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考察国产羟苯磺酸钙人体生物利用度研究。方法:18名男性健康受试者采用随机分组自身交叉对照实验方法。单剂量分别口服500mg进口羟苯磺酸钙胶囊(R),国产羟苯磺酸钙片剂(T1)和胶囊剂(T2)进行人体生物等效性研究。用IIPLC-荧光检测法测定羟苯磺酸钙血药浓度。本法最小检测浓度0.15mg·L-1,血浆浓度曲线为0.15-19.94mg·L-1,绝对回收率>82%,日内、日间变异<3.0%。结果:18名受试者测得的羟苯磺酸钙血药浓度-时间过程数据用3P97程序二房室模型拟合求算药动学参数。参比药和试验药T1和T2的主要药代动力学参数为: T1/2β4.25±1.12h, 4.05 ±1.09h和3.93 ± 0.95h; C max13.89 ± 3.55mg·L-1, 13.11± 3.70mg·L-1和13.77±3.92mg·L-1; Tmax 4.0 ±1.4h, 4.1±1.2h和4.0 ± 1.0h; AUC0-2498.45 ± 22.54mg· h· L1, 94.62 ± 17.74mg· h· L-1和 97.33 ± 20.72mg· h· L-1。T1和T2的相对生物利用度为97.70%和98.86%。结论:三种制?
Study on bioavailability of domestic calcium dobesilate. Methods: Eighteen male healthy subjects were randomized to self-controlled crossover study. A single dose of 500 mg orally administered calcium dobesilate (R), domestic calcium dobesilate tablets (T1) and capsules (T2) were bioequivalence studies. Determination of calcium dobesilate concentration by IIPLC-fluorescence assay. The minimum detectable concentration of this method was 0.15 mg · L-1, and the plasma concentration curve was 0.15-19.94 mg · L-1. The absolute recovery was> 82%. The intra-day and inter-day variability was <3.0%. RESULTS: Eighteen subjects measured calcium dobesilate concentration-time course data and calculated the pharmacokinetic parameters using the 2-compartment model of 3P97 program. The main pharmacokinetic parameters of reference and test drugs T1 and T2 were: T1 / 2β4.25 ± 1.12h, 4.05 ± 1.09h and 3.93 ± 0.95h; Cmax13.89 ± 3 .55 mg · L -1, 13.11 ± 3.70 mg · L -1 and 13.77 ± 3.92 mg · L -1; Tmax 4.0 ± 1.4 h, 4.1 ± 1.2 h and 4. 0 ± 1.0 h; AUC0-2498.45 ± 22.54 mg · h · L1, 94.62 ± 17.74 mg · h · L-1 and 97.33 ± 20.72 mg · h · L-1. The relative bioavailabilities of T1 and T2 were 97.70% and 98.86%. Conclusion: Three kinds of system?