Tyrosine kinase inhibitors (TKIs) play a crucial role in the treatment of various cancers. In particular, this drug is sold as a drug that inhibits abnormal proteins produced by the abnormal chromosome, the Philadelphia chromosome. In this study, we compared the formulation and release characteristics of a new TKI formulation with those of a reference drug. Preformulation studies indicated that the drug absorption site was the upper part of the stomach and small intestine. To optimize the formulation, we conducted dissolution tests on test drugs and the reference drug in pH 1.2 and pH 4.5 solutions. By analyzing the dissolution test results, we compared the release profiles of test drugs and the reference drug. Various formulations were manufactured by altering the disintegrant ratio and coating agent. As a result of In vitro studies revealed that the final formulation, coated with hydroxypropyl methylcellulose and using sodium croscarmellose as the disintegrant, exhibited comparable release profiles and bioavailability to the reference drug. Therefore, the new TKI formulation has been established as therapeutically equivalent to the reference drug, with similar efficacy and safety expectations.
2024 Spring Convention