Soluplus as a Potential Enhancer of Cefixime Biopharmaceutical Properties through Solid Dispersion Prepared by Different Pharmaceutical Interventions

The present study was done for improvement of solubility and thereby bioavailability of Cefixime for its efficient antimicrobial activity by using amphiphilic Soluplus as a carrier. Different methods were used for enhancing the solubility of Cefixime like physical mix, kneading, microwave irradiation, solvent evaporation, lyophilization and spray drying. The plain drug and the prepared SD with various CFX to polymer ratios were characterized in terms of solubility, drug content, IR, DSC, SEM, XRD, dissolution, zone of inhibition and in vivo studies. A noticeable change in the dissolution rate was observed by in vitro dissolution studies in relation with pure CFX. The solid dispersion of CFX prepared showed following order in enhanced amorphous micellerization ratio like Spray drying>Lyophilization>Microwave irradiation>Solvent evaporation>Kneading method>Physical mixture>Pure drug. In addition, spray dried solid dispersion demonstrated remarkable highest inhibition of microbial zone than plain Cefixime (CFX) suggesting improvement in antibacterial activity of Cefixime by solid dispersion. Pharmacokinetic work by (n=6) rats demonstrate a significant difference (a=0.05) when the mean Cmax concentration from spray dried SD and Cefixime (CFX) were compared. The AUC was 1.9 times more in Cefixime (CFX) as SD administration, against the AUC obtained for the plain Cefixime (CFX) suspension. After SD dosing, Tmax (4 h) was different than that obtained in pure drug suspension (3 h). Thus, formulation of Cefixime (CFX) as SD, enhanced amorphous micellerization ratio of the drug and lead to significant (p=0.05) increase in absorption of Cefixime. Hence, Soluplus proved to be potential hydrophile for increasing oral bioavailability of Cefixime using spray drying technique and leading to improved health of patient with reduced dose of drug.

Author(s): Poonam Mogal and Deeliprao Derle

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