Nootan Pharmacy College

Visnagar, India

Nootan Pharmacy College

Visnagar, India
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Patel B.B.,Hemchandracharya North Gujarat University | Patel B.B.,Evonik Industries | Patel J.K.,Nootan Pharmacy College | Chakraborty S.,Evonik Industries | Shukla D.,Banaras Hindu University
Saudi Pharmaceutical Journal | Year: 2015

Poor solubility and bioavailability of an existing or newly synthesized drug always pose challenge in the development of efficient pharmaceutical formulation. Numerous technologies can be used to improve the solubility and among them amorphous solid dispersion based spray drying technology can be successfully useful for development of product from lab scale to commercial scale with a wide range of powder characteristics. Current review deals with the importance of spray drying technology in drug delivery, basically for solubility and bioavailability enhancement. Role of additives, selection of polymer, effect of process and formulation parameters, scale up optimization, and IVIVC have been covered to gain the interest of readers about the technology. Design of experiment (DoE) to optimize the spray drying process has been covered in the review. A lot more research work is required to evaluate spray drying as a technology for screening the right polymer for solid dispersion, especially to overcome the issue related to drug re-crystallization and to achieve a stable product both in vitro and in vivo. Based on the recent FDA recommendation, the need of the hour is also to adopt Quality by Design approach in the manufacturing process to carefully optimize the spray drying technology for its smooth transfer from lab scale to commercial scale. © 2013 King Saud University.

Pandya V.M.,Bspatel Pharmacy College | Patel J.K.,Nootan Pharmacy College | Patel D.J.,Shree Krishna Institute of Pharmacy
Dissolution Technologies | Year: 2011

Simvastatin is a poorly water-soluble drug, and bioavailability from its crystalline form is very low. The purpose of this investigation was to increase the solubility and dissolution rate of simvastatin by the preparation of nanosuspensions with Pluronic F127 and zirconium oxide (ZrO2) beads using a wet-milling technique at the laboratory scale. Prepared nanosuspensions were evaluated for particle size and in vitro dissolution. A 32 central composite design was employed to study the effect of the independent variables (i.e., amount of Pluronic F127, X1, and amount of ZrO2, X2) on the dependent variables (i.e., particle size [nm] and percentage of drug released after 10 min, Q10). The relationship between the dependent and independent variables was further elucidated using multiple liner regression analysis (MLRA) and contour plots. The results show that nanosuspensions prepared with the higher concentrations of Pluronic F127 and the higher quantities of ZrO2 (up to 8 g) reduced the particle size and enhanced the dissolution rate of the formulation. The dissolution rate of the optimized nanosuspension was enhanced (64% in 10 min) relative to that of a micronized suspension of simvastatin (3.5% in 10 min), mainly because of the formation of nanosized particles. These results show that the preparation of simvastatin-loaded nanosuspensions significantly improved the in vitro dissolution rate, thus possibly enhancing the fast onset of therapeutic drug effect.

Patel A.,Bhagwant University | Patel J.,Nootan pharmacy college
Der Pharmacia Lettre | Year: 2012

In present study, mucoadhesive vaginal tablet of sertaconazole was designed using a combination of mucoadhesive polymers like Carbopol 934P, chitosan, carboxymethylcellulose sodium, sodium alginate, methyl cellulose, hydroxypropyl methylcellulose and hydroxypropyl cellulose. Effervescent was incorporated into formulations to enhance swellabilty of mucoadhesive tablet. For various drug-free formulations, the effect of effervescent on polymers swelling characteristics was investigated. Swelling, mucoadhesive property and drug release study of the tablets with different proportions of mucoadhesive polymer and effervescent in formulations were conducted. A good sustained effect and moderate bioadhesion were obtained with the tablets containing 100 mg of effervescent, with Carbopol 934P: HPMC K4M ratio of 1:1 seemed to be the optimum one for the tablet. From the ex vivo retention study it was found that the mucoadhesive polymers hold the tablet for more than 24 hours inside the vaginal tube. Our study may provide a potential vaginal tablet formulation of sertaconazole against Candida albicans.

