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Bhatt C.J.,Kb Institute Of Pharmaceutical Education And Research | Pundarikakshudu K.,Lj Institute Of Pharmacy
Journal of Planar Chromatography - Modern TLC | Year: 2017

Trikatu Churna is an important formulation in Ayurveda - the Traditional System of Indian Medicine. It consists of fine powders of fruits of Piper nigrum L., Piper longum L., and rhizomes of Zingiber officinale Roscoe in equal proportions. Piperine, present in both P. nigrum and P. longum, is considered to be responsible for the improvement of digestion and bioavailability enhancement of many medicaments. Gingerols and 6-shogaol are key chemical molecules in Z. of cinale. Piperlongumine is present in P. longum fruits but absent in the fruits of P. nigrum. We report a validated high-performance thin-layer chromatography (HPTLC) method for the determination of piperine, piperlongumine, and 6-shogaol in these herbs and in Trikatu Churna. Piperine, piperlongumine, and 6-shogaol resolved well in n-hexane-ethyl acetate (8:2) on precoated silica gel 60 F254 plates. The absorption maxima for piperine, piperlongumine, and 6-shogaol were found to be 327, 272 and 235 nm, respectively. Linearity for the corresponding markers was observed between 0.1-0.5, 0.2-1.0, and 0.1-1.6 μg spot-1, respectively. The limit of detection (LOD) and limit of quantification (LOQ) were 28 and 100, 56 and 200, and 32 and 100 ng for piperine, piperlongumine, and 6-shogaol, respectively. Recovery experiments showed 99.6%, 99.5%, and 99.7% recoveries for piperine, piperlongumine, and 6-shogaol, respectively. P. nigrum fruits from Delhi and Ahmedabad had around 2.0% w/w piperine, while fruits of P. longum from these markets were analyzed for 0.8% and 0.6% w/w piperine. Piperlongumine was not found in both samples of P. nigrum, while the fruits of P. longum had 0.36% and 0.26% w/w piperlongumine. Z. officinale from Delhi had 0.19% w/w of 6-shogaol as against 0.16% w/w found in the sample from Ahmedabad. Plant materials procured from Delhi were employed for the preparation of Trikatu Churna which showed 96.5%, 95%, and 103% w/w of the expected values of piperine, piperlongumine, and 6-shogaol, respectively. The present method is simple, reproducible, and reliable which can be applied for the routine analysis of Trikatu Churna and its ingredients in polyherbal formulations. © Akadémiai Kiadó, Budapest.


Jani M.,Kb Institute Of Pharmaceutical Education And Research
Anti-Infective Agents in Medicinal Chemistry | Year: 2010

Tuberculosis (TB) has remained an enemy of humankind before the beginning of recorded history. Although it is curable and preventable, TB claims the lives of more than 5,000 people every day. Despite of availability of effective chemotherapy and BCG vaccine in 21st century, TB remains one of the most deadly infectious diseases. The concomitant resurgence of TB with the Multi-drug resistant (MDR) or Extremely drug resistant (XDR)-TB and HIV/AIDS pandemic raises the threat posed by untreatable and fatal human TB, exposing the frailties of the current drug armatorium. No new drug is available acting through novel mechanism since last 40 years. The genome of Mycobacterium tuberculosis H37Rv was sequenced in 1998 and reannotated in 2002. This coupled with development of new genetic tools, have greatly contributed to the discovery of potential drug targets for new anti-TB agent. It is increasingly acknowledged that new drugs should not only be active against drug resistant TB, but should also kill persisters and shorten the lengthy TB treatment, which underlies the problem of drug resistance due to poor compliance to the length of therapy. This review article describes the current TB drugs, their merits and demerits as well as the new promising anti-TB agents classified on the basis of molecular framework. It is a comprehensive literature compilation on the present research paradigm of anti-TB drug discovery including advances in the new structural analogs reported in last decade. © 2010 Bentham Science Publishers Ltd.


Shah G.,Kb Institute Of Pharmaceutical Education And Research
Canadian Journal of Physiology and Pharmacology | Year: 2010

