尼莫地平缓释胶囊相对生物利用度的研究  

Relative Bioavailability of Nimodipine Sustained-Release Capsules in Healthy Volunteers

作　　者：丁晨光[1] 刘雅伶[1] 陈雨安[1] 贺蕊[1] 高莹[1] 

机构地区：[1]解放军大连医学高等专科学校,大连116017

出　　处：《中国临床药理学杂志》2000年第1期46-48,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：１２例健康志愿者随机交叉口服进口尼莫地平普通片和尼莫地平缓释胶囊６０ｍｇ后，利用高效液相色谱法测定血药浓度并对其生物利用度进行了研究。尼莫地平缓释胶囊和进口片的Ｔ_ １／２。分别为３．７４± ０．８４ ｈ和１．９８± ０．５９ ｈ；Ｃ_ｍａｘ分别为２５．４１±９．３２μｇ Ｌ~－１和８０．０８±１６．６５ μｇ·Ｌ~－１；Ｔ_ｍａｘ分别为３．２５±０．９７ ｈ和０．７５±０．２１ｈ；Ａ ＵＣ分别为 １６７．４±２７．３ μｇ· ｈ· Ｌ~ －１和１９４．７± ２９．７μｇ· ｈ· Ｌ~－１；缓释胶囊的相对生物利用度为 ８７．０７％ ± ９．１９％。 ８例健康志愿者随机交叉多剂量口服尼莫地平缓释胶囊（６０ ｍｇ，ｂｉｄ）和尼莫地平普通片（３０ ｍｇ，ｑｉｄ），达稳态时测得峰浓度分别为２５．８１± ７．１２ μｇ· Ｌ~ －１和 ４１．２１± １０．０４ μｇ· Ｌ~－１；谷浓度分别为 ７．１９ ±１．８４ μｇ· Ｌ~－１和５．５９ ±１． ６２ μｇ·Ｌ~－１；两者血药浓度的波动系数分别为１．１２ ± ０．１６和１．５１± ０．１７。A single and multiple oral dose of Nimodipine conventional tablets and sustainedrelease capsule were given to 12 healthy volunteers in a randomized crossover study. The drug concentration in plasma and relative bioavailability were determined by HPLC. After a single oral dose 60mg, T_1/2 were 3.74 ± 0.84h and l.98 ± 0.59h; C_max were 25.41 ± 9.32 ug·L^-l and 80.08 ± 16.65 ug·L^-1; T_max were 3.25 ± 0.97h and 0.75 ± 0.2lh, AUC were 167.4 ± 27.3 ug· h· L^-1 and 194.7 ± 29.7ug·h·L^-l for sustained-relase capsules and conventional tablets respectively. The relative bioavailability of sustained-release capsules was 87.07 ± 9. 19%. Following multiple dosing, the mean steady state C_max. were 25.81 ± 7.12u·L^-l and 41.21 ± 10.04　ug· L^-l; C_min were 7.19 ± l.84 ug· L^-1 and 5.59 ± 1 .62ug·L^-1, The peak-to-through fluctuation index (FI) for the two formulations were 1.12 ± 0.16 and l.51 ± 0.17 respectively.

关 键 词：缓释胶囊 尼莫地平 生物利用度 血药浓度 药代动力学 

分 类 号：R969.1[医药卫生—药理学] R972[医药卫生—药学]