Acta Pharm. 64 (2014) 29-44
Original research paper
Investigation
of in situ gelling alginate formulations as a sustained release vehicle
for co-precipitates of dextromethrophan and Eudragit S 100
GAMAL
MOHAMED EL MAGHRABY, EHAB MOSTAFA ELZAYAT and FARS KAED ALANAZI
1
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh
11451, P.O. Box: 2457, Saudi Arabia
2
Department of Pharmaceutical Technology, College of Pharmacy, University of
Tanta, Tanta, Egypt
3 Alkayyali
Research Chair for Pharmaceutical Industries, College of Pharmacy, King Saud
University
Accepted September 16, 2013
Alginate vehicles are capable of forming gel matrix in situ, when comes into contact with gastric medium in the presence of calcium ions. However, the gel structure is pH dependent and can break after gastric emptying, leading to dose dumping. The aim of this work was to develop modified in situ gelling alginate formulations capable of sustaining dextromethrophan release throughout the gastrointestinal tract. Alginate solution (2 %, m/m) was used as a vehicle for the tested formulations. Solid matrix of the drug and Eudragit S 100 was prepared by dissolving the drug and polymer in acetone. The organic solvent was then evaporated and the deposited solid matrix was micronized, sieved and dispersed in alginate solution to obtain candidate formulations. The release behavior of dextromethorphan was monitored and evaluated in a medium simulating the gastric and intestinal pH. Drug-polymer compatibility and possible solid-state interactions suggested physical interaction through hydrogen bonding between the drug and the polymer. A significant decrease in the rate and extent of dextromethorphan release was observed with increasing Eudragit S 100 concentration in the prepared particles. Most formulations showed sustained release profiles similar to that of a sustained release commercial liquid which is based on ion exchange resin. The release pattern indicated strict control of drug release both in the gastric and intestinal conditions, suggesting the potential advantage of using solid dispersion of drug-Eudragit S 100 to overcome the problem of dose dumping after the rupture of the pH dependant alginate gels.
Keywords: dextromethorphan, solid dispersion, in situ gelling,
alginate gels