A Study On Donepezil Hydrocloride Tablets

OBJECTS: To prepare Donepezil hydrocloride tablets and to confirm the prescription and technics by pilotscale experiment; To study the quality and the stability of the Donepezil hydrocloride tablets; And to study the relative bioavailability of Donepezil hydrocloride tablets and evaluate the bioequivalence. METHODS: Established two methods for the determination of Donepezil hydrocloride: ultraviolet spectrophotome-try and R-HPLC. Ultraviolet spectrophotometry was used to test content uniformity and dissolution; While R-HPLC was used to test content and related substances. The hygroscopicity of Donepezil hydrocloride was appraised. The interaction of Donepezil hydrocloride and pharmaceutical aids was appraised by appearance, content and related substances.Studied the prescription and technics by the indexs of appearance, hardness and disintegrating time with the single factor design and the uniformal design; Prepared orally disintegrating tablets and common tablets and did pilotscale experiment, then selected the one that can be industried to study. Studied quanlity criterion, and compared the content and dissolution with that of Aricept; Studied the primary stability by appearance, content and related substances; Used R-HPLC method for the determination of Donepezil hydrocloride in plasma, and tested drugs as randomized design. RESULTS: The specificity, linearity, precision, accuracy and ruggedness were all conformed to the Chinese Phamacopoeia. After 10 days of Donepezil hydrocloride and pharmaceutical aids placement under the conditions of stress testing, the content of Donepezil hydrocloride still remained from 90% to 110%. The Donepezil hydrocloride CRH was 73%. The technics of the common tablets were easy and feasible and fit forindustrialization. And every index of the tablets was conformed to the prescript. The dissolution in vitro was according with Weibull psi function and it was above 85% on 15 minutes and the differents of T_d and T₅₀ btween the preparation and Aricept weren't of statistics meaning(P>0.05). The accuracy and precision of the method satisfied the requirements. 3P87 program was applied to calculating the pharmacokinetics parameter and evaluating the bioequivalence. The results of the statistical analysis showed that the reference and the test drugs were bioequivalence; CONCLUSIONS: The qualities of the preparation were stable, and the preparation was easied to be industried. And the reference and the test drugs were bioequivalence.