National Institute of Pharmaceutical Education and Research, Ahmedabad
Ahmadabad, India

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Dash R.P.,A And G Pharmaceutical, Inc. | Chauhan B.F.,A And G Pharmaceutical, Inc. | Anandjiwala S.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Nivsarkar M.,A And G Pharmaceutical, Inc.
Chromatographia | Year: 2010

An RP-LC method was developed and validated for comparing the pharmacokinetics profile of Vasa Swaras (leaf juice of Adhatoda vasica Nees., Fam. Acanthaceae) with that of the pure vasicine and vasicinone (chief marker compounds of A. vasica) upon oral administration of Vasa Swaras in rats, and also in different animal groups. Significant difference with p < 0.05 was found in the oral bioavailability of vasicine and vasicinone when administered as Vasa Swaras and as single vasicine and/or vasicinone. Vasicine and vasicinone were found to be more bioavailable from Vasa Swaras than pure vasicine and/or vasicinone. © 2010 Vieweg+Teubner Verlag | Springer Fachmedien Wiesbaden GmbH.

Patil S.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Dash R.P.,A And G Pharmaceutical, Inc. | Anandjiwala S.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Nivsarkar M.,A And G Pharmaceutical, Inc.
Biomedical Chromatography | Year: 2012

A sensitive and simple HPLC method was developed for the simultaneous quantification of berberine and lysergol in rat plasma. The chromatographic separation was achieved on a C18 column using isocratic elution with methanol-acetonitrile-0.1% ortho-phosphoric acid (25:20:55, v/v/v), pH adjusted to 6.5 with triethylamine and detected at a UV wavelength of 230nm. The extraction of the berberine and lysergol from the rat plasma with methylene chloride resulted in their high recoveries (82.62 and 90.17%). HPLC calibration curves for both berberine and lysergol based on the extracts from the rat plasma were linear over a broad concentration range of 50-1000ng/mL. The limit of quantification was 50ng/mL. Intra- and inter-day precisions were <15% and accuracy was 87.12-92.55% for berberine and 87.01-92.26% for lysergol. Stability studies showed that berberine and lysergol were stable in rat plasma for short- and long-term period for sample preparation and analysis. The described method was successfully applied to study the pharmacokinetics of berberine as well as lysergol following oral administration in Sprague-Dawley rats. The results of the study inferred that lysergol improved the oral bioavailability of berberine. © 2011 John Wiley & Sons, Ltd.

PubMed | A And G Pharmaceutical, Inc. and National Institute of Pharmaceutical Education and Research, Ahmedabad
Type: | Journal: European journal of pharmacology | Year: 2015

The aim of this study was to evaluate the change in the expression and the activity of intestinal P-glycoprotein (efflux transporter) with progression of diabetes in rats. Diabetes was induced in Wistar rats using a combination of low dose streptozotocin along with high fat diet. The expression of intestinal P-glycoprotein significantly increased (P0.05) with the progression of diabetes which was inferred from the mRNA analysis of mdr1a and mdr1b genes in the ileum segment of rat intestine. Furthermore, a significant increase (P0.05) in Na(+)-K(+) ATPase activity was observed in the ileum segment of rat intestine with the progression of diabetes. As a result of this, a significant decrease in the intestinal uptake and peroral bioavailability of the P-glycoprotein substrates (verapamil and atorvastatin) was observed along with the progression of diabetes as compared to normal animals. To address this problem of impaired drug uptake and bioavailability, a reported P-glycoprotein inhibitor, epigallocatechin-3-gallate, was experimentally evaluated. The treatment with epigallocatechin-3-gallate resulted in significant reduction in the expression and activity of P-glycoprotein and subsequent improvement in the intestinal uptake and peroral bioavailability of both verapamil and atorvastatin in normal as well as in diabetic animals. The findings of this study rationalised the use and established the mechanism of action of epigallocatechin-3-gallate to overcome P-glycoprotein mediated drug efflux and will also be helpful in therapeutic drug monitoring in diabetes.

