对乙酰氨基酚薄膜包衣异型片的药代动力学及生物利用度研究

Studies on bioavailability and pharmacokinetics of film coating special shaped tablet of acetaminophen

目的：研究了１０ 名男性健康志愿者单剂量ｐｏ 两种对乙酰氨基酚（ 扑热息痛）异型片５００ ｍｇ 的药代动力学和相对生物利用度。方法：按照随机交叉试验设计，采集服药后０－５ ，１，１－５ ，２ ，３ ，４，６，８，１０ ｈ 的血样本，用ＨＰＬＣ测定扑热息痛的血药浓度。结果：两种制剂的药时曲线符合口服吸收有滞后时间的一级动力学一室模型。受试制剂扑热息痛薄膜包衣异型片（ 康司达） 的主要药代动力学参数：ｃｍａｘ＝ （５－５１ ±１－２４）ｍｇ·Ｌ－１ ，ｔｍａｘ＝ （１－０３ ±０－４３）ｈ ，ｔ１／２ｋａ＝ （０－２７ ±０－１６）ｈ ，ｔ１／２ｋｅ ＝（２－６０ ±０－５１）ｈ，ＡＵＣ０～∞＝ （３４－９１ ±７－９６）ｍｇ·ｈ·Ｌ－１ ，ＭＲＴ＝ （３－６５ ±０－２２）ｈ。参比制剂（ 必理通） 的主要药代动力学参数：ｃｍａｘ ＝ （５－８１ ±１－０１）ｍｇ·Ｌ－ １ ，ｔｍａｘ ＝（０－８８ ±０－３２）ｈ，ｔ１／２ｋａ ＝ （０－１４ ±０－０７）ｈ，ｔ１／２ｋｅ ＝ （２－７１ ±０－９３）ｈ，ＡＵＣ０ ～∞＝ （３３－１４ ±５－６７）ｍｇ·ｈ·Ｌ－１ ，ＭＲＴ＝ （３－６０ ±０－１０）ｈ。两种片剂药代动力学参数（除ｔ１／２ｋａ

OBJECTIVE: The pharmacokinetics and relative bioavailability of domestic film coating special shaped tablet of acetaminophen were studied in 10 healthy male volunteers METHOD: A single oral dose of 500 mg of the two formations (test and reference preparation) was given in a randomized 2 way cross over design Blood samples were withdrawn up to 10 hours post administration Plasma concentrations of acetaminophen were assayed by HPLC RESULTS: The concentration time profiles of two preparations fitted to a one compartment model with first order absorption and lag time The main pharmacokinetic parameters of the test preparation were as following c max (5 51±1 24)mg·L -1 , t max (1 03±0 43)h, t 1/2ka (0 27±0 16)h, t 1/2ke (2 60±0 51)h, AUC 0～∞ (34 91±7 96)mg·h·L -1 ,MRT(3 65±0 22)h,respetively The main pharmacokinetic parameters of the reference preparation were as following: c max (5 81±1 01)mg·L -1 , t max (0 88±0 32)h, t 1/2ka (0 14±0 07)h, t 1/2ke (2 71±0 93)h, AUC 0～∞ (33 14±5 67)mg·h·L -1 ,MRT (3 60±0 10)h, respectively CONCLUSION: The relative bioavailability of the test preparation was (108 29±22 15)% to the reference preparation, indicating that the two kinds of preparations are bioequivalent preparations