配方开发和评估,基PBPK建模和体药动力学研究 clozapine矩阵类型透皮贴片的基PBPK建模和体药动力学研究
Abdul Qadir1, Syed Umer Jan1, Muhammad Harris Shoaib2,3
1Department of Pharmaceutics, Faculty of Pharmacy and Health Sciences, University of Balochistan, Quetta, Pakistan.
这项研究开发了一种优化过皮质矩阵补丁,用于治疗精神分裂症的克洛扎宾. 这种新型贴片表现出良好的稳定性,有效性,并改善了患者的服从性,而不会刺激皮肤.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 克洛扎平是精神分裂症的关键抗精神病药物,但传统的口服药物面临着挑战.
- 通过皮肤递送药物提供了改善患者服药能力和一致的治疗水平的潜力.
- 开发一种稳定有效的透皮克洛沙平贴片需要仔细优化配方变量.
研究的目的:
- 开发和优化用于克洛扎输送的透皮矩阵贴片.
- 调查尤德拉吉特,PEG和油酸对贴片特征的影响.
- 为了验证最优化的配方在体外,体内和体内性能.
主要方法:
- 中央复合设计 (CCD) 用于配方优化.
- 物理化学表征,FTIR,DSC,体外释放和透性研究.
- 在体内药学动力学,在模拟 (GastroPlus TCAT®),皮肤刺激和稳定性测试.
主要成果:
- 优化补丁显示了理想的抗拉强度 (1.220 kg/cm2),流量 (147.376 μg/cm2/h) 和Q24 (94.874%).
- 在体内研究显示,与标准治疗相比,药理动力学结果相似.
- 优化的皮肤贴片是无刺激的,预计保质期为30.41个月.
结论:
- 成功开发和优化了一种矩阵类型的通过皮肤注射的克洛沙平贴片.
- 透皮贴片为精神分裂症管理提供了一个有前途的替代方案,提高了患者的服从性.
- 优化的配方显示出良好的稳定性和治疗潜力.
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