吡罗昔康两种给药途径的血药浓度与局部浓度比较  

COMPARISON OF CONCENTRATION OF PIROXICAM IN BLOOD AND LOCAL SITE AFTER TWO ROUTES OF ADMINISTRATION

作　　者：方晓玲[1] 蒋新国[1] 张志如[1] 奚念朱[1] 

机构地区：[1]上海医科大学生物药剂学研究室

出　　处：《药学学报》1995年第3期226-229,共4页Acta Pharmaceutica Sinica

基　　金：1989年国家教委博士点基金

摘　　要：探讨和比较了吡罗昔康以口服和透皮两种途径给药后的血药浓度与局部浓度。将小鼠随机分组，分别给予口服混悬剂０．０７２ｍｇ·ｍｌ－１或透皮凝胶剂１ｍｇ·ｇ－１（或２ｍｇ·ｇ－１）。以ＨＰＬＣ法测定小鼠的血药浓度（Ｃｓ）和局部浓度（Ｃ１）。结果表明，透皮给药以血药浓度计算凝胶剂的相对生物利用度仅为口服混悬剂的１０％。但是透皮给药的Ｃ１／Ｃｓ＝０．１３，远远大于口服给药的Ｃ１／Ｃｓ（０．０１）。透皮给药后，局部药物浓度—时间曲线下面积为１５．８５μｇ·ｈ－１·ｍｌ－１，远远高于口服给药相应值（１．９３μｇ·ｈ－１·ｍｌ－１）。揭示单纯以血药浓度作为局部作用透皮制剂的生物利用度评价标准是不全面的，应同时考察作用部位的药物浓度。The systematic and local concentrations of piroxicam after oral and transdermaladministration were determined and compared. Mice were randomly grouped,and oral suspensions(0.72 mg· ml-1) or transdermal gels 1 mg· ml-1 were given,Systematic concentration (Cs)andlocal concentration(C1) of the drug in each mouse were determined by HPLC method, Aftertranedermal administration of 0.25 mg of piroxicam gels Cmax(s)=8.06μg· ml-1 and AUC0～ 24(s)=58.36μg·h·ml-1 were obtained, whereas after oral administration of 0.026 mg·10g-1 bodyweight of piroxicam suspensions Cmax(s) was 36.82 μg· ml-1 and AUC0～24(s)was 155.59μg·h·ml-1. The C1/Cs ratio(0. 01) through oral route was far lower than the C1/Cs ratio (0.13)through transdermal route, The area under local concentration time curve(15. 85μg·h·ml-1)calculated from transdermal administration was much higher than that from oral administration (1.93μg·h·ml-1).So,it seems to be unreasonable that only serum concentration is taken as a criterion forbioavailability test of piroxicam for local dosage forms,the local drug concentration should also beinvestigated and evaluated.

关 键 词：吡罗昔康 透皮给药 口服给药 血药浓度 

分 类 号：R971.1[医药卫生—药品]