凯托可纳-阿迪皮酸的制药联合晶体:辅助剂兼容性和抗真菌潜力研究
Flavia Martin1, Maria Miclaus1, Ana Maria Raluca Gherman1
1National Institute for Research and Development of Isotopic and Molecular Technologies, 67-103 Donat, 400293, Cluj-Napoca, Romania.
Pharmaceutical research
|September 4, 2025
概括
凯托可纳- 酸联合晶体与大多数药物辅助剂具有良好的兼容性,保持稳定性并增强抗 Candida albicans 的抗真菌活性.
科学领域:
- 制药科学
- 医学化学
- 固态化学
背景情况:
- 凯托可纳 (KTZ) 是一种溶解不良的抗真菌药物.
- 与酸 (AA) 共同结晶可以改善KTZ溶解.
- 开发固体口服剂型需要对辅助剂的兼容性进行评估.
研究的目的:
- 评估基托可纳 - 酸 (KTZ-AA) 同晶体与常见药物辅助剂的兼容性.
- 评估KTZ-AA共晶体的抗真菌潜力.
- 确认KTZ-AA联合晶体在二元混合物中的稳定性.
主要方法:
- 使用差分扫描热量计 (DSC),热重量计分析 (TGA),里埃变换红外光谱 (FT-IR) 和粉末X射线衍射 (PXRD).
- 分析了KTZ-AA联合晶体和辅助剂的二元物理混合物.
- 分子对接研究针对的是Candida albicans的CYP51酶.
主要成果:
- 该KTZ-AA共晶与六种常见的辅助剂相容,没有显示化学相互作用.
- 通过使用乙酸观察到一种脱氧系统,但热分解没有受到影响.
- 在加速储存条件下,共晶保持化学稳定性.
- 与单独使用KTZ相比,在实验中,对CYP51酶的结合 afinity 增加.
结论:
- 基托可纳 - 酸联合晶体适用于开发固体口服剂型.
- 共同晶体提供了更好的抗真菌活性和稳定性.
- 这种联合晶体为传统可纳配方提供了有希望的替代品.
相关概念视频
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.9K
Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
1.9K
Methods for Studying Drug Absorption: In vitro
327
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...
327
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
258
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...
258
Factors Influencing Drug Absorption: Pharmaceutical Parameters
190
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...
190
Factors Influencing Drug Absorption: Drug Dissolution
690
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...
690
Factors Influencing Drug Absorption: Physicochemical Parameters
425
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...
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
425


