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泊沙康唑口服混悬剂样品制备用于鉴定活性药物成分的晶体形式。

Sample Preparation of Posaconazole Oral Suspensions for Identification of the Crystal Form of the Active Pharmaceutical Ingredient.

机构信息

Department of Pharmacy, University of Patras, GR-26504 Rio Achaias, Greece.

Institute of Chemical Engineering Sciences, Foundation of Research and Technology-Hellas (ICE-HT/FORTH), GR-26504 Platani Achaias, Greece.

出版信息

Molecules. 2020 Dec 19;25(24):6032. doi: 10.3390/molecules25246032.

DOI:10.3390/molecules25246032
PMID:33352808
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7766814/
Abstract

Determination of the polymorphic form of an active pharmaceutical ingredient (API) in a suspension could be really challenging because of the water phase and the low concentration of the API in this formulation. Posaconazole is an antifungal drug available also as an oral suspension. The aim of this study was to develop a sample-preparation method for polymorphic identification of the dispersed API by increasing the concentration of the API but with no compromise of polymorph stability. For this purpose, filtration, drying and centrifugation were tested for separating the API from the suspending medium. Centrifugation was selected because it succeeded in separating Posaconazole API with no polymorph transformation during the process. During this study, it was found that Posaconazole in oral suspensions is Form-S. However, when slower scanning rates were used for acquiring an XRPD pattern with better signal/noise ratio, Posaconazole was converted to Form I due to water loss. In order to protect the sample from conversion, different approaches were tested to secure an airtight sample including a commercially available XRPD sample holder with a dome-like transparent cap, standard polymethylmethacrylate (PMMA) sample holders covered with Mylar film, transparent pressure-sensitive tape and a transparent food membrane. Only usage of the transparent food membrane was found to protect the API from conversion for a period of at least two weeks and resulted in a Posaconazole Form-S XRPD pattern with no artificial peaks.

摘要

由于水相和该制剂中 API 浓度低，混悬剂中活性药物成分（API）的多晶型的测定可能极具挑战性。泊沙康唑是一种抗真菌药物，也有口服混悬剂。本研究旨在开发一种用于通过增加 API 浓度但不影响多晶型稳定性来对分散 API 进行多晶型鉴定的样品制备方法。为此，测试了过滤、干燥和离心以将 API 从悬浮介质中分离出来。选择离心是因为它成功地在不发生多晶型转变的情况下分离了泊沙康唑 API。在这项研究中，发现口服混悬剂中的泊沙康唑为 Form-S。然而，当使用较慢的扫描速率获取具有更好信噪比的 XRPD 图谱时，由于失水，泊沙康唑转变为 Form I。为了防止样品发生转变，测试了不同的方法来确保样品密封，包括带有穹顶透明盖的市售 XRPD 样品架、用聚酯薄膜覆盖的标准聚甲基丙烯酸甲酯（PMMA）样品架、透明压敏胶带和透明食品膜。只有使用透明食品膜被发现可以保护 API 至少两周不发生转变，并且得到的泊沙康唑 Form-S XRPD 图谱没有人为峰。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/2bf2e4ca056a/molecules-25-06032-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/ffad76a1e38c/molecules-25-06032-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/442bea94441f/molecules-25-06032-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/1ad7061b046e/molecules-25-06032-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/acc4d18d47f4/molecules-25-06032-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/97f6a1d6b2d8/molecules-25-06032-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/b5f5e0c680e1/molecules-25-06032-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/865a3caf2729/molecules-25-06032-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/2bf2e4ca056a/molecules-25-06032-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/ffad76a1e38c/molecules-25-06032-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/442bea94441f/molecules-25-06032-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/1ad7061b046e/molecules-25-06032-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/acc4d18d47f4/molecules-25-06032-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/97f6a1d6b2d8/molecules-25-06032-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/b5f5e0c680e1/molecules-25-06032-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/865a3caf2729/molecules-25-06032-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cb32/7766814/2bf2e4ca056a/molecules-25-06032-g008.jpg

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Posaconazole: An Update of Its Clinical Use.泊沙康唑：临床应用最新进展
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