Ahn H J, Kim K M, Kim C K
College of Pharmacy, Seoul National University, Korea.
Drug Dev Ind Pharm. 1998 Jul;24(7):697-701. doi: 10.3109/03639049809082375.
To enhance the dissolution rate and bioavailability of poorly water-soluble ketoprofen, a novel oral dosage form of ketoprofen, termed ketoprofen dry elixir, was developed by the spray-drying technique. Ketoprofen, dextrin, and sodium lauryl sulfate were dissolved in an ethanol-water mixture (20:25 w/w) and thereafter spray-dried to form the ketoprofen dry elixir. Comparative studies on the in vitro dissolution and in vivo adsorption of ketoprofen in the form of dry elixir and powder were carried out. Ketoprofen in the dry elixir completely dissolved within 5 min. On the other hand, only about 50.1% of ketoprofen powder alone dissolved during 60 min. The initial dissolution rate of ketoprofen in the dry elixir markedly increased in distilled water at 37 degrees C, becoming fourfold higher than that of ketoprofen powder alone. The maximal plasma concentration of ketoprofen (Cmax) and the area under the concentration-time curve from zero to 8 hr (AUC0-8 hr) after the oral administration of dry elixir increased about 3.2- (24.6 versus 7.6 micrograms/ml) and 2.2-(38.4 versus 17.3 micrograms hr/ml) fold compared with powder alone. It was obvious that ketoprofen dry elixir might be a useful solid dosage form to improve the dissolution rate and bioavailability of poorly water-soluble ketoprofen.
为提高难溶性酮洛芬的溶出速率和生物利用度，采用喷雾干燥技术研发了一种新型酮洛芬口服剂型——酮洛芬干糖浆剂。将酮洛芬、糊精和十二烷基硫酸钠溶解于乙醇 - 水混合物（20:25 w/w）中，然后喷雾干燥制成酮洛芬干糖浆剂。对酮洛芬干糖浆剂和粉末形式的体外溶出和体内吸收进行了对比研究。酮洛芬干糖浆剂在5分钟内完全溶解。另一方面，单独的酮洛芬粉末在60分钟内仅约50.1%溶解。在37℃蒸馏水中，酮洛芬干糖浆剂的初始溶出速率显著提高，比单独的酮洛芬粉末高出四倍。口服干糖浆剂后，酮洛芬的最大血浆浓度（Cmax）和从零到8小时的浓度 - 时间曲线下面积（AUC0 - 8 hr）分别比单独的粉末增加了约3.2倍（24.6对7.6微克/毫升）和2.2倍（38.4对17.3微克·小时/毫升）。显然，酮洛芬干糖浆剂可能是一种有用的固体剂型，可提高难溶性酮洛芬的溶出速率和生物利用度。
