摘要
目的 :研究健康志愿者单剂口服试验制剂盐酸伊托必利分散片与参比制剂盐酸伊托必利片的药代动力学和相对生物利用度。 方法 :将 18名健康志愿者随机分为两组 ,分别口服试验制剂和参比制剂 10 0 m g,采集服药后 0 .2 5、0 .5、1.0、1.5、2 .0、3.0、4 .0、6 .0、8.0、10 .0、12 .0、2 4 .0 h的血样本 ,采用高效液相色谱法 (HPL C)测定伊托必利经时血浓度。结果 :两种制剂的药 -时曲线符合口服吸收有滞后时间的一级动力学双室模型。试验制剂和参比制剂主要药代动力学参数如下 :t1 /2 分别为 (15 .0± 3.4 1)、(14 .6± 3.13) h,Tmax分别为 (0 .78± 0 .35 )、(0 .78± 0 .35 ) h,cmax分别为 (6 0 1.78± 15 9.2 9)、(6 11.2 2±16 6 .32 ) ng/ m l,AU C0～ 2 4 分别为 (2 72 1.6± 5 77.92 )、(2 6 32 .3± 6 14 .2 7) ng· h/ m l,AUC0～∞ 分别为 (486 0 .6 0± 80 4 .80 )、(46 75 .90± 6 4 5 .0 0 ) ng· h/ m l。试验制剂相对生物利用度为 (10 3.87± 6 .31) %。用 3P97程序统计分析 ,两种制剂各药代动力学参数均无显著性差异 (P>0 .0 5 )。 结论 :试验制剂盐酸伊托必利分散片和参比制剂盐酸伊托必利片具有生物等效性。
Objective:To study the pharmacokinetics and relative bioavailability of itopride hydrochloride dispersion tablets and the reference preparation. Methods: Eighteen healthy male volunteers were divided randomly into 2 groups. The volunteers of one group received single dose of itopride hydrochloride dispersion tablet 100 mg, and those of the other group received single dose of itopride hydrochloride tablet 100 mg. A two-period crossover test was conducted and blood samples were taken for assay by HPLC. Results: The concentration-time profiles of two preparations fitted to a two-compartment model with first order absorption and lag time. The t 1/2 was (15.0±3.41) and (14.6±3.13) h, T max was (0.78±0.35) and (0.78±0.35) h, c max was (601.78±159.29) and (611.22±166.32) ng/ml, AUC 0～24 was (2 721.6± 577.92) and (2 632.3±614.27) ng·h /ml, AUC 0～∞ was (4 860.60± 804.80) and (4 675.90±645.00) ng·h /ml, respectively. The relative bioavailability of the dispersion tablet was (103.87±6.31)%. The results of variance and two one-side test statistical analysis for t 1/2 ? T max ? c max ?AUC 0～24 and AUC 0～∞ showed that two formulations were bioequivalent. Conclusion: The two preparations are of bioequivalence.
出处
《药学服务与研究》
CAS
CSCD
2003年第1期38-40,共3页
Pharmaceutical Care and Research
关键词
盐酸伊托必利分散片
药代动力学
生物利用度
研究
itopride hydrochloride dispersion tablet
itopride hydrochloride tablet
bioavailability
chromatography, high pressure liquid
