聚合物结构和酸性群密度对无形固体分散中的盐形成程度的影响
Amy Lan Neusaenger1, Caroline Fatina1, Junguang Yu1
1School of Pharmacy, University of Wisconsin, 777 Highland Ave., Madison, Wisconsin 53705, United States.
Molecular pharmaceutics
|June 17, 2024
概括
无形药物聚合物盐提供增强的稳定性和快速释放,盐的形成主要是由聚合物酸性群密度决定的,而不是结构. 这指导了无形固体分散的聚合物选择.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 聚合物化学 聚合物化学
背景情况:
- 无形药物聚合物盐表现出更好的稳定性和溶解概况.
- 盐的形成程度对于实现这些好处至关重要.
- 了解控制盐形成的因素是配方开发的关键.
研究的目的:
- 为了研究 lumefantrine (LMF) 和各种酸性聚合物之间的盐形成.
- 为了比较泥合成与传统方法的有效性.
- 确定聚合物酸性群密度和结构对盐形成的影响.
主要方法:
- 用于在室温下形成盐的泥合成.
- 非水性定位以确定聚合物酸性群密度.
- 射线光电子光谱 (XPS) 用于量化LMF质子化程度.
主要成果:
- 泥合成产生了比热挤出或旋转蒸发更完整的盐形成.
- 聚合物对LMF的质子化能力各不相同,但质子化程度与可用的酸性群度相关.
- 盐形成程度主要由酸性群密度控制,而不是聚合物结构.
结论:
- 酸性群密度是无形药物聚合物系统中盐形成程度的主要决定因素.
- 泥合成是制备无形药物聚合物盐的有效方法.
- 这些发现有助于选择最佳的聚合物来控制无形固体分散中的电离.
相关概念视频
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
295
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...
295
Polymer Classification: Crystallinity
2.8K
Unlike ionic or small covalent molecules, polymers do not form crystalline solids due to the diffusion limitations of their long-chain structures. However, polymers contain microscopic crystalline domains separated by amorphous domains.
Crystalline domains are the regions where polymer chains are aligned in an orderly manner and held together in proximity by intermolecular forces. For example, chains in the crystalline domains of polyethylene and nylon are bound together by van der Waals...
Crystalline domains are the regions where polymer chains are aligned in an orderly manner and held together in proximity by intermolecular forces. For example, chains in the crystalline domains of polyethylene and nylon are bound together by van der Waals...
2.8K
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
Polymer Classification: Architecture
2.7K
Polymers are classified as linear or branched on the basis of their chain architecture. The polymer chains in linear polymers have a long chain-like structure with minimal to no branching at all. Even if a polymer features large substituent groups on the monomer, which appear as branches to the skeleton, it is not considered a branched polymer. A branched polymer contains secondary polymer chains that arise from the main polymer chain. The branching occurs when the polymer growth shifts from...
2.7K
Ionic Strength: Effects on Chemical Equilibria
1.4K
The addition of an inert ionic compound increases the solubility of a sparingly soluble salt. For example, adding potassium nitrate to a saturated solution of calcium sulfate significantly enhances the solubility of calcium sulfate. Le Châtelier's principle cannot predict this shift in the equilibrium. Instead, this could be explained in terms of changes in the effective concentration of the ions in solution in the presence of added inert salt.
In this solution, the primary...
In this solution, the primary...
1.4K
Polymers: Molecular Weight Distribution
3.3K
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.
3.3K


