摘要
目的比较2种硝苯地平缓释片在健康人体的药动学和生物等效性。方法40例男性健康志愿者进行随机双交叉试验,分别单剂量和多剂量口服硝苯地平缓释片受试制剂和参比制剂,采用LC-MS/MS法测定血药浓度。用DAS2.0软件计算药动学参数和进行统计分析。结果单剂量时受试制剂和参比制剂的体内药动学参数如下:ρmax分别为(90±s44)和(96±40)μg·L-1,tmax分别为(2.1±0.6)和(2.2±0.8)h,AUC0~36分别为(391±117)和(406±183)μg·h·L-1,t1/2分别为(6.3±2.2)和(5±3)h。受试制剂的相对生物利用度为(101±21)%。多剂量达稳态时受试制剂和参比制剂的体内药动学参数如下:ρmax分别为(84±28)和(93±35)μg·L-1,tmax分别为(2.2±1.1)和(1.8±0.9)h;AUCss分别为(440±152)和(455±190)μg·h·L-1,ρav分别为(37±13)和(38±16)μg·L-1,DF分别为(181±56)和(222±63)%,t1/2分别为(6.7±2.3)和(5±4)h。受试制剂的相对生物利用度为(104±29)%。结论2个制剂在健康人体的处置过程基本一致,具有生物等效性。
AIM To study the pharmacokinetics and bioequivalability of two different nifedipinesustained-release tablets in healthy volunteers. METHODS An open randomized crossover study of 40 healthy male volunteers was carried out with orally single-dose and multiple-dose nifedipine in test and reference preparations. The concentrations of nifedipine in plasma were determined by LC-MS/MS. The Pharmacokinetic parameters and correlative bioavailabilities were statistically calculated with DAS2.0 software. RESULTS The main pharmacokinetie parameters of test and reference preparations after a single dose were: p were (90 ± s 44) vs (96 ± 40) μg·L^-1, tmax (2.1 ± 0.6) vs (2.2 ± 0.8) h, AUC0-36 (391 ± 117) vs (406 ±183) μg·h·L^-1, t1/2 (6.3 ± 2.2) vs (5 ± 3) h, respectively. The correlative bioavailability of the test preparation was (101± 21)%. The main pharmaeokinetie parameters of test and reference preparations after multiple doses under stable condition were: pmax were (84 ± 28) vs (93 ± 35) μg·L^-1, tmax (2.2± 1.1) vs (1.8 ± 0.9) h, AUC, (440 ± 152) vs (455 ± 190) μg·h·L^-1, Pvs (37 ± 13) vs (38 ± 16) μg·L^-1, DF (181 ± 56) vs (222 ± 63)%, tmax (6.7 ±2.3) vs (5±4) h, respectively. The correlative bioavailability of the test preparation was (104 ± 29)%. CONCLUSION There were no significant differences in pharmaeokinetie parameters between the two different formulations of nifedipine sustained-release tablets in healthy volunteers, they were bioequivalent.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2009年第7期541-545,共5页
Chinese Journal of New Drugs and Clinical Remedies
关键词
硝苯地平
迟效制剂
色谱法
高压液相
光谱法
质量
电喷雾电离
药动学
生物等效性
nifedipine
delayed-action preparation
chromatography, high pressure liquid
spectrometry, mass, electrospray ionization
pharmacokinetics
bioequivalence