伊潘立酮片在中国健康受试者空腹和餐后条件下的生物等效性研究

目的 研究伊潘立酮片在中国健康受试者空腹和高脂条件下体内的药动学特征并评价生物等效性.方法 采用开放、随机、两周期、两序列自身交叉试验设计,健康受试者分别空腹和餐后口服1 mg伊潘立酮片受试制剂与参比制剂,采集不同时间点的血样.利用液相色谱-质谱联用法检测血浆样品中伊潘立酮及其代谢物羟基伊潘立酮(P88)的浓度,用Ph...

Bioequivalence Study of Iloperidone Tablets Under Fasting and Fed Conditions in Chinese Healthy Subjects

OBJECTIVE To study the pharmacokinetics and bioequivalence of iloperidone tablets in Chinese healthy subjects under fasting and fed conditions. METHODS An open, randomized, single-dose, double-period, two-sequence and self-crossover design was adopted. Thirty-six Chinese healthy subjects were randomly divided into two groups under fasting and fed conditions. Blood samples were collected at different time points from the subjects after taking a single dose of 1 mg iloperidone test tablets (T) or reference tablets (R) orally. The concentrations of iloperidone and its metabolite P88 in plasma samples were determined by liquid chromatography-mass spectrometry (LC-MS/MS). The main pharmacokinetic parameters of the two preparations were calculated by Phoenix^TM WinNonlin 7.0 software, and the bioequivalence of the two preparations was evaluated. RESULTS Under fasting conditions, the 90% confidence intervals of ρ_max, AUC_0-t and AUC_0-∞ of plasma iloperidone were 89.88%-106.6%, 99.81%-109.40% and 100.06%-110.20%, respectively; the 90% confidence intervals of ρ_max, AUC_0-t and AUC_0-∞ of its metabolite P88 were 90.05%-102.45%, 100.79%-108.17% and 101.58%-110.97%. Under fed conditions, the 90% confidence intervals of ρ_max, AUC_0-t and AUC_0-∞ of plasma iloperidone were 102.06%-118.14%, 103.94%-111.83% and 104.02%-113.02%, respectively; the 90% confidence intervals of ρ_max, AUC_0-t and AUC_0-∞ of its metabolite P88 were100.73%-111.20%, 104.88%-112.29% and 103.29%-111.33%. The 90% confidence intervals of the T:R ratios of ρ_max, AUC_0-t and AUC_0-∞ were all within the equivalent interval of 80.00%-125.00% under fasting and fed conditions. CONCLUSION The test preparation and reference preparation of iloperidone tablets were bioequivalent in Chinese healthy subjects under fasting and fed conditions.