中国临床药理学杂志
中國臨床藥理學雜誌
중국림상약이학잡지
THE CHINESE JOURNAL OF CLINICAL PHARMACOLOGY
2010年
1期
37-39
,共3页
师少军%严慧娟%万元胜%陈华庭%曾繁典
師少軍%嚴慧娟%萬元勝%陳華庭%曾繁典
사소군%엄혜연%만원성%진화정%증번전
硫唑嘌呤%6-巯基嘌呤%生物等效性%反相高效液相色谱
硫唑嘌呤%6-巰基嘌呤%生物等效性%反相高效液相色譜
류서표령%6-구기표령%생물등효성%반상고효액상색보
azathioprine%6-mercaptopurine%bioequivalenee%RP-HPLC
目的 研究硫唑嘌呤片(免疫抑制剂)在健康人体的相对生物利用度并评价其牛物等效性.方法 20名健康志愿者自身交叉、单剂量口服硫唑嘌呤受试和参比制剂各100 mg后,用反相高效液相色谱法测定血浆中其代谢物6-巯基嘌呤浓度.应用DAS软件计算药代动力学参数和相对生物利用度.结果 6-巯基嘌呤受试制剂和参比制剂的平均药物浓度-时间曲线均符合一室模型,主要药代动力学参数:t_(1/2)分别为(1.30±0.25),(1.30±0.34)h;t_(max)分别为(1.25±0.16),(1.24±0.21)h;C_(max)分别为(48.44±17.09),(52.32±24.37)μg·L~(-1);AUC_(0-t)分别为(89.49±19.25),(91.90±25.31)μg·h·L~(-1);AUC_(0-∞)分别为(96.11±19.74),(98.36±24.66)μg·h·L~(-1).与参比制剂比较,受试制剂的相对生物利用度F_(0-t)为(99.62±15.29)%,F_(0-∞)为(99.39±13.59)%.结论 2种硫唑嘌呤制剂具有生物等效性.
目的 研究硫唑嘌呤片(免疫抑製劑)在健康人體的相對生物利用度併評價其牛物等效性.方法 20名健康誌願者自身交扠、單劑量口服硫唑嘌呤受試和參比製劑各100 mg後,用反相高效液相色譜法測定血漿中其代謝物6-巰基嘌呤濃度.應用DAS軟件計算藥代動力學參數和相對生物利用度.結果 6-巰基嘌呤受試製劑和參比製劑的平均藥物濃度-時間麯線均符閤一室模型,主要藥代動力學參數:t_(1/2)分彆為(1.30±0.25),(1.30±0.34)h;t_(max)分彆為(1.25±0.16),(1.24±0.21)h;C_(max)分彆為(48.44±17.09),(52.32±24.37)μg·L~(-1);AUC_(0-t)分彆為(89.49±19.25),(91.90±25.31)μg·h·L~(-1);AUC_(0-∞)分彆為(96.11±19.74),(98.36±24.66)μg·h·L~(-1).與參比製劑比較,受試製劑的相對生物利用度F_(0-t)為(99.62±15.29)%,F_(0-∞)為(99.39±13.59)%.結論 2種硫唑嘌呤製劑具有生物等效性.
목적 연구류서표령편(면역억제제)재건강인체적상대생물이용도병평개기우물등효성.방법 20명건강지원자자신교차、단제량구복류서표령수시화삼비제제각100 mg후,용반상고효액상색보법측정혈장중기대사물6-구기표령농도.응용DAS연건계산약대동역학삼수화상대생물이용도.결과 6-구기표령수시제제화삼비제제적평균약물농도-시간곡선균부합일실모형,주요약대동역학삼수:t_(1/2)분별위(1.30±0.25),(1.30±0.34)h;t_(max)분별위(1.25±0.16),(1.24±0.21)h;C_(max)분별위(48.44±17.09),(52.32±24.37)μg·L~(-1);AUC_(0-t)분별위(89.49±19.25),(91.90±25.31)μg·h·L~(-1);AUC_(0-∞)분별위(96.11±19.74),(98.36±24.66)μg·h·L~(-1).여삼비제제비교,수시제제적상대생물이용도F_(0-t)위(99.62±15.29)%,F_(0-∞)위(99.39±13.59)%.결론 2충류서표령제제구유생물등효성.
Objective To evaluate the relative bioavailability and bio-equivalence of azathiopfine tablets in healthy volunteers.Methods A single oral dose of 100 mg azathioprine test and reference tablets were given to 20 male healthy volunteers in a randomized crossover study.Plasma metabolite 6-mercaptopurine of azathioprine wag determined by RP-HPLC.The pharmacokinetic parameters and relative bioavailability were calculated with DAS program to evaluate the bioequivalence of the two preparations.Results The concentration-time curves were fitted to a one-compartment open modeL The main pharmacokinetic parameters of azathioprine test and reference tablets were as follows:t_(1/2)were(1.30±0.25)and(1.30±0.34)h;t_(max) were(1.25±0.16)and(1.24±0.21)h;C_(max) were(48.44±17.09)and(52.32±24.37)μg·L~(-1);AUC_(0-1)were(89.49±19.25)and(91.90±25.31)μg·h·L~(-1);AUC_(0-∞)were(96.11±19.74)and(98.36±24.66)μg·h·L~(-1),re-spectively.The relative bioavailability of F_(0-t) and F_(0-∞) were(99.62±15.29)%and(99.39±13.59)%,respectively.Conclusion The two azathiprine preparations are bioequivalent.
