Effects of Solvents on Spherical Crystals of Minoxidil

IF 3.4 2区化学 Q2 CHEMISTRY, MULTIDISCIPLINARY

Crystal Growth & Design Pub Date : 2025-09-16 DOI:10.1021/acs.cgd.5c00585

Chenwei Geng, and , Jingtao Wang*,

{"title":"Effects of Solvents on Spherical Crystals of Minoxidil","authors":"Chenwei Geng,  and , Jingtao Wang*, ","doi":"10.1021/acs.cgd.5c00585","DOIUrl":null,"url":null,"abstract":"<p >Minoxidil, a topical vasodilator primarily used to treat androgenetic alopecia, has a huge market but remains underexplored in the control of its spherical crystals. Spherical crystal structure is a vital morphology due to its superior powder characteristics in pharmaceutical manufacturing. Even though solvent-induced single crystals have been well studied, there have been few studies on the solvent-mediated morphology of spherical aggregates. In this paper, several kinds of spherical crystals, such as plate crystal aggregates, nanocrystal aggregates, and core–shell aggregates, are prepared in alcoholic solvents with different carbon chain lengths. Particularly, spherulite aggregates (SLA), which are observed for the first time, are produced in a <i>n</i>-butanol–ethyl acetate mixture. Also, the growth mechanism of SLA is analyzed in detail, and it is found that the addition of ethyl acetate could change the morphology of spherulites and promote agglomeration between them compared to pure solvent systems without ethyl acetate. In addition, the method of generating supersaturation is significant by specifying the morphology of the spherulite. The flowability and other powder properties of SLA are also investigated, with a 15.8% reduction in the repose angle and 24.7% of the Hausner ratio. Furthermore, this paper reports a unique butterfly-shaped crystal of minoxidil, which undergoes a spontaneous growth in a homogeneous solution, not from agglomeration.</p>","PeriodicalId":34,"journal":{"name":"Crystal Growth & Design","volume":"25 19","pages":"8010–8020"},"PeriodicalIF":3.4000,"publicationDate":"2025-09-16","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.5c00585","RegionNum":2,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}

引用次数: 0

Abstract

Minoxidil, a topical vasodilator primarily used to treat androgenetic alopecia, has a huge market but remains underexplored in the control of its spherical crystals. Spherical crystal structure is a vital morphology due to its superior powder characteristics in pharmaceutical manufacturing. Even though solvent-induced single crystals have been well studied, there have been few studies on the solvent-mediated morphology of spherical aggregates. In this paper, several kinds of spherical crystals, such as plate crystal aggregates, nanocrystal aggregates, and core–shell aggregates, are prepared in alcoholic solvents with different carbon chain lengths. Particularly, spherulite aggregates (SLA), which are observed for the first time, are produced in a n-butanol–ethyl acetate mixture. Also, the growth mechanism of SLA is analyzed in detail, and it is found that the addition of ethyl acetate could change the morphology of spherulites and promote agglomeration between them compared to pure solvent systems without ethyl acetate. In addition, the method of generating supersaturation is significant by specifying the morphology of the spherulite. The flowability and other powder properties of SLA are also investigated, with a 15.8% reduction in the repose angle and 24.7% of the Hausner ratio. Furthermore, this paper reports a unique butterfly-shaped crystal of minoxidil, which undergoes a spontaneous growth in a homogeneous solution, not from agglomeration.

Abstract Image

查看原文本刊更多论文

溶剂对米诺地尔球形结晶的影响

米诺地尔是一种局部血管扩张剂，主要用于治疗雄激素性脱发，它有巨大的市场，但在控制其球形晶体方面仍未得到充分开发。球形晶体结构由于其优异的粉体特性，在医药制造中是一种重要的晶体形态。尽管溶剂诱导的单晶已经被很好地研究过，但对溶剂介导的球形聚集体形态的研究还很少。本文在不同碳链长度的酒精溶剂中制备了几种球形晶体，如板晶聚集体、纳米晶聚集体和核壳聚集体。特别是在正丁醇-乙酸乙酯混合物中产生了首次观察到的球晶聚集体（SLA）。并对SLA的生长机理进行了详细的分析，发现与不含乙酸乙酯的纯溶剂体系相比，乙酸乙酯的加入可以改变球晶的形貌，促进球晶之间的团聚。此外，通过指定球晶的形态，产生过饱和的方法是有意义的。同时研究了SLA的流动性和其他粉末性能，其休止角降低了15.8%，豪斯纳比降低了24.7%。此外，本文还报道了一种独特的蝴蝶形米诺地尔晶体，它在均匀溶液中自发生长，而不是聚集。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

求助全文

约1分钟内获得全文求助全文

来源期刊

Crystal Growth & Design 化学-材料科学：综合

CiteScore

6.30

自引率

10.50%

发文量

650

审稿时长

1.9 months

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.