摘要
目的 :用固体分散技术制得无环鸟苷胶囊剂以提高无环鸟苷体外溶出度和体内生物利用度。方法 :8名HBsAg阳性受试者分别单次口服 40 0mg两种剂型后 ,用HPLC方法测定血清中无环鸟苷浓度 ,进行固体分散无环鸟苷胶囊剂与市售片剂的药代动力学和生物利用度研究。结果 :两剂型血清药物浓度有显著差异 ,曲线下面积(AUC)固体分散无环鸟苷胶囊剂为 6 2 71 33h·ng·mL-1,市售片为 410 1 0 0h·ng·mL-1。固体分散无环鸟苷胶囊剂相对市售片剂的相对生物利用度为 15 2 92 %。 30min溶出度在不同的溶出介质中固体分散无环鸟苷胶囊剂也明显快于市售片剂。结论 :经固体分散的无环鸟苷胶囊剂能显著地提高无环鸟苷的生物利用度。
AIM: To evaluate the bioavailability of aciclovir (ACV) capsule prepared by the method of solid dispersion. METHODS: A single oral dose of aciclovir capsule or tablet was administrated to HBsAg positive patients randomly and their serum aciclovir concentrations were determined by HPLC. The dissolution rates of capsule and tablet were investigated by in vitro method. RESULTS: The areas under curve (AUC) of aciclovir capsules and tablets were 6271 33 h·ng·mL -1 and 4101 00 h·ng·mL -1 , respectively. The cumulative release of aciclovir capsule was significantly higher (84 63%) than that of tablets (2 08%) within 30 minutes. CONCLUSION: The bioavailability and dissolution of rates of aciclovir capsule made with the method of solid dispersion method were higher than those of aciclovir tablet.
出处
《药学学报》
CAS
CSCD
北大核心
2000年第4期301-304,共4页
Acta Pharmaceutica Sinica
