Hot-melt coating technology. I. Influence of Compritol 888 Ato and granule size on theophylline release.
The aim of this work was to study the influence of theophylline granule size and the percentage of Compritol 888 Ato on in vitro drug release from granules and tablets. The granules were coated in a fluidized bed apparatus. The dissolution profiles of these granules differed from those of granules coated with classical agents, and there were also differences between the various sieve fractions studied. Drug release was characterized by a rapid-release phase, followed by a slow-release phase. Results indicate that theophylline release can be controlled by controlling granule size. Inspection of the appearance of the tablets at the end of the dissolution test revealed that all tablets containing Compritol 888 Ato remained intact. This indicated that the Compritol 888 Ato used in the tablet formulation created an inert matrix through which the drug diffused. It was found that the Higuchi relationship of linear square root of time was the best model to describe the release kinetics of the drug from tablets. This also confirmed that a matrix diffusion-controlled mechanism was operative. Given the difference between the dissolution profiles of the granules and the tablets, it was concluded that this matrix is formed during compression.
Faham
A
A
Laboratoire de Pharmacie Galénique, Faculty of Pharmacy, Marseille, France.
Prinderre
P
P
Farah
N
N
Eichler
K D
KD
Kalantzis
G
G
Joachim
J
J
D001993:Bronchodilator Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D003692:Delayed-Action Preparations; D005227:Fatty Acids / Q000378:metabolism*; D006358:Hot Temperature; D006801:Humans; D007700:Kinetics; D010316:Particle Size; D013607:Tablets; D013806:Theophylline / Q000008:administration & dosage / Q000493:pharmacokinetics*
D001993:Bronchodilator Agents; D003692:Delayed-Action Preparations; D005227:Fatty Acids; D013607:Tablets; C086409:glyceryl behenate; D013806:Theophylline