INDO AMERICAN JOURNAL OF PHARMACEUTICAL SCIENCES

81-85

Authors: Savkare Anand D*, 2Badhe Nanda R

In this era of competition quality has been given prime magnitude for pharmaceutical product development. Pharmaceutical industries are regulated by various regulatory authorities like ICH, USFDA, Canadian Drug and Health Agency are emphasizing on the purity requirements and the identification of impurities in API’s. Qualification of the impurities is the process of acquiring and evaluating data that establishes biological safety of an individual impurity; thus, revealing the need and scope of impurity profiling of drugs in pharmaceutical research. Quality by Design (QbD) is “a systematic approach to development that begins with predefined objectives and emphasizes product and process understanding and process control, based on sound science and quality risk management” and has the aim of improving product quality and of increasing regulatory flexibility. Impurity level is a critical quality attribute for a drug substance or a drug product because levels higher than the toxicologically qualified amount could affect the safety and efficacy of the product. Control of impurities in drug substance and drug product is described in ICH Q3A, Q3B and with thorough product and process knowledge gained from pharmaceutical development under QbD paradigm, an efficient and comprehensive overall impurity control strategy can be developed to achieve the desired quality of the drug substance/ product. Keywords: Impurity Profiling, Regulatory requirements, QbD approach, Critical Quality Attributes, Control Strategy.

115-128

Authors: Rajendra Kumar Jadi1* and Krishna Mohan Chinnala

The purpose of writing this review was to investigate, compile, recent, current and past literatures. In recent years several advancements has been made in research and development of oral drug delivery system. Various drugs, which are unstable in alkaline pH, soluble in acidic pH, having narrow absorption window, site specific to stomach can be developed by using this technique. Gastroretentive drug delivery systems (GRDDS) can improve the controlled delivery of drugs that have an absorption window by continuously releasing the drug for a prolonged period of time before it reaches absorption site. These include floating system, swelling system, expanding system, low density systems, high density system, bioadhesive and mucoadhesive systems etc. In fact the buoyant dosage unit enhances gastric residence time (GRT) without affecting the intrinsic rate of emptying. GRDDS is an approach to prolong gastric residence time, thereby targeting site-specific drug release in upper gastro intestinal tract improving the oral sustained delivery of drug. For minimizing the limitations and achieving better gastric retention various combinational approaches like floating and swelling, floating and bioadhesion, etc., multi-particulate systems, super porous hydrogel etc., have been discussed. The present review addresses briefly about suitable drug candidates, formulation considerations, physiological difficulties and classification, factors effecting gastric retention, merits, demerits and limitations of gastroretentive drug delivery systems. Keywords: Gastroretentive drug delivery systems, controlled release systems, gastric residence time, gastric emptying time and absorption window.

175-186

Authors: A. Sunil Kumar Reddy*, M. Sambasiva Rao, A. Ashok Kumar

The purpose of the present investigation is aimed to prepare and evaluate simvastatin ethosomes containing different concentration of ethanol and phospholipids by sonication for size reduction of vesicles. Designed ethosomes are characterized for Size and shape, Entrapment efficiency, Release study and Stability study, The effect of sonication also studied on the characteristics of simvastatin ethosomes. To formulate ethosomal gel, characterize the prepared formulation using cold method and carryout various evaluation parameters which includes vesicular shape and surface morphology, vesicular size, size distribution, drug content, storage-physical stability of ethosomes, entrapment efficiency and in vitro drug diffusion study of ethosomal gel. Key words: ethosomes, phospholipids, sonication, gel and cold method.

1-4

Authors: Jumman Ali Ansari* Ajit singh, Neeraj, Ramesh Pandey, Sushma

The research study was undertaken to investigate the effect of different schedules of administration of Arjuna (Terminalia Arjuna) bark powder serum biochemistry of broilers chicks. A total of 72 (Arbor-Acres) day old chicks were used in this study. Four levels of Arjuna (Terminalia Arjuna) bark powder at the rate of .00%, 0.50%, 0.75%, and 1% were incorporated into the basal diet for five weeks. Feeding period for all groups was lasted for 35 days. Relevant data was recorded throughout the experiment till the termination of experiment. Significant decreased total cholesterol, triglycerides and LDL was observed in Treatment T4. It is concluded that schedule on the basis receiving infusion three days in a week is more potent than other schedule of research study. Keywords: Broiler, Arjuna, LDL, H D L, cholesterol.

