{"title":"维生素B2共晶固体溶解度和渗透性的平衡中ph依赖的微物质解离","authors":"Archita Goswami, and , Bipul Sarma*, ","doi":"10.1021/acs.molpharmaceut.4c0151810.1021/acs.molpharmaceut.4c01518","DOIUrl":null,"url":null,"abstract":"<p >The microspecies-specific physicochemical properties of eutectic solids of sparingly water-soluble micronutrient, Vitamin B<sub>2</sub> (Riboflavin), with a few representative BCS drugs, viz., Theophylline, Theobromine, Mesalamine, and Barbituric acid are established. The interplay of solubility and drug permeation behavior is experimentally determined for the eutectic solids, and properties are corroborated with the concomitant relative concentrations of pH-dependent microspecies of Riboflavin and the drugs. Partner drug candidates are selected from different quadrants of BCS classification to apprehend the influence of their solubility on the overall efficacy of the eutectic solids. The coexistence and inseparable ionic, neutral, and/or zwitterionic microspecies are spotted, and the pH-reliant isomer-specific inflection of physicochemical and pharmacokinetic properties in such multicomponent solid formulations is demonstrated.</p>","PeriodicalId":52,"journal":{"name":"Molecular Pharmaceutics","volume":"22 4","pages":"2246–2258 2246–2258"},"PeriodicalIF":4.5000,"publicationDate":"2025-03-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"The pH-Dependent Microspecies Dissociations in the Trade-Off of Solubility and Permeability of Vitamin B2 Eutectic Solids\",\"authors\":\"Archita Goswami, and , Bipul Sarma*, \",\"doi\":\"10.1021/acs.molpharmaceut.4c0151810.1021/acs.molpharmaceut.4c01518\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >The microspecies-specific physicochemical properties of eutectic solids of sparingly water-soluble micronutrient, Vitamin B<sub>2</sub> (Riboflavin), with a few representative BCS drugs, viz., Theophylline, Theobromine, Mesalamine, and Barbituric acid are established. The interplay of solubility and drug permeation behavior is experimentally determined for the eutectic solids, and properties are corroborated with the concomitant relative concentrations of pH-dependent microspecies of Riboflavin and the drugs. Partner drug candidates are selected from different quadrants of BCS classification to apprehend the influence of their solubility on the overall efficacy of the eutectic solids. The coexistence and inseparable ionic, neutral, and/or zwitterionic microspecies are spotted, and the pH-reliant isomer-specific inflection of physicochemical and pharmacokinetic properties in such multicomponent solid formulations is demonstrated.</p>\",\"PeriodicalId\":52,\"journal\":{\"name\":\"Molecular Pharmaceutics\",\"volume\":\"22 4\",\"pages\":\"2246–2258 2246–2258\"},\"PeriodicalIF\":4.5000,\"publicationDate\":\"2025-03-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Molecular Pharmaceutics\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://pubs.acs.org/doi/10.1021/acs.molpharmaceut.4c01518\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"MEDICINE, RESEARCH & EXPERIMENTAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Molecular Pharmaceutics","FirstCategoryId":"3","ListUrlMain":"https://pubs.acs.org/doi/10.1021/acs.molpharmaceut.4c01518","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"MEDICINE, RESEARCH & EXPERIMENTAL","Score":null,"Total":0}
The pH-Dependent Microspecies Dissociations in the Trade-Off of Solubility and Permeability of Vitamin B2 Eutectic Solids
The microspecies-specific physicochemical properties of eutectic solids of sparingly water-soluble micronutrient, Vitamin B2 (Riboflavin), with a few representative BCS drugs, viz., Theophylline, Theobromine, Mesalamine, and Barbituric acid are established. The interplay of solubility and drug permeation behavior is experimentally determined for the eutectic solids, and properties are corroborated with the concomitant relative concentrations of pH-dependent microspecies of Riboflavin and the drugs. Partner drug candidates are selected from different quadrants of BCS classification to apprehend the influence of their solubility on the overall efficacy of the eutectic solids. The coexistence and inseparable ionic, neutral, and/or zwitterionic microspecies are spotted, and the pH-reliant isomer-specific inflection of physicochemical and pharmacokinetic properties in such multicomponent solid formulations is demonstrated.
期刊介绍：
Molecular Pharmaceutics publishes the results of original research that contributes significantly to the molecular mechanistic understanding of drug delivery and drug delivery systems. The journal encourages contributions describing research at the interface of drug discovery and drug development.
Scientific areas within the scope of the journal include physical and pharmaceutical chemistry, biochemistry and biophysics, molecular and cellular biology, and polymer and materials science as they relate to drug and drug delivery system efficacy. Mechanistic Drug Delivery and Drug Targeting research on modulating activity and efficacy of a drug or drug product is within the scope of Molecular Pharmaceutics. Theoretical and experimental peer-reviewed research articles, communications, reviews, and perspectives are welcomed.
求助内容：
应助结果提醒方式：
京公网安备 11010802042870号
