pH依赖型黄连总生物碱结肠靶向微丸的制备及其体内外释放性能评价

凌霄; 胡元利; 陈飞龙; 谭晓梅

doi:10.13422/j.cnki.syfjx.2014210024

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pH依赖型黄连总生物碱结肠靶向微丸的制备及其体内外释放性能评价

工艺与制剂 | 更新时间：2024-01-04

- pH依赖型黄连总生物碱结肠靶向微丸的制备及其体内外释放性能评价
- Preparation of Total Alkaloids from Coptidis Rhizoma Colon Targeted Pellets and Evaluation of Its and Release Characteristics
- 中国实验方剂学杂志 2014年20卷第21期页码：24-27
- 作者机构：
- 作者简介：
- 基金信息：
  
  广州市白云区科技计划项目(2011-kz-64);广州市科技计划重大专项(2012Y2-00018-3)
- DOI：10.13422/j.cnki.syfjx.2014210024
  中图分类号： R283.6
- 纸质出版日期：2014
- 稿件说明：
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凌霄, 胡元利, 陈飞龙, 等. pH依赖型黄连总生物碱结肠靶向微丸的制备及其体内外释放性能评价[J]. 中国实验方剂学杂志, 2014,20(21):24-27.

LING Xiao, HU Yuan-li, CHEN Fei-long, et al. Preparation of Total Alkaloids from Coptidis Rhizoma Colon Targeted Pellets and Evaluation of Its and Release Characteristics[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(21): 24-27.
凌霄, 胡元利, 陈飞龙, 等. pH依赖型黄连总生物碱结肠靶向微丸的制备及其体内外释放性能评价[J]. 中国实验方剂学杂志, 2014,20(21):24-27. DOI： 10.13422/j.cnki.syfjx.2014210024.

LING Xiao, HU Yuan-li, CHEN Fei-long, et al. Preparation of Total Alkaloids from Coptidis Rhizoma Colon Targeted Pellets and Evaluation of Its and Release Characteristics[J]. Chinese journal of experimental traditional medical formulae, 2014, 20(21): 24-27. DOI： 10.13422/j.cnki.syfjx.2014210024.

摘要

目的: 制备用于治疗溃疡性结肠炎的pH依赖型黄连总生物碱靶向微丸并对其体内外释放性能进行评价。方法: 采用丙烯酸树脂(eudragit)S100和eudragit L100-55双层包衣制备pH依赖型黄连总生物碱结肠靶向微丸。以盐酸小檗碱为指标进行了体外释放度和大鼠体内释放的初步评价。结果: 体外释放度试验表明盐酸小檗碱在人工胃液中2 h累计释放度<0.1%

在人工小肠液中4 h累计释放度<10%

在人工结肠液中3 h累计释放度>90%;体内试验表明在大鼠体内包衣微丸大部分能完整到达盲肠或结肠部

并在上述部位开始崩解释放。结论: pH依赖型黄连总生物碱靶向微丸能够实现结肠的定向释放。

Abstract

Objective: To prepare pH-dependent total alkaloids from Coptidis Rhizoma colon targeted pellets for treatment of ulcerative colitis and finish its in vitro and in vivo release performance evaluation. Method: Acrylic resin S100(eudragit S100) and eudragit L100-55 double-coated was adopted to prepare colon targeted pellets of total alkaloids from Coptidis Rhizoma.In vitro release and in vivo site-specific drug release of this preparation were evaluated with berberine hydrochloride as index. Result: In vitro release test showed that cumulative release rate of berberine hydrochloride was less than 0.1% in artificial gastric juice after 2 h and less than 10% in artificial intestinal fluid after 4 h

but cumulative release rate in artificial colon juice after 3 h was more than 90%.In vivo test showed that coated pellets could complete arrive to the cecum or colon in rats

and began to disintegrate and release. Conclusion: Colon targeted pellets of total alkaloids from Coptidis Rhizoma can achieve targeted release in the colon.

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