骨化三醇人体生物等效性研究

Investigation of bioequivalence of calcitriol capsules and Rocaltrol in healthy volunteers

目的:比较试验制剂骨化三醇胶丸与参比制剂市售罗钙全的生物等效性。方法:18名健康志愿者单剂双交叉口服试验制剂或参比制剂4.0μg(0.25μg×16粒),分别取前臂静脉血4ml,离心,分离血清-20℃保存。采用放免法测定骨化三醇血浓度,评价试验制剂和参比制剂的生物等效性。结果:试验制剂骨化三醇胶丸和参比制剂罗钙全主要药代动力学参数t1/2(β)分别为(8.57±1.49)h和(8.60±1.48)h,Tpeak分别为(4.17±1.25)h和(4.33±1.37)h,Cmax分别为(366.22±82.90)pg/ml和(357.03±76.84)pg/ml,AUC0～48分别为(5019.51±1217.04)pg/ml·h和(4986.50±1112.58)pg/ml·h,AUC0～∞分别为(5729.52±1154.64)pg/ml·h和(5790.30±1085.41)pg/ml·h。试验制剂骨化三醇胶丸相对生物利用度F为99.14%±11.25%。结论:骨化三醇胶丸与罗钙全具有生物等效性。

Objective:To study the bioequivalence of calcitriol capsules in healthy volunteers.Methods:Eighteen volunteers were randomly divided into2groups(test and reference),9for each.4ml blood samples were collected before and1,2,3,4,5,6,8,12,24,36and48h after a single oral dose of 4.0μg cal-citriol capsules and Rocaltrol respectively.The time-concentrations of calcitriol were determined by RIA and pharmarcokinetic parameters were calculated with3P97practical pharmacokinetic programme.Results:The pharmarcokinetic parameters of calcitriol capsules and Rocaltrols were as follows:t 1/2(β) (8.57±1.49)h and(8.60±1.48)h,Tpeak (4.17±1.25)h and(4.33±1.37)h,Cmax (366.22±82.90)pg /ml and(357.03±76.84)pg /ml ,AUC 0～48 (5019.51±1217.04)pg /ml ·h and(4986.50±1112.58)pg /ml ·h,AUC 0～∞ (5729.52±1154.64)pg /ml ·h and(5790.30±1085.41)pg /ml ·h。The relative bioavailability of test growp was99.14%±11.25%。Conclusion:All the parameters suggest that calcitriol capsule has bioequivalence with rocaltrol.