PubMed | National Institute of Pharmaceutical Education and Research, Ahmedabad and A And G Pharmaceutical, Inc.
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2015

We report the design, synthesis, biological activity and docking studies of series of novel pyrazolo[3,4-d]pyrimidinones as DPP-IV inhibitors in diabetes. Molecules were synthesized and evaluated for their DPP-IV inhibition activity. Compounds 5e, 5k, 5o and 6a were found to be potent inhibitors of DPP-IV enzyme. Amongst all the synthesized compounds, 6-methyl-5-(4-methylpyridin-2-yl)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one (5k) was found to be the most active based on in vitro DPP-IV studies and also exhibited promising in vivo blood glucose lowering activity in male Wistar rats.

Chaudhary S.A.,National Institute of Pharmaceutical Education and Research, Ahmedabad | Shahiwala A.F.,Dubai Pharmacy College
Expert Opinion on Drug Delivery | Year: 2010

Importance of the field: Over the years, patient convenience and patient compliance-orientated research in the field of drug delivery has resulted in bringing out potential innovative drug delivery options. Out of which, medicated chewing gum (MCG) offers a highly convenient patient-compliant way of dosing medications, not only for special population groups with swallowing difficulties such as children and the elderly, but also for the general population, including the young generation. Areas covered in this review: In this review, various formulation ingredients, different manufacturing processes, and assessment of in vivo and in vitro drug release from MCG are thoroughly discussed along with the therapeutic potential and limitations of MCG. What the reader will gain: Readers will gain knowledge about the rationale and prominent formulation and performance evaluation strategies behind chewing gum as a drug delivery system. Take home message: The availability of directly compressible co-processed gum material enables rapid, safe and low-cost development of MCG as a drug delivery option. By MCG formulation, revitalization of old products and reformulation of new patented products is possible, to differentiate them from upcoming generics competition in the market. © 2010 Informa UK Ltd.

PubMed | B. V. Patel Pharmaceutical Education and Research Development Center and National Institute of Pharmaceutical Education and Research, Ahmedabad
Type: Journal Article | Journal: Acta pharmaceutica Sinica. B | Year: 2015

Intranasal drug administration is receiving increased attention as a delivery method for bypassing the blood-brain barrier and rapidly targeting therapeutics to the CNS. However, rapid mucociliary clearance in the nasal cavity is a major hurdle. The purpose of this study was to evaluate the effect of mucoadhesive polymers in enhancing the delivery of nimodipine microemulsion to the brain via the intranasal route. The optimized mucoadhesive microemulsion was characterized, and the in vitro drug release and in vivo nasal absorption of drug from the new formulation were evaluated in rats. The optimized formulation consisted of Capmul MCM as oil, Labrasol as surfactant, and Transcutol P as co-surfactant, with a particle size of 250nm and zeta potential value of -15mV. In vitro and ex vivo permeation studies showed an initial burst of drug release at 30min and sustained release up to 6h, attributable to the presence of free drug entrapped in the mucoadhesive layer. In vivo pharmacokinetic studies in rats showed that the use of the mucoadhesive microemulsion enhanced brain and plasma concentrations of nimodipine. These results suggest that incorporation of a mucoadhesive agent in a microemulsion intranasal delivery system can increase the retention time of the formulation and enhance brain delivery of drugs.

PubMed | National Institute of Pharmaceutical Education and Research, Ahmedabad
Type: Journal Article | Journal: The Journal of pharmacy and pharmacology | Year: 2013

