西洛他唑片在健康人体的药代动力学和生物等效性

Pharmacokinetics and bioequivalence of cilostazol tablet in healthy volunteers

目的 研究西洛他唑片剂的药代动力学及相对生物利用度。方法 用随机分组自身对照方法,18例健康男性受试者单次口服西洛他唑参比和试验制剂100mg后,用反相高效液相色谱法测定血浆中西洛他唑的浓度,用3P97药代动力学软件进行参数计算及生物等效性评价。结果 2种西洛他唑片在健康受试者体内的药-时曲线均符合二室模型,参比与试验制剂的主要药动学参数:Cmax分别为(844 ± 335),(937 ± 294) ng.mL-1;tmax为(3.17 ± 1.10), (3.22 ± 1.06) h;t1/2α为(2.30 ± 1.08), (2.23 ± 0.93) h;t1/2β为(11.97 ± 3.54), (11.13 ± 2.70) h ;AUC0-t为(10.58 ± 3.50), (10.95 ± 3.23) mg.h.mL-1,AUC0-∞为(11.14 ± 3.50), (11.43 ± 3.23) mg.h.mL-1。试验制剂的相对生物利用度分别为F0-t=(108.39 ± 29.72)%和F0-∞=(106.83 ± 27.84)%。结论 试验和参比制剂具有生物等效性。

Objective To study the pharmacokinetics and bioavailability of twoformulations of cilostazol tablets. Methods A single oral dose 100 mg of twoformulations of cilostazol was given to 18 healthy volunteers in an open randomizedcross-over study. Plasma levels of cilostazol were detected by RP-HPLC method.Results The two-compartment open model with first order absorption was used todescribe the time course of plasma concentrations of two formulations of cilostazol.The main pharmacokinetic parameters for cilostazol were as follows: Cmax of referenceand test tablets were (844 ± 335) and (937 ± 294) ng.mL-1; tmax (3.17 ± 1.10) and(3.22 ± 1.06) h; t1/2α (2.30 ± 1.08) and (2.23 ± 0.93) h; t1/2β(11.97 ± 3.54) and(11.13 ± 2.70) h; AUC0-t (10.58 ± 3.50) and (10.95 ± 3.23) mg.h.mL-1; AUC0-∞(11.14 ± 3.50) and (11.43 ± 3.23) mg.h.mL-1, respectively. The relative bioavailabilityof test formulation were (108.39±29.72)% and (106.83±27.84)%, respectively.Conclusion The results of statistics analysis shown that the reference and the testtablets were bioequivalent.