动态气相吸附法评价利福昔明的吸水性能,优化辅料的选择及利福昔明片的生产环境。

IF 1.7 4区 农林科学 Q3 CHEMISTRY, ANALYTICAL
Naga Venkata Durga Prasad Ketha, Hanimi Reddy Bapatu, Kumara Swami Ummiti, Praveen Kumar Subbappa, Deepti Kolli
{"title":"动态气相吸附法评价利福昔明的吸水性能,优化辅料的选择及利福昔明片的生产环境。","authors":"Naga Venkata Durga Prasad Ketha,&nbsp;Hanimi Reddy Bapatu,&nbsp;Kumara Swami Ummiti,&nbsp;Praveen Kumar Subbappa,&nbsp;Deepti Kolli","doi":"10.1093/jaoacint/qsad103","DOIUrl":null,"url":null,"abstract":"<p><strong>Background: </strong>Rifaximin, a medication of the rifamycin family with two distinct strengths of 200 mg and 550 mg in tablet form, is useful for the treatment of travelers' diarrhea. It has a solid yellow hue and is very hygroscopic in nature. It exhibits a variety of polymorphic forms such as α, β, γ, δ, and ε depending on bonded moisture. These polymorphs' varying chemical and physical characteristics, such as solubility and water content, may have a big impact on in vivo absorption, which in turn affects efficacy and safety. Therefore, understanding the polymorphic stability of rifaximin is crucial for formulating rifaximin tablets.</p><p><strong>Objective: </strong>The current effort focuses on the understanding of water vapor sorption properties to control the polymorphic stability of rifaximin in the tablet formulation using the appropriate selection of excipients and manufacturing process.</p><p><strong>Methods: </strong>The dynamic vapor sorption method in the range of 0-90% relative humidity at 25°C is used for understanding the sorption properties of drug substances and drug excipient mixtures; the state-of-the-art techniques of the X-ray diffraction method are used to identify polymorph conversions; and dissolution procedures are used for in vitro correlation studies.</p><p><strong>Results: </strong>The sorption study data reveals that rifaximin is highly unstable at relative humidity conditions above 36%. When using excipients that have a low tendency to adsorb water in the formulation, the polymorphic results do not show any change in their intended form, and the in vitro dissolution data show an equivalency with the reference drug product.</p><p><strong>Conclusion: </strong>The study prompted a successful outcome-oriented development of the formulation processing environment conditions design to develop a test formulation that has adequate polymorphic stability and also similarity in in-vitro dissolution profiles, with the reference product with highest similarity.</p><p><strong>Highlights: </strong>The overall study described here is useful for swiftly gaining insight into the sorption characteristics of rifaximin, and it contributes to the widespread acceptance of rifaximin tablets as a treatment option.</p>","PeriodicalId":15003,"journal":{"name":"Journal of AOAC International","volume":null,"pages":null},"PeriodicalIF":1.7000,"publicationDate":"2023-11-02","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Assessment of the Water Sorption Capacity of Rifaximin Using the Dynamic Vapor Sorption Technique for Optimization of the Choice of Excipients and the Manufacturing Environment of Rifaximin Tablets.\",\"authors\":\"Naga Venkata Durga Prasad Ketha,&nbsp;Hanimi Reddy Bapatu,&nbsp;Kumara Swami Ummiti,&nbsp;Praveen Kumar Subbappa,&nbsp;Deepti Kolli\",\"doi\":\"10.1093/jaoacint/qsad103\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><strong>Background: </strong>Rifaximin, a medication of the rifamycin family with two distinct strengths of 200 mg and 550 mg in tablet form, is useful for the treatment of travelers' diarrhea. It has a solid yellow hue and is very hygroscopic in nature. It exhibits a variety of polymorphic forms such as α, β, γ, δ, and ε depending on bonded moisture. These polymorphs' varying chemical and physical characteristics, such as solubility and water content, may have a big impact on in vivo absorption, which in turn affects efficacy and safety. Therefore, understanding the polymorphic stability of rifaximin is crucial for formulating rifaximin tablets.</p><p><strong>Objective: </strong>The current effort focuses on the understanding of water vapor sorption properties to control the polymorphic stability of rifaximin in the tablet formulation using the appropriate selection of excipients and manufacturing process.</p><p><strong>Methods: </strong>The dynamic vapor sorption method in the range of 0-90% relative humidity at 25°C is used for understanding the sorption properties of drug substances and drug excipient mixtures; the state-of-the-art techniques of the X-ray diffraction method are used to identify polymorph conversions; and dissolution procedures are used for in vitro correlation studies.</p><p><strong>Results: </strong>The sorption study data reveals that rifaximin is highly unstable at relative humidity conditions above 36%. When using excipients that have a low tendency to adsorb water in the formulation, the polymorphic results do not show any change in their intended form, and the in vitro dissolution data show an equivalency with the reference drug product.</p><p><strong>Conclusion: </strong>The study prompted a successful outcome-oriented development of the formulation processing environment conditions design to develop a test formulation that has adequate polymorphic stability and also similarity in in-vitro dissolution profiles, with the reference product with highest similarity.</p><p><strong>Highlights: </strong>The overall study described here is useful for swiftly gaining insight into the sorption characteristics of rifaximin, and it contributes to the widespread acceptance of rifaximin tablets as a treatment option.</p>\",\"PeriodicalId\":15003,\"journal\":{\"name\":\"Journal of AOAC International\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.7000,\"publicationDate\":\"2023-11-02\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of AOAC International\",\"FirstCategoryId\":\"97\",\"ListUrlMain\":\"https://doi.org/10.1093/jaoacint/qsad103\",\"RegionNum\":4,\"RegionCategory\":\"农林科学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CHEMISTRY, ANALYTICAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of AOAC International","FirstCategoryId":"97","ListUrlMain":"https://doi.org/10.1093/jaoacint/qsad103","RegionNum":4,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CHEMISTRY, ANALYTICAL","Score":null,"Total":0}
引用次数: 0

