卡维迪洛尔制药共晶:制备,高级表征和溶解行为
Angelica Sharapova1, Marina Ol'khovich2, Svetlana Blokhina2
1Institute of Solution Chemistry, Russian Academy of Sciences, 1 Akademicheskaya Street, Ivanovo, 153045, Russia. avs@isc-ras.ru.
AAPS PharmSciTech
|January 21, 2026
概括
这项研究通过与新型共构体共同结晶来增强卡维迪醇 (CVD) 的溶解性和溶解性,显著提高了药物释放率,以提高生物可用性.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 物理化学 物理化学
背景情况:
- 卡维迪洛 (Carvedilol,简称CVD) 是一种可溶性差的心血管药物 (BCS II类).
- 提高溶解度和溶解度对于提高心血管疾病生物可用性至关重要.
- 同结晶为制药配方开发提供了一个有前途的战略.
研究的目的:
- 通过联合结晶来提高卡维迪醇 (CVD) 的可溶性和溶解率.
- 为了合成和描述与2-基胺 (2OHBZA) 和4-基胺 (4OHBZA) 的新型卡维迪醇共晶.
- 评估共结晶对心血管疾病溶解动力学和体外药物释放的影响.
主要方法:
- 使用泥方法制备共晶体.
- 通过PXRD,DSC,TGA,FTIR和UV-VIS光谱学进行固态表征.
- 溶解动力学研究使用振动瓶方法和溶解测试仪.
主要成果:
- 成功合成了新型的CVD与2OHBZA和4OHBZA (1:1摩尔比) 的药物联合晶体.
- 同晶体形成被证实是一种由度决定的过程.
- 卡维迪洛尔联合晶体的平衡溶解度明显超过了原始药物的溶解度.
- 在体外释放研究显示,CVD/2OHBZA的2.6倍和CVD/4OHBZA的1.7倍增加,与原始CVD相比.
结论:
- 与2OHBZA和4OHBZA联合结晶显著提高了卡维迪醇的溶解性和溶解率.
- 合成的共同晶体显示出改善的体外药物释放,表明增强的生物可用性.
- 同结晶是一种可行且有前途的方法,用于开发改进的卡维迪醇剂型.
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