Goto S, Kawata M, Nakamura M, Nagatsuma Y, Fujinaga K, Aoyama T
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
J Microencapsul. 1988 Oct-Dec;5(4):343-60. doi: 10.3109/02652048809036732.
Eudragit RS, RS-RL, RL and S microcapsules containing ketoprofen were prepared by the solvent evaporation process in oil phase. The sustained release effect of these microcapsules and Oruvail, the representative commercial product of ketoprofen, was evaluated by the pH shift dissolution method and in beagle dogs, respectively. The dissolution patterns of ketoprofen from Eudragit RS, RS-RL and RL microcapsules were independent of the pH of the dissolution medium, and its dissolution rate increased with increasing content of ketoprofen in microcapsules. But the dissolution pattern of ketoprofen from Eudragit S microcapsules and Oruvail was found to depend on the pH of the dissolution medium. The rank order of the dissolution rate of ketoprofen from Eudragit RS, RS-RL and RL microcapsules containing 30 and 40 per cent (w/w) ketoprofen was sufficiently clear as to enable prediction of the relative bioavailability of ketoprofen from these microcapsules. In vivo evaluation using beagle dogs, sustained release effects of Eudragit RL and Eudragit S microcapsules containing 30 per cent (w/w) ketoprofen and Eudragit RS-RL microcapsules containing 40 per cent (w/w) ketoprofen were almost the same as or slightly superior to that of Oruvail.
采用油相溶剂蒸发法制备了含酮洛芬的Eudragit RS、RS-RL、RL和S型微胶囊。分别通过pH值改变溶出法和在比格犬体内对这些微胶囊以及酮洛芬的代表性商业产品奥鲁维(Oruvail)的缓释效果进行了评估。酮洛芬从Eudragit RS、RS-RL和RL型微胶囊中的溶出模式与溶出介质的pH值无关,且其溶出速率随微胶囊中酮洛芬含量的增加而提高。但发现酮洛芬从Eudragit S型微胶囊和奥鲁维中的溶出模式取决于溶出介质的pH值。含30%和40%(w/w)酮洛芬的Eudragit RS、RS-RL和RL型微胶囊中酮洛芬的溶出速率排序足够清晰,从而能够预测这些微胶囊中酮洛芬的相对生物利用度。使用比格犬进行的体内评估表明,含30%(w/w)酮洛芬的Eudragit RL和Eudragit S型微胶囊以及含40%(w/w)酮洛芬的Eudragit RS-RL型微胶囊的缓释效果与奥鲁维几乎相同或略优于奥鲁维。