We studied the effect of perindopril (1%) on intraocular pressure (IOP) and compared it with the effect of pilocarpine, a therapeutic agent used in experimentally induced acute and chronic models of glaucoma in rabbits. Acute glaucoma was induced by intravenous administration of 5% glucose. Pretreatment with topical perindopril (1%) and pilocarpine (1%) prevented acute rise in IOP induced by intravenous administration of 5% glucose. For inducing chronic ocular hypertension in rabbits, 50 units of freshly prepared α-chymotrypsin in 0.1 mL of sterile saline was injected in the posterior chamber of the eye. Perindopril (1%) (35 ± 1.38 mm Hg to 22.45 ± 1.42 mm Hg) and pilocarpine (1%) (34.4 ± 0.81 mm Hg to 20.15 ± 0.69 mm Hg) produced a significant fall in IOP in these rabbits; pretreatment with indomethacin (prostaglandin synthesis inhibitor) did not affect the IOP-lowering action of perindopril (1%). Perindopril (2.71 x 10-7 mol/L) and neostigmine (1.49 x 10-7mol/L) inhibited true cholinesterase and pseudocholinesterase enzyme activity in blood. The cholinesterase enzyme inhibition by perindopril was comparable with that by neostigmine. In conclusion, our data suggest that perindopril reduced IOP in experimentally induced acute and chronic glaucoma in rabbits. One of the possible mechanisms of perindopril, apart from the inhibition of angiotensin-converting enzyme, may be inhibition of the enzyme cholinesterase.


Barot B.S.,Kb Institute Of Pharmaceutical Education And Research | Parejiya P.B.,Kb Institute Of Pharmaceutical Education And Research
Advanced Powder Technology | Year: 2012

The objectives of the present study were to address the issues of poor flow and inadequate compressibility of metformin HCl by adopting particle engineering technique. Metformin HCl was crystallized in the presence of polyvinylpyrrolidone (PVP K30). A 32 full factorial design (FFD) was employed for optimization of the processing parameters. Percentage PVP K30 in solution (X1) and crystallization time (X2) were chosen as the independent variables. Percentage yield (Y1), Carr's index (Y2) and tensile strength of compacts (Y3) were selected as dependent variables. Mathematical models were evolved and contour plots were drawn. Metformin HCl particles crystallized in the presence of 2% PVP K30 with crystallization time of four hours (CryMet), showed impressive improvement in flow property, compressibility as well as compactibility as compared to untreated metformin HCl (XMet). The derived compaction parameters 'a', '1/b' and 'Py', obtained using Kawakita and Heckel equations were 0.369, 15.34 and 198.54 MPa for XMet; and 0.249, 11.05 and 143.33 MPa for CryMet respectively. Compressibility evaluation of the samples revealed poor compressibility of XMet while CryMet was directly compressible. DSC and FTIR experiments showed that CryMet particles did not undergo chemical modifications during crystallization. © 2011 The Society of Powder Technology Japan. Published by Elsevier B.V. and The Society of Powder Technology Japan. All rights reserved.


Shah B.,Kadi Sarva Vishwavidyalaya University | Deshpande S.,Kb Institute Of Pharmaceutical Education And Research
Value in Health Regional Issues | Year: 2014

Objective: To assess the influence of diabetes on health-related quality of life (HRQOL) in patients with coronary artery disease (CAD) and identify predictors of health status at 1-year follow-up after an acute coronary event. Methods: A prospective cohort study in patients diagnosed with CAD at a tertiary care hospital from India. The EuroQol five-dimensional (EQ-5D) questionnaire was administered at 1-year follow-up. Multivariate stepwise liner regression was used to assess predictors of EQ visual analogue scale (VAS) and EQ-5D questionnaire utility scores. Respondents reporting problems on the EQ-5D questionnaire were stratified by the presence of diabetes at baseline for comparison. Results: Of 960 (30% diabetic) patients with CAD enrolled in a main study cohort, 306 (76% males, 21% diabetic) responded to the HRQOL questionnaire at 1 year. Diabetic patients reported more difficulties/problems than did nondiabetic patients for EQ-5D questionnaire dimensions (mobility, 12.3% vs. 4.1%, P = 0.03; usual activities, 56.9% vs. 41.3%, P = 0.03; pain/discomfort, 50.8% vs. 17.8%, P < 0.001; anxiety/depression, 33.8% vs. 14.9%, P < 0.001), except for self-care (12.3% vs. 17.5%, P = 0.35). Mean ± SD EQ VAS and EQ-5D questionnaire utility scores were significantly lower for patients with CAD with diabetes versus those without diabetes (0.75 ± 0.15 vs. 0.83 ± 0.15, P = 0.0002, and 67.8 ± 8.8 vs. 73.6 ± 5.4, P = 0.0001, respectively). Presence of diabetes, use of beta-blockers on discharge, and treatment strategy significantly influenced the VAS score, whereas myocardial infarction as final diagnosis and the presence of prior CHF predicted worse EQ-5D questionnaire utility scores. Conclusions: The poorer HRQOL as assessed by the EQ-5D questionnaire among patients with CAD who had diabetes highlights the need of individualized treatment programs to improve outcomes in this most vulnerable population. © 2014 International Society for Pharmacoeconomics and Outcomes Research (ISPOR).


