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磺胺二甲嘧啶在（乙腈 + 1 - 丙醇）混合溶剂中溶解度的溶解热力学

Dissolution Thermodynamics of the Solubility of Sulfamethazine in (Acetonitrile + 1-Propanol) Mixtures.

作者信息

Delgado Daniel Ricardo, Castro-Camacho Jennifer Katiusca, Ortiz Claudia Patricia, Caviedes-Rubio Diego Ivan, Martinez Fleming

机构信息

Programa de Ingeniería Civil, Grupo de Investigación de Ingenierías UCC-Neiva, Facultad de Ingeniería, Universidad Cooperativa de Colombia, Sede Neiva, Calle 11 No. 1-51, Neiva 410001, Huila, Colombia.

Programa de Ingeniería Agroindustrial, Hidroingeniería y Desarrollo Agropecuario, Facultad de Ingeniería, Universidad Surcolombiana, Neiva 410001, Huila, Colombia.

出版信息

Pharmaceuticals (Basel). 2024 Nov 26;17(12):1594. doi: 10.3390/ph17121594.

DOI:10.3390/ph17121594
PMID:39770436
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11677806/
Abstract

: Solubility is one of the most important parameters in the research and development processes of the pharmaceutical industry. In this context, cosolubility is one of the most used strategies to improve the solubility of poorly soluble drugs, besides allowing to identify some factors involved in the dissolution process. The aim of this research is to evaluate the solubility of sulfamethazine in acetotinitrile + 1-propanol cosolvent mixtures at 9 temperatures (278.15, 283.15, 288.15, 293.15, 298.15, 303.15, 308.15, 313.15, and 318.15 K); a drug used in human and veterinary therapy and two solvents of great chemical-pharmaceutical interest. : The determination was carried out by the shaking flask method and the drug was quantified by UV/Vis spectrophotometry. : The solubility of sulfamethazine increases from pure 1-propanol (solvent in which it reaches its lowest solubility at 278.15 K) to pure acetonitrile (solvent in which it reaches its maximum solubility at 318.15 K), behaving in a logarithmic-linear fashion. : The increase in solubility is related to the acid/base character of the cosolvent mixtures and not to the solubility parameter of the mixtures. The dissolution process is endothermic and favored by the solution entropy, and also shows a strong entropic compensation.

摘要

溶解度是制药行业研发过程中最重要的参数之一。在此背景下，共溶是提高难溶性药物溶解度最常用的策略之一，此外还能确定一些参与溶解过程的因素。本研究的目的是评估磺胺二甲嘧啶在9个温度（278.15、283.15、288.15、293.15、298.15、303.15、308.15、313.15和318.15 K）下在乙腈 + 1-丙醇共溶剂混合物中的溶解度；磺胺二甲嘧啶是一种用于人类和兽医治疗的药物，以及两种具有重要化学制药意义的溶剂。溶解度的测定采用摇瓶法，药物通过紫外/可见分光光度法定量。磺胺二甲嘧啶的溶解度从纯1-丙醇（在278.15 K时达到最低溶解度的溶剂）增加到纯乙腈（在318.15 K时达到最高溶解度的溶剂），呈对数线性关系。溶解度的增加与共溶剂混合物的酸碱性质有关，而与混合物的溶解度参数无关。溶解过程是吸热的，受溶液熵的促进，并且还表现出强烈的熵补偿。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/4eb764a536ea/pharmaceuticals-17-01594-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/96aac7c799ff/pharmaceuticals-17-01594-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/b956990911b2/pharmaceuticals-17-01594-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/84ebb1dc947a/pharmaceuticals-17-01594-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/7880d8dffa7a/pharmaceuticals-17-01594-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/d1d677c8e176/pharmaceuticals-17-01594-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/c1495dd81604/pharmaceuticals-17-01594-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/4eb764a536ea/pharmaceuticals-17-01594-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/96aac7c799ff/pharmaceuticals-17-01594-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/b956990911b2/pharmaceuticals-17-01594-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/84ebb1dc947a/pharmaceuticals-17-01594-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/7880d8dffa7a/pharmaceuticals-17-01594-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/d1d677c8e176/pharmaceuticals-17-01594-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/c1495dd81604/pharmaceuticals-17-01594-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/51e6/11677806/4eb764a536ea/pharmaceuticals-17-01594-g007.jpg

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