尼莫地平缓释胶囊生物利用度和药代动力学研究

Studies on the pharmacokinetics and relative bioavailability of nimodipine sustained release capsules in volunteers

目的 研究尼莫地平缓释胶囊在 12名健康受试者中的生物利用度和药代动力学。方法 采用HPLC检测血浆中尼莫地平含量 ,用 3P87软件求药代动力学参数。结果 血浆中尼莫地平回收率大于 90 % ,线性范围为 1.2 5～ 15 0ng·ml-1;单剂量口服缓释胶囊的MRT ,消除和吸收半衰期等均显著大于普通片 (P <0 .0 1) ,AUC为 (94.6± 13.4) % (82 %～ 118% ) ;多剂量口服缓释胶囊和普通片 ,波动系数分别为 (1.6 76± 0 .186 )和 (1.75 1± 0 .15 0 )。结论 尼莫地平缓释胶囊缓释效果明显 ,吸收程度与普通片等效。

OBJECTIVE To study the pharmacokinetics and relative bioavailability of nimodipine sustained release capsules(NSC) in 12 volunteers.METHODS An HPLC assay was employed for the determination of nimodipine in plasma. The pharmacokinetic data was obtained by 3P87 software. RESULTS The recovery of nimodipine from plasma was more than 90%.The linearity was obtained over the range of 1.25～150ng·ml -1 .The pharmacokinetic results showed that the MRT, t 1/2 (K) and t 1/2 (Ka) of NSC were more than that of conventional tablets( P <0.01). The relative bioavailubility of NSC was (94.6±13.4)%(82.0%～118%) after single oral admistration. The fluctuation index of the capsules and the tablets were (1.676±0.186) and (1.751±0.150) respectively after multiple oral administration.CONCLUSION The NSC really had a prolonged effect. The sustained release capsules and the conventional tablets of nimodipine were equivalent in absorption.