R C Patel Institute Of Pharmaceutical Education And Research

Dhule, India

R C Patel Institute Of Pharmaceutical Education And Research

Dhule, India
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Ugale V.G.,R C Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,H R Patel Institute Of Pharmaceutical Education And Research
SAR and QSAR in Environmental Research | Year: 2016

The Gly/NMDA receptor has become known as potential target for the management of neurodegenerative diseases. Discovery of Gly/ NMDA antagonists has thus attracted much attention in recent years. In the present research, a cheminformatics approach has been used to determine structural requirements for Gly/NMDA antagonism and to identify potential antagonists. Here, 37 quinoxaline derivatives were selected to develop a significant pharmacophore model with good certainty. The selected model was validated by leave-one-out crossvalidation, an external test set, decoy set and Y-randomization test. Applicability domain was verified by the standardization approach. The validated 3D-QSAR model was used to screen virtual hits from the ZINC database by pharmacophore mapping. Molecular docking was used for assessment of receptor-ligand binding modes and binding affinities. The GlideScore and molecular interactions with critical amino acids were considered as crucial features to identify final hits. Furthermore, hits were analysed for in silico pharmacokinetic parameters and Lipinski’s rule of five, demonstrating their potential as drug-like candidates. The PubChem and SciFinder search tools were used to authenticate the novelty of leads retrieved. Finally, five different leads have been suggested as putative novel candidates for the exploration of potent Gly/NMDA receptor antagonists. © 2016 Taylor & Francis.

Wani Y.B.,R C Patel Institute Of Pharmaceutical Education And Research | Patil D.D.,H R Patel Institute Of Pharmaceutical Education And Research
International Journal of Pharmacy and Pharmaceutical Sciences | Year: 2013

Objective: Two simple, accurate, precise, reproducible and an economical spectrophotometric methods were developed for the simultaneous estimation of ibuprofen and famotidine in pharmaceutical bulk and synthetic mixture. Methods: The first method was developed on the basis of Q-absorbance ratio method (method I) for analysis of both the drugs. Wavelengths selected for analysis in Q-absorbance ratio method were 263 nm (λmax of ibuprofen) and 273.80 nm (iso-absorptive wavelength) in 0.1N NaOH. The second method was based on derivative spectrophotometric method (method II) involving the determination of both the drugs at their respective zero crossing point. The determinations were made at 252.8 nm (zero crossing point of famotidine) and 304 nm (zero crossing point of ibuprofen) in 0.1N NaOH. Results: Both the method obeys Beer-Lambert's law in the concentration range of 150 - 750 μg/ml for ibuprofen and 5 - 25 μg/ml for famotidine. The assay result of synthetic mixture was found to be 99.13 ± 0.14 for IBU and 100.73 ± 0.57 for FAM by method I and 104.17 ± 1.96 for IBU and 100.88 ± 2.13 for FAM by method II. Proposed methods were validated according to ICH Q2 (R1) analytical method validation guidelines. Conclusion: The proposed methods are suitable for the routine quality control analysis of ibuprofen and famotidine in pharmaceutical formulation.

Kulkarni A.D.,Maharashtra Institute of Pharmacy | Bari D.B.,Maharashtra Institute of Pharmacy | Surana S.J.,R C Patel Institute Of Pharmaceutical Education And Research | Pardeshi C.V.,Maharashtra Institute of Pharmacy
Journal of Drug Delivery Science and Technology | Year: 2016

Present investigation deals with design, development and evaluation of chitosan-based spray-dried nasal mucoadhesive microspheres loaded with diltiazem hydrochloride (DTZ HCl). The principal objectives were to improve therapeutic efficacy through increased residence of microspheres on the nasal mucosa, and avoidance of hepatic first-pass metabolism. Formulation samples were characterized for preliminary physico-chemical parameters, mucoadhesiveness, drug release and release kinetics, mucosal toxicity, stability, and in vivo studies. Central composite experimental design was utilized herein to evaluate the influence of process and formulation variables product performance. Numerical and graphical optimization techniques were used for selecting optimum sample of prepared microspheres, further confirmed by three dimensional response surface plots and multilinear regression model. Results of ANOVA validated the significance of suggested models. Our findings suggest that DTZ-loaded spray-dried chitosan microspheres formulation could be used as a promising approach for intranasal administration which, in sum, improves therapeutic efficacy of the formulation. © 2015 Elsevier B.V. All rights reserved.

