阿昔洛韦复乳的研究:大鼠吸收动力学、生物利用度和趋肝性

目的:研究阿昔洛韦(ACV) 复乳的口服生物利用度和肝靶向性。方法:采用高效液相色谱法测定大鼠口服ACV 复乳和普通片剂后的血药浓度和肝组织分布,对试验数据进行药动学分析。药物浓度对时间数据作房室模型和统计矩解析,并求出相应的药动学参数。结果:大鼠口服ACV 复乳对片剂的相对生物利用度为149-8 % ,达峰时间和血浓维持时间明显延迟。血浓经时过程符合二室开放线性药动学模型。血浓峰值附近的肝组织药物分布是片剂的1-62 倍(P<0.1) ,谷值附近是片剂的5-16 倍(P<0.05) 。结论:大鼠口服ACV 复乳可提高生物利用度,并有一定的肝靶向性。

STUDIES ON ACYCLOVIR MULTIPLE EMULSION: ABSORPTION KINETICS, BIOAVAILABILITY AND HEPATIC TARGETING

AIM: To study the oral bioavailability and hepatic targeting of acyclovir (ACV) multiple emulsion in Sprague Dauley (SD) rats. METHODS: HPLC was testified as a potential method in assaying the concentration of ACV in plasma and tissue in rats after oral administration of multiple emulsion and tablet. Analysis of the data was executed by compartmental model and statistical moment calculation from which pharmacokinetic parameters were obtained. RESULTS: The relative availability of multiple emulsion to tablet was 149 8%. The t max and maitaining time for ACV concentration in plasma were both delayed. The profile of the plasma concentration to time curve was fitted perfectly to two compartment open model. The hepatic drug distribution of multiple emulsion near the peak concentration was 1 62 folds that of the tablet ( P <0 1), and the counterpart trough value was 4 16 folds bigger than tablet ( P <0 05). CONCLUSION: Multiple emulsion administered orally to rats improved the relative bioavailability of the drug ACV and showed hepatic targeting nature to some extent in rats.