Abstract

The main objective of the study is to formulate and evaluate orodispersible tablets of Primaquine with synthetic superdisintegrants. Various formulations of Primaquine were prepared by direct compression method using different ratios of synthetic superdisintegrants (sodium starch glycolate, croscarmellose sodium and crospovidone) at the concentrations ranging from 3%-12%. The drug and excipients compatibility study was performed by IR to study the interaction between drug and excipients. The blend of all formulations were evaluated for various pre-compressional parameters such as angle of repose, bulk, tapped densities, compressibility index, Hausner’s ratio and the prepared tablets were evaluated for various parameters like weight variation, thickness, hardness, friability, wetting time, water absorption ratio, disintegration time, content uniformity and in vitro drug release. Formulations with treated agar have shown promising results compared to other formulations with semisynthetic superdisintegrants. The optimized formulation was subjected to stability studies for three months as per ICH guidelines. Disintegration times of formulations containing treated agar were found to be in the range 30-27sec and 95-100% drug release was observed in 5 min. The optimized formulation was found to be stable with insignificant change in the hardness, disintegration time, drug content and in vitro drug release. In conclusion, it can be stated that the objective of the study has been achieved. From the above study, F6 formulation was concluded as an optimized formulation due to its less disintegration time.

Abstract

The present investigation was aimed at formulation of multiple unit oral gastroretentive floating drug delivery system of ranitidine to prolong the gastric residence time, target stomach mucosa and increase bioavailability. Effervescent calcium alginate beads were prepared by ionotropic gelation technique using different proportions of sodium alginate, hydroxyl propyl methyl cellulose and sodium bicarbonate. Olive oil entrapped beads were also prepared by emulsion gelation method and concentration of oil was optimized. The developed beads were evaluated for mean diameter, surface morphology, floating lag time, buoyancy, entrapment efficiency and in vitro drug release. The optimized formulation of olive oil entrapped microbeads exhibited longer duration of floating time and greater entrapment efficiency than the effervescent formulations. The in vitro release studies in simulated gastric fluid (pH 1.2) indicated that, for optimized formulation (F8); at the end of 8hours, 93% of the entrapped amount of drug was found to release with promising floating characteristics. The drug release data were fitted to release kinetic equations and accelerated stability studies were performed for optimized batch.

Abstract

Citrus grandis (L.) extract was extracted with petroleum ether, ethyl acetate, chloroform, ethanol and aqueous solvents. The extracts were tested against clinical pathogens viz., Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Proteus mirabilis, Penicillium sp., Mucor sp., Aspergillus niger and Candida albicans using disc diffusion method. The ethyl acetate extract showed maximum zone of inhibition against Pseudomonas aeruginosa (15.0±0.1) and Candida albicans (11.0±0.2). On the other hand chloroform extract had no effect against Escherichia coli and none of the extract showed inhibitory activity against Aspergillus niger except for aqueous extract. The observed antimicrobial activity could be due to the presence of alkaloids, flavonoids, saponins, terpenoids, steroids, tannins, cardioglycosides, aminoacids and proteins. Further analysis with Fourier Transform Infrared (FTIR) spectrum revealed the presence of OH stretching for hydroxyl (3408.41 -3352.28 cm-1 ), C=O stretching for carbonyls (1734.01 cm-1 ), C-O stretching for alcohols (1076.28 cm-1 ), C-H stretch for alkane (1249.82-2933.33 cm-1), -C-H bending for alkane (1452.4 cm-1), -C=H bending for alkene (634-850 cm-1), -C=H stretching for alkene (3012.81 cm-1), C=C stretching for alkene (1618.28-1645 cm-1), -C=C- stretching for alkyne (2368.59 cm-1), N-H stretching for amine (3292.49-3300 cm-1 ), C-N stretching for amine (1253.73-1616.35 cm-1), C-O stretching for esters (1049.2 cm-1 ), C=C stretching for aromatic (1402.28-1598.98 cm-1 ), nitro compounds for N-O stretching (1369.46 cm-1). The presence of functional groups indicate the occurrence of alcohol, alkane, amines, aromatics, aldehydes, phenols, esters and nitro compounds in leaves of Citrus grandis (L.) extracts and showed potent antimicrobial activity.

