基于晶工程的基因斯坦的最佳溶解度和生物可用性
Zhipeng Wang1, Qi Li1, Qi An1
1Beijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, 100050, People's Republic of China.
Natural products and bioprospecting
|September 13, 2023
概括
吉尼斯与皮佩拉的共同晶体增强了溶解性和生物可用性,克服了配方挑战. 这种晶工程方法提供了一种绿色方法来改善天然产品的药物输送.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 药物运输 药物运输 药物运输
背景情况:
- 热尼斯坦在各种疾病中显示出有前途的健康益处,但其溶解性和生物可用性较差.
- 这些局限性阻碍了其临床应用和市场发展,需要制定策略.
研究的目的:
- 为了提高基因斯坦的溶解性和生物可用性.
- 准备和表征一个用cocrystal工程原理的genistein-piperazine联合晶体.
主要方法:
- 通过溶剂辅助研磨制成的晶制剂.
- 使用单晶X射线衍射,粉末X射线衍射,FTIR,DSC和TGA进行表征.
- 稳定性,溶解性和生物利用性的评估.
主要成果:
- 成功制备和确认了基因斯坦-皮佩拉共晶.
- 证明了基尼斯坦的可溶性和生物可用性的改善.
- 系统的调查,包括准备,表征和财产评估.
结论:
- 晶工程为优化天然产品的制药特性提供了一种有效的绿色策略.
- 基因斯坦-皮帕拉共晶显示出改善药物配方和输送的潜力.
- 这项研究提供了一种全面的方法来开发基于天然产品的治疗方法.
相关概念视频
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
229
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...
229
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.5K
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...
1.5K
Factors Affecting Solubility
33.5K
Compared with pure water, the solubility of an ionic compound is less in aqueous solutions containing a common ion (one also produced by dissolution of the ionic compound). This is an example of a phenomenon known as the common ion effect, which is a consequence of the law of mass action that may be explained using Le Chȃtelier’s principle. Consider the dissolution of silver iodide:
33.5K
Factors Influencing Drug Absorption: Physicochemical Parameters
322
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...
322
Solubility Equilibria: Overview
710
When a substance such as sodium chloride is added to water, it dissolves, forming an aqueous solution. The extent of dissolution is called solubility. The process of dissolution can exist in equilibrium, just like other chemical processes. Solubility equilibria are also called precipitation equilibria because the process of solubility can be reversible. The reverse of the solubility process is called precipitation.
Solubility is important in biological and environmental processes. A notable...
Solubility is important in biological and environmental processes. A notable...
710
Recrystallization: Solid–Solution Equilibria
1.1K
Recrystallization is a purification technique used to separate impurities from solid compounds. In this technique, no chemical reactions occur. Instead, it exploits physical properties only, specifically, the solubility differences between the desired compound and impurities, either at a single temperature or at different temperatures, and under other selected conditions. The solid-solution equilibrium (solubility equilibrium) of each component in the solution represents a binary phase...
1.1K


