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.
出处
《药学学报》
CAS
CSCD
北大核心
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
关键词
吡罗昔康
透皮给药
口服给药
血药浓度
Piroxicam
Transdermal administration
Oral administration
