Binary Mixtures of Some Active Pharmaceutical Ingredients with Fatty Alcohols—The Criteria of Successful Eutectic Formation and Dissolution Improvement

Pharmaceutical eutectics are solid mixtures, where the crystals of active pharmaceutical ingredients (APIs) are finely divided in the phase-separated microstructures. The size reduction makes the eutectic formation a viable option to improve the dissolution rate of the poorly soluble APIs. In the pr...

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Main Authors:	Songhee Jin, Jisun Jang, Soyeon Lee, Il Won Kim
Format:	Article
Language:	English
Published:	MDPI AG 2020-11-01
Series:	Pharmaceutics
Subjects:	active pharmaceutical ingredient fatty alcohol eutectic dissolution
Online Access:	https://www.mdpi.com/1999-4923/12/11/1098

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spelling	doaj-e79392011925444aa19e99acaf0703e22020-11-25T04:11:17ZengMDPI AGPharmaceutics1999-49232020-11-01121098109810.3390/pharmaceutics12111098Binary Mixtures of Some Active Pharmaceutical Ingredients with Fatty Alcohols—The Criteria of Successful Eutectic Formation and Dissolution ImprovementSonghee Jin0Jisun Jang1Soyeon Lee2Il Won Kim3Department of Chemical Engineering, Soongsil University, Seoul 06978, KoreaDepartment of Chemical Engineering, Soongsil University, Seoul 06978, KoreaDepartment of Chemical Engineering, Soongsil University, Seoul 06978, KoreaDepartment of Chemical Engineering, Soongsil University, Seoul 06978, KoreaPharmaceutical eutectics are solid mixtures, where the crystals of active pharmaceutical ingredients (APIs) are finely divided in the phase-separated microstructures. The size reduction makes the eutectic formation a viable option to improve the dissolution rate of the poorly soluble APIs. In the present study, ibuprofen, naproxen, and sorafenib were investigated in terms of their phase behaviors with fatty alcohols, such as tetradecanol, octadecanol, and docosanol. Among the studied APIs, only ibuprofen was able to form eutectics with the fatty alcohols, and this was in agreement with the feasibility prediction based on the van ’t Hoff equation and solubility parameters. In vitro release behavior was significantly improved for the ibuprofen/octadecanol eutectic mixture, although the practical insolubility of octadecanol in water was the opposite of the outstanding hydrophilicity of usual eutectic formers. The feasibility prediction and the choice of eutectic formers in the present study will be useful in advancing the utility of the pharmaceutical eutectics.https://www.mdpi.com/1999-4923/12/11/1098active pharmaceutical ingredientfatty alcoholeutecticdissolution
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Songhee Jin Jisun Jang Soyeon Lee Il Won Kim
spellingShingle	Songhee Jin Jisun Jang Soyeon Lee Il Won Kim Binary Mixtures of Some Active Pharmaceutical Ingredients with Fatty Alcohols—The Criteria of Successful Eutectic Formation and Dissolution Improvement Pharmaceutics active pharmaceutical ingredient fatty alcohol eutectic dissolution
author_facet	Songhee Jin Jisun Jang Soyeon Lee Il Won Kim
author_sort	Songhee Jin
title	Binary Mixtures of Some Active Pharmaceutical Ingredients with Fatty Alcohols—The Criteria of Successful Eutectic Formation and Dissolution Improvement
title_short	Binary Mixtures of Some Active Pharmaceutical Ingredients with Fatty Alcohols—The Criteria of Successful Eutectic Formation and Dissolution Improvement
title_full	Binary Mixtures of Some Active Pharmaceutical Ingredients with Fatty Alcohols—The Criteria of Successful Eutectic Formation and Dissolution Improvement
title_fullStr	Binary Mixtures of Some Active Pharmaceutical Ingredients with Fatty Alcohols—The Criteria of Successful Eutectic Formation and Dissolution Improvement
title_full_unstemmed	Binary Mixtures of Some Active Pharmaceutical Ingredients with Fatty Alcohols—The Criteria of Successful Eutectic Formation and Dissolution Improvement
title_sort	binary mixtures of some active pharmaceutical ingredients with fatty alcohols—the criteria of successful eutectic formation and dissolution improvement
publisher	MDPI AG
series	Pharmaceutics
issn	1999-4923
publishDate	2020-11-01
description	Pharmaceutical eutectics are solid mixtures, where the crystals of active pharmaceutical ingredients (APIs) are finely divided in the phase-separated microstructures. The size reduction makes the eutectic formation a viable option to improve the dissolution rate of the poorly soluble APIs. In the present study, ibuprofen, naproxen, and sorafenib were investigated in terms of their phase behaviors with fatty alcohols, such as tetradecanol, octadecanol, and docosanol. Among the studied APIs, only ibuprofen was able to form eutectics with the fatty alcohols, and this was in agreement with the feasibility prediction based on the van ’t Hoff equation and solubility parameters. In vitro release behavior was significantly improved for the ibuprofen/octadecanol eutectic mixture, although the practical insolubility of octadecanol in water was the opposite of the outstanding hydrophilicity of usual eutectic formers. The feasibility prediction and the choice of eutectic formers in the present study will be useful in advancing the utility of the pharmaceutical eutectics.
topic	active pharmaceutical ingredient fatty alcohol eutectic dissolution
url	https://www.mdpi.com/1999-4923/12/11/1098
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Binary Mixtures of Some Active Pharmaceutical Ingredients with Fatty Alcohols—The Criteria of Successful Eutectic Formation and Dissolution Improvement

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