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Merck

Modeling of drug release from partially coated matrices made of a high viscosity HPMC.

International journal of pharmaceutics (2004-04-29)
Mario Grassi, Lucia Zema, Maria Edvige Sangalli, Alessandra Maroni, Ferdinando Giordano, Andrea Gazzaniga
RÉSUMÉ

A mathematical model able to describe the release kinetics of two model drugs (Diprophylline and Theophylline) from partially coated hydroxypropylmethylcellulose (HPMC, Methocel) K4M) matrices is presented. As solvent interaction with the system and drug release can only take place in one direction, the physical frame to be modeled turns out simpler. The model was developed starting from the established equation describing drug dissolution and taking into account the resistance to drug release given by the presence of a growing gel barrier around a matrix system. The model fits the release data obtained from both series of hydrophilic matrices containing increasing amounts (from 0.2 to 0.8 mass ratio) of the two xanthine derivatives. Differences were found in drug release rate according to the different solubility of the actives. Interestingly, however, there is no further reduction in the outer gel layer permeability when the polymer mass fraction exceeds a certain value, with both Theophylline and Diprophylline systems. Results confirm the importance of the fraction of the glassy/rubbery interface held by the active substance in defining the release rate from hydrophilic systems.

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Sigma-Aldrich
7-(2,3-Dihydroxypropyl)theophylline