Assessments of Stability and Pharmacokinetics of Gambogenic Acid in Rats

作者：Sun, Jing; Tang, Xiaozhu; Xu, Qianqian; Ge, Tao; Peng, Daiyin; Chen, Weidong^*

来源：Latin American Journal of Pharmacy, 2018, 37(7): 1333-1339.

• absorption
• cytochrome P450
• gambogenic acid
• pharmacokinetic
• stability

Gambogenic acid (GNA), obtained from the resin of Garcinia hanburyi, is a bioactive compound possessing diverse anti-tumor activities. This study was designed to assess the stability and pharmacokinetics of GNA. After intragastric administration (i.g.) and intravenous injection (i.v.) to rats, the pharmacokinetics were investigated. GNA was eliminated relatively rapidly in the rats. The bioavailability of i.g. group was estimated as 21.38%. In the gastrointestinal absorption test, the decreased amount of GNA was approximately 20% in the stomach and 50% in the intestine, respectively. Moreover, GNA was found relatively stable in the simulated gastric fluid (SGF, pH 1.2) and simulated intestinal fluid (SIF, pH 6.8). While in the SIF (pH 7.4) and Krebs-Rings solution (pH 6.8), GNA was unstable, down by 30%. In addition, GNA might be metabolized by cytochrome P450 (CYP450) in rat liver microsomes, such as CYP1A2, CYP2C, CYP2D2 and CYP3A1. Taken together, these results show that the low bioavailability of GNA after oral administration in rats may be affected by chemical stability of GNA, the pH value and CYP450 enzymes.

• 出版日期2018
• 单位安徽大学