通过研磨制备的纳布etone-Cyclodextrins复合物的生物制药特性和稳定性
David Klarić1, Željka Soldin1, Anna Vincze2,3
1Department of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102a, 10 000 Zagreb, Croatia.
纳布米 (NAB) 的溶解性和溶解性通过与环极素 (CD) 的复合,特别是基- (HP-β-CD) 和硫乙烯-β-环极素 (SBE-β-CD) 的复合,通过机械化学激活来增强药物递送,显著改善.
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:
- 纳布 (NAB) 是一种不易溶解的非类固醇抗炎前药物 (BCS II类).
- 低溶解度限制了NAB的治疗疗效.
- 已知循环德克斯 (CDs) 可以增强难溶性药物的可溶性.
研究的目的:
- 为了提高nabumetone的可溶性和溶解特性.
- 通过机械化学激活来研究NAB与β-环氧化 (β-CD) 和其衍生物 (HP-β-CD,SBE-β-CD) 的复合.
- 评估由此产生的NAB-CD复合物的物理化学性质和稳定性.
主要方法:
- 与β-CD,HP-β-CD和SBE-β-CD的NAB固体复合物通过机械化学激活 (研磨) 以1:1的摩尔比率进行制备.
- 使用DSC,PXRD和ATR-FTIR证实了复杂化.
- 评估了复合物的可溶性,体外溶解,透性和化学稳定性.
主要成果:
- 与HP-β-CD和SBE-β-CD共同研磨显著提高了NAB在酸性介质中的体外溶解效率 (34.86-58.30倍).
- NAB-CD复合体显示溶解率增加,并在pH值6.8.8时通过生物模拟膜改善质量传输.
- 在照片和长期储存条件下,NAB复合物表现出良好的稳定性,尽管在酸性和氧化应激下观察到降解.
结论:
- 通过研磨制备的含有HP-β-CD和SBE-β-CD的NAB复合物显示出明显改善的溶解性和溶解性.
- 这些NAB-CD复合体显示出增强口服生物可用性的潜力.
- 开发的复合物是制药产品开发的有希望的候选者.
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