studied for the invitro cytotoxicity against Human liver cancer (Hep G2 cell line).Mentha arvensis treated Hep G2 cell lines with maximum cytotoxicity(46.3 μg mL⁻1).The finding of the present investigation demonstrated that Mentha arvensis significantly suppresses growth and induces apoptosis in Hep G2 cell lines by MTT assay.

24

EFFECT OF SPIRULINA AS A FEED SUPPLEMENT ON SURVIVAL, LENGTH AND WEIGHT OF Cirrhinus mrigala

Shadab Siddiqui, J.D. Saroch, K. Borana and Nahila Sujad

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

Abstract

The present investigation has been conducted to understand the effect of spirulina as a feed supplement on survival, length and weight of Cirrhinus mrigala for a period of  90 days. Highest value for survival, length and weight gain in the fishes was observed in feed impregnated with 5% Spirulina which came out to be 94% survival rate 130.7 mm length and 60.4gm weight, respectively.

25

ANALYTICAL METHOD DEVELOPMENT AND VALIDATION OF DESVENLAFAXINE IN BULK AND TABLETS USING RP-HPLC

B. Mohammed ishaq1, dr. K. Vanitha prakash2*, dr. G. Krishna mohan3

1Research Scholar, Jawaharlal Nehru Technological University, Kakinada, A.P, India

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

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

Abstract

Desvenlafaxine, an antidepressant in a group of drugs called selective serotonin and norepinephrine reuptake inhibitors (SNRI). A simple, precise and accurate High performance liquid chromatography method was developed and validated for the determination of Desvenlafaxine in bulk and tablet dosage forms. Chromatography was carried out by reversed phase technique on a C18 analytical column with a mobile phase composed of acetonitrile: aqueous Trifluoroacetic acid (0.1%) in the ratio of 70:30 v/v pumped at a flow rate of 1.0 ml/min. The detection was carried out at 225 nm at an ambient column temperature. The retention time was around 4.18 min. Calibration curves for Desvenlafaxine was linear over concentration range of 50 – 150 μg/ml with correlation coefficients 0.999. The mean recovery of Desvenlafaxine from different concentrations was 100%. The % RSD of precision was found to be 0.32%. The method was successfully validated in accordance to ICH guidelines. It was observed that excipient present in formulation did not interfere with peak of Desvenlafaxine. In the conclusion, the developed and validated method was successfully employed for the routine quality control analysis of bulk and pharmaceutical formulations and can be applied for bioequivalence study of Desvenlafaxine.

26

PRELIMINARY PHYTOCHEMICAL STUDIES OF LEAVES OF AZADIRCHTA INDICA, CASSIA FISTULA, EUCALYPTUS GLOBULUS AND BULBS OF ALLIUM SATIVUM

Ashwini singh, 1 * N.P.S. Sengar 2

Department of Pharmacy,  Bhawant University,  Ajmer -Rajasthan-305004.

Sagar Institute of Research And Technology –Pharmacy,Bhopal- M.P-462041.

Abstract

Azadirchta indica   is an evergreen plant belongs to the family Meliaccae . Its uses astringent, antiseptic ophthalmic, insecticidal , demulcent, refrigerant appetizer. Cassia fistula is an plant belongs family  Leguminosae and uses as  Antipyretic, purgative, demulcent, throat troubles, disease of eye , asthma, emetic skin disease leprosy tuberculosis gland syphilis . Eucalyptus leaf consists of the dried, mature leaves from older trees of Eucalyptus globulus [Fam. Myrtaceae] uses as Stimulant, antiseptic, aromatic.  Allium sativum belongs to the family Liliaceae uses as Diaphoretic, diuretic, expectorant, stimulant.  In the present study physical parameters of these plants were determined also hydroalcholic extracts of the leaves of Azadirchta indica , Cassia fistula, Eucalyptus globulus and bulbs  of Allium sativum  was investigated for their phytochemical constituents. 

27

Synthesis and Evaluation of Anti-inflammatory and Analgesic Activity of Isoxazoline Bearing Tris (heterocycles)

Sreenivasa S,  Shankar B J,* Mohan N R.  

