复方磺胺甲噁唑人体药动学与生物等效性研究  

Pharmacokinetics and Bioequivalence Studys of CompoundSulfamethoxazole in Healthy Subjects

作　　者：张婷[1,2] 李梦瑶 姜雅琦 田杰 郭东生 甘方良 ZHANG Ting;GUO Dong-sheng;GAN Fang-liang(School of Pharmacy,Xianning Medical College,Hubei University of Science and Technology,Xianning Hubei 437100,China)

机构地区：[1]湖北科技学院医学部药学院,湖北咸宁437100 [2]湖北科技学院附属第一医院临床药理机构办公室

出　　处：《湖北科技学院学报（医学版）》2024年第1期25-29,共5页Journal of Hubei University of Science and Technology(Medical Sciences)

摘　　要：目的研究单次空腹口服复方磺胺甲噁唑片在健康受试者体内的人体药代动力学特征和生物等效性。方法试验采用单中心、随机、开放、单剂量、两制剂、两周期、两序列交叉设计,24例受试者分别空腹口服复方磺胺甲噁唑受试制剂T或参比制剂R。采用超高效液相色谱-串联质谱(UPLC-MS/MS)检测血浆中的磺胺甲噁唑和甲氧苄啶的血药浓度,用Phoenix WinNonlin 8.2软件计算药动学参数,评价两制剂生物等效性。结果空腹试验受试制剂T和参比制剂R的磺胺甲噁唑C max、AUC 0-t、AUC 0-∞分别为(27.340±3.400)和(28.042±3.527)μg/mL、(375.2±38.7)和(371.5±35.4)h·μg/mL、(390.0±42.9)和(386.7±41.0)h·μg/mL;甲氧苄啶C max、AUC 0-t、AUC 0-∞分别为(0.845±0.198)和(0.838±0.144)μg/mL、(8.7±1.3)和(8.2±1.5)h·μg/mL、(8.9±1.3)和(8.4±1.5)h·μg/mL,药动学参数最小二乘几何均值比的90%置信区间均落在80.00%~125.00%判定范围内(P均>0.05)。结论复方磺胺甲噁唑片受试制剂与参比制剂在健康受试者中具有生物等效性。Objective To study the human pharmacokinetic characteristics and bioequivalence of compound sulfamethoxazole tablets taken orally on a single fasting diet in healthy subjects.Methods A single center,randomized,open,single-dose,two-preparation,two-cycle,two-sequence crossover design were used in this study.24 subjects were orally administered sulfamethoxazole test preparation(T)or reference preparation(R)on an empty stomach,respectively.The pharmacokinetic parameters of sulfamethoxazole and trimethopridium in plasma were determined by ultra-high performance liquid chromatoc-tandem mass spectrometry(UPLC MS/MS).The phoenix WinNonlin 8.2 software was used to calculate the pharmacokinetic parameters and evaluate the bioequivalence of these two products.Results The C max,AUC 0-t and AUC 0-∞of sulfamethoxazole in the fasting test preparation and reference preparation were(27.340±3.400)and(28.042±3.527)μg/mL,(375.2±38.7)and(371.5±35.4)h·μg/mL,(390.0±42.9)and(386.7±41.0)h·μg/mL;The C max,AUC 0-t and AUC 0-∞of trimethoprim were(0.845±0.198)and(0.838±0.144)μg/mL,(8.7±1.3)and(8.2±1.5)h·μg/mL,(8.9±1.3)and(8.4±1.5)h·μg/mL.Conclusion The tested preparation and reference preparation of compound sulfamethoxazole tablets were bioequivalent in healthy subjects.

关 键 词：复方磺胺甲噁唑 磺胺甲噁唑 甲氧苄啶 生物等效性 药代动力学 

分 类 号：R696.1[医药卫生—泌尿科学]