Abstract

The identification of primary and secondary phytochemicals has become the most important tool to know the active principles of various medicinal plants. The present work was aimed at identification and evaluation of phytochemical constituents of leaves and seeds of Solanum torvum Sw., used in folk and traditional medicine for treatment of various diseases like asthma, diabetes, gastro intestinal diseases etc. The two different aqueous and organic (Ethanol and Methanol) extracts of the leaves and seeds were used for identification of phytochemical constituents. The analysis revealed the presence of phytochemicals like alkaloids, flavonoids, saponins, steroids, tennins, terpenoids and phenolic compounds. The GCMS analysis depicted presence of 31 phytochemical constituents in seed, whereas 28 compounds in leaf extracts of Solanum torvum Sw. The major compounds present are Quinic Acid, Linoleic Acid, Palmitic Acid, Isopseudocumenol and Phytol, which are of anti-microbial, anti-cancer, cancer preventive, diuretic, anti-inflammatory, anti-influenza / anti-swine flu value. The present work gives scientific support to ethnobotanical uses of the plant and provides a novel broad spectrum protocol for further research and investigation.

Abstract

An isocratic Simultaneous estimation by RP-HPLC Method were developed and validated for the Estimation of Lamivudine, Stavudine and Efavirenz in Bulk and tablet dosage form. Quantification was achieved by using a reversed-phase L10 column (ZORBAX SB CN Column, 5μ, 150 mm × 4.6 mm) at ambient temperature with mobile phase consisting of 0.2% Triethylamine: Acetonitrile (40:60 pH: 2.0)). The flow rate was 0.6 mL/min. Measurements were made at a wavelength of 258nm. The average retention time for Lamivudine, Stavudine and Efavirenz were found to be 2.4 min 2.8 and 5.6. The proposed method was validated for selectivity, precision, linearity and accuracy. The developed method was successfully applied to estimate the amount of Lamivudine, Stavudine and Efavirenz in bulk and tablet dosage form.

Abstract

The vital part of any pharmaceutical manufacturing is that quality cannot be tested into products; i.e., quality should be built in by design. QbD is a systematic approach to pharmaceutical development to design a quality product and its manufacturing process to consistently deliver the intended performance of the product. The information and knowledge gained from pharmaceutical development studies and manufacturing experience provides scientific understanding to support the establishment of the design space, product and process specifications, and manufacturing controls along with quality risk management. This ultimately leads to understand the impact of raw materials i.e. critical material attributes (CMA), critical process parameters (CPP) on the Critical Quality Attributes (CQA’s). As a result of all understanding we can monitor and update manufacturing process to assure consistent product quality. This systematic approach to product development and manufacturing has received a great deal from traditional approach, which was extremely empirical. Implementation of QbD is enabling transformation of the chemistry, manufacturing, and controls (CMC) into review of Abbreviated New Drug Applications (ANDAs) into a modern, science and risk based pharmaceutical quality assessment.

Abstract

Caring for patients with schizophrenia places an enormous economic burden on the caregivers. The magnitude of this problem remains largely unknown in the developing countries. The objective of this study was to determine the Level of the burden reported by caregivers of patients with schizophrenia. A prospective cross sectional study was conducted by using total of 100 patients and their caregivers attending the Hospital. Caregivers were interviewed, using a socio-demographic data collection sheet and the Zarith Burden Interview (ZBI).The majority of patients suffered were in the age group of 30-40 years and males are most commonly affected. Most of the caregivers were females. A severe level of burden was found in 37% of respondents. The level of burden experienced was significantly associated with place of residence and family size. Schizophrenia is associated with a high level of caregiver burden. So rational therapy with in the economic range of patients were provided along with the appropriate counselling in order to alleviate the burden for better outcomes in both patients and caregivers.

