DEVELOPMENT AND CHARACTERIZATION OF INNOVATIVE LIQUID SALT BASED FORMULATIONS OF SPARINGLY SOLUBLE DRUGSAbstract
As a result of tremendous efforts in past few decades, various techniques have been developed in order to resolve solubility issues. However, majority of these techniques offer benefits associated with certain drawbacks; majorly including low drug loading, physical instability on storage and excessive use of environmentally challenging organic solvents. Hence, current effort was to develop an eco-friendly technique using liquid salt, which can offer improvement in dissolution while maintaining long term stability. The liquid salt formulations of poorly soluble model drugs ibuprofen, gemfibrozil and indomethacin were developed using 1-Ethyl-3-methylimidazolium ethyl sulfate (EMIM ES) as a non-toxic and environmentally friendly alternate to organic solvents. Liquid medications containing clear solutions of drug, EMIM ES and polysorbate 20, were adsorbed onto porous carrier Neusilin US2 to form free flowing powder. Liquid loading as high as 70% w/w was achieved while maintaining good flowability and compressibility. The liquid salt based formulations (LSF) demonstrated greater rate and extent of dissolution compared to crystalline drugs. The LSF samples exposed to 40°C/80% RH for 8 weeks, demonstrated excellent physical stability without any signs of precipitation or crystallization. The liquid salt formulation technique served as compelling alternate to the conventional techniques for the development of poorly soluble compounds.
Anant A. Patel and Rutesh H. Dave*
Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Division of Pharmaceutical Sciences, Long Island University, Brooklyn, NY, USA
13 October, 2014
15 January, 2015
17 February, 2015
01 June, 2015