18-21

Authors: Md. Mosiqur Rahman

Alzheimer’s disease (AD), the most common form of dementia, is a degenerative disorder of the brain that leads to memory loss. Alzheimer's disease is a neurological disorder in which the death of brain cells causes memory loss and cognitive decline. The disease starts mild and gets progressively worse. It first involves the parts of the brain that control thought, memory and language. People with AD may have trouble remembering things that happened recently or names of people they know. Dementia is a general term that describes a significant loss of intellectual abilities, including memory, the ability to reason, and other cognitive and behavioral changes that can interfere with daily life. While a number of health conditions can lead to dementia and related brain deterioration, the most common cause is Alzheimer’s disease. Keywords: Alzheimer’s disease, Dementia, Neurological disorder

31-36

Authors: Shital S.Patil* , P. A. Salunke, R. S. Wagh, Dr. S. D. Barhate

A reverse phase method has been developed for the quantitative estimation of Acyclovir in tablet. The quantification was carried out using RP stainless steel column Water HEMA C18 (250 x 4.6) mm 5μ column packing in isocratic mode with mobile phase containing methanol, acetonitrile and water in the ratio of 45:45:10, Flow rate of 1.0 ml/min and the detection wavelength were set at 264 nm and the linearity was found to be in the range of 2-10 µg/ml for acyclovir. The proposed method was found to be simple, precise, accurate, and reproducible for the estimation of acyclovir. Keywords: Acyclovir, method development, validation, high performance liquid chromatography.

44-51

Authors: Hajare Pranit Pandurang*, Laware Ravindra Bhimraj, Bhusal Ramesh Dattatraya, Magar Manisha Mhasu

A simple and reproducible method was developed for Guaifenesin by Reverse Phase High Performance Liquid Chromatography (RP-HPLC). Guaifenesinwas separated on Greece C18 (4.6ID x 250mm, Particle size: 5 micron), using ortho phosphoric acid buffer with pH of 3.0 at the UV detection of 225 nm. Isocratic elution of methanol and water was used as a mobile phase with various ratios and flow rates, eventually 80:20 v/v methanol and water was being set with the flow rate of 0.8mL/min. The statistical validation parameters such as linearity, accuracy, precision, LOD, LOQ, Robustness, system suitability were checked, further the limit of detection and limit of quantification of Guaifenesin concentrations were found to be 57.98µg/mL and 175.71µg/mL . Keywords:Guaifenesin, Methanol, Development, RP-HPLC, Validation.

52-72

Authors: P. A. Salunke* , R. S. Wagh, Shital S.Patil, Dr. S. D. Barhate

The drug delivery system is to provide a therapeutic amount of drug to a proper site in body so that the desired concentration can achieved promptly and then maintained. Site specific drug delivery refers to targeting a drug directly to a certain biological location. Targeted drug delivery implies selective and effective localization of drug into the target at therapeutic concentrations with limited access to non target sites. Recently, greater emphasis has been placed on controlling the rate and or site of drug release from oral formulations for the purposes of improving patient compliance and treatment efficacy. Benefits of site specific drug delivery Drug directly available at the target site, Decrease in dose to be administered, Decrease side effect, improve drug utilization; it is a promising site for drugs which are unstable or poorly absorbed at upper GI tract. It is a challenging task to formulate such kind of drug delivery system. Keywords: targeted drug delivery, site specific drug delivery, Pharmacokinetic, Pharmacodynamic, sustained drug delivery.

1248-1250

Authors: Ansu Anna Dan, Josna James, Anjali George, Unnimaya Premkumar, Apollojames, T.R.Ashok Kumar, T. Sivakumar

Valproic acid (VPA) has been used in clinical practice since 60’s, with a relatively favourable safety and efficacy profile. Pancreatitis, hepatotoxicity and teratogenicity are the most significant adverse drug reactions. VPA-induced hyperammonemia include: lethargy, impaired consciousness, focal neurological signs and symptoms and increased seizure frequency. More rare described symptoms are: aggression, ataxia, asterixis, vomiting and coma. We report a patient with migraine who developed hyperammonemic encephalopathy in association with valproic acid. The condition improved with a strike of valproic acid and the treatment with carnitine at a dose of 50mg/kg/day for four days.