Saiyed M.M.,Kb Institute Of Pharmaceutical Education And Research | Lalwani T.,Kb Institute Of Pharmaceutical Education And Research | Rana D.,Seth Vs General Hospital
International Journal of Risk and Safety in Medicine | Year: 2015

BACKGROUND: The lack of specific medicines and labeling recommendations for the pediatric population is a long-standing problem. Using data from an observational study of adverse drug reactions (ADRs) among pediatric inpatients, we aimed to test the hypothesis that off-label status is a risk factor for ADRs. METHODS: A prospective intensive surveillance was conducted at a pediatric ward of a public teaching hospital. Adverse events to labeled and off-label use were assessed for incidence, severity and predictors. A multivariate Cox proportional hazards regression model used to assess off-label use is a risk factor for ADR occurring. RESULTS: Off-label and labeled use were responsible for 34 (67%) and 17 (33%) ADRs respectively. Medicines which lacked complete pediatric labeling had the greatest odds for ADRs (9.21% of medicines in this category were implicated, OR 2.84 (95% CI 1.37-7.09). Number of off-label medicines given to patient significantly increased the hazard of an ADR (hazard ratio (HR) 1.28, 95% CI 0.43-3.78, P = 0.002). Number of medicines given also significantly increased the hazard (HR 1.2, 95% CI 0.80-1.71, P < 0.001). CONCLUSIONS: Use of off-label medicines were more likely to be implicated in an ADR than labeled medicines. This off-label use would be acceptable if evidence of potential benefits outweighs ADRs risk. © 2015 - IOS Press and the authors. All rights reserved.


Shah S.P.,Kb Institute Of Pharmaceutical Education And Research | Gohil P.V.,Kb Institute Of Pharmaceutical Education And Research | Shah G.B.,Kb Institute Of Pharmaceutical Education And Research
Iranian Biomedical Journal | Year: 2010

Background: Use of hormone replacement therapy (HRT) may increase the risk of adult-onset asthma in women. Various in vitro studies have reported that estradiol stimulates human mast cell lines causing release of allergic mediators which was not observed in estrogen receptor-α (ER-α) knockout mice. Thus, estrogen might be a key element in occurrence of asthma. In the present study, we proposed to determine the role of ER-α in an experimental model of bronchial asthma. Methods: Trypsin and egg albumin induced chronic model of asthma were used. On the 28th day, various parameters such as pO 2 level, serum bicarbonate level, tidal volume, respiratory rate, air flow rate, differential white blood cells count in the bronchoalveolar lavage (BAL) fluid and serum cholesterol level were measured as well as lung histopathological examination and uterine weight measurement were carried out. Results: Estradiol treatment resulted in lower pO 2 level, tidal volume and air flow rate. Also, serum bicarbonate level, respiratory rate and eosinophil rate and eosinophil count in BAL fluid were higher as compared to asthmatic control group. These effects were not observed in methyl-piperidino-pyrazole (MPP) co-treated group. Histopathological data suggested that the destruction of alveolar and muscular layers was more prominent in estradiol-treated group than asthmatic control and MPP co-treated groups. Estradiol-treated group showed lower total serum cholesterol levels and higher uterine weight as compared to asthmatic control group which was not observed in MPP co-treated group; indicating antagonism of estradiol by MPP at ER-α receptor. Conclusion: Estrogen seems to have a strong promoting effect on pathogenesis of bronchial asthma via ER-α receptors.


Patel V.J.,Zydus Research Center | Patel V.J.,Kb Institute Of Pharmaceutical Education And Research | Joharapurkar A.A.,Zydus Research Center | Shah G.B.,Kb Institute Of Pharmaceutical Education And Research | Jain M.R.,Zydus Research Center
Current Diabetes Reviews | Year: 2014

Glucagon-like peptide-1 (GLP-1), is a hormone secreted by small intestine. Consumption of food or glucose stimulates synthesis and secretion of GLP-1 in the bloodstream, which in turn stimulates insulin secretion from pancreas and delays gastric emptying. Owing to the favorable spectrum of effects on reduction of hyperglycemia and body weight, GLP-1 mimetics are intensely pursued as therapies for the treatment of type 2 diabetes (T2DM). Even after intensive control of hyperglycemia, the propensity for cardiovascular disease cannot be totally negated in diabetic patients. A major reason for the cardiovascular disease risk in diabetic patients is underlying dyslipidemia, also termed as diabetic dyslipidemia. It is characterized by high concentrations of triglycerides and LDL cholesterol, and lowered HDL cholesterol in plasma, which are associated with hyperglycemia. Increased insulin resistance gives rise to increased free fatty acids in bloodstream, which is the main reason for the lipid changes appearing in diabetic dyslipidemia. The secondary complications like atherosclerosis and other cardiovascular diseases may be predicted with the blood concentrations of triglycerides and cholesterol, due to the correlation proven in clinic. Hence, new drugs that target diabetic dyslipidemia will always be useful in therapy. Apart from its actions on body weight and glucose, GLP-1 can also regulate cholesterol and triglycerides by numerous ways. Acute and long term treatment with either GLP-1 or its stable analogs reduced fasting as well as postprandial lipids in healthy as well as T2DM patients. GLP-1R signaling reduces VLDL-TG production rate from liver, reduces hepatic TG content by modulating key enzymes of lipid metabolism in liver, and impairs hepatocyte de novo lipogenesis and b-oxidation. GLP-1 can also modulate reverse cholesterol transport. Apart from these direct effects on lipid metabolism, GLP-1 also reduces atherosclerotic events by inhibiting expression of atherogenic inflammatory mediators, suppressing smooth muscle cell proliferation and stimulating NO production. This review mainly deliberates the association of GLP-1 in lipid regulation via lipid absorption, hepatic cholesterol metabolism, reverse cholesterol transport and progression of atherosclerosis. © 2014 Bentham Science Publishers.


