文章基本信息

标题：PLGA Implant Tablet of Ketoprofen: Comparison of in Vitro and in Vivo Releases
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作者：Hiraku Onishi ; Mari Takahashi ; Yoshiharu Machida 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2005
卷号：28
期号：10
页码：2011-2015
DOI：10.1248/bpb.28.2011
出版社：The Pharmaceutical Society of Japan
摘要：An implant tablet of ketoprofen (KP) was developed in order to achieve its sustained supply for approximately one week, and its release was evaluated in vitro and in vivo . Implant tablets (30 mg) containing 1 and 5 mg of ketoprofen, prepared using poly( DL -lactic acid-co-glycolic acid) copolymer (PLGA; MW 10000; lactic acid : glycolic acid = 1 : 1 (mol/mol)) as a matrix, exhibited similar week-long sustained release in vitro . Plasma concentration was monitored after the implant tablet (5 mg of KP) and a KP solution (0.5 mg of KP) were administered subcutaneously to rats, and in vivo release rate was analyzed by deconvolution. The release rate from the implant tablet was faster in vivo than in vitro in the initial phase, but much lower in vivo than in vitro in the later phase. The plasma level decreased to the level less than the minimal effective concentration at 96 h after administration. However, the calculated plasma concentration given by convolution based on in vitro release rate was more than 7 times greater than the minimal effective concentration even at 96 h after administration. As the implant displayed the discrepancy between in vitro and in vivo release rates, the improvement of the in vivo release rate is required.
关键词：implant tablet;in vitro release;in vivo release;ketoprofen;poly( DL -lactic acid-co-glycolic acid) copolymer (PLGA)