关于gliclazide-carplex固体分散剂和用直接可压缩的共同加工辅助剂制备的片剂的物理化学报告
Subrata Paul1, Kaniz Fatema Asha1, Israt Zerin Alam1
1Department of Pharmacy, Faculty of Science, University of Rajshahi, Bangladesh.
Heliyon
|December 11, 2023
概括
这项研究开发了使用固体分散剂 (SD) 和共同加工的辅助剂的改进的gliclazide片剂配方,与商业产品相比,大大提高了药物释放率.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 像gliclazide这样的药物的水溶性差限制了口服生物可用性.
- 固体分散 (SD) 和共同加工的辅助剂是增强药物溶解的策略.
- 为难溶性药物开发有效配方是制药开发中的一个重大挑战.
研究的目的:
- 开发使用带有 carplex 载体的固体分散剂 (SDs) 的 gliclazide 的先进药片配方.
- 将共同加工的辅助成分复合物纳入,以提高gliclazide的释放率.
- 与商业产品相比,评估开发的配方的物理化学性质和体外药物释放.
主要方法:
- 用 carplex 载体使用溶剂蒸发方法制备了 glyclazide 固体分散剂 (SD).
- 共同加工的辅助成分复合物 (SMP和LMPS) 采用共同加工技术制备.
- 使用SD和共同加工的辅助物质制定了片剂批量,并接受了物理化学和体外药物释放测试.
- SDs的表征涉及SEM,DSC,PXRD和FTIR分析.
主要成果:
- 与普通gliclazide相比,gliclazide的SD显示药物释放在30分钟内增加了5-6倍,这归因于无形化和改善的可湿性.
- 所有配方药片 (FGC批) 均表现出令人满意的机械性能,并符合重量变化,易碎性和分解性的综合标准.
- 包括LMPS复合物的FGC-5至8配方表现出卓越的性能,FGC-8在30分钟内释放的药物比市场上销售的产品高3.5倍.
- 稳定性研究表明,在加快条件下储存三个月后,药物含量或释放概况没有显著变化.
结论:
- 基于carplex的SDs和共同加工的辅助剂的组合提供了一种有希望的方法来增强gliclazide释放.
- 这种配方策略可以显著提高水溶性差的药物的治疗疗效.
- 开发的固体剂量形式显示出与现有商业品牌相比的实质优势,用于难以溶解的药物.
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