Effects of liquisolid formulations on dissolution of naproxen

被引:134
|
作者
Tiong, Ngiik [1 ]
Elkordy, Amal A. [1 ]
机构
[1] Univ Sunderland, Fac Sci Appl, Dept Pharm Hlth & Well Being, Sunderland SR1 3SD, Tyne & Wear, England
关键词
Naproxen; Liquisolid tablets; Dissolution; Liquid load factor; Cremophor (R) EL; HYDROXYPROPYL-BETA-CYCLODEXTRIN; WATER-SOLUBLE DRUGS; PHYSICOCHEMICAL PROPERTIES; IN-VITRO; ENHANCEMENT; COMPACTS; IMPROVEMENT; TABLETS; RELEASE; SYSTEM;
D O I
10.1016/j.ejpb.2009.08.002
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The aim of this study was to investigate the use of liquisolid technique in improving the dissolution profiles of naproxen in a solid dosage form. This study was designed to evaluate the effects of different formulation variables, i.e. type of non-volatile liquid vehicles and drug concentrations, on drug dissolution rates. The liquisolid tablets were formulated with three different liquid vehicles, namely Cremophore (R) EL (polyoxyl 35 castor oil), Synperonic (R) PE/L61 (poloxamer 181, polyoxyethylene-polyoxypropylene copolymer) and poly ethylene glycol 400 (PEG400) at two drug concentrations, 20%w/w and 40%wlw. Avicel (R) PH102 was used as a carrier material, Cab-o-sil (R) M-5 as a coating material and maize starch as a disintegrant. The empirical method as introduced by Spireas and Bolton (1999) [11 was applied strictly to calculate the amounts of coating and carrier materials required to prepare naproxen liquisolid tablets. Quality control tests, i.e. uniformity of tablet weight, uniformity of drug content, tablet hardness, friability test, disintegration and dissolution tests were performed to evaluate each batch of prepared tablets. In vitro drug dissolution profiles of the liquisolid formulations were studied and compared with conventional formulation, in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.2) without enzyme. Stability studies were carried out to evaluate the stability of the tablets under humid conditions. Differential scanning calorimetry and Fourier transform infrared were used to investigate physicochemical interaction between naproxen and the excipients. it was found that liquisolid tablets formulated with Cremophor (R) EL at drug concentration of 20%w/w produced high dissolution profile with acceptable tablet properties. The stability studies showed that the dissolution profiles of liquisolid tablets prepared with Cremophor (R) EL were not affected by ageing significantly. Furthermore, DSC revealed that drug particles in liquisolid formulations were completely solubilised. (C) 2009 Elsevier B.V. All rights reserved.
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页码:373 / 384
页数:12
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