优喘平在人体内药物动力学及体内外相关性  

The pharmacokinetic of Protheo tablets and Its Relevance of Release in vitro to Absorption in vivo

作　　者：石克成[1] 曹世珍[1] 程远远[1] 李俊杰[1] 黄佩琨[1] 

机构地区：[1]广州暨南大学医学院第一附属医院

出　　处：《中国医院药学杂志》1998年第2期53-54,共2页Chinese Journal of Hospital Pharmacy

摘　　要：以紫外分光光度法测定优喘平体外释放度，结果表明优喘平在各介质（ｐＨ１～８．４）释药量恒定；以荧光偏振免疫法测定血药浓度，６名志愿者单剂量口服４００ｍｇ·ｄ－１，Ｔｍａｘ１２．７±２．７６ｈ，Ｃｍａｘ３．８±０．９μｇ·ｍｌ－１，Ｔ１／２１１．８±６．２ｈ，ＡＵＣ６３．５±２９．３μｇ·ｈ·ｍｌ－１；多剂量口服４００ｍｇ·ｄ－１，显示间隔２４ｈ用药，茶碱血清浓度差异无显著性，可维持治疗血药浓度（５～１０μｇ·ｍｌ－１）；体外释药量与体内吸收量呈良好的相关性。The release of Protheo tablets(theophylline sustainedrelease tablet)in vitro was measured by UV spectrometry,the results indicated that the amount of release was constant in different media(pH1～8.4);the serum concentration was measured by TDx analyzer.After a single dose of 400mg Protheo tablets,Tmaxwas 12.7±2.76h、Cmax3.8±0.9μg/ml、t1/211.8±6.2h、AUC63.5±29.3μg/ml;After once daily dose of 400mg for five days,the serum concentration of theophylline showed no significant difference at an interval of 24h,remains to be 5～10μg/ml.The release in vitro is highly relevant with absorption in vivo.

关 键 词：茶碱 药物动力学 相关性 血药浓度 

分 类 号：R974.3[医药卫生—药品] R969[医药卫生—药学]