Pardeshi C.V.,R C Patel Institute of Pharmaceutical Education and Research | Belgamwar V.S.,R C Patel Institute of Pharmaceutical Education and Research
Expert Opinion on Drug Delivery | Year: 2013

Introduction: The blood-brain barrier (BBB) represents a stringent barrier for delivery of neurotherapeutics in vivo. An attempt to overcome this barrier is represented by the direct transport of drugs from the nose to the brain along the olfactory and trigeminal nerve pathways. These nerve pathways initiate in the nasal cavity at olfactory neuroepithelium and terminate in the brain. An enormous range of neurotherapeutics, both macromolecules and low molecular weight drugs, can be delivered to the central nervous system (CNS) via this route. Areas covered: Present review highlights the literature on the anatomy-physiology of the nasal cavity, pathways and mechanisms of neurotherapeutic transport across nasal epithelium and their biofate and various strategies to enhance direct nose to brain drug delivery. The authors also emphasize a variety of drug molecules and carrier systems delivered via this route for treating CNS disorders. Patents related to direct nose to brain drug delivery systems have also been listed. Expert opinion: Direct nose to brain drug delivery system is a practical, safe, non-invasive and convenient form of formulation strategy and could be viewed as an excellent alternative approach to conventional dosage forms. Existence of a direct transport route from the nasal cavity to the brain, bypassing the BBB, would offer an exciting mode of delivering neurotherapeutic agents. © 2013 Informa UK, Ltd.

Pritam J.,R C Patel Institute Of Pharmaceutical Education And Research
International Journal of Drug Development and Research | Year: 2011

Objective: A simple, rapid, accurate and economical First order UV-derivative spectrophotometric method has been developed for estimation of sitagliptin from bulk and pharmaceutical formulation. Materials and methods: The λ max of sitagliptin in methanol and water was found to be 267 nm. The same spectrum was derivatised in to first order derivative; showed maximum amplitude of the trough at 275 nm. The drug follows linearity in the concentration range 10-60 μg/ml with correlation coefficient value 0.998. Results: The proposed method was applied to pharmaceutical formulation and % amount of drug estimated 99.19 % was found in good agreement with the label claim. The accuracy of the method was checked by recovery experiment performed at three different levels i.e., 80%, 100% and 120 %. The % recovery was found to be in the range 98.54%- 99.98%. The low values of % R.S.D. are indicative of the accuracy and reproducibility of the method. The precision of the method was studied as an intra-day, inter-day variations and repeatability. The % R.S.D. value less than 2 indicate that the method is precise. Ruggedness of the proposed method was studied with the help of two analysts. Conclusion: The above method was a rapid and costeffective quality-control tool for routine analysis of sitagliptin in bulk and in pharmaceutical dosage form. © 2010 IJDDR.

Ige P.P.,R C Patel Institute Of Pharmaceutical Education And Research | Gattani S.,Swami Ramanand Teerth Marathwada University
Polymer - Plastics Technology and Engineering | Year: 2012

Polymeric floating microspheres of metformin hydrochloride were prepared by a modified solvent evaporation method using ethyl cellulose and HPMC K4M. Microspheres were characterized by SEM, particle size, drug content, in vitro swelling, in vitro buoyancy, in vitro drug release and in vivo X-ray imaging. Formulation D exhibited in vitro swelling, about 48.28 ± 1.03% and the desired floating time and with retention in the upper small intestine of rabbits for 8 h and with release for 12 h. We conclude that ethyl cellulose and HPMC K4M at 0.40:1.50 w/w ratios could be an effective carrier for multiparticulate controlled drug delivery. © 2012 Copyright Taylor and Francis Group, LLC.

Redasani V.K.,R C Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,R C Patel Institute Of Pharmaceutical Education And Research
European Journal of Medicinal Chemistry | Year: 2012

The present works deals with simple and efficient method of improving therapeutic efficacy of racemic ibuprofen by retarding gastrointestinal side effects through masking of carboxylic group chemically. This is achieved by synthesis and evaluation of ester derivatives of ibuprofen as mutual prodrugs with naturally occurring phenolic and alcoholic compounds. Promoieties like menthol; thymol and eugenol were selected with the aim of getting synergistic effect as these are natural analgesic having traditional medicinal values. Prodrugs are found to be highly lipophilic as compared to parent drug. All the prodrugs are found to be highly stable at acidic pH while undergoes hydrolysis at neutral and alkaline pH as indicated by their t1/2 values. Synthesized prodrugs derivatives show increased anti-inflammatory activity that might be attributed to synergistic effect as ibuprofen conjugates to natural analgesics. Ulcer index shows much reduction in gastric ulceration compared to ibuprofen concluding the successful masking of acidic group. © 2012 Elsevier Masson SAS. All rights reserved.

