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

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.