Patel Manali B.,Shankersinh Vaghela Bapu Institute of Pharmacy | Deshpande S.,Kb Institute Of Pharmaceutical Education And Research | Shah G.,Kb Institute Of Pharmaceutical Education And Research
Renal Failure | Year: 2011

Gentamicin (GM), an aminoglycoside, is widely employed in clinical practice for the treatment of serious gram-negative infections. The clinical utility of GM is limited by the frequent incidence of acute renal failure. This study was designed to investigate treatment and posttreatment renoprotective potential of vitamin E and N-acetyl cysteine (NAC) against GM-induced oxidative stress and renal dysfunction. Male Sprague-Dawley rats were divided into six groups: first group is the control group that received olive oil (0.1 mL/100 g B.W.), second is the one that was treated with GM (80 mg/kg/i.p./8 days), third is the one that was treated with GM (80 mg/kg/i.p./8 days) and vitamin E (50 mg/kg/i.p./8 days), fourth is the one that was treated with GM (80 mg/kg/i.p./8 days) and NAC (50 mg/kg/i.p./8 days), fifth is the one that was treated with GM (80 mg/kg/i.p./8 days), vitamin E (50 mg/kg/i.p./8 days), and NAC (50 mg/kg/i.p./8 days), and sixth is the one that was treated with GM initially for 8 days (at 80 mg/kg/i.p.) after which vitamin E (at 50 mg/kg/i.p.) and NAC (at 50 mg/kg/i.p.) were administered for 8 days. Serum creatinine, blood urea nitrogen, serum glucose, renal malondialdehyde, renal reduced glutathione, urine sodium, fractional excretion of sodium, and histopathological examination of kidney were performed after treatment. Gentamicin treatment caused nephrotoxicity as evidenced by marked elevation in serum creatinine, blood urea nitrogen, renal malondialdehyde, urine sodium, and fractional excretion of sodium. Study of renal morphology showed marked loss of epithelium in proximal convoluted tubule, inflammatory infiltrate in the form of lymphocytes, mainly in interstitium. Treatment and posttreatment with vitamin E and NAC significantly restored renal functions, reduced lipid peroxidation, enhanced reduced glutathione level, and restored the biochemical parameters. The results of this study demonstrate the therapeutic potential of vitamin E and NAC in gentamicin-induced nephrotoxicity. © 2011 Informa Healthcare USA, Inc.


Dhanesha N.,Cadila Healthcare Ltd | Joharapurkar A.,Cadila Healthcare Ltd | Shah G.,Kb Institute Of Pharmaceutical Education And Research | Kshirsagar S.,Cadila Healthcare Ltd | And 4 more authors.
European Journal of Pharmacology | Year: 2013

The glucokinase activators improve the fasting as well as postprandial glucose control and are important investigational drugs for the treatment of diabetes. However, recent studies have implicated that continuous activation of glucokinase with a small molecule activator can increase hepatic triglycerides and the long term glucose control is not achieved. In this study, we investigated the effect of combination of glucokinase activator (GKA, Piragliatin) with GLP-1 receptor agonist exendin-4 (Ex-4) in male db/db mice. Twelve weeks combination treatment in the db/db mice resulted in a significant decrease in body weight gain, food consumption, random glucose and %HbA1c. The decrease in serum glucose and % HbA1c in combination group was more profound and significantly different than that of individual treatment (GKA or Ex-4) group. GKA treatment increased hepatic triglycerides, whereas combination of Ex-4 with GKA attenuated hepatic steatosis. The combination of GKA with Ex-4 reduced the hepatic lipid accumulation, improved the insulin sensitivity, and reduced hepatic glucose production in db/db mice. Overall, our data indicate that combination of GKA and GLP-1 receptor agonist Ex-4 improves glucose homeostasis, shows antiobesity activity, without causing harmful side effects like fatty liver. © 2013 Elsevier B.V. All rights reserved.

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