Suppr超能文献

[两种给药途径后吡罗昔康血液及局部浓度的比较]

[Comparison of concentration of piroxicam in blood and local site after two routes of administration].

作者信息

Fang X L, Jiang X G, Zhang Z R, Xi N Z

机构信息

Division of Biopharmaceutics, Shanghai Medical University.

出版信息

Yao Xue Xue Bao. 1995;30(3):226-9.

PMID:7639082
Abstract

The systematic and local concentrations of piroxicam after oral and transdermal administration 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) and local concentration (C1) of the drug in each mouse were determined by HPLC method. After transdermal administration of 0.25 mg of piroxicam gels Cmax(s) = 8.06 micrograms.ml-1 and AUC(s)0-24(s) = 58.36 micrograms.h.ml-1 were obtained, whereas after oral administration of 0.026 mg.10 g-1 body weight of piroxicam suspensions Cmax(s) was 36.82 micrograms.ml-1 and AUC(s)0-24 was 155.59 micrograms.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 (15.85 micrograms.h.ml-1) calculated from transdermal administration was much higher than that from oral administration (1.93 micrograms.h.ml-1). So, it seems to be unreasonable that only serum concentration is taken as a criterion for bioavailability test of piroxicam for local dosage forms, the local drug concentration should also be investigated and evaluated.

摘要

测定并比较了吡罗昔康经口服和透皮给药后的系统浓度和局部浓度。将小鼠随机分组,分别给予口服混悬液(0.72mg·ml-1)或透皮凝胶(1mg·ml-1)。采用高效液相色谱法测定每只小鼠体内药物的系统浓度(Cs)和局部浓度(C1)。经皮给予0.25mg吡罗昔康凝胶后,Cmax(s)=8.06μg·ml-1,AUC(s)0-24(s)=58.36μg·h·ml-1;而口服给予0.026mg·10g-1体重的吡罗昔康混悬液后,Cmax(s)为36.82μg·ml-1,AUC(s)0-24为155.59μg·h·ml-1。经口服途径的C1/Cs比值(0.01)远低于经透皮途径的C1/Cs比值(0.13)。经皮给药计算所得的局部浓度-时间曲线下面积(15.85μg·h·ml-1)远高于口服给药(1.93μg·h·ml-1)。因此,仅以血清浓度作为吡罗昔康局部剂型生物利用度测试的标准似乎不合理,还应研究和评估局部药物浓度。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验