尼胺酸的二进制和三进制含有复合物:合成,表征和溶解概况
Zohra Bouchekhou1, Amel Hadj Ziane-Zafour1, Florentina Geanina Lupascu2
1Chemical Engineering Laboratory, Process Engineering Department, Faculty of Technology, University of Blida 1, Road of Soumaa, BP 270, Blida 09000, Algeria.
Pharmaceutics
|September 28, 2024
概括
尼胺酸 (NA) 复合与2-基-β-环氧化 (2HP-β-CD) 和基甲基纤维素 (HPMC) 改善了药物的溶解性和溶解性. 纳斯-2HP-β-CD-HPMC复合体显示出最高的复合效率,为增强治疗效率提供了潜力.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 尼酸 (NA) 是一种广泛使用的NSAID,具有较差的溶解性,较低的生物可用性和不良影响.
- 循环德克斯 (CD) 复合是一种提高药物特性的策略,但像NA这样的低分子量药物可能导致复合效率 (CE) 低.
研究的目的:
- 开发NA的纳入复合物与2-基基-β-环氧二二二二二 (2HP-β-CD).
- 研究将NA转化为其盐 (NAs) 的效果,并将基甲基纤维素 (HPMC) 纳入复合物的形成,CE和药物释放.
- 描述开发的复合物的物理化学性质和溶解概况.
主要方法:
- 使用共蒸发溶剂和冷干燥技术制备了包含复合物.
- 使用相位溶解性研究来确定复合效率 (CE) 和结合常量 (Ks).
- 物理化学表征涉及FT-IR,DSC,SEM,XRD,DLS,UV-Vis,1H-NMR和1H-ROESY分析.这些分析对FT-IR,DSC,SEM,XRD,DLS,UV-Vis,1H-NMR和1H-ROESY进行了分析.
主要成果:
- 在所有系统中都证实了复杂的形成,表明药物 - 环氧氨酸相互作用,无形药物状态和形态变化.
- 纳斯-2HP-β-CD-HPMC复合体表现出最高的CE和Ks值,其宿主-客比为1:1.
- 对于开发的包容复合物,特别是NAs-2HP-β-CD-HPMC配方,观察到可溶性和溶解概况的改善.
结论:
- 开发的纳入复合物,特别是NAs-2HP-β-CD-HPMC,显示了NA溶解度和溶解度的显著改善.
- 这种配方有可能提高NA的治疗疗效,同时尽量减少不良影响.
- 这项研究强调了2HP-β-CD和HPMC在开发难溶性NSAIDs的先进药物递送系统中的成功应用.
相关概念视频
01:11Nomenclature of Carboxylic Acid Derivatives: Amides and Nitriles
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Naming Amides
The IUPAC and common names of amides are derived from the parent carboxylic acid, by replacing the suffix “oic acid” and “ic acid,” respectively, with “amide.” In the following example, the IUPAC name ethanamide is derived from ethanoic acid, and the common name, acetamide, is obtained from acetic acid.
The IUPAC and common names of amides are derived from the parent carboxylic acid, by replacing the suffix “oic acid” and “ic acid,” respectively, with “amide.” In the following example, the IUPAC name ethanamide is derived from ethanoic acid, and the common name, acetamide, is obtained from acetic acid.
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01:08Nitriles to Carboxylic Acids: Hydrolysis
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Nitriles undergo acid-catalyzed hydrolysis or base-catalyzed hydrolysis to form a carboxylic acid. These reactions proceed via an amide intermediate.
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01:19Preparation of Carboxylic Acids: Hydrolysis of Nitriles
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Nitriles (R–CN) can be converted into carboxylic acids (R–COOH) upon treatment with aqueous acids, i.e., upon hydrolysis of nitriles. Under base-catalyzed conditions, carboxylate anions (R–COO−) are formed.
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01:28Structures of Carboxylic Acid Derivatives
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Structure of Carboxylic Acid Derivatives
Carboxylic acid derivatives contain an acyl group attached to a heteroatom such as chlorine, oxygen, or nitrogen. The carbonyl carbon and oxygen are both sp2-hybridized with an unhybridized p orbital.
The three sp2 orbitals of the carbonyl carbon form three σ bonds, one each with the carbonyl oxygen, the α carbon, and the heteroatom, whereas the other two sp2 orbitals of the carbonyl oxygen are occupied by the lone pairs. Further, the...
Carboxylic acid derivatives contain an acyl group attached to a heteroatom such as chlorine, oxygen, or nitrogen. The carbonyl carbon and oxygen are both sp2-hybridized with an unhybridized p orbital.
The three sp2 orbitals of the carbonyl carbon form three σ bonds, one each with the carbonyl oxygen, the α carbon, and the heteroatom, whereas the other two sp2 orbitals of the carbonyl oxygen are occupied by the lone pairs. Further, the...
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01:12Preparation of Nitriles
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One of the common methods to prepare nitriles is the dehydration of amides. This method requires strong dehydrating agents like phosphorous pentoxide or boiling acetic anhydride for converting amides to nitriles. Another reagent namely, thionyl chloride also accomplishes the dehydration of amides, where amide acts as a nucleophile. The first step of the mechanism involves the nucleophilic attack by the amide on the thionyl chloride to form an intermediate. In the next step, the electron pairs...
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01:19Diazonium Group Substitution: –OH and –H
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Nitrous acid, a weak acid, is prepared in situ via the reaction of sodium nitrite with a strong acid under cold conditions. This nitrous acid prepared in situ reacts with primary arylamines to form arenediazonium salts. Such reactions are known as diazotization reactions. As shown in Figure 1, the formation of arenediazonium salts begins with the decomposition of nitrous acid in an acidic solution to give nitrosonium ions.
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