双细胞组合中增强的孕激素口服生物可用性:制造,统计优化和药物动力学研究
Ronak Maheshwari1, Lokesh Kumar Bhatt2, Sarika Wairkar3
1Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, V.L. Mehta Road, Vile Parle (W), Mumbai, Maharashtra, 400056, India.
AAPS PharmSciTech
|February 1, 2024
概括
这项研究开发了新型药物递送系统 - - 孕双体,以显著提高孕的口服生物可用性和持续释放. 优化的配方在老鼠中显示了增强的吸收,为改善孕激素治疗提供了潜力.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物输送系统 药物输送系统
- 生物技术是生物技术.
背景情况:
- 孕激素是一种重要的女性激素,由于其脂爱性质,因此口服生物可用性较差.
- 现有的配方面临着酶降解和有限吸收的挑战.
- 需要新的输送系统来提高口服疗效和治疗潜力.
研究的目的:
- 开发和优化孕激素双体系统,以提高口服生物可用性.
- 为了研究发育的双体体的物理化学特性和体外药物释放.
- 为了评估孕激素双体体的体内药理动力学性能.
主要方法:
- 用胆汁盐的薄膜水化方法制备了孕激素双体体.
- 使用Box-Behnken设计来统计优化脂胆,胆固醇和脱氧化.
- 进行了囊泡大小,泽塔潜力,捕获效率,ATR-FTIR,TEM,体外释放和药理动力学研究.
主要成果:
- 经过优化后的双体体具有239.5nm的大小,zeta潜力为-28.2mV,捕获效率为84.08%.
- ATR-FTIR和TEM证实了成功的孕激素结合和均的囊泡结构.
- 试验室研究显示持续释放 (48小时内90%),药理动力学分析显示,大鼠的口服生物利用率提高了4.287倍和9.75倍.
结论:
- 孕激素双体体是改善口服药物输送的有希望的配方.
- 开发的系统克服了生物利用性差和降解的局限性.
- 这种方法有可能在慢性疾病中增强孕激素治疗.
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