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目的研究外消旋体酮洛芬(rac-Ket)在酸性释放介质中的立体选择性释放行为。方法以专属性的手性HPLC考察酮洛芬可注射植入剂在pH 2.5释放介质中的对映体选择性释放行为。结果体外释放实验结果表明,以可生物降解的乳酸-乙醇酸共聚物(D,L-PLG)为载体制成的外消旋体酮洛芬可注射植入剂,在pH 2.5的酸性释放介质中可维持约2.5月的缓慢释放。从立体选择性的角度观察,S(-+)-Ket的释放略快于R(--)-Ket,S/R-Ket的比值在1.01~1.03之间,但经独立样本的t检验,认为这种差异没有显著性(P>0.05)。这与我们过去以pH 7.4为介质的对映体释放结果不同,显示载体D,L-PLG在不同pH条件下的降解方式可能影响对映体的释放行为。结论与在pH 7.4释放介质中的研究结果不同,7%rac-Ket可注射植入剂在酸性条件下(pH 2.5)的对映体释放缺少选择性。
Objective To study the stereoselective release behavior of rac-Ket in acid release media. Methods Chiral HPLC was used to investigate the enantioselective release behavior of ketoprofen injectable implants in pH 2.5 release medium. Results The results of in vitro release experiments showed that racemic ketoprofen injectable implant made of biodegradable lactic acid-glycolic acid copolymer (D, L-PLG) In about 2.5 months to maintain a slow release. From stereoselectivity, the release of S (- +) - Ket was slightly faster than that of R (-) - Ket with the ratio of S / R-Ket between 1.01 and 1.03. This difference was not considered significant (P> 0.05). This is in contrast to our previous release of enantiomers at pH 7.4, indicating that degradation of the carrier D, L-PLG at different pH levels may affect the enantiomeric release behavior. Conclusions Unlike the findings in media release at pH 7.4, the 7% rac-Ket injectable implants lack selectivity of enantiomeric release under acidic conditions (pH 2.5).