聚合物粘合剂类型和度对SMEDDS加载的半孔基颗粒的流量和溶解特性的影响
Mila Kovačević1, Alenka Zvonar Pobirk1, Ilija German Ilić1
1Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, Ljubljana 1000, Slovenia.
概括
这项研究表明,湿颗粒中的聚合物结合剂增强了自我微乳化药物输送系统 (SMEDDS) 颗粒. 优化的SMEDDS带有中孔二氧化的片剂提供快速释放的卡维迪醇,适用于口腔可分散的配方.
科学领域:
- 制药技术 制药技术 制药技术
- 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:
- 自行微乳化药物递送系统 (SMEDDS) 对于提高水溶性差的药物的可溶性和生物利用性至关重要.
- 半孔二氧化是固化SMEDDS的常见助剂,湿颗粒化是生产高负荷,自由流动颗粒的有效技术.
- 聚合物结合物的选择显著影响SMEDDS颗粒的物理化学特性和药物释放概况.
研究的目的:
- 研究六种不同的聚合物结合剂对通过湿颗粒制备的基于半孔二氧化的SMEDDS颗粒的特性的影响.
- 评估粘合剂类型,度和颗粒化方法对卡维迪洛在体外释放的影响.
- 为了优化SMEDDS片剂配方,以获得最大颗粒含量,足够的硬度和适合作为口腔可分散剂型.
主要方法:
- 用六种不同的聚合物结合剂 (povidone K30,K90,copovidone,Pharmacoat® 603,615,MethocelTM K100 Premium LV) 制备SMEDDS颗粒,其中使用半孔和湿颗粒.
- 评价颗粒性质,包括自微乳化特征和体药物释放动力学卡维迪洛.
- 优化SMEDDS药片配方,评估颗粒含量对药片硬度和分解时间的影响.
主要成果:
- 聚合物结合剂使得自由流动的SMEDDS颗粒的生产成为可能,具有保存的自我微乳化特性,并增强了体外卡维迪的释放.
- 较高分子量结合剂导致药物释放速度较慢,而增加的结合剂度 (特别是7.45%的povidone K30) 加快了释放速度,在5分钟内达到100%.
- 与高剪切颗粒相比,手动颗粒化导致卡维迪醇的释放速度更快. 优化的片 (25%颗粒含量) 达到适当的硬度和短解体时间,表明具有可溶解的潜力.
结论:
- 聚合物结合剂通过湿颗粒处理有效地产生稳定和功能性的SMEDDS颗粒,改善药物释放.
- 结合剂的选择和度极大地影响药物释放率,波维K30在最佳度下释放速度最快.
- 优化SMEDDS含有半孔二氧化的片剂是一种有希望的口腔可溶剂剂型,用于像卡维迪醇这样的溶性较差的药物.
相关概念视频
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
154
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
154
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
332
Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
332