Shingade S.G.,R C Patel Institute Of Pharmaceutical Education And Research | Bari S.B.,R C Patel Institute Of Pharmaceutical Education And Research
Medicinal Chemistry Research | Year: 2013

The Schiff's bases 3a-3h were synthesized by reacting substituted/ unsubstituted aromatic aldehydes 2a-2h with 1-(2-aminoethyl)-piperazine 1. A series of novel aryl-3-(2-piperazin-1-ylethyl)-1,3-thiazolidin-4-one 4a-4h and 3-chloro-1-{2-[4-(chloroacetyl)piperazin-1-yl]ethyl}-4-arylazetidin-2-one 5a-5h were synthesized from the Schiff's bases of 1-(2-aminoethyl)-piperazine 3a-3h. The structures of synthesized compounds were confirmed by analytical (C, H, and N) and spectral (FT-IR, 1H NMR, 13C NMR, and Mass) data. The compounds 4a-4h and 5a-5h were screened for antimicrobial activity. The compounds 4a, 4d, 4f, 4g, 5a, 5d, 5f, and 5g exhibited substantially significant antibacterial as well as antifungal activity. © 2012 Springer Science+Business Media, LLC.

Ige P.P.,R C Patel Institute Of Pharmaceutical Education And Research | Gattani S.G.,H R Patel Institute Of Pharmaceutical Education And Research
Archives of Pharmacal Research | Year: 2012

The aim of the current work was to design and develop matrix pellets of hydroxy propyl methyl cellulose K200M and microcrystalline cellulose in an admixture for a mucoadhesive gastroretentive drug delivery system. Pellets containing metformin hydrochloride (500 mg) were prepared by the pelletization technique using an extruder-spheronizer. Pellets were characterized by differential scanning calorimetry (DSC), x-ray diffraction (XRD), scanning electron microscopy (SEM), circularity, roundness, percent drug content, percent production yield, in vitro swelling, ex vivo mucoadhesion, in vitro drug release and in vivo x-ray imaging studies. Optimized pellets were sufficiently porous spheroids, free flowing, had smooth surfaces, had yields up to 75.45 ± 0.52% and had drug content up to 96.45 ± 0.19%. The average particle size of formulations MF2 and MF6 were 1.13 ± 0.41 mm and 1.22 ± 0.18 mm, respectively. Formulation MF6 exhibited strong adhesion, about 94.67%, to goat mucosal tissue, and the desired in vitro swelling, with a sustained drug release profile for 12 h and with retention in the upper small intestine of rabbits for 10 h. We conclude that hydroxy propyl methyl cellulose K200M and microcrystalline cellulose at a 2.80:1.00 w/w ratio could be an effective carrier for multiple unit controlled delivery of metformin hydrochloride.

Wagh V.D.,R C Patel Institute Of Pharmaceutical Education And Research
Advances in Pharmacological Sciences | Year: 2013

Propolis is a natural resinous mixture produced by honey bees from substances collected from parts of plants, buds, and exudates. Due to its waxy nature and mechanical properties, bees use propolis in the construction and repair of their hives for sealing openings and cracks and smoothing out the internal walls and as a protective barrier against external invaders like snakes, lizards, and so forth, or against weathering threats like wind and rain. Bees gather propolis from different plants, in the temperate climate zone mainly from poplar. Current antimicrobial applications of propolis include formulations for cold syndrome (upper respiratory tract infections, common cold, and flu-like infections), wound healing, treatment of burns, acne, herpes simplex and genitalis, and neurodermatitis. Worldwide propolis has a tremendous popularity, but in India the studies over propolis have just started, not extensively reported except few regions of India like Maharashtra, West Bengal, Tamil Nadu, Gujrat, and Madhya Pradesh. © 2013 Vijay D. Wagh.

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