Department of Studies and Research in Chemistry, Tumkur University, Tumkur-572103, Karnataka, INDIA

Abstract

Series of tris(heterocycle) bearing isoxazoline ring in combination with imidazole ring has been synthesized via 1,3-dipolar cycloaddition reactions of N-(substituted)methyl-imidazole nitrile oxides with different dipolarophiles. All the newly synthesized compounds were characterized by infrared spectroscopy (IR), 1H and 13C nuclear magnetic resonance (NMR) and elemental analysis. Compounds were screened for their anti-inflammatory and analgesic activity. Compounds 4d, 4e and 4f were discovered as significant anti-inflammatory and analgesic agents showing activity comparable to that of standard drugs.

28

FREE RADICAL SCAVENGING ACTIVITY OF THE METHANOL EXTRACT OF HERACLEAM CANDOLLEANUM (WIGHT-ET-ARN)

Divya Nambath Purushothaman and Subban Ravi

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

Abstract

H.candolleanum (wight et arn) belongs to the family Apiaceae and is used in folk and tribal medicine as an antiarthritic and nerve tonic. The methanol extract of the seed of  H. Candolleanum  was analysed for their total antioxidant activity. The various assays used for the present study was ABTS, DPPH, NOS And SOS Assays. The IC50 value of the antioxidant activity for the above mentioned methods are 79.05, 71.29, 42.60 and 61.20µg/ml respectively. It acts as a source of natural antioxidants, which might be useful as preventive agents against oxidative stress.

29

SYNTHESIS OF NOVEL SUBSTITUTED QUINOLINE DERIVATIVES WITH 2-AMINO-5-METHYLTHIOPHENE-3-CARBONITRILE

Jalindar Jaware & Shobha Borhade

Dept. of Chemistry, Shri Jagdish Prasad Jhabarmal Tiberewala University (JJTU) Vidya Nagari, Churu road, Chudela, Jhunjhunu Rajastan, India-333001.

Abstract

Efficient synthesis of novel substituted quinolone derivatives with substituted amino-thiophene at third position of quinoline and morpholine at second position. The new compounds (1a-d) synthesized from condensation of 2-morpholinoquinoline-3-carbaldehyde with 2-Amino-5-methylthiophene-3-carbonitrile by refluxing in alcoholic solvent to form corresponding Schiff’s bases followed by imine(C=N) bond reduction in to corresponding amine using sodium borohydride in alcoholic solvent at elevated temperature. The newly synthesized compounds (1a-d) were isolated in pure form by means of crystalization & characterized using Mass Spectrometry, IR, and 1H-NMR, 13C-NMR spectroscopy and shows encouraging  results of  activity study in antibacterial and antifungal area

30

UV SPECTROPHOTOMETRIC METHODS FOR ESTIMATION OF RAMIPRIL AND HYDROCHLOROTHIAZIDE BY ABSORBANCE CORRECTION METHOD

Anjan De* , Suddhasattya Dey, Abhishek Jha, Kaushik Mandal Dr. B.C. Roy College of Pharmacy and Allied Health Sciences, Bidhan Nagar, Durgapur-713 206, W.B. India

Abstract A new, simple, rapid and novel spectrophotometric method has been developed for estimation of Ramipril (RAM) and Hydrochlorothiazide (HCT) in bulk and combined pharmaceutical formulations using absorbance correction method (ACM). λmax of RAM was found at 209nm and HCT was at270nm respectively. This method involved measurement of absorbance at two wavelengths of RAM & HCT i.e., 209 nm and 270 nm for RAM and 270nm & 209nm for HCT. The combination is also estimated by ACM. It showed linearity of both the drugs at two wave lengths. Calibration curve was constructed at 209nm & 270nm for RAM and 270nm & 209nm for HCT respectively. Beer’s law obeyed in concentration range of 0.1‐ 0.5 μg/ mL for RAM and 0.25‐ 1.25 μg/ mL for HCT respectively by the method. These methods were validated for precision, reproducibility, linearity and accuracy as per ICH guidelines. The proposed methods are recommended for routine analysis since they are rapid, simple, accurate, cost effective and also sensitive and specific. It involves neither heating nor use of any organic solvent for separation of the combination. This study thus exploits the possibility for determining Pharmacokinetic data of the combined formulation which may be required in pre-clinical and clinical study in near future

31

Isolation and characterization of phytoconstituents from the leaves of RICHARDIA SCABRA LINN

PoonkodiKathirvelandSubbanRavi*

Department of Chemistry, Karpagam University, Coimbatore-21

Abstract

The aim of this study is to identify and characterize the bioactive compounds from the leaves of Richardiascabra Linn (Rubiaceae). It is an annual and abundant herb and is used in skin diseases in folklore medicine have been investigated phytochemically for the first time. General phytochemical screening of the leaves of R.scabra revealed the presence of steroids, alkaloids, fatty acids and tannins. The extensive phytochemical investigation of the petroleum ether extract of leaves  afforded two white crystalline substances, Stigmasterol and β-Sitosterol and their structures were established on the basis of their spectral (IR, NMR, MS) data. This work reports the isolation and structural identification of Stigmasterol and β-Sitosterol, aiming at contributing to the chemotaxonomy of the genus Richardia. Both of them were isolated for the first time in the genus, therby presenting chemotaxonmic importance to it.

