吗替麦考酚酯软胶囊及普通胶囊在健康人体的生物等效性

Bioequivalence of bisoprolol fumarate soft capsules and common capsules in healthy volunteers

目的评价男性健康志愿者单剂量口服吗替麦考酚酯(免疫抑制剂)软胶囊与普通胶囊在健康人体内的生物等效性。方法用2制剂2周期随机交叉设计,20名男性健康志愿者单剂量口服受试软胶囊和参比胶囊,采用高效液相色谱-紫外检测法测定血浆中霉酚酸浓度变化并进行统计学分析,对2种制剂做出生物等效性评价。结果吗替麦考酚酯受试软胶囊与参比胶囊的AUC0→t分别为(69.95±14.13)和(66.95±19.05)μg·h·mL-1;AUC0→∞分别为(85.18±20.51)和(77.39±23.78)μg·h·mL-1;Cmax分别为(31.26±13.09)和(31.90±14.45)μg·mL-1;tmax分别为(0.88±0.36)和(0.78±0.29)h;t1/2分别为(20.34±12.55)和(18.84±11.58)h。吗替麦考酚酯软胶囊相对生物利用度为(109.6±26.9)%。结论受试软胶囊与参比胶囊具有生物等效性。

Objective To evaluate the bioequivalence of bisoprolol fumarate soft capsules and common capsules in healthy volunteers. Methods Concentrations of mycophenolic acid in plasma were determined by HPLC - UV after 20 healthy male volunteers received a single dose of two bisoprolol fumarate praperations soft capsules and reference capsules in two - treatment, two - period, crossover design. Results The main pharmaeokinetic parameters of two bisoprolol fumarate were as follows： AUC0→t were （69.95±14.13） and （66.95 ±19.05）ug .h . mL-1; AUC0→∞ were （85.18 ±20.51） and （77.39 ±23.78） ug . h . mL-l; Cmax were （ 31. 26 ±13. 09 ） and （ 31. 90 ±14. 45 ） ug . mL-1;tmax were （0.88 ±0.36）and （0.78 ±0.29）h;t1/2were （20. 34 ± 12. 55） and （ 18.84 ± 11.58 ） h, respectively. The relative bioavailability of bisoprolol fumarate soft capsules to common capsules was （109. 6 ± 26. 9）%. Conclusion The results of statistic analysis shown that two preparations of bisoprolol fumarate were bioequivalent.