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Visnagar, India

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.

Joshi H.V.,Jodhpur National University | Patel J.K.,Nootan Pharmacy College
Journal of Applied Pharmaceutical Science | Year: 2011

Two simple, accurate, precise, reproducible, requiring no prior separation and economical procedures for simultaneous estimation of Amlodipine besylate (AML) and Lisinopril (LIS) in tablet dosage form have been developed. First method is simultaneous equation method; in this method 360.0 nm and 248.0 nm were selected to measure the absorbance of drugs at both wavelengths. The second method is Q-value analysis based on measurement of absorptivity at 300.0 nm (as an iso-absorptive point) and 360.0 nm. AMD and LIS at maximum wavelength of AML, 360.0 nm and at isoabsorptive point 300.0 nm shows linearity in a concentration range of 5- 40 μg/mL. Recovery studies range from >99.82% for AMD and >98.09% for LIS in case of simultaneous equation method and >100% for AMD and >98.45% for LIS in case of Q-analysis method confirming the accuracy of the proposed method. The proposed methods are recommended for routine analysis since it is rapid, simple, accurate and also sensitive and specific (no heating and no organic solvent extraction is required).

Patel B.B.,Hemchandracharya North Gujarat University | Patel B.B.,Evonik Industries | Patel J.K.,Nootan Pharmacy College | Chakraborty S.,Evonik Industries
Recent Patents on Drug Delivery and Formulation | Year: 2014

Spray drying has always remained an energetic field of innovation in pharmaceutical, food and flavor industry since last couple of decades. The current communication embodies an in-depth application of spray drying in pulmonary drug delivery for production of uniform and respirable size particles suitable for nebulizers, dry powder inhalers (DPI) and pressurized metered dose inhalers (pMDI). The review also highlights spray drying application in the manufacturing of mucoadhesive formulation suitable for nasal cavities to improve the drug absorption and bioavailability. Recent research works and patents filed by various researchers on spray drying technology for solubility enhancement have also been accentuated. Benefits of spray drying in production of dry flavorings to meet a product with maximum yield and least flavor loss are also discussed. The use of spray drying in production of various food products like milk or soymilk powder, tomato pulp, dry fruit juice etc, and in encapsulation of vegetable oil or fish oil and dry creamer has been discussed. Current review also highlights the application of spray drying in the biotechnology field like production of dry influenza or measles vaccine as well as application in ceramic industry. Spray drying based patents issued by the U.S. Patent and Trademark Office in the area of drug delivery have also been included in the current review to emphasize importance of spray drying in the recent research scenario. © 2014 Bentham Science Publishers.

Patel J.K.,Nootan Pharmacy College | Sutariya V.B.,University of South Florida
Journal of Microencapsulation | Year: 2015

Micronisation of simvastatin dissolved in acetone, dimethyl sulfoxide and ethanol with supercritical carbon dioxide as antisolvent was successfully performed using a supercritical antisolvent technique. The effect of a few process parameters such as precipitation temperature, the pressure and solute concentration in the liquid solution has been studied to evaluate their influence on morphology and size of particles. The micronised simvastatin were evaluated for drug content, particle size analysis and in vitro dissolution profiles. Fourier transform infrared spectroscopy, differential scanning calorimetry and PXRD patterns was used to study the possible changes after micronisation of simvastatin. The dissolution rate was increased after micronised compared with pure simvastatin in distilled water, pH 1.2 buffer and pH 7.0 buffer. In vivo performance of the optimised formulation was evaluated in rats using pharmacodynamic marker parameters like serum total cholesterol (CH) and triglycerides (TG) for 21 days. Pharmacodynamic studies of micronised simvastatin revealed improved reduction in CH and TG values as compared with pure simvastatin indicating improved bioavailability. In vivo pharmacokinetics in rats showed an increase in bioavailability of micronised simvastatin (3.14 times) compared with plain simvastatin. © 2014 Informa UK Ltd. All rights reserved: reproduction in whole or part not permitted.

Patel J.,Nootan Pharmacy College | Patel D.,Ganpat University | Raval J.,Ganpat University
Iranian Journal of Pharmaceutical Research | Year: 2010

The purpose of this research was to formulate and systemically evaluate in-vitro and in-vivo performances of mucoadhesive propranolol hydrochloride microspheres for its potential use in the treatment of hypertension, myocardial infraction and cardiac arrhythmias. Propranolol hydrochloride mucoadhesive microspheres, containing carbopol-934P as mucoadhesive polymer and ethyl cellulose as carrier polymer, were prepared by an emulsion-solvent evaporation technique. Results of preliminary trials indicated that the quantity of emulsifying agent, time for stirring, drug-to-polymers ratio, and speed of rotation affected various characteristics of microspheres. Microspheres were discrete, spherical, free-flowing and showed a good percentage of drug entrapment efficiency. An in-vitro mucoadhesive test showed that propranolol hydrochloride mucoadhesive microspheres adhered more strongly to the gastric mucous layer and could be retained in the gastrointestinal tract for an extended period of time. A 32 full factorial design was employed to study the effect of independent variables, drug-to-polymer-to-polymer ratio (propranolol hydrochloride-ethyl cellulose-carbopol-934P) (X 1), and stirring speed (X 2) on dependent variables, i.e. percentage of mucoadhesion, drug entrapment efficiency, particle size and t 80. The best batch exhibited a high drug entrapment efficiency of 54 %; 82% mucoadhesion after 1 h and particle size of 110 μm. A sustained pattern of drug release was obtained for more than 12 h. The drug-to-polymer-to-polymer ratio had a more significant effect on the dependent variables. The morphological characteristics of the mucoadhesive microspheres were studied under a scanning electron microscope. In-vivo evaluation studies on propranolol hydrochloride mucoadhesive microspheres and propranolol hydrochloride powder were performed on normal healthy rabbits. The results showed a sustained anti-hypertensive effect over a longer period of time in case of mucoadhesive microspheres, compared to the powder. In conclusion, the prolonged gastrointestinal residence time and slow release of propranolol hydrochloride resulting from the mucoadhesive microspheres, could contribute to the provision of a sustained anti-hypertensive effect. © 2010 by School of Pharmacy Shaheed Beheshti University of Medical Sciences and Health Services.

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