32

CLINICAL PRESENTATION, TREATMENT AND OUTCOME ANALYSIS OF PATIENTS WITH PERFORATED PEPTIC ULCER IN THE DEPARTMENT OF SURGERY AT RMMCH.

N.Junior Sundresh*1, S.Narendran2, K.Haritha3, B.Anil Kumar3.

1Surgery Department, RMMCH.

2Surgery Department, MGR University.

3Department Of Pharmacy Practice,Annamalai University.

Abstract

Corruent study was made to study about the treatment ,clinical presentations and outcomes of the patients suffering from perforated peptic ulcer disease.Peptic ulcer perforation (PUP) is one of the commonest perforations of GIT. The peptic ulcer disease has reduced due to improvements in diagnosis by endoscopy and anti-ulcer drugs advancement with eradication of Helicobacter pylori. Perforation occurs in approximately 7% of patients hospitalized for peptic ulcer disease. Duodenal perforation tends to occur in the anterior wall while gastric ulcers may perforate anteriorly or posteriorly. Concomitant hemorrhage should suggest the presence of a ‘kissing’ulcer (ulcers involving anterior and posterior duodenal walls simultaneously).*The objective of this study was to analyze the clinical presentation, treatment and outcomes of the patients with perforated pepticulcer.It was a prospective observational study and was conducted at RMMCH between November 2008 and April 2009. Data collected from the data collection form were entered in the Microsoft excel programme and analyzed.Total 65 patients were studied during this study. Male to female ratio was represented by 1.1: 1. Their median age was 30 years and the age group was 21- 30 years. The average duration of disease was 7 days. 63.07% of the patients had no previous history of peptic ulcer disease. 18.4% of the patients has  previous history of taking NSAID’s, 58.4% of patients has the history of taking alcohol, 40% of the patients are smokers.Complicati0on rate was 21.5%.Factors related to the complications are past illness, delay bin the treatment & acute perforation. The mortality rate was 6.1%. Factors associated with the mortality are the patients with ≥40 years of age, shock at admission, gastric ulcers, co-morbidities, poly-pharmacy. The average duration of hospital stay was 14 days.In patients with perforated peptic ulcer, the non-operative treatment with careful observation and resuscitation may be safely allowed, except in patients over 70 years old, and that the use of such an observation period can obviate the need for emergency surgery.It is the most common problem mainly affecting the males. Simple closure with omental patch is giving better results. But omental closure followed by the eradication of Helicobacter pylori was giving more excellent results.outcomes were Fourteen (21.5%) patients were reported with post-operative complications. Of these Cellulitis (50%) was the most common complication. The overall length of hospital stay ranged from 1 to 50 days with an average of 14 days. During this study nine patients were died. So the mortality rate was 6.1%.

33

STUDIES ON ISOLATION AND OPTIMIZATION OF PROTEASE PRODUCTION FROM BACILLUS SPECIES AND THEIR APPLICATION

R. Caroline Jeba* chandresh kumar and sarvesh kumar Yadav

Department of Industrial Biotechnology, Dr. MGR Educational and Research Institute, University, Maduravoyal, Chennai-600 095

Abstract

Two different type of  soil sample was collected.Fish market soil sample was collected from Patna(Bihar).Vermi compost soil sample was collected from Varanasi.Both soil sample were serial diluted and plated on nutrient agar medium.Identification and characterization of  Bacillus species was performed by different tests.Three different media were used.Soyabean, green peas and rice bran were used as the natural media.Nutrient broth was used as the synthetic media.Pure culture was isolated for the production of protease enzyme by Bacillus species.The secretion of protease enzyme was achieved by three natural media and one synthetic media(nutrient broth).Among the two different soil sample Vermi -compost soil sample was proved to be better than the fish market soil sample.In the case of natural media green peas shows the better enzymatic activity followed by the rice bran and soya bean. The optimum temperature and pH for the production of protease enzyme was analyzed on 40 ˚C and 8.0 respectively. Protease enzymes produced by the  Bacillus species is widely used in the various industries like leather,food,detergent and pharmaceutical industries.

