The invention relates to a water-
insoluble drug, namely,
tacrolimus sustained-release tablets. The
tacrolimus sustained-release tablets take a lipid material, a water-soluble material, a stabilizer and the like as a carrier, and are prepared by adopting a melting method to prepare a
solid dispersion which is stable in properties and is capable of obviously improving the
dissolution rate of
tacrolimus, blending the prepared
solid dispersion with a sustained-release material, a
diluent and other pharmaceutical necessities, and tabletting the mixture. The tacrolimus sustained-release tablets have the unique advantages that (1) the sustained-release tablets are simple in formulation and technology, and can be formed by directly tabletting
powder without adding auxiliary materials such as a lubricating agent and a binding agent; (2) the low-melting-point lipid material is used, the
medicine can be directly dissolved in the molten lipid material and is then cooled and cured, and a volatile
organic solvent does not need to be treated, so that the production safety is greatly improved, and the environmental
pollution is reduced; (3) the
quaternary solid dispersion formed by the
medicine, the lipid material, the water-soluble material and the stabilizer is good in stability, so that the
dissolution rate of the tacrolimus sustained-release tablets does not change significantly after the tacrolimus sustained-release tablets are placed for a period of time; (4) the tacrolimus sustained-release tablets can reduce the times of administration, thus reducing the fluctuation of
plasma concentration.