An evaluation of the mechanisms of drug release from glyceride bases.
A series of dispersions containing theophylline in Gelucires 43/01, 54/02, 50/02, 50/13 and 55/18 was prepared and the physical structures studied using differential scanning calorimetry. The dissolution, erosion and swelling profiles of the drug dispersions were assessed. Gelucire 43/01 and 54/02 systems were found to release the drug by a simple diffusion mechanism, with no evidence for erosion or swelling being noted. Gelucire 55/18, however, showed a more complex mechanism involving both diffusion and erosion. On increasing the drug load within the matrices, the predominance of the erosion mechanism increased. Drug release from Gelucire 50/13 matrices took place principally by erosion, although the process was dominated by swelling and subsequent disintegration of the matrix, rather than simple dissolution of the base as was found for Gelucire 55/18. Gelucire 50/02 matrices also exhibited swelling, although drug release occurred predominantly via diffusion. The study, therefore, demonstrates that Gelucires may release incorporated drugs by a number of mechanisms depending on the chemical composition of the base.
Sutananta
W
W
Centre for Materials Science, School of Pharmacy, University of London, UK.
Craig
D Q
DQ
Newton
J M
JM
D000042:Absorption; D001665:Binding Sites; D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations; D004058:Diffusion; D016503:Drug Delivery Systems / Q000592:standards; D004952:Esters; D005079:Excipients / Q000737:chemistry / Q000378:metabolism; D005223:Fats / Q000737:chemistry / Q000378:metabolism*; D005227:Fatty Acids / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry / Q000378:metabolism*; D007700:Kinetics; D008859:Microscopy, Polarization; D009821:Oils / Q000737:chemistry / Q000378:metabolism*; D011092:Polyethylene Glycols / Q000737:chemistry; D013806:Theophylline / Q000378:metabolism* / Q000493:pharmacokinetics
D003692:Delayed-Action Preparations; D004952:Esters; D005079:Excipients; D005223:Fats; D005227:Fatty Acids; D005989:Glycerides; D009821:Oils; C071184:Gelucire 50-13; C071183:Gelucire 50-02; D011092:Polyethylene Glycols; D013806:Theophylline