Journal of Pharmaceutical Research International

To increase the effectiveness of tacrolimus, the present study sought to develop extended-release tablets. It is used to treat mild to severe atopic dermatitis as well as to prevent organ rejection after organ transplantation. Tacrolimus, on the other hand, has a poor bioavailability and a short half-life. The current research aims to create extended-release tacrolimus tablets by melting and granulating utilizing lipid and adsorbent materials to ensure excellent flow and a hypromellose matrix system to regulate release for 12 hr. Tacrolimus granules were prepared by melting with glyceryl behenate in rapid mixer granulator in the presence of polyethylene glycol followed by magnesium alumino metasilicate for adsorption purposes. Adsorbed granules were milled, sifted, and mixed with extra granular material such as hypromellose, lactose monohydrate and magnesium stearate. Granules were compressed to tablets using oval-shaped plain tooling. In vitro dissolution profile of solid dispersion and extended release tablets were investigated. Release profile of tablets and solid dispersion were improved by melt granulation due to the polymorphic form conversion of drug substance from crystalline to amorphous.Release kinetics of tacrolimus extended release tablets were fitted with zero order release with R² value of 0.964, which designate constant release for 12 hr. Therefore, the present findings from the study revealed that the formulation was successfully prepared and showed extended release pattern over 12 hr.