Establishment And Application Of In-vitro Dissolution Evaluation Model Of Tacrolimus Capsules

Tacrolimus is a poorly water-soluble and macromolecular drug.and its individual bioavailability is very different.At present,tacrolimus capsules have not been registered in Chinese pharmacopoeia.This research establishes a dissolution method which could evaluate the quality of tacrolimus generic capsules,and evaluates the formulation by comparison of in-vitro dissolution profiles between tacrolimus generic drug and Prograf.In this paper,the solubility and apparent oil-water partition coefficient of tacrolimus amorphous and crystalline material have been investigated.The dissolution parameters including dissolution apparatus,medium,preparation method of medium,and rotate speed,etc.were improved as a new method.This paper also analyzed the tacrolimus reference listed drug(RLD).Formulation of tacrolimus capsules was evaluated by usingthe discriminative method.And effects of different particle sizes of intermediate product were studied.The similarity factor ?2 was calculated to compare dissolution profile of generic drug and RLD in different mediums.The in-vitro drug release behaviors of generic drug and RLD were similar.The method of dissolution was studies with tacrolimus as a model drug.It could provide suggestions and guidance for researching and establishing rational dissolution methods.The reasonable evaluation method of dissolution was prepared for genetic capsules,which provided a useful reference for generic conformance assessment.