制备和配制具有更好的溶解和稳定性的孕激素Para-aminobenzoic酸共晶体
Thomas Hibbard1, Kenneth Shankland1, Hisham Al-Obaidi1
1School of Pharmacy, University of Reading, Reading RG6 6AD, UK.
概括
一种新的孕激素 (PROG) 与亚胺酸 (PABA) 的联合晶体显著增强了PROG.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 晶体学 晶体学是指结晶学.
背景情况:
- 孕激素 (PROG) 是一种重要的激素,口服生物可用性有限.
- 开发改进的PROG口服配方对于治疗疗效至关重要.
研究的目的:
- 开发一种具有增强溶解性和溶解性质的新型孕激素联合晶体.
- 研究共晶技术在改善口服药物输送方面的潜力.
主要方法:
- 使用CSD协同晶体设计功能的in silico选来识别潜在的协同形成物.
- 通过溶液蒸发和使用X射线衍射,DSC和FTIR进行表征的共同晶体形成.
- 使用液体辅助研磨和评估水溶性,稳定性和溶解的扩大规模.
- 同晶体片与商业PROG囊的比较溶解研究.
主要成果:
- 一个新的PROG-PABA联合晶体成功合成和表征.
- 与PROG单独相比,PROG-PABA联合晶体显著提高了水溶性和溶解率.
- 同晶体在加速条件下表现出良好的稳定性 (75%RH3个月).
- 与PROG-PABA配制的药片显示,PROG溶解的30倍以上的增加与Utrogestan®囊相比,在3小时后.
结论:
- PROG-PABA联合晶体代表了一种有前途的方法,用于增强口服孕激素的输送.
- 共同晶体形成可以克服像孕激素这样的溶解不良药物的生物可用性限制.
- 这一战略有可能开发出更有效的口服PROG配方.
相关概念视频
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