替米沙坦片剂与胶囊剂在健康人体内的生物等效性  

Study on Bioequivalence of Telmisartan Tablets and Capsules in Chinese Healthy Volunteers

作　　者：舒成仁[1,2] 黄露[2] 葛苗苗[2] 卫乐乐[2] 黎维勇[2] 

机构地区：[1]黄石市中心医院药剂科,湖北黄石435000 [2]华中科技大学同济医学院附属协和医院临床药学室

出　　处：《中国药师》2011年第8期1134-1136,共3页China Pharmacist

摘　　要：目的:评价健康受试者单剂量口服替米沙坦片和胶囊剂人体药物动力学与生物等效性。方法:按照三制剂三周期自身对照三交叉试验设计,18位健康受试者交叉口服试验片剂、试验胶囊剂或对照片剂各80mg。采用HPLC-MS/MS测定血浆中替米沙坦浓度,并进行药物动力学与生物等效性评价。结果:受试片剂、胶囊剂和参比片剂药物动力学参数分别为:AUC_(0～120)分别为(5281.66±2162.88),(5155.91±2327.20),(4893.306±1774.901)ng·ml^(-1);AUC_(0～∞)分别为(5514.20±2347.33),(5451.75±2548.66),(5083.83±1862.78)ng·ml^(-1);C_(max)分别为(729.43±438.96),(660.74±469.94),(684.48±435.70)ng·ml^(-1);t_(max)分别为(1.50±0.74),(1.49±1.04),(1.22±1.05)h;t_(1/2)分别为(27.28±10.09),(30.80±9.65),(28.10±6.68)h。试验片剂、胶囊剂相对参比片剂AUC_(0～120)90%的可信区间分别为(93.6～118.3)%,(90.5～114.4)%;AUC_(0～∞)90%的可信区间分别为(93.3～119.1)%,(91.3～116.5)%;C_(max)90%的可信区间为(81.2～140.8)%,(73.0～126.6)%,均落在相应参比药范围内。t_(max)经非参数检验,在两制剂间差异无统计学意义。受试片剂、胶囊剂相对于参比片剂的生物利用度分别为:(108.4±26.6)%,(107.5±35.3)%。结论:受试片及胶囊与参比片具生物等效性。Objective：To evaluate the bioequivalence and pharmacokinetics of telmisartan tablets and capsules in Chinese healthy volunteers.Method：An open randomized,three periods and three-way crossover shelf-control study recruiting eighteen healthy male volunteers was employed.Each volunteer was randomly administered a single oral dose of telmisartan 80 mg（test tablets or capsules, reference tablets）.The plasma concentrations of telmisartan were determined by HPLC-MS/MS.Non-compartment models were used in analysis of pharmacokinetic parameters.Logarithm-transformed Cmaxand AUC were analyzed by the analysis of variance and 90%confidence intervals.Result：The main parameters of the test telmisartan tablets,capsules and reference tablets were as the follows：Cmaxwas （729.43±438.96）,（660.74±469.94）and（684.48±435.70）ng·ml^-1,tmaxwas（1.50±0.74）,（1.49±1.04）and（1.22±1.05）h,t1/2was（27.28±10.09）,（30.80±9.65）and（28.10±6.68）h,AUC0-120was（5 281.66±2 162.88）,（5 155.91±2 327.20）and（4 893.306±1 774.901）ng·ml^-1,and AUC0-∞was（5 514.20±2 347.33）,（5 451.75±2 548.66）and （5 083.83±1 862.78）ng·ml^-1,Respectively.Conclusion：The test telmisartan tablets and capsules are bioequivalent with the reference tablets.

关 键 词：替米沙坦 药物动力学 生物等效性 

分 类 号：R969.1[医药卫生—药理学]