摘要
目的研究尼索地平口腔崩解片和普通片在健康志愿者体内的生物等效性。方法 20例男性健康志愿者,随机交叉口服尼索地平口腔崩解片10 mg和普通片10 mg,间隔7 d。用高效液相色谱串联质谱法测定血浆中尼索地平的血药浓度,计算主要药动学参数。结果尼索地平口腔崩解片和普通片中尼索地平的tmax分别为(1.50±0.40)h和(1.43±0.49)h,ρmax分别为(1 252.5±918.6)ng·L-1和(1 240.6±757.7)ng·L-1,t1/2分别为(8.07±2.00)h和(8.77±2.46)h,AUC0-t分别为(5 505.3±3 398.3)ng·h·L-1和(4 781.1±2 102.8)ng·h·L-1,AUC0-∞分别为(6 053.0±3 603.8)ng·h·L-1和(5 413.6±2 388.3)ng·h·L-1。以AUC0-t计算,尼索地平口腔崩解片的相对生物利用度为(113.1±31.3)%。两种片剂的药动学参数均无显著差异(P>0.05)。结论尼索地平口腔崩解片和普通片在健康人体内具有生物等效性。
AIM To investigate the bioequivalence of orally disintegrating tablets and normal tablets of nisoldipine in healthy volunteers. METHODS A single oral dose of nisoldipine orally disintegrating tablets 10 mg and normal tablets 10 mg were administered to 20 healthy volunteers in an open, randomized and crossover test for a period of 7 days. After dosing, serial blood samples were collected, and plasma nisoldipine concentrations were determined by LC-MS/MS. The pharmacokinetic parameters were calculated. RESULTS The major pharmacokinetic parameters of nisoldipine orally disintegrating tablets and normal tablets were as follows： tmax were （1.50 ± 0.40） h and （1.43 ± 0.49） h; tOm=were （1 252.5 ± 918.6） ng.L-1 and （1 240.6± 757.7） ng.L-1; tl/2 were （8.07 ± 2.00） h and （8.77±2.46） h; AUC0-∞ were （5 505.3 ± 3 398.3） ng.h.L-1 and （4 781.1± 2 102.8） ng-h.L-1, AUC0-∞ were （6 053.0 ± 3 603.8） ng.h.L-1 and （5 413.6 ±2 388.3） ng-h-L-1, respectively. The relative bioavailability was （113.1 ± 31.3） %. There were no significant differences in pharmacokinetic parameters between two nisoldipine tablets （P 〉 0.05）. CONCLUSION The orally disinte- grating tablets is bioequivalent to the normal tablets in healthy volunteers.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2013年第2期140-144,共5页
Chinese Journal of New Drugs and Clinical Remedies
关键词
尼索地平
生物等效性
色谱法
高压液相
串联质谱法
药动学
口腔崩解片
nisoldipine
bioequivalence
chromatography, high pressure liquid
tandem mass spectro-metry
pharmacokinetics
orally disintegrating tablet