34

Comparative study of Qualitative Phytochemical screening and antioxidant activity of Mentha arvensis, Elettaria cardamomum and Allium porrum

Subash Vishwakarma, Kumar Chandan,  R. Caroline Jeba, Sheikh Khushbu

Department of Industrial Biotechnology, Dr. MGR Educational and Research Institute, University, Maduravoyal, Chennai-600 095, India.

Abstract

In the current study, we carried out a comparative analysis of qualitative phytochemical screening and the antioxidant activities of 75% Ethanol, Acetone, Chloroform, Petroleum ether and aqueous extracts of the selected species (Mentha arvensis, Allium porrum and Elettaria cardamomum) was studied. Five solvents via; 75% Ethanol, Acetone, Chloroform, Petroleum ether and aqueous were used to obtain extracts from powdered plants parts. The extracts were subjected to qualitative Phytochemical screening using standard procedures. Antioxidant activity of the five extracts using free radical scavenging assays like DPPH was determined. It was observed that presence of greater amount of phenolic compounds leads to a more powerful radical scavenging effect as was shown by ethanolic extract of the leaves and seeds when compared to the other extracts investigated by us  during flavonoids and phenol test. Mentha arvensis leaves exhibited the maximum content of phenols and flavonoids compounds hence greatest antioxidant profile when compared to two other plants.

35

MANAGING PRURITUS- A THERAPEUTIC CHALLENGE

Sarita Goyal1*, Kamal Aggarwal2, M.C Gupta1

1Pharmacology Department, Pt. BD Sharma PGIMS, Rohtak (Haryana)

2Dematology, Venereology and Leprosy, Skin & VD Department, Pt. BD Sharma PGIMS, Rohtak (Haryana)

Abstract

Pruritus or itch is defined as an uncomfortable sensation of the skin that provokes the desire to scratch. It can be severe enough to cause interference with work and restful sleep and have a significant impact on quality of life. It has a manifold etiology, is a characteristic feature of many skin diseases and an unusual sign of some systemic diseases such as cholestasis or hyperthyroidism, or simply be caused by dry skin, especially in the cold, winter months. Pruritus may be localized or generalized and can occur as an acute or chronic condition. Therapy is often aimed at eliminating the underlying cause first, followed by the management of the itchy sensation. Treatment options include pharmacological and non-pharmacological measures such as herbal remedies, hydrotherapy, phototherapy, and ultraviolet therapy. This overview provides information regarding the various management and treatment options for pruritus.

36

SYNERGISTIC ANTIOXIDANT ACTIVITY OF THREE MEDICINAL PLANTS HYPERICUM PERFORATUM, BACOPA MONNIERI AND CAMELLIA SINENSIS

Ishan Tewari, Lalit Sharma, Girdhari Lal Gupta*

Department of Pharmacy, Jaypee University of Information Technology, Waknaghat-173 234 Solan, Himachal Pradesh, India.

Abstract

Antioxidant activity of hydroalcoholic extracts of three widely used medicinal herbs Hypericum perforatum, Bacopa monnieri, Camellia sinensis and their combinations was evaluated and compared. Hydroalcoholic extract was prepared by subjecting plant material to soxhlet extraction. Qualitative phytochemical screening was performed to check the presence of major phytochemical constituents of each plant. Free radical scavenging activity was evaluated using 1,1-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging assay and nitric oxide scavenging assay. Our study reveals that Camellia sinensis possesses more antioxidant activity than other extracts, when compared with individual plant. Our results also suggest that different combination of all these herbs at equal proportion at same doses as in individual plant showed synergistic antioxidant activity. Thus lower doses of mixture of herb may be used in place of individual higher dose to minimize side effects.

37

CYTOTOXIC POTENTIAL OF ANDROGRAPHOLIDE AGAINST HUMAN LUNG ADENOCARCINOMA CELL LINES - A 549

Ashish Shrivastava1 and H.K. Garg2

1Research Scholar, Department of Biotechnology, CSA Govt. Post Graduate Nodal College, Sehore-466001 (India)

2Professor of Cell & Molecular Biology, Genetics and Biotechnology, Sarojini Naidu Govt. Girls Post Graduate (Autonomous) College Shivaji Nagar, Bhopal-462016 (India).

