对乙酰氨基酚（扑热息痛）PVP片的药代动力学及生物利用度研究  

PHARMACOKINETICS AND BIOAVAILABILITY OF TABLET PVP-ACETAMINOPHEN IN HEALTHY VOLUNTEERS AFTER A SINGLE ORAL DOSE STUDY

作　　者：赵奕[1] 阮邹荣[1] 袁虹 周莹[1] 丁德云[1] 

机构地区：[1]浙江医科大学临床药理研究所

出　　处：《中国临床药理学杂志》1995年第4期229-233,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：本文建立了高效液相色谱法测定人血清中的对乙酰氨基酚浓度，结果表明该方法精密度高，灵敏度好，线性关系良好，ｒ＝０．９９９８（ｎ＝６），最低检测浓度为０．１ｍｇ／ｌ，平均日内和日间变异系数＜９％。８名健康志愿者交叉口服对乙酰氨基酚片和对乙酰氨基酚ＰＶＰ片，药代动力学参数分别为，Ｋａ：１．８６±０．９５，３．２３±２．６０１／ｈ；Ｔ１／２：３．１７±１．１３，２．７０±０．８５ｈ；Ｃｍａｘ：７．５６±２．０８，８．２４±１．３７ｍｇ／ｌ；Ｔｐｋ：１．０６±０．３９，０．７９±０．３０ｈ，ＡＵＣ：３２．９１±８．４５，３４．２５±８．４５ｍｇ·ｈ^（－１）·ｌ^（－１）。两种片剂的药代动力学参数（除Ｋａ值外）均无显著性差异，Ｐ＞０．０５。其中对乙酰氨基酚ＰＶＰ片吸收明显快于对乙酰氨基酚（Ｐ＜０．０５）。平均生物利用度为１０４．０７％，两种片剂生物等效。The pharmacokinetics and bioavailability of tablet acetaminophen and PVP-acetaminophen were studied in 8 healthy volunteers.The HPLC assay method has high selectivity and reproducibility.The relation between the ratio of hight and concentration was very good r=0.9998.The lower limit of detection was 0.1mg/l.The average of within-day and between-day CV was <9%.The pharmacokinetic parameters showed that there was no significant difference between the two formations except Ka which were 3.25±2.60,1.87±0.95 h￣(-1). The concentration-time curve fitted in with two-compartment model.The pharmacokinetic parameters of control and PVP formation were:T1/2:3.17 ± 1.13,2.70 ± 0.85 h ; Cmax:7.56±2.08,8.24 ±1.37 mg/l;Tpk:1.06±0.39,0.79±0.30 h; AUC:31.91±8.45,34.25±8.45 mg·h￣(-1)·l￣(-1) respectively. The absorption rate for PVP-acetaminophen was faster than acetaminophen,(P<0.05).The average data of bioavailability was 104.07%,so it demonstrated that both formations had bioequivalence.

关 键 词：扑热息痛 药代动力学 生物利用度 

分 类 号：R971.1[医药卫生—药品]