CRITICALITY OF SOLUBILIZER SELECTION DURING FORMULATION DEVELOPMENT OF POORLY WATER SOLUBLE CEFIXIME

In Recent Years, The Pharma Industry Has A Wide Variety Of Excipients Available For The Formulation Development, Where Selecting The Effective Functional Excipient Is A Critical Step In Early Stage. For Selecting Suitable Type Of Solubilizer Through Its Solubilizing And Absorption Enhancer Property Towards Cefixime, Various Solubilizers Like Urea, PEG, HPMC, Kollidon 64 And Gaur Gum Were Investigated. Solid Binary Systems Prepared At Various Drug–Polymer Ratios By Mixing, Kneading, Solvent Evaporation, Lyophilization, Microwave Irradiation & Spray Drying Were Characterized By DSC, XRD, SEM, Attenuated Total Reflectance, Saturated Solubility Study And Tested For Dissolution Behavior. The Solubilizing Effect Of Polymers On Poorly Soluble Cefixime Was Found To Be Of Following Order: Kollidon 64>Urea>Gaur>PEG>HPMC. The Dissolution Studies Displayed A Noticeable Augment In The Dissolution Rate Than Neat Cefixime. The Dispersion Of Drug Processed By Spray Drying Demonstrated Higher Drug Dissolution Rates In Comparison To Physical Mixture And Pure Cefixime. In Vivo Experiments In Mice Demonstrated That Administration Of 4 Mg/Kg Of Drug Spray Dried Systems With Kollidon 64 Resulted In Statistically Significant (P = 0.006) Increase (227%) In Cmax With Tmax (P = 0.03) Of 4 Hr. The 1/1 (W/W) Drug–Carrier Spray Dried Systems With Kollidon 64 Was The Best Product Enabling An Improvement Of 4.8 Times Of Drug Dissolution Efficiency And Better Antibacterial Activity With Zone Of Inhibition 2.4 Times Higher Than The Pure Cefixime. Thus, The Demonstrated Solubilizing Ability And Antibacterial Enhancer Effect Towards Cefixime Make Kollidon 64 Peculiarly Suitable For Development Of Poorly Soluble Cefixime.