头孢氨苄缓释片的研制

Development of Cefalexin Sustained-Release Tablets

目的:制备头孢氨苄缓释片,通过溶出度试验研究其生物利用度和药代动力学。方法:EudragitⅡ和HPMC作为缓释材料制备头孢氨苄缓释片,并与日本进口头孢氨苄缓释片(Syncl SR tablets)进行了体外释放度比较。结果:本制备品与进口片溶出结果相似,经人体生物利用度研究表明,头孢氨苄缓释片比普通胶囊口服后能明显推迟达峰时间,并降低峰浓度(P<0.01),缓释片与普通胶囊的AUC_(0→24)之间没有显著性差异(P>0.05)。缓释片相对于普通胶囊生物利用度为(104.90±8.35)％。结论:体内和体外实验结果表明本品达到预期效果。

AIM: The aim is to prepare Cefalexin sustained-release (SR) tablets, to study its dissolution rate in vitro and to investigate its bioavailability and pharmacokinetics in aim. METHODS Eudragit II and HPMC were used as disintegrating agent to prepare SR tablet. The dissolution rate of Cefalexin SR tablet was investigated, compared with that of the Syncl SR tablets. The bioavailability and pharmacokinetics of SR tablets using Cefalexin conventional capsules as the reference were evaluated. RESULTS; Drug release from the SR tablets prepared was similar to that of the Syncl SR tablets. It was found that the mean Cmax for the SR tablets was significantly lower than that for the conventional tablets and the mean Tmax was significantly later for the SR tablets. The AUC0→24 was not significantly different between the two formulations(P>0. 05) ;the relative bioavailability of Cefalexin SR tablets to conventional capsule was(104. 90 ±8. 35)%. CONCLUSION: Through in vitro and in invo tests, the results showed that Cefalexin SR tablets prepared has reached the anticipated objective.