相关实验视频

Updated: Jul 5, 2025

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid

Published on: September 20, 2017

使用β-环氧德克斯特林衍生物提高piperine的可溶性和稳定性:计算和实验研究

Saba Ali¹, Phattharapawn Saokaew², Aamir Aman³

¹Center of Excellence in Structural and Computational Biology, Department of Biochemistry, Faculty of Science, Chulalongkorn University, Bangkok, Thailand.

Journal of biomolecular structure & dynamics

|January 23, 2024

概括

使用循环德克斯 (CD) 衍生物改善了皮佩林 (PP) 的溶解性和稳定性. 硫乙β-环氧化 (SBEβCD) 和基β-环氧化 (HPβCD) 显示出对药物应用最有前途的结果.

科学领域:

制药科学制药科学
药物输送系统药物输送系统
自然产品化学自然产品化学

背景情况:

来自黑胡的生物活性化物皮佩林 (PP) 面临着由于水溶性差和紫外线光敏感性而面临的制药限制.
克服这些挑战对于释放皮佩林的治疗潜力至关重要.

研究的目的:

为了研究 piperine 与β-cyclodextrin (βCD) 和其衍生物 (DMβCD,HPβCD,SBEβCD) 的复合.
通过纳入复合体形成来评估piperine的可溶性和稳定性的增强.

主要方法:

使用计算建模和实验技术研究了皮佩林-βCD相互作用.
进行了差分扫描热量计 (DSC) 和可溶性研究,以确认复合物形成并评估稳定性.
对βCD,DMβCD,HPβCD和SBEβCD分析了复杂化行为和稳定常数.

主要成果:

皮佩林与βCD及其衍生物形成了包含复合体,主要是通过范德瓦尔斯相互作用.
由于最佳的原子接触和减少溶剂可访问性,PP/SBEβCD复合体表现出最高的稳定性,其次是PP/HPβCD,由于最佳的原子接触和减少溶剂可访问性.
复杂化发生在1:1的摩尔比率下,与原生βCD相比,SBEβCD和HPβCD显著增加了稳定常数.

结论:

β-环极衍生物,特别是SBEβCD和HPβCD,有效地提高了皮佩林的可溶性和稳定性.
这些发现表明,开发新型药物配方的 piperine 有希望的途径.

关键词:

皮佩林 (Piperine) 是一种天然的糖.在 silico 和 in vitro 研究中.包容性复杂的包容性复杂的可溶性增强提高可溶性的 β-环氧德克斯特林衍生物.

更多相关视频

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs

Published on: July 27, 2022

Using Multiple Light Scattering to Examine the Stability of Phyllanthus emblica L. Extracts Obtained with Different Extraction Methods

Using Multiple Light Scattering to Examine the Stability of Phyllanthus emblica L. Extracts Obtained with Different Extraction Methods

Published on: April 14, 2023

相关概念视频

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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...

Factors Influencing Drug Absorption: Physicochemical Parameters

Factors Influencing Drug Absorption: Physicochemical Parameters

The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...

Factors Influencing Drug Absorption: Pharmaceutical Parameters

Factors Influencing Drug Absorption: Pharmaceutical Parameters

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...

Factors Influencing Drug Absorption: Drug Dissolution

Factors Influencing Drug Absorption: Drug Dissolution

The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

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...

Stability of Substituted Cyclohexanes

Stability of Substituted Cyclohexanes

This lesson discusses the stability of substituted cyclohexanes with a focus on energies of various conformers and the effect of 1,3-diaxial interactions.
The two chair conformations of cyclohexanes undergo rapid interconversion at room temperature. Both forms have identical energies and stabilities, each comprising equal amounts of the equilibrium mixture. Replacing a hydrogen atom with a functional group makes the two conformations energetically non-equivalent.
For example, in...