中国组织工程研究 ›› 2012, Vol. 16 ›› Issue (16): 2901-2904.doi: 10.3969/j.issn.1673-8225.2012.16.012

• 药物控释材料 drug delivery materials • 上一篇    下一篇

低浓度N-三甲基壳聚糖对依托泊苷经肠黏膜透过性的影响

于金玲1,张铁成2   

  1. 1解放军北京军区天津疗养院,天津市  300382;2上海交通大学,上海市  200240
  • 收稿日期:2012-02-28 修回日期:2012-03-06 出版日期:2012-04-15 发布日期:2012-04-15
  • 作者简介:于金玲,女,1973年生,河北省隆化县人,蒙古族,2002解放军年第一军医大学毕业,主管药师,主要从事临床药学方面的研究。yujinling.1351206@163.com

Modulation effects of low-concentration N-trimethyl chitosan chloride on the permeability of etoposide across different intestinal membranes  

Yu Jin-ling1, Zhang Tie-cheng2   

  1. 1Tianjin Sanatorium of Beijing Military Area Comman of Chinese PLA, Tianjin  300382, China; 2Shanghai Jiao Tong University, Shanghai  200240, China
  • Received:2012-02-28 Revised:2012-03-06 Online:2012-04-15 Published:2012-04-15
  • About author:Yu Jin-ling, Pharmacist in Charge, Tianjin Sanatorium of Beijing Military Area Comman of Chinese PLA, Tianjin 300382, China yujinling.1351206@ 163.com

摘要:

背景:N-三甲基壳聚糖作为透皮吸收促进剂,可以影响口服药物在体内经肠黏膜的透过性。
目的:考察低浓度N-三甲基壳聚糖对依托泊苷经肠黏膜透过性的影响。
方法:使用体外扩散池法评价依托泊苷经肠黏膜经时吸收方向和分泌方向的透过量和透过系数,并测定10%N-三甲基壳聚糖对依托泊苷经肠黏膜透过性的影响。依托泊苷在接受室中的浓度用高效液相色谱法测定。
结果与结论:10%N-三甲基壳聚糖具有增加依托泊苷经吸收方向的透过性,减少经分泌方向的透过性。说明低浓度的N-三甲基壳聚糖可用于改善受P-糖蛋白介导药物的吸收,有望提高此类药物的口服生物利用度。
关键词:依托泊苷;P-糖蛋白; N-三甲基壳聚糖;扩散池;透过性
doi:10.3969/j.issn.1673-8225.2012.16.012

关键词: 依托泊苷, P-糖蛋白, N-三甲基壳聚糖, 扩散池, 透过性

Abstract:

BACKGROUND: N-trimethyl chitosan as a transdermal enhancer can affect the permeability of oral drugs through the intestinal mucosa.
OBJECTIVE: To investigate the modulation effects of N-trimethyl chitosan chloride on the permeability of etoposide across different intestinal membranes.
METHODS: The permeability of etoposide via rat intestinal membranes was evaluated by an in vitro diffusion chamber system after the membranes were isolated from the intestine in rats with or without the co-administration of 10% N-trimethyl chitosan chloride. The concentration of etoposide in the receptor was determined by the high performance liquid chromatography.
RESULTS AND CONCLUSION: With co-administration of N-trimethyl chitosan chloride at a low concentration, the absorptive directed transport of etoposide was significantly increased while its secretory directed transport was decreased. It might be possible to improve the absorption of P-glycoprotein mediated drugs by co-administration of N-trimethyl chitosan chloride at a low concentration, therefore to improve the oral bioavailability of these drugs.

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