梅洛西卡姆-氨基酸盐/离子对复合物具有高级可溶性,溶解性和胃安全性
Hamdy Abdelkader1, Adel Al Fatease1, Zeinab Fathalla2
1Department of Pharmaceutics, College of Pharmacy, King Khalid University, Abha, Saudi Arabia.
Pharmaceutical development and technology
|October 18, 2024
概括
氨酸增强了梅洛西卡姆的溶解性和溶解性,显著减少了胃部的副作用. 这项研究强调了阿尔金宁作为一种功能辅助剂,用于改善药物输送和患者安全.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 生物相容性材料 生物相容性材料
背景情况:
- 溶性较差的药物往往表现出低于最佳的生物制药特性.
- 氨基酸是生物相容,低分子量化合物,具有作为功能辅助剂的潜力.
- 梅洛西卡姆是一种非类固醇抗炎药物 (NSAID),具有极低的溶解度和常见的胃部副作用.
研究的目的:
- 为了研究氨酸和氨酸作为 meloxicam 的功能辅助剂的潜力.
- 为了提高梅洛西卡姆的溶解性,溶解率和胃耐受性.
- 阐明 meloxicam 和氨基酸之间的相互作用机制.
主要方法:
- 用沉和物理混合来制备梅洛西卡姆与氨酸和氨酸的固体分散剂.
- 评估了大鼠的药物溶解性,体外溶解和胃的形成.
- 通过对接研究,差分扫描热度计 (DSC),里埃变换红外光谱 (FTIR) 和X射线衍射 (XRD) 进行了相互作用的特征.
主要成果:
- 对接研究表明,阿尔金因和梅洛西卡姆之间形成离子对/盐.
- 梅洛西卡姆的溶解率和溶解率分别增加了3000倍和12倍,与阿尔金因.
- 在老鼠中,阿基尼因的使用可保持胃粘膜的完整性,与单独的梅洛西卡姆不同.
结论:
- 氨酸作为一种功能辅助剂,显著增强了梅洛西卡姆的溶解性和溶解性.
- 氨酸改善了与梅洛西卡姆药物管理相关的胃部副作用.
- 氨酸中的瓜尼丁组在保护胃粘膜方面发挥着作用.
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