Key Research Center of Liver Regulation for Hyperlipemia SATCM/Class III Laboratory of Lipid Metabolism SATCM, Guangdong TCM Key Laboratory for Metabolic Diseases, Guangdong Pharmaceutical University, Guangzhou 510006, China.
Int J Mol Sci. 2013 Dec 13;14(12):24305-19. doi: 10.3390/ijms141224305.
This study aimed to research the preparation and content determination of capsaicin-chitosan microspheres (CCMS) enteric coated tablets. The core tablets were prepared with the method of wet granulation. Nine formulae were designed to determine the optimal formula of the core tablet. Eudragit L100 was used to prepare the CCMS enteric-coated tablets. The effect of enteric coated formulation variables such as content of talc (10%, 25% and 40%), plasticisers (TEC and DBS), dosage of plasticiser (10%, 20% and 30%) and coating weight (2%, 3% and 5%) were evaluated for drug release characteristics. The in vitro release was studied using 0.1 N HCl and pH 6.8 phosphate buffer. Enteric coated tablets without ruptures or swelling behaviour over 2 h in 0.1 N HCl indicated that these tablets showed acid resistance. The accumulated release rate in phosphate buffer (pH 6.8) revealed that the prepared tablets were able to sustain drug release into the intestine and a first-order release was obtained for capsaicin. This research is the first report of the preparation and content determination of CCMS enteric coated tablets. The sustained release behavior of enteric coated formulations in pH 6.8 phosphate buffer demonstrated that it would be a potential drug delivery platform for sustained delivery of gastric irritant drugs.
本研究旨在研究辣椒素-壳聚糖微球(CCMS)肠溶包衣片的制备和含量测定。采用湿法制粒法制备核心片。设计了九个配方,以确定核心片的最佳配方。采用 Eudragit L100 制备 CCMS 肠溶包衣片。考察了滑石粉(10%、25%和 40%)、增塑剂(TEC 和 DBS)、增塑剂用量(10%、20%和 30%)和包衣增重(2%、3%和 5%)等肠溶包衣制剂变量对药物释放特性的影响。采用 0.1N HCl 和 pH6.8 磷酸盐缓冲液进行体外释放研究。在 0.1N HCl 中 2 小时内没有破裂或膨胀的肠溶包衣片表明这些片剂具有耐酸性。在 pH6.8 的磷酸盐缓冲液(pH6.8)中的累积释放率表明,所制备的片剂能够将药物持续释放到肠道中,并且获得了辣椒素的一级释放。本研究是首次报道 CCMS 肠溶包衣片的制备和含量测定。在 pH6.8 磷酸盐缓冲液中的肠溶包衣制剂的持续释放行为表明,它将是一种用于胃刺激性药物持续递送的潜在药物递送平台。