己酮可可碱缓释胶囊在家兔体内的药动学研究

STUDY ON THE PHARMACOKINETICS OF PENTOXIFYLLINE MODIFIED RELEASE CAPSULE IN RABBITS

目的:研究己酮可可碱缓释胶囊在家兔体内的药动学与生物利用度。方法:10只健康家兔随机分为两组,每组5只,单剂量分别给予己酮可可碱肠溶片和缓释胶囊200mg,采用高效液相色谱法测定其血药浓度,比较己酮可可碱肠溶片和缓释胶囊的生物利用度与药动学参数的差异。结果:给药后,血药浓度变化符合一室模型,己酮可可碱肠溶片和缓释胶囊的T1/2分别为(1．608±0．534)h和(4．187±0．617)h;肠溶片的AUC0-∞、Cmax和Tmax分别为(2018．59±161．70)ng／ml／h、383．39ng／ml、1．012h;缓释胶囊的AUC0-∞、Cmax和Tmax分别为(2338．6±241．70)ng／ml／h、177．61ng／ml、3．37h。以肠溶片为参比制剂,缓释胶囊的生物利用度为110．81％。结论:己酮可可碱缓释胶囊在家兔体内表现出较好的缓释特性,其生物利用度明显高于肠溶片。

Objective：To study the pharmacokinetics and the bioavailability of pentoxifylline modified release capsule in rabbits.Methods： 10 healthy rabbits were divided into 2 groups at random, and were given pentoxifylline enteric-coated tablets and modified release capsule respectively.The pentoxifylline concentration in blood were determined by HPLC.The pharmacokinetics parameters and the relative bioavailability were measured and compared between pentoxifylline enteric-coated tablets and modified release capsule.Results：A one-compartment open model with first-order absorption kinetics best fitted the concentration-time data.The T1/2, AUC0-∞, Cmax and Tmax of pentoxifylline enteric-coated tablets were（1.608 ± 0.534）h,（2018.59 ± 161.70）ng/ml/h,383.39ng/ml and 1.102h;those of modified release capsule were（4.187 ± 0.617）h,（2338.6 ± 241.70）ng/ml/h, 177.61ng/ml and 3.37h respectively.The relative bioavailability of pentoxifylline modified release capsule was 110.81% compared with pentoxifylline enteric-coated tablets. Conclusions：Pentoxifylline modified release capsule has satisfactory properties in slow release of drug and has much higher bioavailability than pentoxifylline enteric-coated tables.