Abstract

Zanthoxylum acanthopodium D.C., commonly known as Mukthrubi in Manipur, India; is known for its varied medicinal properties such as in the treatment of toothache, stomachache, cough, bronchitis and also as an insecticide. In the present study, the phytochemicals from Z. acanthopodium leaves were extracted with ethyl acetate and subjected to column chromatography. The chemical composition of petroleum ether: ethyl acetate (10:90, v/v) fractions (1-5) was determined by Gas Chromatography-Mass Spectrophotometry (GC-MS) technique and the identification of compounds was done by comparing the mass spectra of the unknown compounds with entries in the National Institute of Standards and Technology (NIST) and Wiley (John Wiley & Sons Ltd) libraries. The GC-MS analysis showed the presence of five compounds viz., paulownin (93.17 %), lariciresinol (4.08 %), bis(2-ethylhexyl) phthalate (1.58 %), 2-[1-(3-methoxy-phenyl)-1h-tetrazol-5-ylsulfanyl]-N-(2,4,6-trimethyl-phenyl)-acetamide (0.71 %) and 5,5-diethyl-6-methylspiro[2.3]hexan-4-one (0.46 %). From the results it can be concluded that Z. acanthopodium leaves extract shows the presence of 5 phytocompounds and Paulownin is the major compound having highest peak area. The presence of various bioactive compounds justifies the medicinal use of Z. acanthopodium leaves.

Abstract

Outcome of Peptic Ulcer Disease (PUD) is more dangerous than others. Modern drugs used for the prevention and treatment of Ulcer cases may cause serious side effects. To overcome these problems, peoples now searching drug from the nature especially from plants. Hemidesmus indicus is one of the traditionally used plants for gastro intestinal disorders in the form of syrubath in Tamilnadu, India. In this study ethanolic extract of Hemidesmus indicus root (HIREE) is used to assay antiulcer potentials on acid alcohol induced ulcer model. The result revealed that HIREE reduces ulcer and showed 92% protection, which is greater than standard drug ranitidine. The level of antioxidant enzymes like LPO, SOD, catalase, GSH and GPx were restored as normal by HIREE 400mg/kg bw treatment. HIREE also provides hepatic protection along with ulcer protection, which is indicated by normal level of liver marker enzymes. Overall HIREE showed very effective for Ulcer prevention and treatment. HIREE will be considered as a safe drug for the treatment of ulcer with no side effects.

Abstract

Coronary Artery Disease (CAD) in a major cause of morbidity and mortality in developing countries. PTCA, has become the most frequently used treatment for CAD. Measuring and understanding the current status of Health-Related Quality of Life (HRQoL) of patients before and after PTCA is essential in order to manage the disease more effectively.The objective of the study was to evaluate the changes in HRQoL before and after PTCA. A Prospective, Observational study was conducted for a period of six months in all patients admitted for non-emergency PTCA at the study site and who met inclusion criteria. 80 patients agreed to participate and the informed consent was obtained from the patients. However, 14 patients dropped out during the follow-up period. So the study comprised of 66 patients. The demographics of patients, including clinical parameters such as medical history, diagnosis of CAD and disease severity was collected. Patients were interviewed using SF-36 questionnaire. The HRQoL of patients was measured before(baseline), 1-month and 3-months after PTCA. All the 8 domains of SF-36 (Physical Functioning, Role Physical, Bodily Pain, General Health, Vitality, Social Functioning, Role Emotional, Mental Health) improved slightly from before(baseline) to 1-month after PTCA and improved significantly (P<0.05)from 1-month to 3-months after PTCA. The results of the study quantify the benefits of PTCA on HRQoL of patients. This study also revealed the desired prognosis of our patients. Nursing interventions are needed to maintain and further enhance the HRQoL of the patients and the interventions should come into play immediately after PTCA.

Abstract

Unani tibb is a non-conventional system of medicine based on a holistic approach towards promotion of health and prevention of disease. In ancient literature, the preparation of salt through lixiviation has been mentioned as an art and a profession too. Later on, this procedure was refined and became a pharmaceutical process as amal-e-iqla by the medieval al-chemist and therapeutically used by the physicians. Amal-e-iqla, a pharmaceutical term means process of salt production. Its equivalent term is lixiviation that is a physico-chemical process by which a soluble substance, i.e., salt, is extracted through dissolution (solution) in water. The soluble substance is subsequently recovered from the solution through evaporation. The recovered substance is known as salt or khar or namak. Thus, it is obtained from a number of plants e.g. barley (Hordeum vulgare) known as jaokhar, musk melon (Cucumis melo) known as namak-e-kharpaza, radish (Raphanus sativus) known as namak-e-turb etc. A pharmaceutical strategy was made to prepare khar-e-chirchita as per Unani Pharmacopoeia of India (UPI) and standardize it. The standardization was done by evaluation of its organo-leptic characters, composition and fingerprinting. The composition and fingerprinting were detected by using atomic absorption spectroscopy (AAS), flame photometry and Fourier transform infrared spectroscopy (FTIR), respectively. For the purpose of composition, it was analyzed for the presence of sodium, chloride, phosphorus and magnesium by AAS and flame photometry. The fingerprinting was done by using FTIR in fingerprinting range i.e. from 400-1500cm -1. This study was the first attempt to standardize it.

