Enhancement of intestinal absorption of poorly absorbed Ceftriaxone Sodium by using mixed micelles of Polyoxy Ethylene (20) Cetyl Ether & Oleic Acid as peroral absorption enhancers

By Singh Neelam, Gupta Puneet, Bhattacharyya Arundhati




Abstract

Ceftriaxone sodium is a third generation cephalosporin. This antibiotic cannot be absorbed orally owing to its very less permeation through GI epithelia. Other problem associated with the drug is its acid labile nature. The present study attempts to increase the intestinal permeability of BCS Class III drug ceftriaxone sodium by using certain intestinal absorption enhancers. The blend of permeation enhancer, drug, and other excipients were incorporated into Beads to formulate the final dosage form. To enhance the permeation, intestinal permeation enhancers were used in various molar ratios with the drug. The effect of absorption enhancers on the lipophilicity of ceftriaxone sodium was determined by means of the n-octanol/water system. The changes in partition coefficient by the octanol/water system were confirmed using an in vitro transport model with excised animal intestinal membrane. The results indicated that there is significant improvement in the permeability of the drug and the extent of enhancement was highly dependent on the type of used absorption enhancer. Permeation enhancer and drug were formulated into beads further evaluated for permeability by using biological membrane. The release profile of ceftriaxone from beads was observed in both gastric and intestinal pH (7.4 buffer). Release of drug from the beads in both the media was found to occur predominantly by diffusion following non Fickian transport mechanism and was higher and more rapid in intestinal pH than in gastric pH. The results obtained from this study indicate that ceftriaxone sodium could be successfully delivered orally when formulated with permeation enhancers.

Keywords: Intestinal permeability, permeation enhancers, beads, ceftriaxone sodium

 

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