Abstract

The present communication offers a new insight to the cytotoxic potential of Andrographolide against Human Lung Adenocarcinoma Epithelial Cell Lines, A-549 and its insensitivity against normal cell lines, L-132, employing MTT colorimetric assay. On the basis of viability, proliferation and activation of cells, andrographolide was found to be 77.52 % toxic for A-549 cell lines at 100µg/ml concentration whereas it did not show any remarkable toxicity against L-132 cell lines. Thus, Andrographolide may prove to be an anti-proliferative agent against tuberculosis associated lung cancer.

38

FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF LOSARTAN POTASSIUM

B.Venkateswara Reddy1, K.Navaneetha1, K.Venkata Ramana Reddy2,P.Poli Reddy3,P. Ujwala Reddy1, T.Lavanya1, Ch. Divya1.

1. Department of Pharmaceutics, St.Pauls College of Pharmacy, Turkayamjal (V), Hayathnagar (M), R.R.Dist.

2. Department of Pharmaceutics, sree Datta college of Pharmacy, Sheriguda(v),R.R.Dist.

3. Department of Pharmacology,Swami Ramananda Theertha College of Pharmacy,Nalgonda.

Abstract

In the present work, fast dissolving tablets of Losartan Potassium were prepared by mass extrusion method. As precision of dosing and patient's compliance become important prerequisites for a long-term treatment, there is a need to develop a formulation for Losartan Potassium which overcomes the problems such as difficulty in swallowing, inconvenience in administration while travelling, and patient’s acceptability. Hence, the present investigation was undertaken with a view to develop a fast disintegrating tablet of Losartan Potassium which offers a new range of products having desired characteristics and intended benefits. Three super-disintegrants viz., sodium starch glycolate (SSG), Avicel pH(MCC) and L-HPC were used in different ratios. The prepared batches of tablets were evaluated for different parameters. In all the formulations, in vitro disintegration, in vitro dispersion and wetting time found less than 30 seconds. This indicates rapid disintegration. Water absorption ratio showed good absorptivity in all formulations. In vitro release studies revealed that 96% of drug releases from SSG, MCC (90%), and L-HPC (85%) for all the formulations were within 15 min. Stability studies were conducted for formulations F3, F6 and F9 at 250C/60% RH and 400C/75% RH for 30 days.  Not much variation or change was observed in any parameters throughout the study period. Losartan Potassium mouth dissolving tablets formulated by using sodium starch glycolate as superdisintegrant have shown good in vitro disintegration time (8.00sec), in vitro dispersion time (14.33sec), compared to other superdisintegrants. Thus it can be better used as fast dissolving tablet to increase patients acceptability.

39

METHOD DEVELOPMENT AND VALIDATION FOR THE QUANTITATIVE ESTIMATION OF ZOLMITRIPTAN IN BULK AND FORMULATED FAST DISINTEGRATING SUBLINGUAL TABLETS BY RP-HPLC

B. Haarika 1*, Selina Sravanthi2, V. Prabhakar Reddy 3

1 Department of Pharmaceutics, Sarojini Naidu Vanitha Pharmacy Maha Vidyalaya, Hyderabad -500 001, Andhra Pradesh, India.

2 Department of Pharmaceutical Analysis, Sarojini Naidu Vanitha Pharmacy Maha Vidyalaya, Hyderabad -500 001, Andhra Pradesh, India.

3Department of Pharmaceutics, College of Pharmacy, Palamuru University, Mahboob Nagar, Andhra Pradesh, India.

Abstract

A simple, accurate, precise RP-HPLC method was developed for Zolmitriptan determination in bulk and in formulation. The use of chromatographic conditions such as YMC-Pack ODS-AQ column (150 mm x 4.6 mm i.d, 5 µm particle size) as stationary phase, 0.05M potassium dihydrogen orthophosphate buffer (pH 4): acetonitrile (90: 10) as mobile phase with isocratic elution mode. The flow rate was set at 1.0 ml/ minutes. The detection wavelength of 210 nm was optimized to attain a good chromatographic separation. The retention time was noticed to be 9.15 minutes for the drug, Zolmitriptan. The proposed method was applied to the fast disintegrating Zolmitriptan sublingual tablets and the percentage assay was found to be 101.9%.This method was confirmed by system suitability, precision, specificity, linearity and range, accuracy, limit of detection, limit of quantification and robustness as per ICH recommended guidelines. The linearity was established over a concentration range of 25 to 150 µg/ml with a value of 0.999 as correlation coefficient. The mean recovery percentage of Zolmitriptan was attained to be 99.96%. The method was precise with percentage RSD value less than 0.2.

