羟苯磺酸钙颗粒剂在健康人体的药代动力学和生物等效性

Pharmacokinetics and bioequivalence of calcium dobesilate granules in healthy volunteers

目的研究羟苯磺酸钙(改善微循环、抗血栓药)颗粒剂和胶囊在健康人体的药代动力学及生物等效性。方法20名健康志愿者随机双交叉、单剂量口服受试制剂和参比制剂0.5 g,剂间间隔为1周,用高效液相色谱-紫外检测法测定血浆中羟苯磺酸钙浓度,用DAs ver 2.0药代动力学程序进行有关药代动力学参数、相对生物利用度计算,并评价2种制剂生物等效性。结果受试与参比制剂的药代动力学参数如下:t_(max)分别为(4.33±0.92)和(4.50±0.83)h,t_(1/2)分别为(4.05±1.37)和(4.06±1.53)h,C_(max)分别为(10.77±2.96)和(11.77±3.26)mg·L^(-1),AUC_(0-t)分别为(85.22±18.76)和(86.75±18.67)mg·h·L^(-1),AUC_(0-∞)分别为(88.69±21.14)和(89.71±19.88)mg.h·L^(-1),羟苯磺酸钙颗粒剂的相对生物利用度为(98.90±12.11)%。结论2种制剂具有生物等效性。

Objective To study the pharmacokinetics and bioequivalence calcium dobesilate granules and capsules in healthy volunteers. Methods A single oral dose（0.5 g test and reference formulations）was given to 20 healthy volunteers according to an open randomized crossover design. The calcium dobesilate concentrations of plasma were determined by HPLC -UV. The pharmacokinetic parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by DAS ver 2.0 program. Results The main pharmacokinetic parameters of calcium dobesilate granules and capsules were as follows：tmax were （4.33 ±0.92）and（4.50±0.83）h,t1/2 were （4.05 ±1.37） and （4.06± 1.53）h,Cmax were （10.77 ±2.96）and（11.77 ±3.26）mg ·L^-1, AUC0-t were （85.22±18.76） and （86.75±18.67） mg · h· L^-1, AUC0-∞ were （88.69±21.14） and （89.71 ±19.88） mg · h· L^-1. The relative bioavailability of drug was （98.90 ± 12.11 ） %. Conclusion The two calcium dobesilate formulations are bioequivalent.