1256-1263

Authors: Pradeep Pal*1 , Ajay Sharma1 , Mukesh Mehra1 , Anil Choudhary1 , A.K. Ghosh2 , Praveen S Nayak3 , Shweta P Nayak3

Objective: Diabetes mellitus is a serious health problem with continuously increasing rates of incidence and mortality. Diabetes mellitus is characterized by elevated plasma glucose concentrations resulting from insufficient insulin and insulin resistance, or both, leading to metabolic abnormalities in carbohydrates, lipids and proteins. The primary objective of this study was to determine the anti-diabetic activity of Artemisia nilagirica (clark) in streptozotocin induced diabetic rats. Methods: The anti diabetic effect of ethanol extract of leaf and flowering top of Artemisia nilagirica (clark) (200 and 400 mg/kg body weight) were administered orally in diabetic rats. After the oral administration of ethanol extract of Artemisia nilagirica (clark), blood glucose levels were monitored at specific intervals. Results: It was found that ethanolic leaf and flower extract were significant lowered blood glucose level. In the same study the action of the extract on diabetes induced hyperlipidemia was analyzed where the extract significantly lowered the elevated total cholesterol, triglycerides (TGL) and low density lipoprotein (LDL) level while increased the High density lipoprotein (HDL). Glibenclamide was used as a standard drug at a dose of 0.25 mg/kg. Conclusion: The experimental data revealed that the ethanolic extract has significant antidiabetic activity in Streptozotocin-induced rats compared to the standard drug. Keywords: Artemisia nilagirica (clark), antidiabetic, glibenclamide, streptozotocin.

1274-1279

Authors: Mehedi Hasan* 1 , Mofazzal Hossain1 , Masiur Rhaman2

This prescription survey was carried out to find the most frequently used benzodiazepine class (e.g. Clonazepam, Diazepam, Bromazepam, Clobazam, Midazolam, Flurazepam and Alprazolam) and their rational use as antianxiety agents in the Comilla and Feni District of Bangladesh. All the prescriptions were collected in the June 2015, prescribed by psychiatrists throughout the month of May 2015. We have found prescription containing 21% Clonazepam, 12% Flurazepam, 6% Midazolam, 4% Alprazolam, 2% Bromazepam, 2% Diazepam and 2% Clobazam in Comilla district. 51% prescription did not contain any benzodiazepines. In Feni district, we have found 22% Clonazepam, 0% Flurazepam, 0% Midazolam, 11% Alprazolam, 6% Bromazepam, 0% Diazepam and 0% Clobazam in the prescription. 61% prescription in this district did not contain benzodiazepines. We found 1 prescription containing Midazolam and Flurazepam (both are benzodiazepines). In another prescription collected from Feni district we got 1 prescription containing Clonazepam and Alprazolam. But we recommend the citation of the chief complain or diagnosis in the prescription for better understanding and justification of using any drug especially when it is sedative, hypnotic or narcotic drug. Keywords: Psychiatric diseases, benzodiazepines, Insomnia, Anxiety, Schizophrenia

1289-1297

Authors: Pragati Lingwal *, Ganesh Kumar Bhatt, Preeti Kothiyal

The objective of this study was to prepare ampicillin–loaded nanoparticles for controlled delivery through the intravenous (i.v.) route to reduce the frequency of administration, increasing the bioavailability. Ampicillin nanoparticles were prepared by Desolvation method and characterized for drug content, particle size and size distribution, zeta potential, and in vitro drug-release study. In this method the Bovine Serum Albumin nanoparticles were prepared by Desolvation technique. Ampicillin Belonging to the penicillin group of beta-lactam antibiotics.It is used for the treatment of infections known to be or highly likely to be caused by bacteria. All formulations were further checked for evaluation parameters. Particle size of all formulation was found to be 200 to 500nm. Zeta potential for all formulated nanoparticles were in the range of 64.1which indicates excellent stability. The maximum percentage yield was found to be 78.66% for the formulation F4.The maximum drug content was found to be 71.90% for the formulation F1.The cumulative percentage release after 11 h was found to be 53.24 to 75.60.From results it was observed as increase polymer concentration, drug release from the nanoparticles decreases. Keywords: Bovine serum albumin, Nanoparticles, Ampicillin.