40

CARDIOPROTECTIVE EFFECT OF NARINGIN AGAINST DOXORUBICIN INDUCED CARDIOMYOPATHY IN RATS

V. Madhava Reddy Papasani*, B. Hanumantharayappa, A. Annapurna

Department of Pharmacology, A.U College of Pharmaceutical Sciences, Andhra University,Visakhapatnam-530 003, Andhra Pradesh, India

Abstract

The objective of present study is to evaluate the cardioprotective activity of Naringin against doxorubicin induced cardiomyopathy in male albino rats. Naringin is a flavanone glycoside has the ability to act against oxidative stress, and increase the levels of enzymes that counteract oxidative stress. Rats were divided into 4  groups of 6 animals in each and treated for 8 weeks with naringin against doxorubicin. Doxorubicin was administered i.p. for a cumulative dose of 24 mg/kg body weight over a period of eight weeks in eight consecutive doses. Naringin 100 & 200 mg/kg dose were started one week prior to Doxorubicin, and was continued with daily dose of 100 & 200 mg/kg body weight.  Serum samples and heart homogenates were used to estimate Troponin I, Creatine Kinase, LDH, SGPT, SGOT, LDH, SOD, CAT, GSH, MDA, Iron and Calcium. The results were expressed as the mean ± S.E.M. The results obtained were analyzed using One way ANOVA followed by Tukeys post hoc test. Doxorubicin treated rats showed significant increase in serum and oxidative biomarkers indicating cardiomyopathy. Naringin treatment significantly decreased  serum biomarkers levels  Troponin I, Creatine Kinase, SGPT, SGOT, Iron and Calcium. It also decreased oxidative biomarkers LDH and MDA and whereas it increased SOD and CAT levels. In conclusion, the present study indicates that Naringin offered dose dependent significant cardiac protection and healing effect against doxorubicin induced Cardiomyopathy in rats. The possible mechanisms involved in the cardioprotection of Naringin might be antioxidant and free radical scavenging properties.

41

RAPID AND SENSITIVE RP-HPLC ANALYTICAL METHOD DEVELOPMENT & VALIDATION FOR ESTIMATION OF PIOGLITAZONE HYDROCHLORIDE IN BULK AS WELL AS IN PHARMACEUTICAL FORMULATION BY USING PDA DETECTOR

S. Ashutosh Kumar*1, Manidipa Debnath2, Dr. J. V. L. N. Seshagiri Rao3, B. Sravani, M. Z. V. Hamuthal1, H. V. Jyothi Swarupa1, A. Durga Pavani1, G. P. Sri Ramya1, M. Ujjwala1

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

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

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

Abstract

APPROACH: The present work was undertaken with the aim to develop and validate a rapid and consistent RP-HPLC method development in which the peaks will be appear with short period of time as per ICH Guidelines. A simple, rapid, and precise method was developed for quantitative analysis of Pioglitazone in bulk as well as in pharmaceutical dosage forms. SUMMARY: The chromatographic separation of Pioglitazone was achieved on an ODS C18 (4.6 x 150mm, 3.5µm) analytical column with Disodium Hydrogen Phosphate Buffer (pH adjusted to 4.0 by using Orthophosphoric Acid) & Acetonitrile [HPLC Grade] in the ratio of 30:70 (v/v), as mobile phase at ambient temperature. The flow rate was 1.0 ml/min and detection was by absorption at 318 nm using a PDA detector. The number of theoretical plates and tailing factor for Pioglitazone were 2016.823 and 1.52 respectively. The linearity of the method was excellent over the range 50–90 ppm for the drug Pioglitazone. The correlation coefficient was 0.9999. The relative standard deviations of peak areas from five measurements were always less than 2%. The LOD for Pioglitazone was found to be 0.063µg/ml. The LOQ for Pioglitazone was found to be 0.224μg/ml .The drug content formulations were quantified by using the proposed analytical method. CONCLUSION: The proposed method was found to be suitable and accurate for quantitative analysis of Pioglitazone. The proposed method was adequate sensitive, reproducible, and specific for the determination of Pioglitazone bulk as well as in its Pharmaceutical dosage form. The validation of method was carried out utilizing ICH-guidelines. The described RP-HPLC method was successfully employed for the analysis of pharmaceutical formulations containing the dosage form. The proposed method was simple, fast, Accurate and precise method for the Quantification of drug in the dosage form, bulk drug as well as for routine analysis in Quality control. Overall the proposed method was found to be suitable and Accurate for the Quantitative determination of the drug in Pharmaceutical dosage form.

