Fixed artesunate-amodiaquine combined pre-formulation study for the treatment of malaria

被引：10

作者：

Kauss, Tina ^{[1
]}

Fawaz, Fawaz ^{[1
]}

Guyot, Michel ^{[1
]}

Lagueny, Anne-Marie ^{[1
]}

Dos Santos, Isabelle ^{[1
]}

Bonini, Francois ^{[1
]}

Olliaro, Piero ^{[2
,3
]}

Caminiti, Antonella ^{[4
]}

Millet, Pascal ^{[4
]}

机构：

[1] Univ Bordeaux 2, Pharm Galen & Biopharm Lab, F-33076 Bordeaux, France

[2] UNICEF UNDP WB WHO Special Program Res & Training, Geneva, Switzerland

[3] Univ Oxford, Nuffield Dept Med, Ctr Trop Med, Oxford OX1 2JD, England

[4] Univ Bordeaux 2, Ctr Rene Labusquiere, F-33076 Bordeaux, France

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2010年 / 395卷 / 1-2期

关键词：

Artesunate; Amodiaquine; Pre-formulation; Malaria; UNCOMPLICATED PLASMODIUM-FALCIPARUM; COMBINATION; EFFICACY; SAFETY;

D O I：

10.1016/j.ijpharm.2010.05.038

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Artemisinin-based combination therapies, including artesunate (AS)+ amodiaquine (AQ), are the currently recommended first-line treatment of uncomplicated falciparum malaria. Fixed-dose co-formulations offer logistic and adherence advantages. This paper reports the initial research phase of the pre-development process of an AS-AQ formulation, further developed by the Drug for Neglected Diseases Initiative (DNDi). Results demonstrate that AS and AQ are not compatible, and AS degradation is related to three main parameters: water content (>1%), elevated temperature (80 degrees C in dry condition) and possibly the 4-aminoquinoline moiety. Furthermore. AS and AQ incompatibility led to AS degradation and pharmaco-technical changes in classical wet granulation tablets. Both active principles are stable as dry powders. These investigations led to further development of various co-formulations, including the bilayer tablet currently on the market. (C) 2010 Elsevier B.V. All rights reserved.

引用

页码：198 / 204

页数：7

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