Abstract

Reverse Phase - High performance liquid chromatographic (RP - HPLC) method was described for determination of Ambroxol Hydrochloride (AMB) and Cefixime Trihydrate (CEF). The chromatographic separation was achieved using mobile phase mixture of Acetonitrile and 0.03 M Tetra Butyl Ammonium Hydrogen Sulphate (pH 6.5 adjusted with Sodium Hydroxide Solution) in the ratio of 25:75 (%v/v) and Zorbex Bonus C18, (250 x 4.6 mm i.d), Particle size 5 m column at 1.2 ml/min flow rate. 20 μL of standard preparation containing 150 μg/ml AMB and 500 μg/ml CEF was injected into the column and the component was separated by carrying out elution for a run time of 15 minutes and detected at 240 nm wavelength. The described method shows excellent linearity over a range of 6 to 60 μg/ml and 20 to 200 μg/ml for AMB and CEF, respectively. AMB and CEF were subjected to stress degradation conditions of hydrolysis (acid and base), oxidation and thermal degradation. Stressed samples were analysed by the developed method. The proposed method is simple, highly fast, economical, sensitive and reliable and is found to be more precise, accurate, specific, stability indicating, rugged and robust. It was readily applied for the assay of pharmaceutical formulations and the results were found to be accepted, therefore the proposed method can be adopted for the routine analysis of any quality control laboratory.

Abstract

The aim of the present study was to investigate the antioxidant and anti-urolithiatic effect of Terminalia bellirica Roxb. fruits on ethylene glycol-induced renal calculi in albino rats. Renal stone was induced in animals by 0.75% ethylene glycol in drinking water for 28 days. The test groups of animals were administered with methanolic extract of T. bellirica (MeTB) at the doses 100, 200 and 400mg/kg b.w. (p.o.) once in a day from 15th day to 28th day. Cystone (750 mg/kg body weight) was used as standard drug. The effect of T. bellirica on various physical and biochemical parameters in urine as well as in serum was evaluated. In vivo antioxidant activity and lithiatic markers were estimated in kidney homogenate. The results demonstrated that MeTB (400 mg/kg b.w.) significantly reduced the ethylene glycol induced disturbance in various physical and biochemical parameters in urine as well as in serum. MeTB (400 mg/kg b.w.) prevented the depletion of GSH level and decrease in the level of SOD in ethylene glycol induced renal injury in rats. In addition, MeTB also showed a significant decrease in the LPO levels signifying the potent antioxidant activity. All of our findings suggest that T. bellirica could protect the kidney from glycol induced calculi.

Abstract

Irrational use of drugs is a major health problem whose consequences include ineffective treatment, unnecessary prescription, development of resistance to antibiotics, adverse effects and economic burden to the patients. A study of prescription patterns is an important tool to determine rational drug therapy and maximize utilization of resources. Periodic assessment of the prescribing pattern in a health facility helps to identify specific drug use problems, promote rational drug prescription and helps in implementation of drug procurement policies on drug prescribing practices.The objective of the study was to assess the drug prescribing practice of the physicians using WHO prescribing indicators in tertiary care teaching hospital and to promote rational prescribing. A descriptive and quantitative survey was carried out taking 205 inpatient prescriptions, designed to evaluate the prescribing practice of the physicians for a period of 6 months.Overall 205 patients were encountered in the study in which 116 were male and 89 were female. A total of 1366 drugs were prescribed with a range of 3 to 5 drugs. 67.32% of the prescriptions were with more than 5 drugs. Brand prescription dominated the generic prescription.57.07% of the total prescriptions were prescribed with antibiotics. 42.44% of the prescriptions were found to be prescribed with no any injectables. Out of 1366 drugs prescribed, 971 (71.03%) were included in National List of Essential Medicine of India 2011.This study reveled that poly-pharmacy and prescription by brand name were common. It is necessary to make doctors aware about the use of drugs and importance of prescribing drugs with their generic names. There is also a need for the development of prescribing guidelines and educational initiatives to encourage the rational and appropriate use of drugs.