1309-1313

Authors: R.B. Saxena

The genus crocus (family – iridaceae) contains ca. 150, small, corm bearing, perennial species having an old world distribution, primarily in Mediterranean- Europe, west Asia and west China. These species are highly valuated as ornamental applications. Sub-genus crocus – crocus aleppici – series are closely related, and are difficult to be separated taxonomically and have a complex cytology. Botany of crocus aleppici – series, taxonomy of their species and their infra-specific taxa are presented, and their distribution, ecology and phenology; description and chromosome counts are provided with key to their identification. Key words : Crocus, geographic area, Classification, Chromosome, Cytology, alpine – series.

1323-1331

Authors: Princy Louis Palatty1 , Sana Aboobaker2 , Ibel Chiramel Fredy3

OCD belongs to the group of personality disorders and is characterized by recurrent uncomfortable thoughts (obsessions) and/or repetitive behaviours (compulsions). Altered levels of neurotransmitters like serotonin, norepinephrine, dopamine and glutamate have been observed to be responsible for this condition. Various brain areas including orbitofrontal cortex, caudate nucleus and cingulated cortex shows dysfunction in OCD patients, thus contributing to the pathophysiology. The most effective lines of treatment present today are pharmacotherapy and cognitive behavioural therapy. Selective serotonin reuptake inhibitors like fluvoxamine, fluoxetine, sertraline etc are the first line of drugs. In subjects who are not responsive, other drugs like tricyclic antidepressants, SNRIs, SARIs and MAOIs are tried. But for a better prognosis, pharmacotherapy and cognitive behavioral therapy are practiced simultaneously. In patients who are resistant to all the above mentioned treatments, electro convulsive therapy or psychosurgery can be tried. Key words: Obsessive compulsive disorder, serotonin, noradrenaline, cognitive behavioural therapy

1141-1146

Authors: Dr.Satish Kumar NS1,MD, Mrs.Pavana K2,Dr.Aswini Dutt R3, MD

Background:Type 2 diabetes and obesity have reached epidemic proportions all over the world. Women will account for the majority of diabetic cases by the year 2050. Effect of age on Cardio-metabolic risk factors in red meat consuming female type 2 diabetic patients needs to be studied. Objective:The aim of this study was to retrospectively assess the relation between red meat consumption and glycemic control, blood pressure and obesity in young and aged female patients of type 2 diabetes. Methods: This is a retrospective study done from the medical records of the patients of type 2 diabetes attending the YMC hospital, Mangalore. The study group consisted of female diabetic patients predominantly consuming red meat diet aged between 27 to 65 years. They were divided into two groups based on their age (viz. <40 years, >40 years of age). Their FBS, PPBS, Blood pressure and BMI were noted. These parameters between two age groups of red meat consumers were measured by unpaired t-test. Results: The data when analysed statistically revealed that female diabetic patients aged above 40 years was positively associated with poor glycemic control in terms of both FBS and PPBS(p < 0.0005).There was significantly higher BMI and BP in elderly female diabetic patients (p < 0.0005 & p< 0.005 respectively). Conclusions: We found that a consumption of red meat was associated with poor glycemic control, hypertension and obesity in patients of type 2 diabetes in elderly-aged women, which is likely due to their hormonal fluctuations. Keywords: Diabetes, Red Meat, Blood Pressure, Body mass Index, Female

1154-1166

Authors: M.Naga Ganesh* , Jamjala Naveen, T.Mangilal,M.Ravi Kumar

he present investigation is aimed to formulate floating gastroretentive tablets containing Quetiapine Fumerate using a sublimation material. The effect of the amount of HPMC K4M on swelling and eroding of the tablets was determined. The water-uptake and erosion behavior of the gastroretentive tablets were highly dependent on the amount of HPMC K4M. The water-uptake increased with increasing HPMC K4M concentration in the tablet matrix. The weight loss from tablets decreased with increasing amounts of HPMC K4M. Camphor was used as the sublimation material to prepare gastroretentive tablets that are low-density and easily floatable.Floating properties of tablets and tablet density were affected by the sublimation of camphor. Prepared floating gastroretentive tablets floated for over 24 hrs and had no floating lag time. However, as the amount of camphor in the tablet matrix increased, the crushing strength of the tablet decreased after sublimation. The release profiles of the drug from the gastroretentive tablets were not affected by tablet density or porosity. From the Formulation, Kinetic, FTIR and DSC Studies indicated that the drug was stable in the tablets. HPMC K4M can be used as a rate controlling polymer by appropriate selection in different ratios. The release of the drug from a matrix tablet was highly dependent on the polymer concentrations. Key words: Gastroretentive Quetiapine fumerate floating tablets, Effervescent method, Non Effervescent method,