42

PHARMACOLOGICAL AND SYNTHETIC PROFILE OF 1, 3-BENZOXAZIN -4-ONE: A REVIEW

Nachiket S. Dighe*1, Govind S. Asane2, Deepak S. Musmade3, Ravindra B. Laware2, Pankaj S. Shinde1 and Suraj B. Vikhe1

1Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy, Loni, MS, India-413736.

2Department of Pharmaceutics, Pravara Rural College of Pharmacy, Loni, MS, India-413736.

3Department of Pharmaceutical Chemistry, SRES’s Sanjivani College of Pharmaceutical Education And Research, Kopargaon, Maharashtra, India-423603.

Abstract

Benzoxazin-4-one is a heterocyclic aromatic organic compound. It consist of fusion of benzene and 1, 3-oxazinan-6-one. Benzoxazin-4-one has been found with enormous biological activities with the suitable modifications in the structure. The present review is an attempt made to direct the attention of the researchers towards the Benzoxazin-4-one ring for the development of newer chemical entities which are quite useful in the treatment of various life threatening diseases and disorders This review article covers the most active Benzoxazin-4-one derivatives that have shown considerable biological actions such as anticancer, antitubercular, antifungal and hypolipidaemic activity. This review also discusses the structure-activity relationship of the most potent compounds. It can act as an important tool for medicinal chemists to develop newer compounds possessing Benzoxazin-4-one moiety that could be better agents in terms of efficacy and safety.

43

ISOLATION AND CHARACTERIZATION OF FLAVONOID TRICIN FROM SUGARCANE SLUDGE

Priya Karambelkar, Dr. V.M. Jadhav, Dr. Vilasrao Kadam

Bharati Vidyapeeth’s college of Pharmacy, Navi Mumbai.

Abstract

This study established a new method for the isolation of tricin from extracts of sugarcane sludge i.e. the dried form of sugarcane distillery spentwash. Tricin (5,7,4′-trihydroxy-3′,5′-dimethoxyflavone) occurs in its glycosidic form in many grass species like wheat, barley, and maize. It also occurs in rice bran, bamboo and Sugarcane. Tricin is considered sufficiently safe for clinical development as a cancer chemopreventive agent, therefore it can be used for cancer prevention. In this study the major waste product of sugarcane industry was used. So this process also provided a way to utilize sugarcane sludge in a novel way. This method of isolation successfully separated tricin from the sugarcane sludge extract. It can be used further for such isolation purpose. 

44

ANTIOXIDANT AND HPLC PROFILE OF WILD AND MICROPROPAGATED AERVA LANATA (LINN.) JUSS. EX. SCHULT. - A COMPARATIVE STUDY

Kamalanathan D, Ragavendran C, Natarajan D*

Natural Drug Research Laboratory, Department of Biotechnology, Periyar University, Salem – 636 011, Tamilnadu, India

Abstract

Aerva lanata (Linn.) Juss. Ex. Schult. (Amaranthaceae) is a wonderful herb, based on their chemical constituents and pharmaceutical applications. The prime of this investigation was deals with the comparison of antioxidant and phytochemical properties of in vivo and invitro propagated Aerva lanata leaves. The micropropagation results express higher rate of multiple shoots from node and shoot-tip explants in BAP alone rather combinations of BAP + KIN on modified MS medium produced comparable rates of regeneration. Phytochemical analysis revealed the presence of alkaloids, flavanoids, total phenols, tannins, and saponins. Plant extracts at lower concentration show potential antioxidant properties (DPPH, FRAP, metal chelation and phosphomolybdenum assays) of both invivo and invitro leaf extracts. The HPLC profile of plant extract shown the occurrence of four sharp peaks was confirmed the presence of phenolic compounds. The overall results indicate that micropropagated A. lanata can be used for preparation of foods and pharmaceutical formulations. 

