开发用于长效注射剂的高度贝达基林悬浮剂
Mads Fahnøe Hansen1, Nadina Zulbeari1, René Holm1
1Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, 5230 Odense, Denmark.
International journal of pharmaceutics
|August 24, 2025
概括
这项研究开发了一种用于治疗结核病的长效注射制剂. 这种新型药物可能持续治疗3个月,改善药物坚持性和预防耐药性.
科学领域:
- 制药科学
- 药物输送系统
- 传染性疾病
背景情况:
- 结核病 (TB) 构成了严重的全球卫生挑战,因患者的不良依赖性和抗药性菌株的增加而加剧.
- 目前的结核病治疗方案漫长而苛刻,导致结果不佳,抗药性出现.
- 长效注射剂 (LAI) 提供了一种改善治疗坚持和疗效的潜在策略.
研究的目的:
- 研究制造高度,长效注射剂 (LAI) 的可行性.
- 评估 LAI bedaquiline fumarate 配方的物理稳定性,药物负载能力和药物动力学特性.
- 评估这种LAI配方作为结核病的新长期治疗策略和预防耐药性的潜力.
主要方法:
- 使用湿媒粉碎制备贝达基林 fumarate 的微和纳米悬浮剂.
- 药物配方被评估为稳定剂的适用性,药物负载能力和六个月的颗粒大小稳定性.
- 在肌肉内注射不同颗粒大小的配方后,对Sprague- Dawley大鼠进行了药理动力学研究.
主要成果:
- 与自由基相比,贝达基林酸盐具有更高的药物载荷能力,使其在可流动液体中的度更高.
- 颗粒大小显著影响了最初的药物释放动力学,较小的颗粒导致更高的血度.
- 所有经过测试的LAI配方在三个月的时间内在老鼠中达到长时间的血度,这表明可能存在更长时间的效果.
结论:
- 开发LAI bedaquiline fumarate配方是可行的,治疗结核病的持续时间为三个月,并且可能具有更长的疗效.
- 在LAI悬浮剂中达到高药载荷时,酸盐形式是有利的.
- 需要进一步研究以优化这些有前途的LAI配方的物理稳定性.
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