{"title":"含人工甜味剂莫西沙星共晶、共无定形盐的研制","authors":"Peiwen Mo, Yuta Hatanaka, Saki Ohta, Yuzuki Nakayama, Yasuteru Mawatari, Shinya Yamanaka, Katsuhiko Minoura, Mitsunobu Doi, Hiromasa Uchiyama, Kazunori Kadota* and Yuichi Tozuka*, ","doi":"10.1021/acs.cgd.5c0017010.1021/acs.cgd.5c00170","DOIUrl":null,"url":null,"abstract":"<p >This study explores the formation of a molecular complex between moxifloxacin (MFX) and the artificial sweetener saccharin (SAC) as a strategy to mask the drug’s undesirable taste. MFX particles were combined with SAC in a 1:1 ratio using ball milling, a process that facilitated the formation of both cocrystal and coamorphous salts through ionic interactions. Structural analysis of the MFX-SAC complex revealed intermolecular ionic bonds between the amino group of MFX and the sulfonamide group of SAC. Solid-state nuclear magnetic resonance spectroscopy further confirmed that MFX interacts with SAC via ionic bonding. Electronic taste evaluations demonstrated that the MFX-SAC complex not only significantly reduced the bitterness of MFX but also suppressed the overall taste intensity to levels below the quinine reference standard. These findings highlight the potential of molecular complex formation between artificial sweeteners and bitter-tasting drugs as an effective approach for taste modification and masking, offering promising implications for pharmaceutical formulation development.</p>","PeriodicalId":34,"journal":{"name":"Crystal Growth & Design","volume":"25 12","pages":"4283–4294 4283–4294"},"PeriodicalIF":3.2000,"publicationDate":"2025-06-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Development of Cocrystal and Coamorphous Salts of Moxifloxacin with Artificial Sweeteners to Suppress Bitterness\",\"authors\":\"Peiwen Mo, Yuta Hatanaka, Saki Ohta, Yuzuki Nakayama, Yasuteru Mawatari, Shinya Yamanaka, Katsuhiko Minoura, Mitsunobu Doi, Hiromasa Uchiyama, Kazunori Kadota* and Yuichi Tozuka*, \",\"doi\":\"10.1021/acs.cgd.5c0017010.1021/acs.cgd.5c00170\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p >This study explores the formation of a molecular complex between moxifloxacin (MFX) and the artificial sweetener saccharin (SAC) as a strategy to mask the drug’s undesirable taste. MFX particles were combined with SAC in a 1:1 ratio using ball milling, a process that facilitated the formation of both cocrystal and coamorphous salts through ionic interactions. Structural analysis of the MFX-SAC complex revealed intermolecular ionic bonds between the amino group of MFX and the sulfonamide group of SAC. Solid-state nuclear magnetic resonance spectroscopy further confirmed that MFX interacts with SAC via ionic bonding. Electronic taste evaluations demonstrated that the MFX-SAC complex not only significantly reduced the bitterness of MFX but also suppressed the overall taste intensity to levels below the quinine reference standard. These findings highlight the potential of molecular complex formation between artificial sweeteners and bitter-tasting drugs as an effective approach for taste modification and masking, offering promising implications for pharmaceutical formulation development.</p>\",\"PeriodicalId\":34,\"journal\":{\"name\":\"Crystal Growth & Design\",\"volume\":\"25 12\",\"pages\":\"4283–4294 4283–4294\"},\"PeriodicalIF\":3.2000,\"publicationDate\":\"2025-06-04\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Crystal Growth & Design\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://pubs.acs.org/doi/10.1021/acs.cgd.5c00170\",\"RegionNum\":2,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MULTIDISCIPLINARY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Crystal Growth & Design","FirstCategoryId":"92","ListUrlMain":"https://pubs.acs.org/doi/10.1021/acs.cgd.5c00170","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
Development of Cocrystal and Coamorphous Salts of Moxifloxacin with Artificial Sweeteners to Suppress Bitterness
This study explores the formation of a molecular complex between moxifloxacin (MFX) and the artificial sweetener saccharin (SAC) as a strategy to mask the drug’s undesirable taste. MFX particles were combined with SAC in a 1:1 ratio using ball milling, a process that facilitated the formation of both cocrystal and coamorphous salts through ionic interactions. Structural analysis of the MFX-SAC complex revealed intermolecular ionic bonds between the amino group of MFX and the sulfonamide group of SAC. Solid-state nuclear magnetic resonance spectroscopy further confirmed that MFX interacts with SAC via ionic bonding. Electronic taste evaluations demonstrated that the MFX-SAC complex not only significantly reduced the bitterness of MFX but also suppressed the overall taste intensity to levels below the quinine reference standard. These findings highlight the potential of molecular complex formation between artificial sweeteners and bitter-tasting drugs as an effective approach for taste modification and masking, offering promising implications for pharmaceutical formulation development.
期刊介绍:
The aim of Crystal Growth & Design is to stimulate crossfertilization of knowledge among scientists and engineers working in the fields of crystal growth, crystal engineering, and the industrial application of crystalline materials.
Crystal Growth & Design publishes theoretical and experimental studies of the physical, chemical, and biological phenomena and processes related to the design, growth, and application of crystalline materials. Synergistic approaches originating from different disciplines and technologies and integrating the fields of crystal growth, crystal engineering, intermolecular interactions, and industrial application are encouraged.