甲磺酸酚妥拉明口腔崩解片在健康人体的药代动力学和生物等效性

Pharmacokinetics and bioequivalence of phentolamine mesilate orally disintegrating tablets in healthy volunteers

目的研究甲磺酸酚妥拉明(抗男性勃起功能障碍药)口腔崩解片和分散片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,剂量均为40mg,剂间间隔为1周,用反相高效液相色谱-紫外检测法测定血浆中甲磺酸酚妥拉明浓度,用DAS药代动力学程序计算有关药代动力学参数、相对生物利用度,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:tmax分别为(0.69±0.20)和(0.81±0.32)h,t1/2分别为(4.99±1.48)和(4.41±1.73)h,Cmax分别为(34.50±8.79)和(35.17±11.19)mg.L-1,AUC0-t分别为(100.30±23.14)和(99.95±27.51)mg.h.L-1,AUC0-∞分别为(104.81±23.46)和(104.85±28.61)mg.h.L-1。甲磺酸酚妥拉明的相对生物利用度为(103.10±20.60)%。结论2种制剂具有生物等效性。

Objective To study the pharmacokinetics and bioequivalence of pehntolamine mesilate oral disintegrating tablets and dispersible tablets in healthy volunteers. Methods A single oral dose （40 mg tested and reference formulations）was given to 20 healthy volunteers according to an open randomized crossover design. The pehntolamine mesilate concentrations of plasma were determined by RP - HPLC - UV. The pharmacokinetic parameters were calculated by DAS program and the bioavailability and bioequivalence of two formulations were evaluated. Resuits The main pharmacokinetic parameters of pehntolamine mesilate oral disintegrating and dispersible tablets were as follows： t were （0.69 ±0.20） and（0.81 ±0.32） h,t1/2 were（4.99 ± 1.48）and（4.41 ± 1.73 ） h , Cmax were （ 34. 50 ± 8. 79 ） and （ 35. 17±11. 19mg · L^-1, AUC0-t, were（100.30±23. 14）and（99.95 ±27.51）mg · h · L^-1,AUC0-∞ were （ 104.81 ± 23.46） and （ 104.85 ±28.61 ）mg· h ·L^ - 1. The relative bioavailability of drug was （ 103.10 ± 20.60） %. Conclusion The two pehntolamine mesilate formulations are bioequivalent.