Abstract

The aim of this study is to deliver a drug into the brain via intranasal route using transfersomal in situ gel. For this purpose Carbamazepine (CBZ) which is used for the management of epilepsy was selected as a model drug. Transfersomes were formulated by thin film hydration method using Lipoid S100 and sodium cholate in 85:15% (W/W) concentration. Formed transfersomes were found to show the entrapment efficiency of 96.13±0.16%, 2.12±0.47μ particle size and cumulative CBZ release of 98.45% after 12hours. Developed transfersomes were further incorporated into in situ gel. The transfersomal in situ gel was formulated with plain Carbopol 934P and characterized for gelling ability and gelling strength. Formulation F2 with ++ gelling ability and 22±0.56 sec gelling strength was selected for further modification with HPMC K4M. Furthermore formulation F6 with +++ gelling ability, 31.87±1.21 sec gelling strength, 278±2cps viscosity for solution and 1120±20 cps for gel, 93.38% in vitro CBZ release and good mucoadhesive strength of 55.38±0.69 dyne/cm2 was optimized. From the results it can be concluded that transfersomal in situ gel of CBZ can be used to reduce the frequency of administration and increase patient compliance in the treatment of epilepsy.

Abstract

G. sylvestre (Asclepiadaceae) a vulnerable species is a slow growing, has been shown to display a wide array of pharmacological activities (hypoglycemic and hypolipidemic). The present study was designed to investigate the Antidiabetic effects of Gymnema sylvestre extract in experimental diabetes. Necessary approval from the Institutional Animal Ethics Committee was taken for the study. Experimental diabetes was produced with single dose of Streptozotocin (STZ): 45mg/kg ip. After the confirmation of diabetes on 7th day (>200mg/dl), Gymnema Sylvestre (400mg/kg) was administered orally to experimental rats from day 8th day and continued for 30 days thereafter. Various anti diabetic (Glucose, HbA1C), cardioprotective (CPK-MB), metabolic (Lipid Profile), safety {liver (SGPT, albumin were evaluated in sham (healthy control), STZ- Control and Gymnema treated groups. Administration of STZ resulted in a significant decrease in diabetic changes (increase in blood glucose, HbA1C), cardiac injury (myocardial CPK-MB loss), altered lipid profile, SGPT, Albumin, (p<0.01) in the STZ- control group rats as compared to sham. Gymnema treatment demonstrated significant antidiabetic indicated by restoration of blood glucose, HbA1C and CPK-MB levels (p<0.01) compared to STZ Control group. In addition, Gymnema also favorably modulated the lipid parameters (total cholesterol, triglycerides,). In addition, Gymnema treatment was found to be safe to the liver. The Present study concluded that, the Gymnema Sylvestre extract exhibit the antidiabetic activity.

Abstract 

The present research work was done to develop the formulation of two antidiabetic drugs i.e. Metformin HCl (500 mg) and Voglibose (0.3 mg) in bilayer tablet formulation. The tablet consist of two drug containing layers which comprises Metformin sustained release layer (blue colored layer with break line ) and an immediate release layer of Voglibose (white colored layer ) was optimized separately and constituted in bilayer tablet, a common analytical method by HPLC for quantitative combined drug evaluation (assay and dissolution ) was employed. Two different matrix formulations were developed, one matrix layer with hydrophilic swellable polymer and another with hydrophobic polymer. Hydroxypropylmethylcellulose and Colloidal silicon dioxide was used as polymers in order to get the sustained release profile for Metformin over a period of 24 h. Tablets were evaluated for physical properties as well as drug content (assay) and in vitro drug release (dissolution) were compared with standard commercial tablets. The excipients used in this formulation did not alter physicochemical properties of drug, as tested by HPLC. This formulation also best fitted formulation into zero order kinetics of the drug from the tablets was confirmed. The evaluation of bilayer tablet prepared from optimized formula was found to be best suited method for fixed dose combination of sustained release Metformin HCl and immediate release Voglibose as comparison to other marketed available formulation. The method of evaluation by HPLC was not developed separately, but it was common method used in laboratory for drug estimation in this combination.

