Drug Solubility Enhancement through the Preparation of Multicomponent Organic Materials: Eutectics of Lovastatin with Carboxylic Acids

التفاصيل البيبلوغرافية
العنوان:	Drug Solubility Enhancement through the Preparation of Multicomponent Organic Materials: Eutectics of Lovastatin with Carboxylic Acids
المؤلفون:	Araya Sibaja, Andrea Mariela, Jose-Roberto, Vega-Baudrit, Guillen-Girón, Teodolito, Navarro-Hoyos, Mirtha, Cuffini, Silvia Lucia
المصدر:	Pharmaceutics vol.11 no.3 1-16 2019
بيانات النشر:	MDPI AG
سنة النشر:	2019
المجموعة:	Universidad Nacional Costa Rica (UNA): Repositorio Institucional
مصطلحات موضوعية:	LOVASTATIN, EUTECTIC MIXTURES, CARBOXYLIC ACIDS, MULTICOMPONENT ORGANIC MATERIALS, GRAS SUBSTANCES, DROGAS, FARMACOLOGÍA, QUÍMICA FARMACEUTICA
الوصف:	Lovastatin (LOV) is a drug used to treat hypercholesterolemia. Recent studies have identified its antioxidant effects and potential use in the treatment of some types of cancer. However, the low bioavailability related to its poor water solubility limits its use in solid oral dosage forms. Therefore, to improve the solubility of LOV three eutectic systems of LOV with the carboxylic acids benzoic (BEN), salicylic (SAL) and cinnamic (CIN) were obtained. Both binary phase and Tammann diagrams were constructed using differential scanning calorimetry (DSC) data of mixtures prepared from 0.1 to 1.0 molar ratios. Binary mixtures and eutectics were prepared by liquid-assisted grinding. The eutectics were further characterized by DSC and powder X-ray diffraction (PXRD), Fourier-transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM). The LOV-BEN, LOV-SAL and LOV-CIN system formed a eutectic at an LOV mole fraction of 0.19, 0.60 and 0.14, respectively. The systems exhibited improvements in LOV solubility, becoming more soluble by five-fold in the LOV-SAL system and approximately four-fold in the other two systems. Considering that the solubility enhancements and the carboxylic acids used are generally recognized as safe by the U.S. Food and Drug Administration (FDA), the LOV eutectic systems are promising materials to be used in a solubility enhancement strategy for pharmaceutical product formulation. ; La lovastatina (LOV) es un medicamento que se usa para tratar la hipercolesterolemia. Estudios recientes han identificado sus efectos antioxidantes y su uso potencial en el tratamiento de algunos tipos de cáncer. Sin embargo, la baja biodisponibilidad relacionada con su escasa solubilidad en agua limita su uso en formas sólidas de dosificación oral. Por tanto, para mejorar la solubilidad de LOV se obtuvieron tres sistemas eutécticos de LOV con los ácidos carboxílicos benzoico (BEN), salicílico (SAL) y cinámico (CIN). Tanto los diagramas de fase binaria como de Tammann se construyeron usando datos de ...
نوع الوثيقة:	article in journal/newspaper
وصف الملف:	application/pdf
اللغة:	English
تدمد:	19994923
Relation:	http://hdl.handle.net/11056/22184
DOI:	10.3390/pharmaceutics11030112
الاتاحة:	http://hdl.handle.net/11056/22184 https://doi.org/10.3390/pharmaceutics11030112
Rights:	Acceso abierto ; http://creativecommons.org/licenses/by/4.0/
رقم الانضمام:	edsbas.995A9C02
قاعدة البيانات:	BASE

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الوصف
تدمد:	19994923
DOI:	10.3390/pharmaceutics11030112