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STUDIES ON MICROCRYSTALS FOR IMPROVED DISSOLUTION OF MELOXICAM

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Author(s): Nagoba Shivappa N. | Purushotham Rao K. | Zakaullah S. | Pratima S.

Journal: International Research Journal of Pharmacy
ISSN 2230-8407

Volume: 2;
Issue: 11;
Start page: 136;
Date: 2011;
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Keywords: Meloxicam | Microcrystals | Dichloromethane | Ethyl Acetate & Chloroform.

ABSTRACT
Meloxicam is practically insoluble in water and its dissolution is the rate-limiting step for its absorption, which leads variable bioavailability. The aim of this investigation was to enhance the dissolution rate of Meloxicam by formation of microcrystals using solvent change method. Improved bioavailability is an added advantage for most of the poorly soluble drugs in water. In recent years research work is concentrated on various methods to improve the solubility characteristics of poorly soluble drugs and crystallization phenomenon is one among them. The solubility problem can be solved by changing the crystal habit of drug, which improves the solubility and dissolution. Crystallization is also a purification process to remove the impurities from pharmaceutical products by, recrystallization technique. So, in the present investigation an attempt has been made to improve the solubility characteristics of Meloxicam (NSAID’s) using crystallization method by solvent evaporation technique. To increase the therapeutic efficiency and quality of existing marketed dosage formulations. In this method, crystallization takes places mainly due to the removal of solvent by evaporation and reprecipitation in water in which drug is insoluble. The biphasic layer formed due to water immiscible solvent and is evaporated by maintaining the temperature above to corresponding boiling point of solvents. In our work three immiscible solvents, chloroform, ethyl acetate and dichloromethane used and microcrystals prepared under slow and turbulent stirring conditions. The precipitated crystals were filtered using whatmann paper and dried at 60° C for 1 hour. The formulated crystals of Meloxicam were subjected to various physico-chemical parameters like size distribution, shape and drug, solvent interactions with DSC, IR, XRD etc., and found to be smaller in size than pure and crystalline in nature with free from any interactions. For all the samples in-vitro drug release parameters studied U.S.P. XXIII dissolution rate test apparatus (Electrolab) employing paddle stirrer for one hour. In 900 ml phosphate buffer (pH 7.4) and compared with pure drug samples. The microcrystals produced with 30% v/v chloroform, 30% v/v dichloromethane and 30% v/v ethyl acetate as solvents prepared under turbulent stirring conditions precipitated in water as crystallization media found to be best formulations for improved drug dissolution when compared to the pure drug for Meloxicam respectively. The results thus conclusively proved that the method of precipitation by solvent evaporation technique can be used to produce microcrystals of poorly soluble non-steroidal anti-inflammatory drugs.
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