Abstract

The antidiabetic activity of Momordica cymbalaria was investigated specifically in its ability to increase the uptake of glucose. A triterpenoid saponin of oleanane-type (SMC) was isolated from the roots of Momordica cymbalaria. Glucose uptake experiment by isolated diaphragms of both diabetic, following streptozotocin administration, and non-diabetic animals (Swiss Albino mice) was carried in the presence and absence of SMC. To determine the in vitro cytotoxicity, MTT assay was performed on L6 cell line (mouse skeletal muscle) for test dose fixation. Further, glucose uptake by L6 cell line in the presence of SMC was performed. Glucose uptake was determined by glucose oxidase-peroxidase (GOD-POD) method. SMC did not show cytotoxicity against L6 cells and significantly increased glucose uptake up to 242.75% over control in a dose-dependent manner. Diabetic and non-diabetic diaphragms also showed increase in glucose uptake in the presence of SMC over control. Data from both the models (cells and isolated diaphragms) indicate that SMC enhances glucose uptake thereby exhibiting hypoglycemic activity. The findings suggest that SMC can prove to be very effective against hyperglycemia due to insulin resistance, as in Type 2 Diabetes Mellitus.

Abstract

Thiazole derivatives are present in many natural and synthetic products with a wide range of pharmacological activities such as anticancer, antibacterial, antifungal, anti-inflammatory activities. Thiazole derivatives particularly amino thiazoles play a vital role in pharmaceutical practice owing to their wide biological activities. In continuation to these efforts and with an objective to develop novel and potent therapeutic agents of synthetic origin, it was decided to synthesize certain thiazole prepared by reacting protected acetophenones like 1-[4-(2-Amino-thiazol-4-yl)-phenyl]-pyrrole-2,5-dione (2a), synthesized by reacting maleic anhydride with p-amino acetophenone, 2-[4-(2-Amino-thiazol-4-yl)-phenyl]-isoindole-1,3-dione (2b), synthesized by reacting phthalic anhydride with p-amino acetophenone, N-[4-(2-Amino-thiazol-4-yl)-phenyl]-benzamide (2c), synthesized by reacting benzoyl anhydride with p-amino acetophenone. These thiazoles were further reacted with various aldehydes in ethanol to form Schiff bases [2a1-5, 2b1-2, 2c1-5]. The structure of the new synthesized compounds were authentically establishedby their Rf value, melting point, IR, 1HNMR, 13C-NMR, mass spectral analysis and CHN analysis and they were evaluated for their anti-oxidant and anti-inflammatory studies. Among all the eighteen synthesized compounds,mostof the compounds exhibited excellent to very good anti-inflammatory and antioxidant activity.CompoundN-(4-{2-[(2-Nitro-benzylidene)-amino]-thiazol-4-yl}-phenyl)-benzamide (2c2) exhibited antioxidant activity and compound (N-[4-(2-Amino-thiazol-4-yl)-phenyl]-benzamide (2c) exhibited excellent anti- inflammatory and antioxidant activity.

Abstract

The use of plant derivatives as the source of medicine to treat many diseases has become a universal among non-industrised sectors. More than two third of the World’s plant species, 35,000 plants are known for its medicinal values. The phytochemicals produced by the plants proved to have normal metabolic activities in human body and serve more specific functions. The present article, emphasize the importance of safflower, which is an annual plant, glabrous, branching stem of 1-3 feet high and are alternate, sessile, oblong, dark green, shiny leaves with orange or yellow flowers.

Abstract

Although many Respiratory Tract Infections (RTIs) require antimicrobial therapy for optimal management (such as Bronchopneumonia), most “acute self-limiting” RTIs (i.e., acute bronchitis, pharyngitis or common cold) are caused by respiratory viruses for which antibiotic use is not warranted. Hence the prescription of antibiotics in RTIs has been found out to provide both risks as well as benefits. The aim of this study is to analyze the prescribing pattern of antibiotics in RTIs and assess their risks and benefits from antibiotic guidelines. A prospective study was conducted in BMCH&RC, Chitradurga, for a period of six months. . The data from the record of each patient prescribed with antibiotics for RTIs was collected in a separate proforma and subjected to descriptive statistical analysis using Microsoft Excel .In our study 597 antibiotics were prescribed to 362 patients. The most frequently diagnosed were self-limiting RTIs, where antibiotics were first line therapy. More ADR were seen in common cold (81.4%) followed by Acute bronchitis (4.8%) and viral pharyngitis (3%). More ADR were associated with Cephalosporins (37%) followed by Beta lactamase inhibitors (29.6%), Fluroquinolones (22.2%) and Tetracyclines (11%). Patients with bacterial infections received appropriate antibiotic treatment showed shortened duration of hospital stay and better survival. Inappropriate antibiotic prescription were analyzed in acute self-limiting RTIs, where it showed risks, While appropriate antibiotic prescription were analyzed in patients who acutely needed it, where it proved beneficial.

