The invention provides a
tacrolimus sustained-release preparation and a preparation method thereof. The invention adopts a
solid dispersion technology, or
cyclodextrin inclusion technology or a solubilizing method for micronizing drugs and then adding one or more types of surfactants and the like, and obviously improves
solubility thereof so as to improve the
bioavailability thereof, then adds oneor more types of skeleton materials and other auxiliary materials so as to prepare a skeleton type sustained-release preparation, or adopts a sustained-release material to carry out
coating so as toprepare a diaphragm-controlled type or
osmotic pump type sustained-release preparation. The
tacrolimus sustained-release preparation has better
solubility and
dissolution rate, high
bioavailability and sustained-controlled-release effect, thus maintaining stable blood and
drug concentration, reducing the occurrence rate of adverse reaction, and improving clinical
drug safety; in addition, the invention has easy obtaining for materials, simple and feasible preparation technique, high yield and low cost, can realize large-scale industrialized production and has obviously economical benefit.