·制剂研究·

解毒止泻结肠缓释微丸释放度的方法学研究

武小赟，马静，王俊涛，夏成夫，赵小鹏

(百花医药集团股份有限公司，贵州 遵义 563000)

摘要：目的建立解毒止泻结肠缓释微丸释放度的检查方法并进行方法学验证。方法采用高效液相色谱法测定制剂中槲皮素的含量，参照《中国药典》2010年版的规定研究本制剂的释放度检查方法并进行方法学验证。结果依次在人工胃液、人工肠液、人工结肠液中对微丸进行释放度考察，人工胃液2 h不释放，人工肠液3 h内释放在15%以内，人工结肠液5 h释放完全。结论该法简单、灵敏、准确，可有效监控本品的质量。

关键词：微丸；结肠定位；释放度

基金项目：贵州省中药现代化科技产业研究开发专项(No.S2012ZP00503644369)

作者简介：武小赟，女，研究方向：中药化学及中药制剂，E-mail：wuxiaoyunbingxue@163.com

中图分类号：R944.9文献标识码：A

Study on the dissolution of Jiedu Zhixie Colon-targeted Sustained-release Pellets

WUXiao-yun,MAJing,WANGJun-tao,XIACheng-fu,ZHAOXiao-peng

(BaihuaMedicalPharmaceuticalGroupCo.,Ltd.,Zunyi563000,China)

Abstract：ObjectiveTo establish a method for the dissolution of Jiedu Zhixie Colon-targeted Sustained-release Pellets,and prove that the method is reliable and durable.Methods The content of quercetin was determined by HPLC,the dissolution test of pellets was researched and avalidated according to requirement in China Phannacopeia 2010 Edition.Results The release in vitro was studied in the artificial gastric fluid,artificial intestinal fluid and artificial colon fluid in sequence.Quercetin was not released in artificial gastric fluid,less than 15% in artificial intestinal fluid,slowly in artificial colon fluid and completely at 5 h.Conclusion This method was simple,sensitive and accurate.It can be used for the quality control of pellets.

Key words:Pellet；Colon-targeted；Release

溃疡性结肠炎(ulcerative colitis，UC)属于炎症性肠病的一种，是消化内科常见病。多为直肠和结肠的慢性非特异性炎症性病变，多呈反复发作的慢性过程，其发病机制尚不明确，治疗难度大。当前临床治疗手段繁多，有肠内营养、西药和中药药物治疗、手术治疗、生物靶向治疗、干细胞移植等疗法[1]。解毒止泻结肠缓释微丸由单一苗药对坐叶组成，对坐叶为茜草科植物对坐叶HedyotisuncinellaHook.et Arn．的干燥全草，夏、秋二季采收，具有清热解毒、调中止泻之功效，用于治疗腹泻、腹胀、腹痛、里急后重以及痢疾、急慢性胃肠炎等证[2]。该味药材在治疗胃肠道疾病方面具有独到疗效。将其开发制成结肠缓释制剂，使药物主要在结肠定位缓慢释放，提高结肠病变部位的药物浓度，发挥治疗结肠炎的最佳疗效，为中药新型结肠靶向给药系统的研究积累实验基础。……