Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100
Alginate vehicles are capable of forming a gel matrix in situ when they come 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 sit...
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2014-03-01
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| Series: | Acta Pharmaceutica |
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| author | Maghraby Gamal Mohamed El Elzayat Ehab Mostafa Alanazi Fars Kaed |
| author_facet | Maghraby Gamal Mohamed El Elzayat Ehab Mostafa Alanazi Fars Kaed |
| author_sort | Maghraby Gamal Mohamed El |
| collection | DOAJ |
| description | Alginate vehicles are capable of forming a gel matrix in situ when they come 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 dextromethorphan 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 commercial sustained-release liquid based on ion exchange resin. The release pattern indicated strict control of drug release both under gastric and intestinal conditions, suggesting the potential advantage of using a solid dispersion of drug-Eudragit S 100 to overcome the problem of dose dumping after the rupture of the pH dependent alginate gels |
| format | Article |
| id | doaj-art-5dfeb3a4d8cd4e21a700c4380d1696e7 |
| institution | Kabale University |
| issn | 1330-0075 1846-9558 |
| language | English |
| publishDate | 2014-03-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj-art-5dfeb3a4d8cd4e21a700c4380d1696e72025-02-03T02:42:39ZengSciendoActa Pharmaceutica1330-00751846-95582014-03-01641294410.2478/acph-2014-0002acph-2014-0002Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100Maghraby Gamal Mohamed El0Elzayat Ehab Mostafa1Alanazi Fars Kaed2Department of Pharmaceutics College of Pharmacy, King Saud University Riyadh 11451, P.O. Box 2457 Saudi Arabia / Department of Pharmaceutical Technology College of Pharmacy, University of Tanta Tanta, EgyptDepartment of Pharmaceutics College of Pharmacy, King Saud University Riyadh 11451, P.O. Box 2457 Saudi ArabiaDepartment of Pharmaceutics College of Pharmacy, King Saud University Riyadh 11451, P.O. Box 2457 Saudi Arabia / Alkayyali Research Chair for Pharmaceutical Industries College of Pharmacy, King Saud UniversityAlginate vehicles are capable of forming a gel matrix in situ when they come 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 dextromethorphan 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 commercial sustained-release liquid based on ion exchange resin. The release pattern indicated strict control of drug release both under gastric and intestinal conditions, suggesting the potential advantage of using a solid dispersion of drug-Eudragit S 100 to overcome the problem of dose dumping after the rupture of the pH dependent alginate gelshttp://www.degruyter.com/view/j/acph.2014.64.issue-1/acph-2014-0002/acph-2014-0002.xml?format=INTdextromethorphansolid dispersionin situ gellingalginate gels |
| spellingShingle | Maghraby Gamal Mohamed El Elzayat Ehab Mostafa Alanazi Fars Kaed Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100 Acta Pharmaceutica dextromethorphan solid dispersion in situ gelling alginate gels |
| title | Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100 |
| title_full | Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100 |
| title_fullStr | Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100 |
| title_full_unstemmed | Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100 |
| title_short | Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100 |
| title_sort | investigation of in situ gelling alginate formulations as a sustained release vehicle for co precipitates of dextromethrophan and eudragit s 100 |
| topic | dextromethorphan solid dispersion in situ gelling alginate gels |
| url | http://www.degruyter.com/view/j/acph.2014.64.issue-1/acph-2014-0002/acph-2014-0002.xml?format=INT |
| work_keys_str_mv | AT maghrabygamalmohamedel investigationofinsitugellingalginateformulationsasasustainedreleasevehicleforcoprecipitatesofdextromethrophanandeudragits100 AT elzayatehabmostafa investigationofinsitugellingalginateformulationsasasustainedreleasevehicleforcoprecipitatesofdextromethrophanandeudragits100 AT alanazifarskaed investigationofinsitugellingalginateformulationsasasustainedreleasevehicleforcoprecipitatesofdextromethrophanandeudragits100 |