摘要
以紫杉醇(paclitaxel,PTX)注射剂Taxol为对照,通过大鼠药代动力学及在体肠吸收实验考察N-辛基-O,N-羧甲基壳聚糖(OCC)胶束作为PTX口服给药系统的可行性。结果表明,与Taxol相比,PTX-OCC胶束经口给药在大鼠体内的cmax、AUC均显著提高(P<0.05),相对生物利用度为331.4%;PTX-OCC胶束在各个肠段吸收均显著高于Taxol(P<0.05),且十二指肠吸收略优于其他肠段,结肠、空肠和回肠吸收相近,说明OCC胶束具有显著的促吸收效果,作为难溶性药物口服递送载体具有优良的应用前景。
The aim of this study was to investigate the potential feasibility of the N-octyl-O,N-carboxymethyl chitosan（OCC） micelles as oral administration carriers for paclitaxel（PTX） by pharmacokinetics and in situ absorption in rat intestine using Taxol as control.After oral administration of PTX-OCC micelles,the area under the plasma concentration-time curve（AUC） and the maximum concentration（cmax） were significantly larger than those of Taxol（P0.05）.Relative bioavailability for PTX-OCC micelles was 331.4% of that of Taxol.The absorption of PTX-OCC at different segments of intestine was significantly higher than those of Taxol（P0.05）.The apparent absorption rate（Ka） and the effective permeation coefficient（Peff） at the duodenum were a little higher than those of jejunum,ileum and colon（P0.05）.In conclusion,OCC might be a promising carrier for oral administration of poorly water-soluble drugs.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2012年第5期401-405,共5页
Journal of China Pharmaceutical University
基金
国家自然科学基金资助项目(No.81102397)
国家"重大新药创制"科技重大专项资助项目(No.2009ZX09310-004)
天然药物活性组分与药效国家重点实验室资助项目(No.JKGQ201107)~~
关键词
壳聚糖
聚合物胶束
紫杉醇
药代动力学
肠吸收
chitosan
self-assembled polymeric micelle
paclitaxel
pharmacokinetics
intestinal absorption
