Combination of liquisolid and co-grinding technologies for enhancing dissolution rate of furosemide

Abstract

Introduction: Furosemide is one of the widely used diuretic or antihypertensive drugs. Furosemide is a poorly solubale, highly permeable drug (class 2) and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. There are several techniques to enhance the dissolution rate of poorly soluble drugs. The most promising method for promoting dissolution is the formation of liquisolid tablets. Goals: A new concept was examined in this research for obtaining better dissolution rate of furosemide. For this mean combination of ball milling and liuqisolid technology was investigated. Methods: Liquid medications were prepared by dispersing the drug in liquid vehicle (PEG200) and grinding them in ballmill for 3 hours. After that, other excipients like microcrystalline cellulose as the carrier powder and silica as the coating material were added. Direct compression tablets were prepared using mentioned exipiens non volatile solvent. Then dissolution test were done in SIF and SGF media. The effect of aging on hardness and dissolution profile was also studied. DSC thermograms were used for study of any crystallinity change or complex formation. Results: Prepared compacts, had good properties in view poit of hardness and friability. These formulations showed higher dissolution rate than those of conventional tablets or classic liquisolid formulations. Aging had no effect of hardness and dissolution properties of prepared compacts. In examining the DSC spectra, the peak of the drug is eliminated,which can be due to solubility of part of the drug in the solvent, as well as the effect of dilution and amorphous drug. Conclusion: Obtained dissolution rate is due to enhanced special surface of drug to the medium in liquisolid state and also micronized drugs during ball mill process. The results showed that the liquiground technique could be a promising alternative technique to increase dissolution rate of water insoluble drugs without any change in crystallinity