The purpose of this research was to formulate and systemically evaluate in vitro and in vivo performances of mucoadhesive amoxicillin microparticles for the potential use in the treatment of gastric and duodenal ulcers, which were associated with Helicobacter pylori. The chitosan/amoxicillin microparticles were successfully prepared in a process of solution-enhanced dispersion by supercritical CO 2 (SEDS). The morphological characteristics of the mucoadhesive microparticles were studied under scanning electron microscope. The resulted microparticles with mean sizes ranged from 1.0 and 2.5m had good mucoadhesive properties. In vitro and in vivo mucoadhesive tests showed that chitosan/amoxicillin mucoadhesive microparticles adhered more strongly to gastric mucous layer and could retain in gastrointestinal tract for an extended period of time. The X-Ray Powder Diffractometry and Differential Scanning Calorimetry analysis demonstrated that the SEDS process was a typical physical coating process to produce drug-polymer composite microparticles, which is favourable for drugs since there is no changes in chemistry. In vitro release test showed that amoxicillin released faster in pH 1.0 hydrochloric acid (HCl) than in pH 7.8 phosphate buffer. In vivo H. pylori clearance tests were also carried out by administering amoxicillin powder and mucoadhesive microparticles to H. pylori infectious Wistar rats under fed conditions at single dose or multiple dose(s) in oral administration. The results showed that amoxicillin mucoadhesive microparticles had a better clearance effect than amoxicillin powder. In conclusion, the prolonged gastrointestinal residence time and enhanced amoxicillin stability resulting from the mucoadhesive microparticles of amoxicillin might make a contribution to H. pylori complete eradication. © 2012 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted.

Gevariya H.B.,Dharmsinh Desai University | Patel J.K.,Nootan Pharmacy College
Current Drug Delivery | Year: 2013

Poor bioavailability and therapeutic response of conventional therapy due to many pre-corneal constraints necessitate the development of novel controlled and sustained ocular drug delivery to become a standard one in modern pharmaceutical era. This investigation aimed to study the drug release kinetics of betaxolol hydrochloride from a hydrophobic matrix system of PMMA cast with incorporating different proportions of polyethylene oxide (PEO) and evaluate its ability to improve ocular bioavailability and duration of action for the drug. Matrix type ocular inserts were prepared by the film casting technique and characterized in vitro by drug release studies using a flow through apparatus that simulated the eye conditions. All the formulations were subjected to physicochemical evaluation. Rabbit model with steroid induced glaucoma was used to establish in vivo efficacy of inserts. Polymer composition and concentration significantly affected the drug release based on change in diffusional path length and formation of gelaneous pores by polymer erosion. Formulations released the drug by non-fickian diffusion including anomalous transport (0.51). It was also observed that increasing the proportion of PEO in to PMMA does not affect the blend miscibility. IVIVC suggested no significant difference (P< 0.001) between in vitro and in vivo release of drug from inserts. In vivo IOP lowering activity was better for optimized insert F8 (for 24 h) as compared to eye drops (10 h). This ocular insert could be a promising once-a-day sustained release formulation for treating glaucoma. © 2013 Bentham Science Publishers.

Patel M.P.,Nootan Pharmacy College | Patel R.R.,Nootan Pharmacy College | Patel J.K.,Nootan Pharmacy College
Journal of Pharmacy and Pharmaceutical Sciences | Year: 2010

Chitosan has prompted the continuous movement for the development of safe and effective drug delivery systems because of its unique physicochemical and biological characteristics. The primary hydroxyl and amine groups located on the backbone of chitosan allow for chemical modification to control its physical properties. When the hydrophobic moiety is conjugated to a chitosan molecule, the resulting amphiphile may form self-assembled nanoparticles that can encapsulate a quantity of drugs and deliver them to a specific site of action. Chemical attachment of the drug to the chitosan throughout the functional linker may produce useful prodrugs, exhibiting the appropriate biological activity at the target site. Mucoadhesive and absorption enhancement properties of chitosan increase the in vivo residence time of the dosage form in the gastrointestinal tract and improve the bioavailability of various drugs. The main objective of this review is to provide an insight into various target-specific carriers, based on chitosan and its derivatives. The first part of the review is concerned with the organ-specific delivery system using chitosan and its derivatives. The subsequent section considers the recent developments of drug delivery carriers for cancer therapy with special focus on various targeting strategies.

