Dissolution Enhancement in Cocoa Extract, Combining Hydrophilic Polymers through Hot-Melt Extrusion

被引:10
作者
Pinho, Ludmila A. G. [1 ]
Souza, Saulo G. [1 ]
Marreto, Ricardo N. [2 ]
Sa-Barreto, Livia L. [1 ]
Gratieri, Tais [1 ]
Gelfuso, Guilherme M. [1 ]
Cunha-Filho, Marcilio [1 ]
机构
[1] Univ Brasilia UnB, Lab Food Drugs & Cosmet LTMAC, BR-70910900 Brasilia, DF, Brazil
[2] Univ Fed Goias, Sch Pharm, BR-74605170 Goiania, Go, Brazil
关键词
hot-melt extrusion; cocoa extract; mixture design; flowability; dissolution rate; SOLID DISPERSION; ORAL BIOAVAILABILITY; THEOBROMINE; BENZNIDAZOLE; IMPROVEMENT;
D O I
10.3390/pharmaceutics10030135
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of this study was to improve the physicochemical properties of cocoa extract (CE) using hot-melt extrusion (HME) for pharmaceutical proposes. A mixture design was applied using three distinct hydrophilic polymeric matrices (Soluplus, Plasdone S630, and Eudragit E). Systems obtained by HME were evaluated using morphologic, chromatographic, thermic, spectroscopic, and diffractometric assays. The flow, wettability, and dissolution rate of HME powders were also assessed. Both CE and its marker theobromine proved to be stable under heating according to thermal analysis and Arrhenius plot under isothermal conditions. Physicochemical analysis confirmed the stability of CE HME preparations and provided evidence of drug-polymer interactions. Improvements in the functional characteristics of CE were observed after the extrusion process, particularly in dissolution and flow properties. In addition, the use of a mixture design allowed the identification of synergic effects by excipient combination. The optimized combination of polymers obtained considering four different aspects showed that a mixture of the Soluplus, Plasdone S630, and Eudragit E in equal proportions produced the best results (flowability index 88%; contact angle 47 degrees; dispersibility 7.5%; and dissolution efficiency 87%), therefore making the pharmaceutical use of CE more feasible.
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页数:14
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