1173-1177

Authors: Swetha1 , B. Mohammed Ishaq*1 , Hindustan Abdul Ahad1 , Vanitha Prakash2

Lenalidomide, a thalidomide analogue, is an immune-modulatory agent with antiangiogenic and antineoplastic properties. The chemical name is 3-(4-amino-1-oxo 1,3-dihydro-2H-isoindol-2-yl) piperidine- ,6-dione. Lenalidomide is indicated for the treatment of patients with transfusion-dependent anemia due to Low- or Intermediate-1-risk myelodysplastic syndromes associated with a deletion cytogenetic abnormality with or without additional cytogenetic abnormalities. Lenalidomide possesses antineoplastic, immuno- modulatory and antiangiogenic properties. The present work explains the development and validation of a simple and reliable liquid chromatographic method for the quantitative determination of Lenalidomide in bulk and in tablet formulation. Chromatography was carried out by reversed phase technique on a Waters X-terra RP 18 (250mm x 4.6mm x 5µ) with a mobile phase composed of Methanol and Acetonitrile in the ratio of 60:40 (v/v) pumped at a flow-rate of 1.0 ml/min. The detection was carried out at 210 nm at the ambient column temperature of. The method was evaluated according to ICH guidelines for the various validation parameters, such as linearity, accuracy, precision, LOD, LOQ, specificity, and Forced degradation studies. The results of intraday and inter-day validation (n = 3) showed the method to be efficient and the same was applied in the assay of lenalidomide in tablet formulation. In conclusion, this was a simple and effective method using HPLC to detect lenalidomide in tablet formulation, which may be useful for routine quality control analysis. Keywords: Lenalidomide, antineoplastic, Waters X-terra, Methanol, Acetonitrile, HPLC.

1190-1197

Authors: P. Sravan Kumar1 , Asish Bhaumik*2 , Mrinal Kanti Sarkar3 , Nibedita Roy3 , Mahendar Boddupally4

Abstract: The main aim and objective of the present research work was to extract the potential biomolecules present in the fruit seeds of Glycosmis pentaphylla L and to evaluate the in vitro and in vivo Hepatoprotective activity. The in vitro Hepatoprotective activity was carried out by DPPH assay. The IC50 value (50% inhibition) of the EEFSGP was found to be 212.96 µg/ml. The in-vivo Hepatoprotective activity was carried out by using albino rats. The results displayed that the elevated levels of SGOT, SGPT, ALP and Serum bilirubin were mainly due to CCl4 intoxication, reduced significantly (*P<0.05) in rats, after treatment with ethanolic extract of fruit seeds of Glycosmis pentaphylla (EEFSGP). Treatment with EEFSGP at a dose of 250 mg/kg b.w. decreased the SGOT, SGPT, ALP, Serum Bilirubin levels by 6.23% ns(non significantly), 28.96, 8.81, and 11.11%ns (non significantly) respectively, while a higher dose of 500 mg/kg b. wt. was more effective, causing a reduction of 25.02, 47.65, 24.09, and 27.35%. Silymarin used as standard showed a reduction of 55.09, 68.98, 57.46 and 35.04% receiving CCl4 alone. So depending upon the experimental data it was confirmed that the biochemical parameters of the group treated with ethanolic extract was significantly lower than the CCl4 treated group. Moreover the treatment with the extract significantly reduced the previously raised levels of AST, ALT, ALP and bilirubin in hepatotoxic rats. Histopathological investigation displayed that at both doses (250 mg/kg b.w. and 500 mg/kg b.w.), the EEFSGP was possessed moderate to good hepatoprotective activity, but at 500 mg/kg b.w. executed excellent hepatoprotective activity against CCl4 induced damaged hepatocytes. Key words : Biomolecules, DPPH assay, Intoxication, Hepatocyte, SGOT, SGPT, SALP.

