Pharmacokinetics, tissue distribution, and excretion study of Neocryptotanshinone in rats using liquid chromatography‐tandem mass spectrometry

Abstract

Salvia miltiorrhiza Bunge is a Traditional Chinese Medicine used for the treatment of diseases related to the heart and liver. Owing to the abundance of salvianolic acids and tanshinones, S. miltiorrhiza exhibits various pharmacological activities, such as stimulating blood circulation, eliminating blood stasis, relieving menorrhea and pain, and improving polydipsia. Neocryptotanshinone (NCTS) is one of the tanshinones isolated from S. miltiorrhiza and exhibits anti‐inflammatory, hypoglycemic, and preventive effects against cardiovascular diseases; however, its pharmacokinetic properties have not been reported to date. Therefore, a simple and reliable LC–MS/MS method was developed to determine absorption, distribution, and excretion of NCTS in rat physiological samples. We demonstrated that NCTS had high oral absolute bioavailability of 85.96% ± 25.32%, and it was rapidly distributed in both the heart and brain, and the fecal excretion of NCTS was the highest. This study provides a theoretical basis for further development of NCTS as a potential clinical candidate.