Document Detail

An investigation into the mechanisms of drug release from taste-masking fatty acid microspheres.
MedLine Citation:
PMID:  18200505     Owner:  NLM     Status:  MEDLINE    
Fatty acid microspheres based on stearic and palmitic acids are known to form effective taste masking systems, although the mechanisms by which the drug is preferentially released in the lower gastrointestinal tract are not known. The objective of the present study was to identify the mechanisms involved, with a particular view to clarify the role of acid soap formation in the dissolution process. Microspheres were prepared by a spray chilling process. Using benzoic acid as a model drug and an alkaline dissolution medium, a faster drug release was observed in the mixed fatty acid formulation (50:50 stearic:palmitic acid (w/w)) compared to the single fatty acid component systems. Thermal and powder X-ray diffraction studies indicated a greater degree of acid soap formation for the mixed formulation in alkaline media compared to the single fatty acid systems. Particle size and porosity studies indicated a modest reduction in size for the mixed systems and an increase in porosity on immersion in the dissolution medium. It is proposed that the mixed fatty acid system form a mixed crystal system which in turn facilitates interaction with the dissolution medium, thereby leading to a greater propensity for acid soap formation which in turn forms a permeable liquid crystalline phase through which the drug may diffuse. The role of dissolution of palmitic acid into the dissolution medium is also discussed as a secondary mechanism.
Sheng Qi; David Deutsch; Duncan Q M Craig
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  97     ISSN:  1520-6017     ISO Abbreviation:  J Pharm Sci     Publication Date:  2008 Sep 
Date Detail:
Created Date:  2008-08-05     Completed Date:  2008-12-05     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  3842-54     Citation Subset:  IM    
School of Chemical Sciences and Pharmacy, University of East Anglia, Norwich, Norfolk NR4 7TJ, UK.
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MeSH Terms
Calorimetry, Differential Scanning
Drug Carriers*
Fatty Acids / chemistry*
Microscopy, Electron, Scanning
Particle Size
Sensitivity and Specificity
X-Ray Diffraction
Reg. No./Substance:
0/Drug Carriers; 0/Fatty Acids

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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