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COATED TABLETS CONSISTING OF A SUPER DISINTEGRANT CORE AND ITS EFFECT ON DRUG RELEASE
Third-party funded project
Project title COATED TABLETS CONSISTING OF A SUPER DISINTEGRANT CORE AND ITS EFFECT ON DRUG RELEASE
Principal Investigator(s) Betz, Gabriele
Co-Investigator(s) Darronqui, Elaine
Organisation / Research unit Departement Pharmazeutische Wissenschaften / Pharmaceutical Technology (Huwyler),
Departement Pharmazeutische Wissenschaften / Industrial Pharmacy Lab (Betz)
Project start 01.10.2008
Probable end 30.09.2011
Status Completed
Abstract

Microcrystalline Cellulose (MCC), and its modifications, are well known and wide spread used excipients in the pharmaceutical industry. Cellulose II polymorph, which is obtained by mercerization from cellulose I polymorph (MCC), shows to behave as multifunctional excipient, working like filler as well as a super disintegrant. The objective of the present work was to investigate the possibility to create a modified drug release system based on rupturable coating applying to the cellulose II polymorph core, as well as to check the behavior of this core during an aqueous coating process. Three formulations containing cellulose II and proquazone, a poor water soluble drug, were produced. The amount of cellulose II in the mixtures was 10, 50 and 90% (w/w). Granules were produced using a lab scale high shear mixer and the power consumption was measured to monitor the process. After compression the tablet cores were coated in a bottom spray lab scale fluidized bed with Eudragit RS® 30D, Eudragit RL® 30D and Aquacoat ECD® 30%. Subsequently, the drug release profile was analyzed using USP paddle method. The results showed that an aqueous coating process is possible using a core with a high load of a super disintegrant if the proper parameters are set, regarding the inlet temperature, atomizing air and spray rate. The drug release showed to be dependent on the polymer type, the thickness of the coating layer and core composition. A sustained drug release with no lag time was obtained using different mixtures of Eudragit® polymers. A delayed drug release, with a sigmoidal curve, and presenting different lag times according to the coating thickness, was obtained with Aquacoat. With thinner coating layers the lag time showed to be similar between the tablets containing 50 and 90% of cellulose II, showing the influence of this excipient in the core by swelling and coating disruption. These findings reveal a good opportunity to develop a modified drug delivery system based on approved and well known excipients and also applying conventional processes.

Financed by Foundations and Associations
   

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