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Effect of Different Polymers on the Release of Diclofenac Sodium Controlled Release Drug Delivery System

Esmat Zien El-Deen*, Mamdouh Ghorab, Shadeed Gad and Heba Yassin

Diclofenac sodium (DS) is a potent non-steroidal drug with potent analgesic and anti-inflammatory activity. Its oral administration is associated with a high risk of adverse effect such as irritation, ulceration and bleeding of gastrointestinal tract. The present study focuses on the development of controlled release drug delivery system of DS. Non-aqueous emulsification solvent evaporation method was used to prepare controlled release DS particles having high DS content to obtain prolonged drug delivery in order to decrease ulcerogenicity, improve bioavailability, stability and target the drug at specific sites. Solid dispersions were prepared using EudragitRS100, EudragitRL100 and ethyl cellulose in ratios of 1:1, 1:2 and 1:3 drug to polymer. The effect of various formulations and process variables on the flowability drug loading and in-vitro drug release was studied. IR investigation revealed that there was no interaction between the drug and the polymers used. Differential thermal analysis and Powder x-ray diffractometry confirmed that the drug was reduced to molecular or microcrystalline form in the hydrophobic polymeric matrices, which could be responsible for the controlled drug release from the solid dispersions. The flow characteristic showed Hausner's ratios and Carr's index of the systems prepared indicating good and excellent flow of the systems. DS content in different solid dispersion formulations was not affected by neither the polymer type nor drug to polymer ratio and ranged between 98-100%. This study presents a new approach based on solid dispersion technique for obtaining modified release drug delivery system.

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日内瓦医学教育与研究基金会
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