48

Determination of Artemisinin In Selected Artemisia L. Species By HPLC

Rashmi T. R.*, Francis M. S. & Soumya Murali

 Department of Botany, Centre For Postgraduate Studies and Research, Sacred Heart College, Thevara, Ernakulam, Kerala, India

 

Abstract

Malaria is an infectious disease that has been the cause of mortality of hundreds of people around the world. Through screening of many traditional Chinese medicinal plants, the Chinese team of experts discovered, the powerful antimalarial artemisinin, from Artemisia annua. This study deals with the quantification of artemisinin using standard HPLC procedure in selected Artemisia sp. (Artemisia vulgaris and Artemisia japonica). Mobile phase for HPLC analysis was 45% (v/v) methanol and 55% 0.01M sodium phosphate buffer (pH 7.0). Chromatographic separation was performed with Shimadzu LC 2010 AHT/2010 CHT system and the samples were analysed with a reverse phase phenomenex Luna 5u C18 (2) 100A column (250×4.6mm). Isocratic elution was carried out with a flow rate of 1.0ml/min. The temperature was set at the range of 20-250C. Artemisinin was detected at 260 nm. Seasonal and Geographical variations in the concentration of artemisinin was also studied to know whether these factors have any influence in the concentration of artemisinin. The presence of artemisinin in the studied Artemisia sp. ranges from 0.0040-0.01%. Out of the two species studied, A. japonica possess the higher artemisinin content (0.01%) in summer and monsoon seasons.

49

HISTOLOGICAL EFFECT OF ANTICANCER DRUG CYCLOPHOSPHAMIDE (CPA) ON TESTIS OF RATTUS rattus

Mohd. Asif Kanth1, Pinky Kaur1, Bashir Ahmad2, Shivani Sharma1

1Department of Zoology and Applied Aquaculture, Barkatullah University, Bhopal (M.P.)

2Department of Biosciences, Barkatullah University, Bhopal (M.P.)

Abstract

Present investigation deals with the study of the effect of Cyclophosphamide (CP), a widely used anticancer and immunosuppressive drug, on the histological changes in testis of Rattus rattus. Adult male rats were injected with CP at the level of 40mg/kg body weight alternately for 15 days. This chemotherapeutic drug is delivered intraperitonially up to 15 days. Testis of Rattus rattus treated up to 15 days with low dose (40mg/kg body weight) of Cyclophosphamide (CP) showing several histological alteration including less number of spermatozoa in lumen (reduction in the number of spermatozoa). Disorganized spermatogenic cells with reduced number of spermatids. Leydig cells are also prominent and   lumens are filled with relatively less number of spermatozoa.

50

SIMULTANEOUS ESTIMATION OF EPALRESTAT AND METHYLCOBALAMIN IN BULK AND TABLET FORMULATION BY UV SPECTROPHOTOMETRY AND LIQUID CHROMATOGAPHY

PATEL CHANDANI. D. *, PATEL RAJAN. J, SHAH SHRUTI. S, R. B. MARDIA, S .P. CHAUHAN, Dr. B.N. SUHAGIA

Department of Quality Assurance, Faculty of Pharmacy, Dharmsinh Desai University, Nadiad, Gujarat, India.

Abstract

Simple, accurate and sensitive spectrophotometric and RP-HPLC methods requiring no prior separation have been developed and validated for simultaneous estimation of Epalrestat and Methylcobalamin in tablet dosage form. The absorption correction method (method: A) is based on direct determination of Epalrestat at 389 nm and Methylcobalamin at 264 nm by correcting the absorbance of the Methylcobalamin at 264 nm by deducting standard absorbance of Epalrestat at 264 nm. The RP-HPLC method (method: B) was performed using Hyper chrome ODS, 250mm × 4.6mm, 5μ (particle size) as a stationary phase and Methanol: Water (80:20, v/v) as a mobile phase at 0.8 ml/min Flow rate. The detection was done at 210nm. The beer’s law was followed from 4-20µg/ml and 20-60µg/ml for method A and method B respectively. The proposed methods were validated according to ICH guideline (Q2R1) and the results for validation parameters were within specification limit for both the drugs. The proposed methods were applied for determination of Epalrestat and Methylcobalamin in the marketed formulation in which % assay was found to be 99.33% and 100.44 respectively by method A as well as 99.38 % and 97.77 % for same method B. The proposed methods were found to be accurate, precise, repeatable and robust so, these can be applied for routine analysis of both the drugs in their quality control.