Enhancement of albendazole dissolution properties using solid dispersions with Gelucire 50/13 and PEG 15000

被引：29
作者：
Jimenez de los Santos, Cesareo J. [1 ]
Perez-Martinez, Jose I. [1 ]
Eulalia Gomez-Pantoja, M. [2 ]
Moyano, Jose R. [1 ]
机构：
[1] Univ Seville, Fac Pharm, Dept Pharm & Pharmaceut Technol, C Prof Garcia Gonzalez 2, Seville 41012, Spain
[2] CSIC, Sci Res Council, Inst Nat Resources & Agrobiol Seville, Agrochem & Soil Conservat Dept,IRNAS, Avda Reina Mercedes 10, Seville 41012, Spain
来源：
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY | 2017年 / 42卷
关键词：
Albendazole; Gelucire; 50/13; PEG; 15000; Solid dispersion; DSC; HSM; PXRD; FTIR; Dissolution kinetics; BIOPHARMACEUTICS CLASSIFICATION-SYSTEM; WATER-SOLUBLE DRUGS; HOT-MELT EXTRUSION; ORAL BIOAVAILABILITY; FORMULATION; RELEASE; SOLUBILITY; PELLETS;
D O I：
10.1016/j.jddst.2017.03.030
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The role of two carriers -Gelucire 50/13 and PEG 15000- was evaluated to improve the characteristics of the dissolution of albendazole, an anthelmintic drug with very low solubility and dissolution rate. Solid dispersions were elaborated by using the fusion method. The results from solid-state characterisation techniques (DSC, HSM, FTIR and PXRD) reported immiscibility and absence of interactions in the solid phase. In vitro release studies of binary systems showed a substantial enhancement of dissolution performance when compared with the control, which constitutes an actual alternative to increase the bioavalilability and/or reduce the dosage of the currently marketed formulations. (C) 2017 Elsevier B.V. All rights reserved.
引用
收藏
页码：261 / 272
页数：12
相关论文
共 31 条
[1]   Studies on dissolution enhancement and mathematical modeling of drug release of a poorly water-soluble drug using water-soluble carriers [J].
Ahuja, Naveen ;
Katare, Om Prakash ;
Singh, Bhupinder .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2007, 65 (01) :26-38
[2]   Preparation of starch-based pellets by hot-melt extrusion [J].
Bialleck, Sebastian ;
Rein, Hubert .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2011, 79 (02) :440-448
[3]   Albendazole as a promising molecule for tumor control [J].
Castro, L. S. E. P. W. ;
Kviecinski, M. R. ;
Ourique, F. ;
Parisotto, E. B. ;
Grinevicius, V. M. A. S. ;
Correia, J. F. G. ;
Wilhelm Filho, D. ;
Pedrosa, R. C. .
REDOX BIOLOGY, 2016, 10 :90-99
[4]   Physicochemical characterization of solid dispersions of the antiviral agent UC-781 with polyethylene glycol 6000 and Gelucire 44/14 [J].
Damian, F ;
Blaton, N ;
Naesens, L ;
Balzarini, J ;
Kinget, R ;
Augustijns, P ;
Van den Mooter, G .
EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2000, 10 (04) :311-322
[5]  
Djuris J., 2013, J PHARM BIOPHARM, V84, P228
[6]   Oral bioavailability in sheep of albendazole from a suspension and from a solution containing hydroxypropyl-β-cyclodextrin [J].
Evrard, B ;
Chiap, P ;
DeTullio, P ;
Ghalmi, F ;
Piel, G ;
Van Hees, T ;
Crommen, J ;
Losson, B ;
Delattre, L .
JOURNAL OF CONTROLLED RELEASE, 2002, 85 (1-3) :45-50
[7]   Diclofenac salts, II.: Solid dispersions in PEG6000 and Gelucire 50/13 [J].
Fini, A ;
Moyano, JR ;
Ginés, JM ;
Perez-Martinez, JI ;
Rabasco, AM .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2005, 60 (01) :99-111
[8]   Spectroscopic and spectrofluorimetric studies on the interaction of albendazole and trimethoprim with iodine [J].
Ganesh, K. ;
Elango, K. P. .
SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY, 2012, 93 :185-197
[9]   Inclusion of the herbicide 2,4-dichlorophenoxyacetic acid (2,4-D) with beta-cyclodextrin by different processing methods [J].
Gines, JM ;
PerezMartinez, JI ;
Arias, MJ ;
Moyano, JR ;
Morillo, E ;
RuizConde, A ;
SanchezSoto, PJ .
CHEMOSPHERE, 1996, 33 (02) :321-334
[10]   Elaboration and thermal study of interactions between cinnarizine and gelucire(R) 53/10 physical mixtures and solid dispersions [J].
Gines, JM ;
Veiga, MD ;
Arias, MJ ;
Rabasco, AM .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1995, 126 (1-2) :287-291
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