家兔多剂量口服溴吡斯的明缓释片的药动学和生物利用度评价

目的 以溴吡斯的明普通片为对照，通过多剂量口服给药后，评价溴吡斯的明缓释片的药动学和生物利用。方法 6只新西兰兔随机分成2组，采用自身交叉对照实验，多剂量口服溴吡斯的明缓释制片或普通片后，采用高效液相色谱法测定血浆中溴吡斯的明浓度，计算药动学参数和相对生物利用度。 结果 溴吡斯的明普通片与缓释片给药后，药动学参数如下：tmax分别为（2.00 ± 0）h和（4.00 ± 0）h； Cmax 分别为（25.477 ± 0.177）mg•L-1和（19.236 ± 0.446）mg•L-1；AUC0-∞分别为（321.424 ± 4.955）mg•h•L-1和（370.083 ± 12.229）mg•h•L-1；与普通片相比，缓释片的相对生物利用度为119.15%。结论 溴吡斯的明缓释片具有缓释动力学特征，与普通片生物等效。

Pharmacokinetics and relative bioavailability study of multiple oral doses of pyridostigmine bromide sustained-release tablets in rabbits

Objective To evaluate the pharmacokinetics and the relative bioavailability of pyridostigmine bromide sustained-release tablets(PBSTs) by comparing with the conventional tablets using a multiple-dose design. Methods Six rabbits were randomly divided into 2 groups and were assigned to a self crossover design.The plasma pyridostigmine bromide concentration was determined by high-performance liquid chromatography as multiple oral dose of PBSTs(90 mg each time,and twice a day) or conventional tablets(60 mg each time,three times a day).The pharmacokinetic parameters and relative bioavailability were calculated.Results A two-compartment model was used to describe the in vivo behavior of PBSTs after oral administration.The main pharmacokinetic parameters for conventional tablets and multiple oral dose of PBSTs were calculated as the follows: tmax(2.00±0) and(4.00±0) h;Cmax(25.48±0.18) mg/L and(19.24±0.45) mg/L;AUC0-∞(321.42±5.00) mg·h·L-1 and(370.08±12.23) mg·h·L-1.The relative bioavailability of the sustained-release tablets was 119.15% compared with the conventional tablets. Conclusion PBSTs has the property of sustained-relsease and is bioequivalent to the conventional tablets.