熊去氧胆酸胶囊人体生物等效性研究

Study on Bioequivalence of Ursodexycholic Acid Capsules

目的评价熊去氧胆酸胶囊(受试制剂)与进口熊去氧胆酸胶囊(参比制剂)的人体生物等效性。方法20名男性健康受试者,采用随机双周期交叉试验。单剂量po受试制剂或参比制剂500mg,HPLC-MS测定血浆中熊去氧胆酸的含量;2种制剂的熊去氧胆酸血药浓度经BAPP2.0程序处理,计算药动学参数及相对生物利用度。结果参比制剂与受试制剂的tmax分别为(3.0±0.8),(2.8±0.9)h;ρmax分别为:(8565.69±2692.58),(7184.87±2396.34)μg.L-1,用梯形法计算所得的AUC0-10分别为:(23488.34±6594.56),(22725.19±6083.04)μg.h.L-1,t1/2分别为(1.53±0.55)和(1.56±0.61)h。熊去氧胆酸受试制剂的相对生物利用度为:(98.5±13.8)%,对ρmax,AUC0-10经对数转换,方差分析后进行双单侧检验及90%可信限判断,差异无统计学意义。结论两制剂具有生物等效性。

OBJECTIVE To evaluate the bioequivalence of ursodexycholic acid capsules （test samples） and imported ursodexycholic acid capsules （reference samples）. METHODS 20 Healthy male volunteers were randomly administered with an oral single crossover dose of test and referemce ursodexycholic acid capsules 500 mg. The plasma samples were then collected from volunteers to measure ursodexycholic acid concentrations by HPLC-MS. The pharmacokinetic parameters of ursodexycholic acid casuples were calculated using BAPP2.0 practical pharmacokinetic program. RESULTS The pharmacokinetics of reference and test samples were as follows ： tmax （3. 0 ± 0. 8 ）, （ 2. 8 ± 0. 9 ） h ; ρmax （ 8 565.69 ± 2 692. 58 ）, （ 7 184. 87±2 396. 34 ） μg·L^-1, AUC0-10（ 23 488.34 ± 6 594. 56）, （22 725.19±6 083.04 ） μg·h·L^-1, t1/2 （ 1.53 ± 0. 55 ）, （ 1.56 ± 0. 61 ） h .The relative bioavailability of test samples was （98.5 ± 13.8）% . CONCLUSION The test eapsules are bioequivalent to the reference eapsules.