Abstract

A novel stability indicating liquid chromatographic assay method was developed and validated as per ICH guidelines for the quantitative estimation of Afatinib in tablet formulation. An gradient reverse phase LC-method was developed using X-Terra RP-8, 250 x 4.6mm, 5μm column and a mobile phase were aqueous Potassium dihydrogen orthophosphate buffer adjusted pH at 3.0 with o-phosphoric acid (mobile phase solvent-A) and Acetonitrile:Methanol(70:30v/v) (mobile phase solvent-B) in a gradient mode. The detector set at 258nm with flow rate of 1.0mL min-1. The method is linear between 0.12 to 0.36 mg/mL with a good linear relationship (r2=0.998) was observed and the limit of detection (LOD) is 0.06 μg/ mL 0.02% and limit of quantification (LOQ) is 0.06 mg/mL 0.06%. The Accuracy of the method was found to be in the range of 99.70% to 100.26%. The mean Inter and Intraday Precision has Relative Standard deviation (%RSD) were less than 0.147. Robustness was done by change in column, variation in change of flow rate of +/- 0.2 mL/min. the values were found to be within the limits. The Proposed method was found to be Linear, precise and accurate for the quantitative estimation of Afatinib in tablet formulations and can be used for commercial purposes.

Abstract

Insulin released by the β cells of pancreatic islets is the main regulator of glucose levels, the quantitative modelling of their glucose stimulated insulin secretion is of obvious interest not only to improve our understanding of the processes involved, but also to allow better assessment of β cell function and the development of improved artificial or bioartificial pancreas devices. Since previous studies from our lab have shown that the aqueous extracts of Ocimum sanctum and Allium sativam have antihyperglycemic potential in alloxan induced diabetic rats, the present study was aimed to evaluate whether the extracts of Ocimum sanctum and Allium sativam improve the insulin secretion in vitro in glucose challenged cultured pancreatic islet cells of Wistar rats. Normal islet cells and glucose challenged islet cells treated with aqueous suspension of Ocimum sanctum and Allium sativam showed increased viability and insulin level. In vitro treatment of Ocimum sanctum and Allium sativam showed insulin secretagogue activity in cultured β islet cells of rats.

Abstract

Adverse drug reactions (ADRs) are considered as one among the leading causes of morbidity and mortality. The aim of the study is to conduct the surveillance of adverse drug reaction and minimize them for better patient care.A Prospective Adverse Drug Reaction Reporting Method was conducted in the General Medicine Department of a tertiary care teaching hospital for 6 months from September 2014 to February 2015 to detect and suspect ADRs and to analyse the causality, severity and preventability using appropriate validated scales. ADR alert card was prepared and given to patients. Therapeutic guidelines were prepared and given to the relevant departments. A total no. of 184 patients were followed among them males were (39.13%) and females were (60.87%). 8.6% were from paediatrics department, 78.4%patients were from general medicine and 13.0% patients were from geriatrics. A total of 128 ADRS from in-patient department and 56 ADRS from out- patient department were reported & the highest no. of ADRs was found with antibiotics. Gastro intestinal system 76(41.30%) was the most commonly affected organ. 110(59.78%) adverse drug reactions were due to predisposing factors. 94.56% ADRs required medical intervention to prevent permanent impairment or damage .In majority of the ADRs the suspected drug was withdrawn 62(33.69%) and 74(40.21%) required symptomatic treatment. 79 ADRs (42.93%) recovered after the management. Maximum reporting of the ADRs was done by the clinical pharmacist 126(68.47%).This study helped in a better monitoring of the therapy given to the patient, helps in the drug safety and efficacy.

