Zia H, Rashed S F, Quadir M, Needham T E, Squillante E
Department of Pharmaceutics, College of Pharmacy, University of Rhode Island, Kingston, RI.
Int J Pharm Compd. 1998 Sep-Oct;2(5):390-3.
Ketorolac tromethamine suppositories (30 mg) and ketoprofen suppositories (50 mg) were made by the fusion method with various bases such as cocoa butter, Witepsol H15, Witepsol W25, Witepsol W35, Witepsol E75, Suppocire AML and Hydrokote AP5-1. Also, ketorolac tromethamine and ketoprofen suppositories were prepared using Eudragit L100 and propylene glycol. The release rates for both ketorolac tromethamine and ketoprofen suppositories in Sorensen's phosphate buffer pH 7.4 were determined and found to be: cocoa butter greater than Witepsol H15 greater than Witepsol W25 greater than Suppocire AML greater than witepsol W35 greater than Hydrokote AP5-1> Witepsol E75. Drug-release studies showed that ketorolac tromethamine demonstrates faster release profiles from these selected bases in comparison to those seen for ketoprofen. Analysis of the relaease kinetics for ketorolac tromethamine and ketoprofen from the various bases suggests that a combination of release mechanisms such as melting of the base followed by partititoning of the drug, along with some diffusion of the drug from the base to the dissolution media, seems to be operative in these systems. The absolute bioavailabilty of the suppository formulaion made with ketorolac tromethamine in cocoa butter base was found to be 61% in rabbits.
酮咯酸氨丁三醇栓剂（30毫克）和酮洛芬栓剂（50毫克）采用融合法，以可可脂、Witepsol H15、Witepsol W25、Witepsol W35、Witepsol E75、Suppocire AML和Hydrokote AP5 - 1等各种基质制成。此外，酮咯酸氨丁三醇和酮洛芬栓剂还使用了丙烯酸树脂L100和丙二醇制备。测定了酮咯酸氨丁三醇和酮洛芬栓剂在pH 7.4的索伦森磷酸盐缓冲液中的释放速率，结果发现：可可脂＞Witepsol H15＞Witepsol W25＞Suppocire AML＞Witepsol W35＞Hydrokote AP5 - 1＞Witepsol E75。药物释放研究表明，与酮洛芬相比，酮咯酸氨丁三醇从这些选定基质中的释放曲线更快。对酮咯酸氨丁三醇和酮洛芬从各种基质中的释放动力学分析表明，诸如基质熔化后药物分配，以及药物从基质向溶解介质的一些扩散等释放机制的组合，似乎在这些系统中起作用。在兔体内，以可可脂为基质制成的酮咯酸氨丁三醇栓剂配方的绝对生物利用度为61%。