Patel R.,Jodhpur National University | Patel J.,Nootan Pharmacy College
Acta Pharmaceutica | Year: 2011

In situ forming intragastric controlled-release formulation is a new technology in the field of oral controlled-release delivery systems. The objective of this study was to develop formulations that can control drug release up to 24 hours. In addition, a combination of appropriate polymers and solvents was selected that could form a drug loaded gel at the process temperature of 60-70 °C, which gel could turn into a rigid mass upon exposure to dissolution fluid at body temperature. The drug release mechanism from this rigid mass was controlled by different formulation factors such as different polymer grades, polymer concentrations, hydrophobicity or hydrophilicity of solvents, different drug loadings, and physicochemical properties of additional excipients. After evaluating different formulation factors, Ethocel 10 FP and triethyl citrate were selected for further studies using hydrochlorothiazide as a model drug. Polynomial correlation between viscosity of the blank gel and drug release profile was also obtained.

Patel N.,Anand Pharmacy College | Patel J.,Nootan Pharmacy College | Shah S.,L J Institute Of Pharmacy
Acta Pharmaceutica | Year: 2010

The aim of this study was to investigate the combined influence of 3 independent variables in the compression coated tablet of mesalamine for ulcerative colitis. A 3-factor, 3-level Box-Behnken design was used to derive a second order polynomial equation and construct contour plots to predict responses. The independent variables selected were: percentage of polymers (pectin and compritol ATO 888) in compression coating (X1), coating mass (X2) and coating force (X3). Fifteen batches were prepared and evaluated for percent of drug released in 5 h (Y5), time required for 50 % mesalamine to dissolve (t50) with rat cecal (RC) content and without rat cecal content (t50), percent of drug released in 24 h in the presence of rat cecal content (Y24 with RC). Transformed values of independent and dependent variables were subjected to multiple regressions to establish a full-model second-order polynomial equation. F was calculated to confirm the omission of insignificant terms from the full-model equation. The computer optimization process and contour plots predicted the levels of independent variables X1, X2, and X3 (0, 0.2 and -0.15, respectively) for colon targeting and total percent of drug released up to 24 h.

The mucoadhesive microparticles (CHCNZ) composed of chitosan (CH) and cinnarizine (CNZ) hydrochloride were successfully prepared, in a process of solution-enhanced dispersion, by supercritical CO2 (SEDS) technique. Scanning electron microscopy was used to reveal the morphological characteristics of mucoadhesive microparticles. The average particle size of microparticles was in the range from 1.9 to 12.8 μm. In vitro and in vivo mucoadhesive tests showed that CHCNZ mucoadhesive microparticles adhered more strongly to gastric mucous layer. Thereby retaining in gastrointestinal tract for an extended period of time and exhibiting good mucoadhesive properties. The X-ray powder diffractometry and differential scanning calorimetry analysis demonstrated that the SEDS process was an efficient physical coating process to produce CHCNZ composite microparticles. It also suggests that CNZ did not undergo chemical changes during the production of microparticles. The optimized batch exhibited a high drug entrapment efficiency of 67% with particle size of 3.9 μm. A sustained pattern of drug release was obtained for more than 20 h. In vivo studies were carried out by administering orally cinnarizine HCl (CNZ) suspension and mucoadhesive microparticles to rabbits under fasted (for 12 h) conditions. The results showed that CNZ mucoadhesive microparticles had a better bioavailability than CNZ suspension due to longer retention in the gastric environment of the test animals.

Deshmukh A.B.,Shankersinh Vaghela Bapu Institute of Pharmacy | Patel M.C.,Shankersinh Vaghela Bapu Institute of Pharmacy | Mishra B.,Nootan Pharmacy College
Renal Failure | Year: 2013

The role of the kidney in glucose homeostasis and the potential of the kidney as a therapeutic target in type 2 diabetes is little appreciated. Hyperglycemia is an important pathogenic component in the development of microvascular and macrovascular complications in type 2 diabetes mellitus. Inhibition of renal tubular glucose re-absorption that leads to glycosuria has been proposed as a new mechanism to attain normoglycemia and thus prevent and diminish these complications, thus representing an innovative therapeutic strategy for the treatment of hyperglycemia and/or obesity in patients with type 1 or type 2 diabetes by enhancing glucose and energy loss through the urine. Sodium glucose co-transporter 2 (SGLT2) has a key role in re-absorption of glucose in kidney. Competitive inhibitors of SGLT2 have been discovered and a few of them have also been advanced in clinical trials for the treatment of diabetes. Copyrigh © Informa Healthcare USA, Inc.

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