Abstract

Background: Janus kinase 2 (JAK2) is a significant enzyme, which plays an essential role in myeloproliferative disorders (MPDs) and many other diseases. Inhibition of JAK2 activity by small molecule inhibitors has been attracting a great deal of MPDs and cancer therapy. Method: Pharmacophore modeling, atom-based 3D-QSAR and molecular docking studies were carried out for a set of 30 compounds belonging to 2,4-diamino-1,3,5-triazine derivatives for potent JAK2 inhibitory activity. The data set of the compounds was also docked into the binding site of JAK2 using GLIDE and the active residues of the binding site were analyzed. A five-point pharmacophore model AADDH, with two hydrogen bond acceptors (A), two hydrogen bond donors (D) and one hydrophobic region (H) was developed by PHASE module of Schrödinger suite Maestro 9. Results: The generated pharmacophore model was used to derive a predictive atom-based 3D quantitative structure-activity relationship analysis (3D-QSAR) model for the training set (R2 = 0.96, SD = 0.21, F = 124.5, N = 24) and test set (Q2 = 0.76, RMSE = 0.44, Pearson R = 0.87, N = 6) molecules. It was found that the most active compound 19 interacted with the active residues namely Leu932 (2), Arg980, Leu855 (Glide score = -7.37), whereas the reference compound Ruxolitinib interacted with the active residues, Leu932, Glu930 (Glide score = -9.26). Conclusion: The above 3D-QSAR model illustrates that electron-withdrawing and hydrophobic groups might prove efficacious for JAK2 inhibitory activity as evident from the docking results, which clearly show the hydrogen bond interactions with the active residues of these compounds. Thus, it is contemplated that the substitution of methoxy, phenoxy, morpholinoacetamide, oxyalkyl & oxyaryl groups on 2,4-diamino-1,3,5-triazine scaffold might increase the activity of the compounds against JAK2 protein. The above result provides an insight for further design and development of newer chemical entities as JAK2 inhibitors.

Abstract

Calophyllum inophyllum L. has been used as folk medicine in the treatment of ocular burn and it has demonstrated potential pharmacological activities. The aim of the study is to perform preliminary phytochemical screening, and to evaluate the nootropic and antidepressant activity effect of methanolic extracts of Calophyllum inophyllum. Calophyllum inophyllum leaves and stem bark were extracted using methanol as solvent by Soxhlet apparatus. The percentage yield of CILE was found to be 16.27% and percentage yield of CISBE was found to be 17.62%. Preliminary phytochemical screening revealed the presence of alkaloids, carbohydrates, glycosides, saponins, tannins, flavonoids, proteins, amino acids and steroids. Doses up to 2000mg/kg were found to be safe after acute toxicity tests. The results for tail suspension test and forced swim suggest antidepressant activity and the electro shock induced amnesia and diazepam induced amnesia suggest nootropic activity of the extract with p value<0.005.

Abstract

Azadirachta indica (Neem) is known to possess various pharmacological properties and is used worldwide. The present investigation aims to study the effects of methanol and hexane fractions of seed extract of A. indica on fertility in albino rats. Seeds of shade dried matured drupes were powered and methanol and hexane fractions were extracted at 35°C. Mature cyclic female albino rats weighing 135±10 gm were used under standard laboratory conditions. The fractions were tested for their effect on cyclicity, fertility and implantation activity @ 1mg, 3mg and 6mg/kg body weight, orally. The percent occurrence of proestrous was significantly reduced @3mg/ kg bw methanol fraction. There was no significant change in the estrous stage of estrous cycle in all the treatment groups depicting anti-estrogenic nature of fractions. Pre-implantation mortality was high at 3mg/kg bw methanol fraction, post-and total prenatal mortality was high at 3mg/kg bw hexane fraction when administered for 18 days. Not even a single corpus luteum was observed at 6mg/kg bw methanol and hexane fraction treated rats. The average number of embryos was significantly reduced during D1-D7 pc treatment @ 6mg/kg bw of both the fractions as compared to control. Significant increase in post-implantation and total prenatal mortality was observed in methanol and hexane fraction treated rats @ 6mg/kg bw during D7-D18 pc. The average gestation period was increased by 7.5-9 days and litter size, live birth index and average life span of young ones decreased in both the treatment groups. The results indicate that methanol and hexane fractions of seed extract of A. indica possess significant antifertility and anti-implantation activities. The research work on fertility regulating properties of various fractions of A. indica should be continued as it may lead to breakthrough in achieving population control as it is found to interfere with the reproductive potential.