Enhancing the Dissolution and Sustaining the Release of Diclofenac Sodium Using the Method Liquisolid Technology

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Addis Ababa University


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.



Liquisolid compact; Diclofenac Sodium;Solubility; Dissolution; Sustained release