The objective of this study was to synthesize and identify potential leads for the management of Alzheimers disease (AD).A series of bis-imidazopyridines were synthesized and assessed preclinically for anti-inflammatory and antioxidant activity in aluminium chloride-induced rat model for AD. The two targets, anti-inflammatory and antioxidant, hold a significant relevance in AD. The compounds were also screened for their role of protein phosphatase 2A (PP2A) activity in brain which is responsible for tau dephosphorylation and alleviation of AD.The results of our study identified NIPERAMCD-KTB7 (dose: 50mg/kg bodyweight, orally), as a potential molecule with good inhibitory activity in acute (67% oedema protection) as well as chronic (61% oedema protection) model of inflammation. This compound also showed good antioxidant activity as inferred from the inhibition of lipid peroxidation and superoxide dismutase activity in rats at the dose mentioned above. More significantly, PP2A activity was found to be increased in the brains of the animals treated with NIPERAMCD-KTB7 suggesting its potential role in management of AD.These preliminary findings indicate that NIPERAMCD-KTB7 holds potential to serve as a basic lead for further structural modification and development of other new chemical entities for combating AD.

PubMed | National Institute of Pharmaceutical Education and Research, Ahmedabad
Type: | Journal: Journal of biomedical materials research. Part B, Applied biomaterials | Year: 2016

Bone morphogenetic protein-2 (BMP-2) has unique bone regeneration property. The powerful osteoinductive nature makes it considered as second line of therapy in nonunion bone defect. A large number of carriers and delivery systems made up of different materials have been investigated for controlled and sustained release of BMP-2. The delivery systems are in the form of hydrogel, microsphere, nanoparticles, and fibers. The carriers used for the delivery are made up of metals, ceramics, polymers, and composites. Implantation of these protein-loaded carrier leads to cell adhesion, degradation which eventually releases the drug/protein at site specific. But, problems like ectopic growth, lesser protein delivery, inactivation of the protein are reported in the available carrier systems. Therefore, it is need of an hour to modify the available carrier systems as well as explore other biomaterials with desired properties. In this review, all the reported carrier systems made of metals, ceramics, polymers, composites are evaluated in terms of their processing conditions, loading capacity and release pattern of BMP-2. Along with these biomaterials, the attempts of protein modification by adding some functional group to BMP-2 or extracting functional peptides from the protein to achieve the desired effect, is also evaluated. 2016 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2016.

PubMed | National Institute of Pharmaceutical Education and Research and National Institute of Pharmaceutical Education and Research, Ahmedabad
Type: Journal Article | Journal: Critical reviews in eukaryotic gene expression | Year: 2015

Cell competition is a type of short-range cell-cell interaction first observed in Drosophila melanogaster. In two heterogeneous cell populations, cells that have a higher fitness level would have a competitive advantage and grow at the cost of neighbor cells that have comparatively lower fitness. This interaction is due to differences in expression levels of a specific protein in the two cell populations, and it is known as cell competition. In this review, we have studied recent findings of cell competition in different biological processes in Drosophila as well as mammalian systems. The purpose of this review is to collate important studies of competitive cell interactions, and to understand its roles and importance as a central phenomenon. This review provides evidence of the relevance of cell competition in various physiological and pathological conditions, such as size control in organ development, stem cell maintenance, tissue repair, organ regeneration, aging, formation of memory, and cancer.

PubMed | National Institute of Pharmaceutical Education and Research, Ahmedabad
Type: Journal Article | Journal: Journal of enzyme inhibition and medicinal chemistry | Year: 2015

Asthma is multifaceted disease where many targets contribute towards its development and progression. Among these, adenosine receptor subtypes play a major role.MCD-KV-10, a novel thiazolo-thiophene was designed and evaluated pre-clinically for its implication in management of asthma.This compound showed good affinity and selectivity towards A(2A)/A3 adenosine receptor (AR) subtypes. Furthermore, MCD-KV-10 was evaluated for in vitro lipoxygenase inhibition activity; in vivo mast cell stabilization potential and in vivo anti-asthmatic activity was done in ovalbumin-induced airway inflammation model in guinea pigs.The compound showed good (>57%) inhibition of lipoxygenase enzyme and also effectively protected mast cell degranulation (>63%). The compound showed good anti-asthmatic activity as inferred from the in vivo studies.These results indicate that MCD-KV-10 has an inhibitory effect on airway inflammation.Though, we have identified a potential candidate for management of asthma, further mechanistic studies are needed.

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