己酮可可碱渗透泵控释片在家兔体内的药动学和相对生物利用度

The bioavilability and pharmacokinetics study of pentoxifylline osmotic pump controlled release tablets in rabbits

目的:研究家兔口服己酮可可碱渗透泵控释片的药动学和相对生物利用度,对体外释放和体内吸收的相关性做出评价。方法:家兔12只采用双周期交叉给药,用高效液相色谱法测定己酮可可碱的血药浓度,用3P87处理药动学参数进而计算相对生物利用度。Wanger-Nelson法计算体内吸收百分数,并与相应时间体外累积释放百分率线性回归。结果:己酮可可碱渗透泵控释片和己酮可可碱肠溶片在家兔体内过程均符合单室模型,其主要药动学参数分别为Tmax(3.41±0.7)和(1.36±0.26)h;Cmax(172.65±1.32)和(430.51±1.45)ng·mL-1;AUC0～∞(2264.74±3.1)和(2418.22±3.7)ng·h·mL-1;且体内外相关性较好。结论:己酮可可碱渗透泵控释片控释特征明显,生物利用度与市售肠溶片等效。

Objective：To study the pharmacokinetics and relative bioavilability of pentoxifylline osmotic pump controlled release tablets in rabbits,and investigate its in vitro and in vivo correlation.Methods：Twelve rabbits were divided into two groups by double crossing method.The pentoxifylline in plasma was measured by HPLC.The relative bioavilability and pharmacokinetic parameters of pentoxifylline osmotic pump controlled release tablets were computed by 3P 87,and the correlation was studied by in vitro dissolution and in vivo pharmacokinetics with Wanger-Nelson method.Results：The pharmacokinetic parameters of test and reference preparation for pentoxifylline are：Tmax（3.41±0.7）and（1.36±0.26）h;Cmax（172.65±1.32）and（430.51±1.45）ng·mL-1AUC0-∞（2264.74±3.1）and（2418.22±3.7）ng·h·mL^-1,respectively.Conclusion：Pentoxifylline osmotic pump controlled release tablets have marked controlled-release characters.The Pentoxifylline osmotic pump controlled release tablets and the PTX tablets are bioequivalent.