Influence of eutectic mixture as a multi -component system in the improvement of physicomechanical and pharmacokinetic properties of diacerein

被引：15
|
作者：
Patel, Rajeshri D. [1 ]
Raval, Mihir K. [1 ]
Pethani, Trupesh M. [1 ]
Sheth, Navin R. [2 ]
机构：
[1] Saurashtra Univ, Dept Pharmaceut Sci, Rajkot 360005, Gujarat, India
[2] Gujarat Technol Univ, Ahmadabad 382424, Gujarat, India
来源：
ADVANCED POWDER TECHNOLOGY | 2020年 / 31卷 / 04期
关键词：
SOLID-STATE CHARACTERIZATIONS; SPHERICAL CRYSTALLIZATION; DISINTEGRATING TABLETS; AGGLOMERATED CRYSTALS; DRUG; ACID; DISSOLUTION; COCRYSTAL; COMPACTION; BEHAVIOR;
D O I：
10.1016/j.apt.2020.01.021
中图分类号：
TQ [化学工业];
学科分类号：
0817 ;
摘要：
A multi-component system of diacerein (DIA) with 2, 4 – dihydroxybenzoic acid (DHA) as coformer at various molar compositions was formulated to simultaneously improve solubility, compressibility and bioavailability of DIA by applying acetone assistant grinding technique. Various evaluation parameters pertaining to measure physicomechanical properties were conducted. Thermal analysis revealed a ‘V’-shaped binary phase diagram along with single melting event as a possibility of eutectic formation between drug and coformer. It was further confirmed PXRD and FT-IR. Equidimensional shape with platy nature of eutectic material was observed in SEM images imparting its better flow and compressibility. Solubility and dissolution study showed 2 and 1.8 folds enhancement respectively compared to pure DIA and control batch. Pharmacokinetic study proved 2.1 times higher bioavailability in case of prepared eutectic compared to DIA along with its stable nature. Hence, the multi-component system can become a potential way for the improvement of material characteristics. © 2020 Society of Powder Technology Japan
引用
收藏
页码：1441 / 1456
页数：16
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