Ursodeoxycholic 酸纳米悬浮的配方和表征基于自下而上的技术和盒子内设计优化
Oriana Boscolo1,2,3, Sabrina Flor1,2,3, Leandro Salvo1,2
1Universidad de Buenos Aires, Facultad de Farmacia y Bioquímica, Departamento de Tecnología Farmacéutica, Buenos Aires C1113AAD, Argentina.
Pharmaceutics
|August 26, 2023
概括
这项研究使用沉超声波开发了ursodeoxycholic acid (UDCA) 纳米悬浮,显著改善了小儿胆固醇性肝病治疗的口服吸收和生物可用性.
科学领域:
- 制药纳米技术 制药纳米技术
- 药物输送系统 药物输送系统
- 儿科药理学 儿科药理学
背景情况:
- 乌尔索多氧胆酸 (UDCA) 对于儿科胆固醇肝胆道疾病至关重要,但由于溶解性低 (BCS II 类),口服吸收不佳.
- 现有的UDCA配方在儿童群体中实现最佳治疗疗效方面存在挑战.
- 改善UDCA的可溶性,溶解性和生物利用性对于有效治疗至关重要.
研究的目的:
- 使用沉超声波方法设计和优化UDCA纳米悬浮.
- 提高UDCA的可溶性,溶解率和口服生物可用性.
- 开发一个适合儿科用药的剂型.
主要方法:
- 采用了Box-Behnken设计,以优化纳米悬浮颗粒大小的稳定器百分比,振幅和超声波时间.
- 沉超声波方法涉及将UDCA溶解在乙:PEG 400中,并将其纳入HPMC E-15水性分散液中.
- 纳米悬浮用DLS,XRD,SEM进行了表征;稳定性,含量,体外溶解和大鼠口服生物可用性进行了评估.
主要成果:
- 优化的纳米悬浮 (0.3%稳定剂,50W,5分钟) 实现了352.4nm的粒子大小,具有良好的稳定性和含量.
- 试管溶解显示了86%的UDCA释放,大鼠的口服生物可用性与商业药片相当,但结果更一致.
- 药物动力学分析显示,纳米悬浮剂的AUC明显高于商用药片 (p < 0.02).
结论:
- 开发的UDCA纳米悬浮是一种适合儿科患者的剂量形式.
- 该纳米悬浮配方显示了UDCA的充分吸收和改善的口服生物可用性.
- 这种方法提供了一种有希望的策略,可以增强UDCA等溶解不良药物的治疗潜力.
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