高效液相色谱法测定盐酸曲普利啶血浆浓度及药动学

 目的 对健康受试者进行盐酸曲普利啶的药物动力学研究，以评价胶囊剂的生物等效性。 方法 18名健康志愿受试者，随机分组，自身交叉口服盐酸曲普利啶胶囊和片剂。用反相高效液相色谱法测定盐酸曲普利啶血浆浓度，3P87拟合药动学参数，计算药动学参数，并以AUC_0～∞，t_max,c_max为指标，用方差分析、双单侧t检验及12α置信区间分析片剂与胶囊的生物等效性。结果盐酸曲普利啶胶囊与片剂的主要药动学参数分别为c_max(42.1±6.3)和(40.7±6.4) μg·L^-1,t_max(1.8±0.3)和(1.8±0.3) h，AUC_0～∞(156.5±28.4)和(160.9±26.7) μg·h·L,胶囊剂的相对生物利用度为(98.3±5.4)%。结论两制剂均符合一房室模型，为生物等效制剂。

Studies on pharmacokinetics and bioavailability of triprolidine hydrochloride by means of HPLC assay

OBJECTIVE To determine the plasma concentrations of triprolidine hydrochloride and evaluate the bioavailability of triprolidine capsule.METHODS 18 healthy male volunteers were given triprolidine hydrochloride capsules and tablets in a randomized cross over design.The plasma concentrations of triprolidine were determined with reverse HPLC.The pharmacokinetic parameters of two preparations were calculated with the 3P87 software.The t_max,c_maxand AUC_0～∞were used to evaluate the bioequivalence of capsule and tablet with analysis of variance,two one sided t test and (1-2α) confidence intervals. RESULTS The pharmacokinetic parameters of triprolidine hydrochloride capsules and tablets were as follow: t_max(1.8±0.3) and (1.8±0.3) h,c_max(42.1±6.3) and (40.7±6.4) μg·L^-1,AUC_0～∞(156.5±28.4) and (160.9±26.7) μg·h·L^-1,respectively.The relative bioavailability of capsule was (98.3±5.4)%. CONCLUSION The two preparations were coincident with two compartment model and were bioequivalent.