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。
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 withβ-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 was172%. 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.
出处
《中国实验方剂学杂志》
CAS
CSCD
北大核心
2016年第21期1-5,共5页
Chinese Journal of Experimental Traditional Medical Formulae
基金
河北省高等学校科学技术研究项目(QN20131011)
河北省自然科学基金青年基金项目(20130142)
河北医科大学2013科研骨干人才培育计划项目(0621090001)
关键词
斑蝥素
壳聚糖
卡波姆
胃黏附
片剂
cantharidin
chitosan
carbomer
stomach bioadhesive
tablets
