Preparation and Evaluation of Releasing Properties  of Oxymatrine Colonic Localization Tablets

LU Xiao-hui; ZHOU Yi-sheng; LV Jie; LIANG Mei-yi; HUANG Yun-ran

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Preparation and Evaluation of Releasing Properties of Oxymatrine Colonic Localization Tablets

更新时间：2024-01-04

- Preparation and Evaluation of Releasing Properties of Oxymatrine Colonic Localization Tablets
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 17, Issue 17, Pages: 33-36(2011)
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- Published：2011
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LU Xiao-hui, ZHOU Yi-sheng, LV Jie, et al. Preparation and Evaluation of Releasing Properties of Oxymatrine Colonic Localization Tablets[J]. Chinese journal of experimental traditional medical formulae, 2011, 17(17): 33-36.
DOI：

LU Xiao-hui, ZHOU Yi-sheng, LV Jie, et al. Preparation and Evaluation of Releasing Properties of Oxymatrine Colonic Localization Tablets[J]. Chinese journal of experimental traditional medical formulae, 2011, 17(17): 33-36. DOI：

摘要

目的: 制备pH依赖、酶触和时间三重控制的苦参素结肠定位片释药系统

并考察其体外释放度。方法: 从内到外分别以羟丙甲纤维素和聚乙二醇作为隔离层

以渗透型丙烯酸树脂Eudaragit RS 30D和Eudaragit RL 30D混合溶液作为时滞层

以渗透型丙烯酸树脂Eudaragit RS 30D

Eudaragit RL 30D和壳聚糖的混合溶液作为酶触层

以pH依赖型丙烯酸树脂Eudaragit L100-55的水分散体雅克宜作为外层肠溶层。考察了包衣片在体外模拟人体胃肠道环境中的释药情况。结果: 制备的苦参素结肠定位片在pH 1.2模拟胃液中2 h不释药

在pH 6.8模拟小肠液中6 h释药量小于10%

在模拟结肠液中8 h部分释放或大部分释放。结论: 所制备的苦参素结肠定位片具有良好的结肠定位效果。

Abstract

Objective: To prepare oxymatrine colonic localization tablets controlled by pH-dependent

colonic microflora-activated and time-dependent effects

and evaluated its release characteristics in vitro. Method: The oxymatrine colonic localization tablets were coated from inside to outside with isolated layer of HPMC and PEG6000

time-dependent layer of the mixed solution with Eudargit RS 30D and Eudargit RL 30D

enzyme-triggering layer of chitosan and Eudargit RS 30D/RL 30D

outermost enteric coating layer of Acryi-EZE.And investigated conditions of the coated tablets released in artificial gastrointestinal fluid in vitro. Result: The oxymatrine colonic localization tablets didn't release in simulated gastric fluid(pH 1.2) within 2 hours

the accumulative release was less than 10% in the simulated intestinal fluid within 6 hours

whereas it released mostly in the similated colon fluid(pH 6.0) within 8 hours. Conclusion: This study reveals that oxymatrine colon targeting tablets can delivery effectively in the specific location of colon.

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