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美洛昔康在多孔硅酸钙上的吸附:表征与片剂配方

Adsorption of meloxicam on porous calcium silicate: characterization and tablet formulation.

作者信息

Sharma Sameer, Sher Praveen, Badve Shraddha, Pawar Atmaram P

机构信息

Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandawane, Pune-411038, Maharashtra State, India.

出版信息

AAPS PharmSciTech. 2005 Dec 7;6(4):E618-25. doi: 10.1208/pt060476.

Abstract

The purpose of the present study was characterization of microparticles obtained by adsorption of poorly water soluble drug, meloxicam, on a porous silicate carrier Florite RE (FLR) and development of a tablet formulation using these microparticles, with improved drug dissolution properties. The study also reveals the use of FLR as a pharmaceutical excipient. Meloxicam was adsorbed on the FLR in 2 proportions (1:1 and 1:3), by fast evaporation of solvent from drug solution containing dispersed FLR. Drug adsorbed FLR microparticles were evaluated for surface topography, thermal analysis, X-ray diffraction properties, infrared spectrum, residual solvent, micromeritic properties, drug content, solubility, and dissolution studies. Microparticles showed bulk density in the range of 0.10 to 0.12 g/cm(3). Dissolution of drug from microparticles containing 1:3, drug:FLR ratio was faster than microparticles containing 1:1, drug:FLR ratio. These microparticles were used for formulating directly compressible tablets. Prepared tablets were compared with a commercial tablet. All the prepared tablets showed acceptable mechanical properties. Disintegration time of prepared tablets was in the range of 18 to 38 seconds, and drug dissolution was much faster in both acidic and basic medium from prepared tablets as compared with commercial tablet. The results suggest that FLR provides a large surface area for drug adsorption and also that a reduction in crystallinity of drug occurs. Increase in surface area and reduction in drug crystallinity result in improved drug dissolution from microparticles.

摘要

本研究的目的是对通过将难溶性药物美洛昔康吸附在多孔硅酸盐载体Florite RE(FLR)上获得的微粒进行表征,并使用这些微粒开发具有改善药物溶解特性的片剂制剂。该研究还揭示了FLR作为药用辅料的用途。通过从含有分散FLR的药物溶液中快速蒸发溶剂,将美洛昔康以两种比例(1:1和1:3)吸附在FLR上。对吸附了药物的FLR微粒进行了表面形貌、热分析、X射线衍射特性、红外光谱、残留溶剂、粉体学特性、药物含量、溶解度和溶出度研究。微粒的堆密度在0.10至0.12 g/cm³范围内。药物与FLR比例为1:3的微粒中药物的溶出速度比药物与FLR比例为1:1的微粒快。这些微粒用于制备直接压片。将制备的片剂与市售片剂进行比较。所有制备的片剂均显示出可接受的机械性能。制备片剂的崩解时间在18至38秒范围内,与市售片剂相比,制备片剂在酸性和碱性介质中的药物溶出速度都快得多。结果表明,FLR为药物吸附提供了大的表面积,并且药物的结晶度降低。表面积的增加和药物结晶度的降低导致微粒中药物溶出度提高。

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