制备和体外/体内特征持续释放的西普罗夫洛素-卡拉基南复合物
Samaa Abdullah1, Ahmad Bani-Jaber2, Nabil A Alhakamy3
1Health Sciences Research Centre, Princess Nourah bint Abdulrahman University, Riyadh 84428, Saudi Arabia.
概括
这项研究开发了一种持续释放矩阵,使用西普洛素 (Cipro) 和羊-卡拉基 (CRG) 复合. 与即时释放片相比,Cipro-CRG矩阵表明口服药物吸收时间长,突发释放减少.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 药物输送系统旨在提高治疗疗效和患者的遵守性.
- 聚电解质复合物为受控药物释放应用提供了潜力.
研究的目的:
- 为了研究西普罗夫洛克萨和兰巴卡拉基南之间的药物多电解质复合.
- 为了利用开发的复合物作为持续释放的矩阵,用于ciprofloxacin.
- 评估普洛素 - 卡拉基南矩阵的物理化学,体外和体内性能.
主要方法:
- 使用透析袋方法优化复合,以确定最大结合能力.
- 复杂的特征包括差异扫描热度计,FTIR,XRD和SEM.
- 在0.1M HCl中进行了药物释放,胀和侵蚀研究.
- 在体内药理动力学研究比较Cipro-CRG矩阵与即时释放配方.
主要成果:
- 西普罗夫洛克萨与兰巴卡拉基南的最大结合能力为55% (w/w).
- 复杂化涉及静电相互作用,范德瓦尔斯力和键,导致药物无形化.
- 与自由CRG相比,Cipro-CRG矩阵表现出较少的胀和侵蚀.
- 与Cipro-HPMC相比,Cipro-CRG的体外药物释放显著减少了爆发效应,释放速度较慢.
- 在体内研究表明,缓慢和长时间的口服药物吸收与改变的药理学参数.
结论:
- 对于创建持续释放矩阵来说,西普罗素-兰巴达-卡拉基复合是可行的和有效的.
- 在控制药物释放和延长吸收方面,Cipro-CRG矩阵提供了优势.
- 这种方法有望为开发更好的口服药物输送系统,用于西普洛素.
相关概念视频
01:16Methods for Studying Drug Absorption: In vitro
256
In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
256
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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