Orally Disintegrating Drug Delivery System

Orally disintegrating tablet (ODT) is a new strategic tool for Drug delivery system. Many ODT products have come to global market, and the researches are moving rapidly. In this paper, we focused on the formulation and process design, as well as the development of taste masking system and extended release system. The investigation aimed to provide practice and theory on the drug delivery system.In this paper, the co-processed excipient (Pharmaburst Powder) was applied to prepare ODTs by direct compression. Three model drugs with different physicochemical properties (5-hydroxytryptophan, famotidine, and acetaminophen) were used and evaluated. The final formulation was model drug 24.5%, the co-processed material 60%, HPMC 7.5%, PVP 5%, citric acid 1%,SSF 2%. The additions of polymer improve the wettability and dissolution.Three different taste masking systems (granulation, coating granulation and spray-dried microspheres) were prepared and evaluated. The conclusion was the spray-dried microspheres can not only improve the taste and mouth feel but also one step process and easy to control. So the spray-dried microsphere was the best taste masking system. The microspheres were produced by spray drying a mixture of the famotidine with polymer (drug:Eudragit EPO?:glidant:PEG 400=1:2:1:0.2). The spray process was optimized using a central composite design and the final parameters were inlet temperature 110℃; aspirator setting 90%; solid concentration 34 mg/ml; flow rate 7 ml/min. The encapsulation efficiency was 61.56%. SEM proves the integrated structure of the tabletted microspheres. The taste masking ODTs can disintegrate in buccal cavity within 1 min.For preparation of the extended release microspheres, the mixture of Eudragit RS 30D? and acetaminophen was spray dried. The ODTs with the microspheres can extend the release to 12h and follow the first order release kinetics. The tablet with microspheres can disintegrate in buccal cavity within 1 min. DSC proved the drug completely entrapped in the polymer matrix.The stability test demonstrated the acceptable stability of the final products. However the storage of the products should keep in dryness.In vivo the taste masking famotidine ODTs improved the bioavailability and exhibited fast release profile. And the extended release acetaminophen ODTs exhibited the extended release profile.In conclusion, we prepared the good quality ODTs by direct compression. Spray-dried microspheres can be applied as taste masking or the extended release system. The investigation has important meaning for the future research and product development.