聚合物类型和比例的综合评估喷雾干燥分散:压缩,溶解和物理稳定性
Dongyue Yu1, Haichen Nie2, Stephen W Hoag1
1University of Maryland, Baltimore, School of Pharmacy, Baltimore, MD 21201, United States.
International journal of pharmaceutics
|December 7, 2023
概括
无形固体分散剂 (ASD) 片的制造能力取决于药物加载和聚合物选择. 较低的药物负载通常会提高可平板性,颗粒表面积是拉伸强度的关键.
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:
- 无形固体分散 (ASDs) 增强难溶性药物的溶解性和生物可用性.
- 药片是ASD的常见剂型,但其制造性尚未完全理解.
- 聚合物类型和药物负载等关键因素需要进一步调查.
研究的目的:
- 为了研究药物加载和聚合物选择对喷雾干燥ASDs的药片化特性的影响.
- 为了评估ASD药片的生理化学和机械特性.
- 确定影响无形制药产品制造能力的关键属性.
主要方法:
- 喷雾干燥无形固体分散剂 (ASDs) 的制备,使用伊特拉科纳 (ITZ) 和印梅他 (IND) 在不同的药物负载下 (10-50%).
- 配方与基甲基纤维素酸糖 (HPMCAS) 和聚烯 (PVP) 作为代表性聚合物.
- 评估颗粒性质 (表面积),压缩行为 (可性,抗拉强度),药物释放和物理稳定性.
主要成果:
- 增加的药物负载减少了大多数自闭症的表面积,除了ITZ-PVP.
- 随着较低的药物负载,药片可用性得到改善,ITZ-PVP是例外.
- 粒子表面积被确定为影响ASD平板电脑拉伸强度的主要因素.
- ITZ-PVP ASDs显示了最差的药物释放和稳定性.
结论:
- 药物装载和聚合物选择显著影响ASD片的制造能力.
- 颗粒表面积是实现所需的平板电脑机械性能的一个关键参数.
- 了解这些关系对于成功下游加工无形药品至关重要.
相关概念视频
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
311
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...
311
Factors Influencing Drug Absorption: Pharmaceutical Parameters
134
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...
134
Polymers: Molecular Weight Distribution
3.4K
For any given polymer, the weight average molecular weight (Mw) is higher than, if not equal to, the number average molecular weight (Mn). The only situation in which the weight average molecular weight and the number average molecular weight are equal is when a polymer consists only of chains with equal molecular weight. However, this never happens in a synthetic polymer, since it is difficult to control the polymerization process up to a molecular level with accuracy to a hundred percent.
3.4K
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
208
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...
208
Polymer Classification: Stereospecificity
2.4K
Polymerization generates chiral centers along the entire backbone of a polymer chain. Accordingly, the stereochemistry of the substituent group has a significant effect on polymer properties. Polymers formed from monosubstituted alkene monomers feature chiral carbons at every alternate position in the polymer backbone. Relative to the predominant orientation of substituents at the adjacent chiral carbons, the polymer can exist in three different configurations: isotactic, syndiotactic, and...
2.4K
Factors Affecting Dissolution: Particle Size and Effective Surface Area
853
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
853


