肠道微囊 封装Roxithromycin-PVP复合核心颗粒,以抑制药物结晶在液化床方法上,用于口服
Nan Liu1, Ling-He Zang2, Dong-Chun Liu3
1School of Pharmacy, Shenyang Pharmaceutical University.
Chemical & pharmaceutical bulletin
|December 22, 2024
概括
内涂层的微囊保护罗西胺 (ROX) 免受胃酸的影响,提高其有效性. 这种新型配方非常适合儿科使用和患有吞问题的患者,表现出极好的稳定性和溶解性质.
科学领域:
- 制药技术 制药技术 制药技术
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- рокситромицин (ROX) 是一种易受酸水解的抗生素,限制了其口服生物利用性.
- 肠膜涂层配方提供了对胃酸的保护,提高了药物的有效性和患者的遵守性.
- 儿童和老年人群经常因吞困难而面临传统口服剂型的挑战.
研究的目的:
- 开发和表征肠涂层微囊的罗西胺素 (ROX) 改善口服输送.
- 为了评估开发的ROX微囊的酸稳定性和溶解概况.
- 评估这种配方对儿科患者和吞障碍患者的适用性.
主要方法:
- 使用聚烯化 (PVP) K30作为粘合剂,制备了罗西胺 (ROX) 层层的核心颗粒.
- 用Eudragit L30 D-55进行液化床涂层 (Wurster工艺),用于肠道涂层.
- 描述涉及粉末X射线衍射,差分扫描热度计,显微镜,抗酸和溶解测试.
主要成果:
- 肠膜涂层有效地抑制了ROX结晶性,将其分散在PVP K30粘合剂中.
- 具有>50%涂层水平和20-25%塑化剂含量的微囊在模拟的胃液中表现出极好的ROX稳定性,持续2小时.
- 该配方在pH 1.2下保护ROX,并在45分钟内在模拟的肠液 (pH 6.8) 中释放超过75%的ROX.
结论:
- 通过Wurster流化床方法制备的肠膜涂层微囊有效地保护罗西斯素免受酸水解.
- 优化的配方表现出有利的溶解特性,确保药物的有效性.
- 这种先进的药物输送系统对制药应用具有重大潜力,特别是对于儿科和消化障碍患者.
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