摘要

背景:利福霉素家族的一种药物,具有两种不同的200 mg和550 片剂形式的mg可用于治疗旅行者腹泻。它有一个坚实的黄色色调,是非常吸湿性的性质。根据结合水分的不同,它表现出多种多晶型,如α、β、γ、δ和ε。这些多晶型物不同的化学和物理特性,如溶解度和含水量,可能会对体内吸收产生重大影响,进而影响疗效和安全性。因此,了解利福昔明的多态性稳定性对于配制利福昔敏片剂至关重要。目的:目前的工作重点是了解水蒸气吸附特性,通过适当选择辅料和生产工艺来控制利福昔明在片剂配方中的多态性稳定性。方法:采用25°C相对湿度0-90%范围内的动态气相吸附法,了解原料药和辅料混合物的吸附性能;使用X射线衍射方法的最先进技术来鉴定多晶型转化率;以及溶出程序用于体外相关性研究。结果:吸附研究数据表明,利福昔明在相对湿度超过36%的条件下是高度不稳定的。当使用制剂中吸水性低的赋形剂时,多晶型结果没有显示其预期形式的任何变化,体外溶出度数据显示与参考药物产品相当。结论:该研究促进了以结果为导向的制剂加工环境条件设计的成功开发,以开发一种具有足够多态性稳定性和体外溶出度相似性的试验制剂,与相似性最高的参考产品。亮点:本文所述的整体研究有助于迅速深入了解利福昔明的吸附特性,并有助于利福昔敏片作为一种治疗选择的广泛接受。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Assessment of the Water Sorption Capacity of Rifaximin Using the Dynamic Vapor Sorption Technique for Optimization of the Choice of Excipients and the Manufacturing Environment of Rifaximin Tablets.

Background: Rifaximin, a medication of the rifamycin family with two distinct strengths of 200 mg and 550 mg in tablet form, is useful for the treatment of travelers' diarrhea. It has a solid yellow hue and is very hygroscopic in nature. It exhibits a variety of polymorphic forms such as α, β, γ, δ, and ε depending on bonded moisture. These polymorphs' varying chemical and physical characteristics, such as solubility and water content, may have a big impact on in vivo absorption, which in turn affects efficacy and safety. Therefore, understanding the polymorphic stability of rifaximin is crucial for formulating rifaximin tablets.

Objective: The current effort focuses on the understanding of water vapor sorption properties to control the polymorphic stability of rifaximin in the tablet formulation using the appropriate selection of excipients and manufacturing process.

Methods: The dynamic vapor sorption method in the range of 0-90% relative humidity at 25°C is used for understanding the sorption properties of drug substances and drug excipient mixtures; the state-of-the-art techniques of the X-ray diffraction method are used to identify polymorph conversions; and dissolution procedures are used for in vitro correlation studies.

Results: The sorption study data reveals that rifaximin is highly unstable at relative humidity conditions above 36%. When using excipients that have a low tendency to adsorb water in the formulation, the polymorphic results do not show any change in their intended form, and the in vitro dissolution data show an equivalency with the reference drug product.

Conclusion: The study prompted a successful outcome-oriented development of the formulation processing environment conditions design to develop a test formulation that has adequate polymorphic stability and also similarity in in-vitro dissolution profiles, with the reference product with highest similarity.

Highlights: The overall study described here is useful for swiftly gaining insight into the sorption characteristics of rifaximin, and it contributes to the widespread acceptance of rifaximin tablets as a treatment option.

求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
Journal of AOAC International
Journal of AOAC International 医学-分析化学
CiteScore
3.10
自引率
12.50%
发文量
144
审稿时长
2.7 months
期刊介绍: The Journal of AOAC INTERNATIONAL publishes the latest in basic and applied research in analytical sciences related to foods, drugs, agriculture, the environment, and more. The Journal is the method researchers'' forum for exchanging information and keeping informed of new technology and techniques pertinent to regulatory agencies and regulated industries.
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
确定
请完成安全验证×
copy
已复制链接
快去分享给好友吧!
我知道了
右上角分享
点击右上角分享
0
联系我们:info@booksci.cn Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。 Copyright © 2023 布克学术 All rights reserved.
京ICP备2023020795号-1
ghs 京公网安备 11010802042870号
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术官方微信