CAJ | 학술논문

目的:研究替米沙坦在中国人体内的药代动力学和相对生物利用度.方法:20名男性健康志愿者单剂量随机交叉口服 80 mg 国产替米沙坦胶囊(试验片)和进口替米沙坦片(参比片),采用HPLC-荧光检测法测定受试者 96 h 的血药浓度,生物等效性采用双侧t检验.结果:国产和进口的替米沙坦血药浓度-时间曲线符合二室开放模型,其主要药代动力学参数:Cmax分别为 456.28±252.56 和 759.54±313.54 μg·L-1,Tmax分别为 1.61±0.71 和 1.08±0.36 h,T1/2β分别为 22.39±6.29 和 21.08±5.24,MRT分别为 27.02±6.23 和 24.27±5.79 h,AUC0-t分别为3454±1050和3636±1300 μg·h·L-1,统计分析,试验片与参比片的Cmax、Tmax有统计学差异(P<0.05),而AUC0-t没有显著性差异(P>0.05),试验片相对生物利用度为97.28%±12.74%.结论:国产替米沙坦胶囊和进口片剂具有生物等效性.
목적:연구체미사탄재중국인체내적약대동역학화상대생물이용도.방법:20명남성건강지원자단제량수궤교차구복 80 mg 국산체미사탄효낭(시험편)화진구체미사탄편(삼비편),채용HPLC-형광검측법측정수시자 96 h 적혈약농도,생물등효성채용쌍측t검험.결과:국산화진구적체미사탄혈약농도-시간곡선부합이실개방모형,기주요약대동역학삼수:Cmax분별위 456.28±252.56 화 759.54±313.54 μg·L-1,Tmax분별위 1.61±0.71 화 1.08±0.36 h,T1/2β분별위 22.39±6.29 화 21.08±5.24,MRT분별위 27.02±6.23 화 24.27±5.79 h,AUC0-t분별위3454±1050화3636±1300 μg·h·L-1,통계분석,시험편여삼비편적Cmax、Tmax유통계학차이(P<0.05),이AUC0-t몰유현저성차이(P>0.05),시험편상대생물이용도위97.28%±12.74%.결론:국산체미사탄효낭화진구편제구유생물등효성.
AIM: To compare pharmacokinetics and relative bioavailability of telmisartan capsule (T) and telmisartan tablet(R). METHODS: 20 male healthy Chinese volunteers were enrolled in a randomized two-way crossover designs with a single-oral dose study(80 mg once per day for each preparation). The plasma telmisatan concentration was determined by HPLC- fluorescence detector. Plasma levels of telmisatan were followed up to 96 h. Area under the telmisartan concentration time curve was calculated by variance analysis and the bioequivalent was determined by two one-side t-test. RESULTS: A two-compartment model was adopted in telmisartan plasma concentration-time data analysis. The pharmacokinetic parameters of T and R in single-dose study including Cmax (μg·L-1), Tmax (h), T1/2β (h), MRT(h), AUC0-92(μg·h·L-1) were as following: 456±253 and 760±314, 1.61±0.71 and 1.08±0.36, 22.39±6.29 and 21.08±5.24, 27.02±6.23 and 24.27±5.79, 3454±1050 and 3635±1300, respectively. Statistically significant differences were observed between the parameter values of the two products in Cmax and Tmax; whereas there was no statistically significant difference between AUC0-∞μg·h·L-1 (3601±1095 and 3767±1399). The relative bioavailability for T was 97.28%±12.74%. CONCLUSION: The test telmisartan capsule is bioequivalent to the reference tablet.