1206-1215

Authors: M. Purushothaman*, B. Narasimha Rao, V.Viswanath, A. Sowmya latha

In the present work, an attempt has been made to develop controlled release tablets of Quetiapine fumarate by selecting different grades of HPMC and Ethyl cellulose as retarding polymers. All the formulations were prepared by direct compression method using 12mm punch on 8 station rotary tablet punching machine. The blend of all the formulations showed god flow properties such as angle of repose, bulk density, tapped density. The prepared tablets were shown good post compression parameters and they passed all the quality control evaluation parameters as per I.P limits. Among all the formulations F3 formulation showed maximum % drug release i.e., 97.3 % in 8 hours hence it is considered as optimized formulation. Whereas the formulations containing HPMCK100M showed more retarding with increasing concentration of polymer. The formulations with Guar gum were unable to produce the desired rug release pattern. Key Words: Quetiapine fumarate, HPMC K15M, HPMC K100 M, Guar gum, Controlled Release tablets.

1227-1239

Authors: Athiya Sulthana*1 , A. Ravi kiran1 , Suneetha Gowdu.R2 , K. Vanitha Prakash2

Background: Colon cancer is the most common cancer and fourth most frequent cause of cancer deaths worldwide. 1,2 dimethyl hydrazine (DMH) is a toxic environmental pollutant which as reported as a specific colon procarcinogen. Aberrant Crypt Foci (ACF) in the colonic mucosa have been hypothesized to represent precursor lesions of chemically induced colon cancer. Cassia absus has been traditionally claimed to be an anti tumor agent but no studies has been done so far. Based on the traditional claims, we presumed that Cassia absus as a potential anti-oxidant and anti-tumor agent, may show ameliorating effect on DMH induced colon cancer in mice. Objective: The objective of the present study was to evaluate the ameliorating effect of ethnolic extract of whole plant of Cassia absus on DMH induced colon cancer in mice. Method: 30 mice (either sex) of 10 weeks old were divided into five groups (n=6)Group I - served as normal control group received vehicle p.o. Group II- disease control group received DMH (20mg/kg s.c.) twice a week for 2 weeks. Group-III and IV – drug treated group received DMH (20 mg/kg sc.) twice a week for 2 weeks and Cassia absus (200 and 400 mg/kg, p.o.) for 7 weeks. Group V received DMH (20 mg/kg s.c.) twice a week for 2 weeks and 5- fluorouracil (20 mg\kg i.p.) once daily up to 2 weeks. During the treatment period body weights was measured at weekly intervals. At the end of seventh week all the animals were sacrificed and their colons were isolated for quantification of Aberrant Crypt Foci, Biochemical estimations (MDA, GSH, Catalase, SOD) and Histological studies. Results: Induction of colon cancer by DMH administration significantly decreased high incidence of ACF, aberrant crypts and crypt multiplicity along with decreased anti oxidant levels and increased colonic MDA levels. Administration of Cassia absus resulted in the decrease in the number of ACF and crypt multiplicity, antioxidant enzymes levels which reflect a favorable balance between potentially harmful oxidants and natural anti oxidants which may be attributed to the chemo preventive effect of Cassia absus. Conclusion: In conclusion, the present study suggests that treatment with ethnolic extract of whole plant of Cassia absusexerts beneficial effect in DMH induced colon cancer in mice probably due to their anti oxidant and anti tumor properties. Key words: 1,2 dimethyl hydrazine (DMH), Aberrant Crypt Foci, Cassia absus

1082-1086

Authors: Alvin Jogy , Pratibha S. Kamble , Princy L. Palatty ,Clafid Lobo, Ibel Chiramel Fredy

Despite the veritable drug explosion since the 1950s, a large number of drugs is being dispensed with a significant amount of returned drugs. Little is known of the specific details of such returns. These could be contributing as a subset of wasted medications.Indigenously prepared case records form conserning details of drugs returned was prepared and administered to the drug sales persons at various local pharmacies, after a short briefing session. This study indication that returned medicines were only a subset of the unused medications. The relevant reasons included death of the patient, wrong medication, change in medication, similar looking or sounding drugs. Key words: Returned drugs, expired drugs, similar sounding/looking drugs, drug utilization, drug policy making, discarded drug disposal

1096-1102

Authors: Loganathan Velupillai*1 , Prashant P Dixit2 , M.S. Shingare1 , D.V.Mane1 , Choudhari B R

