The Formulation And Pharmacokinetics Research Of Donepezil Hydrochloride Extended-Release Tablets

Donepezil Hydrochloride Extended-Release Tablets (Strength:23mg) was developed by Eisai and Pfizer, and was approved by FDA on July 23,2010. This product is indicated for moderate and server Alzheimer disease. Ethyl Cellulose and Methacrylic acid copolymer, which are insoluble materials, are used as extended release matrix in the brand formulation. Lactose Monohydrate and the above insoluble sustained release materials can solve the stability of amino groups mixed with the extended release matrix, and the formulation is patented.Therefore, soluble sustained release materials were developed as the extended release matrix in this study. Analytical methods of assay, dissolution and related substance were established. Donepezil Hydrochloride extended release tablets were produced by dry granulation process. The formulation and process were optimized by orthogonal design, and in-vitro dissolution results matched with the brand well. The accelerated stability and bioequivalence was studied.The bioequivalence result shows that:test sample is bioequivalent to the brand in fast study. However, it is not bioequivalent to the brand in fed study. The results provide reference for the future study.