Preparation and Evaluation of Cantharidin Gastrointestinal Bioadhesive Tablets

DANG Yun-jie; WANG Guo-jie; DU Yu-kun; HE Xiao-ming; DU Qing

doi:10.13422/j.cnki.syfjx.2016210001

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Preparation and Evaluation of Cantharidin Gastrointestinal Bioadhesive Tablets

更新时间：2024-01-04

- Preparation and Evaluation of Cantharidin Gastrointestinal Bioadhesive Tablets
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 22, Issue 21, Pages: 1-5(2016)
- 作者机构：
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2016210001
  CLC： R943
- Published：2016
- 稿件说明：
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DANG Yun-jie, WANG Guo-jie, DU Yu-kun, et al. Preparation and Evaluation of Cantharidin Gastrointestinal Bioadhesive Tablets[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(21): 1-5.
DOI：

DANG Yun-jie, WANG Guo-jie, DU Yu-kun, et al. Preparation and Evaluation of Cantharidin Gastrointestinal Bioadhesive Tablets[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(21): 1-5. DOI： 10.13422/j.cnki.syfjx.2016210001.

摘要

目的：以卡波姆和壳聚糖为生物黏附材料，制备斑蝥素多单元胃黏附缓释片，以提高斑蝥素的口服生物利用度，并得到平稳持久的释药效果。方法：制备斑蝥素β-环糊精包合物，通过单因素试验筛选黏附材料，正交试验优选斑蝥素胃黏附缓释片的处方，考察该制剂在大鼠体内的黏附性、体外释放度及其在比格犬体内的口服生物利用度。结果：以卡波姆934-壳聚糖（1∶1）为黏附材料，每片黏附片的处方为斑蝥素5 mg，β-环糊精175 mg，卡波姆934 50 mg，壳聚糖50 mg，交联聚维酮80 mg，硬脂酸镁4 mg。斑蝥素胃黏附缓释片在体外3 h时释放度25%~35%，12 h时释放度≥85%。8 h后制剂依然黏附在Wistar大鼠的胃黏膜表面。Beagle犬口服片剂后，药物在体内可缓慢、持久释放，相对生物利用度172%。结论：体内、外研究表明制备的斑蝥素黏附片具有良好的胃黏附性能和缓释特性，且血药浓度平稳持久，生物利用度显著提高。

Abstract

Objective: In order to improve the oral bioavailability of cantharidin and get in vivo sustained release effect

carbomer and chitosan were used as bioadhesive materials to prepare stomach bioadhesive sustained release tablets of cantharidin. Method: Cantharidin was firstly prepared into inclusion with β-cyclodextrin to increase its solubility.Adhesive materials were screened by single factor tests.Orthogonal test was used to optimize prescription of stomach bioadhesive sustained release tablets of cantharidin.Adhesive effect of this preparation in rats was evaluated

in vitro release properties and oral bioavailability in Beagle dogs of this preparation were investigated. Result: Carbomer 934 and chitosan were used as adhesive material.Prescription of each tablet was cantharidin of 5 mg

β-cyclodextrin of 175 mg

carbomer 934 of 50 mg

chitosan of 50 mg

crospovidone of 80 mg

magnesium stearate of 4 mg.In vitro release of cantharidin in stomach bioadhesive sustained release tablets was 25%-35% after 3 h

it was more than 85% after 12 h.The tablets could adhered on surface of the gastric mucosa in Wistar rats after 8 h.The relative bioavailability of cantharidin in Beagle dog was 172%. Conclusion: Adhesive tablets of cantharidin has good stomach bioadhesive properties and sustained release.Cantharidin from the tablets releases stable and durable in Beagle dogs

its bioavailability significantly improves.

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