国产富马酸比索洛尔胶囊的人体相对生物利用度研究  

Relative Bioavailability of Domestic Bisoprolol Hemifumarate Capsule in Healthy Volunteers

作　　者：刘锡钧[1] 陈鹭颖[1] 杨正管[1] 王庆彪[1] 刘莹[1] 裴仁九[1] 翁东明[1] 

机构地区：[1]南京军区福州总医院,福州350001

出　　处：《中国临床药理学杂志》2000年第1期40-42,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：摘要 为了考察富马酸比索洛尔胶囊新剂型的人体生物利用度，本文取１０名男性健康志愿受试者单剂量交叉口服 １０ ｍｇ富马酸比索洛尔胶囊和富马酸比索洛尔片，用高效液相色谱荧光检测法测定血浆富马酸比索洛尔浓度，进行富马酸比索洛尔胶囊的药代动力学和相对生物利用度研究。结果表明：富马酸比索洛尔胶囊和片剂的血药浓度时间曲线图均符合口服吸收二室模型，主要药代动力学参数Ｔｍａｘ分别为２．０５±１．８９ ｈ和２．２０±１．７５ｈ，Ｃｍａｘ分别为６３．２７±１６．０５ μ ｇ·Ｌ－１和５７．４９±１０．４９ μｇ· Ｌ－１， Ｔ１／２β分别为 １２．７９± ２．８６ ｈ和 １３．１１± ３．９３ ｈ， ＡＵＣ０～∞分别为 １３９０．９５±１３９．２２ μｇ·ｈ·Ｌ－１和１３８１．０４± １５１．５６ μｇ·ｈ·Ｌ－１。两种剂型的药代动力学参数经统计学分析无显著性差异（Ｐ＞０．０５）。富马酸比索洛尔胶囊的相对生物利用度为１００．１％±１８．７％，结果提示受试的胶囊剂和对照的片剂生物等效。The pharmacokinetic profiles and the bioavailability of domestic Bisoprolol hemifumarate capsules were studied in 10 healthy male volunteers. A single oral dose of 10mg bisoprolol capsules and tablets were given according to a cross over design. Plasma concentrations were measured by HPLC. The concentration-time curves of the two products of bisoprolol were fitted to a two-comparment model with oral absorption. There was no significant difference in each pharmacokinetic parameters between the capsules and the tablets (P>0.05 ) .Tmax were 2.05 ± 1.89 h and 2.20 ± l.75 h, Cmax were 63.76 ± 16.05 u g · L-1　and 57.49 ± 10.49 ｕ g·L-1, T1/2β were 12.79 ± 2.86 h and 13.11 ± 3.93 h, AUC0~∞ were 1390.95 ± 139.22 μg·h· L-1 and 1381.04 ± 151.56μg　· h· L-1.The relative bioavailability of the bisoprolol capsule to the tablet was l00. 1 % ± 18.7%. These results suggested that the two products are bioequivalent.

关 键 词：富马酸比索洛尔 生物利用度 血药浓度 胶囊剂 片剂 高效液相色谱法 药代动力学 

分 类 号：R969.1[医药卫生—药理学]