合成,表征,生物可用性和抗微生物研究,以塞福洛キシ姆为基础的有机盐和离子液体
Francisco Faísca1, Željko Petrovski1, Inês Grilo2
1LAQV-REQUIMTE, Department of Chemistry, NOVA School of Science and Technology, NOVA University of Lisbon, 2819-516 Caparica, Portugal.
Pharmaceutics
|October 26, 2024
概括
研究人员开发了新型的素有机盐,以增强药物输送. 一种盐,[PyC10Py][CFX]2,保持了抗菌活性,并显著改善了水溶性,为黄素的使用提供了有希望的替代品.
科学领域:
- 制药化学 制药化学 制药化学
- 药物输送系统 药物输送系统
- 药用化学 医学化学
背景情况:
- 诸如 cefuroxime 等药物的低口服生物可用性限制了临床疗效和施用途径.
- 素通常以素乙烯的形式使用,因此需要额外的步骤来激活.
- 形成活性药物成分 (API) 的有机盐是一种提高药物的可溶性和透性的策略.
研究的目的:
- 为了准备和表征新型有机盐的 cefuroxime.
- 为了评估这些素盐的物理化学性质,细胞活力和抗菌活性.
- 为了识别具有更好的溶解性,透性和保持有效性的 cefuroxime盐.
主要方法:
- 通过缓冲辅助中和,利用金和伊米达离子合成五种氧化有机盐.
- 在37°C的水溶性和八醇-水分区系数的评估.
- 在体外评估对*大肠杆菌*,*P. aeruginosa*和*B. subtilis*的抗菌活性.
- 使用3T3细胞进行细胞活力研究.
主要成果:
- 与原始药物相比,Cefuroxime有机盐具有8至200倍的水溶性.
- 大多数盐在体外失去了抗菌活性,但[PyC10Py][CFX]2保留了对测试细菌的活性.
- 具有较长基链的盐表现出较高的细胞毒性;物理化学性质随着离子结构的变化而变化.
结论:
- 有机盐的形成是一种有效的策略,可以提高素的水溶性.
- 锡素盐[PyC10Py][CFX]2显示出因抗菌活性保留和可溶性增强而改善药物输送的潜力.
- 仔细选择对抗基因对平衡溶解性,透性和生物活性至关重要,同时最大限度地降低细胞毒性.
相关概念视频
02:55Solubility of Ionic Compounds
62.6K
Solubility is the measure of the maximum amount of solute that can be dissolved in a given quantity of solvent at a given temperature and pressure. Solubility is usually measured in molarity (M) or moles per liter (mol/L). A compound is termed soluble if it dissolves in water.
62.6K
01:21Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism
288
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...
288
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
179
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...
179
01:19Ionic 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
02:54Ions as Acids and Bases
23.6K
Salts with Acidic Ions
Salts are ionic compounds composed of cations and anions, either of which may be capable of undergoing an acid or base ionization reaction with water. Aqueous salt solutions, therefore, may be acidic, basic, or neutral, depending on the relative acid-base strengths of the salt’s constituent ions. For example, dissolving the ammonium chloride in water results in its dissociation, as described by the equation:
Salts are ionic compounds composed of cations and anions, either of which may be capable of undergoing an acid or base ionization reaction with water. Aqueous salt solutions, therefore, may be acidic, basic, or neutral, depending on the relative acid-base strengths of the salt’s constituent ions. For example, dissolving the ammonium chloride in water results in its dissociation, as described by the equation:
23.6K
01:12Ionic Strength: Overview
1.3K
The ionic strength of a solution is a quantitative way of expressing the total electrolyte concentration of a solution. This concept was first introduced in 1921 by two American physical chemists, Gilbert N. Lewis and Merle Randall, while describing the activity coefficient of strong electrolytes. During the calculation of ionic strength (I or μ), all the cations and anions are considered. However, the concentration (c) of an ion with a greater charge number (z) has a greater contribution...
1.3K