A series of seven compounds 4-(2,3-dihydro-4H-pyrido[3,2-b][1,4]oxazin-4-yl)-3-fluoroaniline derivatives (5I e – 5I k) was prepared from commercially available 2-Amino-3-Hdroxy Pyridine. The morpholine, pyridine, fluorine, aniline and amides were introduced in our moiety considering the better biological results in vaster range of therapeutic area. The compound bearing such moieties gives good bio-active data. The more yield and good quality of the synthesized product was shows that there is no side reaction and by product while the organic synthesis. The structure confirmation of the synthesized molecules was confirmed by means of proton nuclear magnetic resonance spectroscopy and LC-MS spectroscopy. The synthesized NCE’s were further tested for their antibacterial and antifungal studies. Some of the molecules were identified to show better antibacterial and antifulgul activity. Keywords: Pyridine morpholine, Morpholine, Fluoroaniline, Antibacterial, Antifungal

1110-1113

Authors: A. Naga Jyothi*, E. Priyanka, D. Eswar Tony, Rama Rao Nadendla

Chamaecostus cuspidatus is commonly known as fiery costus, it is a member of costaceae, and it is a newly introduced plant in India from south-central America. The leaves of this plant are used as a dietary supplement in treatment of diabetes mellitus. A number of researches have been carried out to evaluate the antidiabetic potential of plant. It has been proven to posses various pharmacological activities on diuretics, antioxidant, antimicrobial and anti-cancerous. Key words: insulin plant, antidiabetic activity, quercetin, spiral flag.

1119-1125

Authors: A. T. Sharma*1, Dr. S. M. Vadvalkar2, S. B. Dhoot3

Immunotoxins are composed of a protein toxin connected to a binding ligand such as an antibody or growth factor. These molecules bind to surface antigens and kill cells by catalytic inhibition of protein synthesis within the cell cytosol. Immunotoxins have evolved with time and technology and recently, third generation immunotoxins are made by recombinant DNA techniques. The majority of these immunotoxins targeted antigens selectively expressed on cancer cells. It has been hoped that these agents could cause regression of malignant disease in patients. The studies carried over the plasma clearance of antibody-ricin-A-chain immunotoxins have been shown that after intravenous injection in animals of different species, immunotoxins are rapidly eliminated from the bloodstream. It is due to the mannose residues on the rich A-chain moiety which are specifically recognized by liver cells. The coadministration of yeast mannan with immunotoxin enhances the level of active immunotoxin in circulation by inhibition of liver uptake, which drastically improves the anti-cancer efficacy of immunotoxin in vivo. Immunotoxins can be given in combination with other anticancer therapies to manage tumour penetration. Immunotoxins also firmly increase the viral mortality when used along with effective anti-retroviral drugs. Besides many advantages, the development of many immunotoxins for cancer therapy has still many challenges like immunogenicity, unwanted toxicity, and difficulty in production, limited half-life, and resistance. Key words: Immunotoxins, antitumor, rDNA technique, ricin-A-chain immunotoxins, antiretroviral.

1133-1140

Authors: Arun Kumar Arumugarajan1*, G. Geetha2, Bhabani Shankar Nayak3

Background: The most prominent advantages of extended release formulations of non-steroidal anti-inflammatory drugs (NSAIDs) are their ability to maintain optimal and therapeutically effective drug levels for prolonged duration with reduction in dosing frequency and side effects associated with NSAIDs. Aim: The objective of the present study to develop diffusion controlled matrix tablets for extended release of a model NSAID drug, Etodolac. Materials and Methodology: Etodolac control release tablets were prepared by wet granulation method using Kollidon® SR in different ratios as release rate controlling polymers. The granules were evaluated for flow properties by evaluating bulk density, tapped density, Carr’s index, Hausner’s ratio and angle of repose. The tablets were evaluated for drug polymer compatibility study by FTIR, diameter, weight variation test, hardness, friability, disintegration test, in vitro drug release, release kinetics and stability studies. Results and Discussions: The FTIR study revealed that no such interactions being taking place in between drug and polymers. The flow property of granules of all tablet batches was found to be good. All the tablet formulations had good tablet physiochemical properties. In-vitro release data showed dependence of release kinetics on different percent of drug to polymer in cross-linked matrix systems. Conclusion: The results of in vitro study, it was concluded that Etodolac matrix tablet containing Kollidon® SR (10.0 %) provided most controlled release of water-soluble Etodolac over extended period of time. Keywords: Extended release, NSAIDS, Etodolac, matrix tablet, wet granulation.