Enhancing the Dissolution and Sustaining the Release of Diclofenac Sodium Using the Method Liquisolid Technology
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Date
2014-05
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Addis Ababa University
Abstract
Various methods of modifying solubility and dissolution properties of drugs have been
developed over the years. Methods such as liquisolid technology, which can be used to
enhance or sustain dissolution, have raised a lot of interest in many researchers. In this
study different liquisolid compacts of diclofenac sodium containing either propylene
glycol or polyethylene glycol 400 for the enhanced dissolution preparations; and
Polysorbate 80 as a non-volatile solvent for sustained preparation were prepared using a
mathematical model for calculating required quantities of powder and liquid ingredients
to produce acceptably flowable and compressible admixture. Microcrystalline cellulose,
colloidal silica and sodium starch glycolate were employed as carrier, coating material
and disintegrant, respectively. Formulation of liquisolid compacts having various ratio of
carrier to coating material (ranging from 10 to 30) and 50 to 70% concentration of liquid
medication (drug:non-volatile solvent) were prepared and evaluated for their powder,
tablet property and drug release profile. The liquisolid compacts demonstrate
considerably higher dissolution rate than marketed tablets. This was due to increased
wetting properties and surface of drug available for dissolution. Also it has been shown
that the fraction of molecularly dispersed drug in the liquid medication of liquisolid
system was directly proportional to the dissolution rate and the percentage drug dissolved
in 10 minute was correlated with solubility of the drug in different vehicle. A plot of the
percentage drug dissolved against the solubility of diclofenac sodium showed that the
amount of drug dissolved increased linearly with an increase in solubility of diclofenac
sodium in the vehicle. Diclofenac sodium tablets prepared by liquisolid technique also
showed release retardation properties. This study revealed that Polysorbate 80 and
Eudragit® RL has important role in sustaining the release of drug from liquisolid
matrices. It is generally proven that liquisolid technique is a promising alternative as a
tool to enhance or sustain the release of diclofenac sodium.
Key words: Liquisolid compact, Diclofenac Sodium, Solubility, Dissolution, Sustained
release.
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Keywords
Liquisolid compact; Diclofenac Sodium;Solubility; Dissolution; Sustained release