Muatlik S, Usha A N, Reddy M S, Ranjith A K, Pandey S
Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal 576104, Karnataka State, India.
Pak J Pharm Sci. 2007 Jul;20(3):218-26.
The objective of present study was to improve the solubility, dissolution rate, micromeritic properties and bioavailability of aceclofenac (NSAID) by formulating its spherical agglomerates. They were prepared with different water soluble polymers (polyvinylpyrrolidone-K30, polyvinylpyrrolidone-K90 and sodium alginate) by using acetone-water-dichloromethane solvent system. The agglomerates were subjected to various physicochemical properties, DSC, IR spectroscopy, scanning electron microscopy (SEM), micromeritic properties and dissolution studies. The in vivo studies (anti-inflammatory, analgesic and pharmacokinetic studies) were conducted in Wistar rats and Swiss albino mice. SEM studies showed that agglomerates were spherical in structure and formed by cluster of small crystals. The agglomerates prepared with polyvinylpyrrolidone-K90 exhibited improved solubility, dissolution rate and micromeritic properties compared to those prepared with other polymers and pure drug. These optimized agglomerates showed rapid analgesic and anti-inflammatory activity besides exhibiting improved bioavailability of drug when compared to pure drug.
本研究的目的是通过制备醋氯芬酸（一种非甾体抗炎药）的球形团聚物来提高其溶解度、溶出速率、粉体学性质和生物利用度。使用丙酮-水-二氯甲烷溶剂体系，将其与不同的水溶性聚合物（聚乙烯吡咯烷酮-K30、聚乙烯吡咯烷酮-K90和海藻酸钠）一起制备团聚物。对团聚物进行了各种物理化学性质、差示扫描量热法（DSC）、红外光谱（IR）、扫描电子显微镜（SEM）、粉体学性质和溶出度研究。在Wistar大鼠和瑞士白化小鼠中进行了体内研究（抗炎、镇痛和药代动力学研究）。SEM研究表明，团聚物呈球形结构，由小晶体簇形成。与用其他聚合物和纯药物制备的团聚物相比，用聚乙烯吡咯烷酮-K90制备的团聚物表现出更好的溶解度、溶出速率和粉体学性质。与纯药物相比，这些优化后的团聚物除了具有更高的药物生物利用度外，还表现出快速的镇痛和抗炎活性。
