Integrating In Vitro Dissolution and Physiologically Based Pharmacokinetic Modeling for Generic Drug Development: Evaluation of Amorphous Solid Dispersion Formulations for Tacrolimus.

ABSTRACT: Objectives: Tacrolimus, a Biopharmaceutics Classification System (BCS) class II drug, is widely used for transplant patients to prevent graft rejection. To enhance its bioavailability, amorphous solid dispersion (ASD) formulations were developed and evaluated. The release properties of several ASD-based tacrolimus formulations were studied using an in-house USP IV dissolution method. Methods: The pharmacokinetics of a promising test product were compared with the commercially available Advagraf^® in a pilot clinical bioequivalence study with 12 healthy subjects. A previously published PBPK model for tacrolimus was validated using in vivo data and then applied to predict the human pharmacokinetics of several ASD-based tacrolimus formulations. Results: This stu

SUBMITTER: Karakitsios E 

PROVIDER: S-EPMC11858865 | biostudies-literature | 2025 Feb

REPOSITORIES: biostudies-literature