国产羟苯磺酸钙人体生物利用度研究  

Relative Bioavailability of Caecium Dobesilate in Healthy Volunteers

作　　者：卓海通[1] 卜一珊[2] 曹小梅 周燕[1] 常成方[3] 凌树森[1] 

机构地区：[1]南京军区南京总医院临床药理科,南京210002 [2]天津市第一中心医院药学部,天津300192 [3]河南省三门峡市黄河医院药学部,三门峡472000

出　　处：《中国临床药理学杂志》2000年第4期295-297,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：考察国产羟苯磺酸钙人体生物利用度研究。方法：１８名男性健康受试者采用随机分组自身交叉对照实验方法。单剂量分别口服５００ｍｇ进口羟苯磺酸钙胶囊（Ｒ），国产羟苯磺酸钙片剂（Ｔ１）和胶囊剂（Ｔ２）进行人体生物等效性研究。用ＩＩＰＬＣ－荧光检测法测定羟苯磺酸钙血药浓度。本法最小检测浓度０．１５ｍｇ·Ｌ－１，血浆浓度曲线为０．１５－１９．９４ｍｇ·Ｌ－１，绝对回收率＞８２％，日内、日间变异＜３．０％。结果：１８名受试者测得的羟苯磺酸钙血药浓度－时间过程数据用３Ｐ９７程序二房室模型拟合求算药动学参数。参比药和试验药Ｔ１和Ｔ２的主要药代动力学参数为： Ｔ１／２β４．２５±１．１２ｈ， ４．０５ ±１．０９ｈ和３．９３ ± ０．９５ｈ； Ｃ ｍａｘ１３．８９ ± ３．５５ｍｇ·Ｌ－１， １３．１１± ３．７０ｍｇ·Ｌ－１和１３．７７±３．９２ｍｇ·Ｌ－１； Ｔｍａｘ ４．０ ±１．４ｈ， ４．１±１．２ｈ和４．０ ± １．０ｈ； ＡＵＣ０－２４９８．４５ ± ２２．５４ｍｇ· ｈ· Ｌ１， ９４．６２ ± １７．７４ｍｇ· ｈ· Ｌ－１和 ９７．３３ ± ２０．７２ｍｇ· ｈ· Ｌ－１。Ｔ１和Ｔ２的相对生物利用度为９７．７０％和９８．８６％。结论：三种制?OBJECTIVE:To study relative bioavailability of caecicum dobesilate in healthy volunteers. METHODS: This is an open randomized, three-period crossover study in 18 healthy male volunteers. Subjects received a single oral dose of 500 mg calcium dobesilate capsule and tablet produced by imported (R) and domestic (T1,T2). The plasma concentrations of calcium dobesilate were determined by using HPLC-fluorescence detection. RESULTS: The main pharmacokinetic parameters were as follows: T1/2β 4.25 ± 1 .12 h (R), 4.05 ± 1 .09 h (T1) and 3.93 ± 0.95 h (T2); Cmax. 13.89 ±3.55 mg· L-1, 13.11 ± 3.70 mg·L-1 and 13.77 ± 3.92 mg· L-1 Tmax 4.0 ± 1.4 h, 4.1± 1.2 h and 4.0 ± 1.0 h, AUC0-24 98.45 ± 22.54 mg·h· L-1, 94.62 ± 17.74 mg· h· L-1 and 97.33 ± 20.72 mg· h· L-1. The relative bioavailability of test drug were 97.70 ± 13.5%(T1) and 98.86 ± 11 .98%(T2), respectively. CONCLUSION: The results of statistical analysis showed that the three formulations were bioequivalent.

关 键 词：生物利用度 羟苯磺酸钙 生物等效性 药代动力学 

分 类 号：R969.1[医药卫生—药理学]