Author(s): Gu Y, Wang GJ, Sun JG, Jia YW, Wang W, et al.
The pharmacokinetic characteristics of ginsenoside Rh2, an anticancer nutrient, were analyzed in dogs and rats, including plasma kinetics, bioavailability, tissue distribution, plasma protein binding and excretion. The bioavailability of Rh2 is about 5% in rats and 16% in dogs. Multiple-dosing (7 days, 1 mg/kg bid) did not affect the pharmacokinetics in dogs. After oral dosing, Rh2 distributed mainly to the liver and gastrointestinal tissues in rats. In rats, the circulating fraction of Rh2 bound to plasma proteins was around 70%. The systemic clearance, however, was low -- around 2 and 20 ml/min/kg in dogs and rats, respectively. Only 1% of dosed Rh2 were recovered in excreta of rats as the intact form after oral administration, while 30% was excreted unchanged in bile after i.v. dosing. We subsequently investigated the membrane permeability of Rh2 across Caco-2 cell monolayers, stability and elimination profiles in the gastrointestinal environment. Low membrane permeability (P(app)(AP-BL): 1.91 x 10(-8)cm/s), efflux transport (efflux ratio: 9.8), pre-systemic elimination (degradation in acidic condition; metabolism in intestine tissue and contents), as well as low solubility largely accounted for the low bioavailability of Rh2. Regarding the low solubility of Rh2, micronization of the dose almost doubled the rate of absorption in dogs. Preliminary metabolite profiling confirmed the presence of the deglycosidating product protopanaxadiol in rat feces. A possible metabolite in rat bile and a potential sulfate-conjugate in rat urine were also detected.
Referred From: https://www.ncbi.nlm.nih.gov/pubmed/19524010
Author(s): Middleton E Jr, Kandaswami C, Theoharides TC
Author(s): Mozaffarian D, Rimm EB
Author(s): Calder PC, Yaqoob P
Author(s): Zuchi C, Ambrosio G, Luscher TF, Landmesser U
Author(s): Shukla SK, Gupta S, Ojha SK, Sharma SB
Author(s): Ceylan-Isik AF, Fliethman RM, Wold LE, Ren J
Author(s): Hsiao WL, Liu L
Author(s): Chan E, Tan M, Xin J, Sudarsanam S, Johnson DE
Author(s): Xiang YZ, Shang HC, Gao XM, Zhang BL
Author(s): Berman M, Erman A, Ben-Gal T, Dvir D, Georghiou GP, et al.
Author(s): Weant KA, Smith KM
Author(s): Sander S, Coleman CI, Patel AA, Kluger J, White CM
Author(s): Shibata S, Fujita M, Itokawa H, Tanaka O, Ishii T
Author(s): Lu JM, Yao Q, Chen C
Author(s): Deng J, Lv XT, Wu Q, Huang XN
Author(s): Chan RY, Chen WF, Dong A, Guo D, Wong MS
Author(s): Hasegawa H, Uchiyama M
Author(s): Leung KW, Cheung LW, Pon YL, Wong RN, Mak NK, et al.
Author(s): Kitagawa I, Yoshikawa M, Yoshihara M, Hayashi T, Taniyama T
Author(s): Fei XF, Wang BX, Tashiro S, Li TJ, Ma JS, et al.
Author(s): Kim HS, Lee EH, Ko SR, Choi KJ, Park JH, et al.
Author(s): Hasegawa H, Sung JH, Matsumiya S, Uchiyama M, Inouye Y, et al.
Author(s): Jia WW, Bu X, Philips D, Yan H, Liu G, et al.
Author(s): Xie X, Eberding A, Madera C, Fazli L, Jia W, et al.
Author(s): Wang Z, Zheng Q, Liu K, Li G, Zheng R
Author(s): Zhang J, Zhou F, Wu X, Gu Y, Ai H, et al.
Author(s): Wang H, Zou H, Kong L, Zhang Y, Pang H, et al.
Author(s): Shangguan D, Han H, Zhao R, Zhao Y, Xiong S, et al.
Author(s): Kwon SW, Han SB, Park IH, Kim JM, Park MK, et al.
Author(s): Li L, Zhang JL, Sheng YX, Ye G, Guo HZ, et al.
Author(s): Yu K, Ma Y, Shao Q, Qu H, Cheng Y
Author(s): Li X, Sun J, Wang G, Hao H, Liang Y, et al.
Author(s): Joo KM, Lee JH, Jeon HY, Park CW, Hong DK, et al.
Author(s): Zhang X, Zhang D, Xu J, Gu J, Zhao Y
Author(s): Yang L, Xu SJ, Zeng X, Liu YM, Deng SG, et al.
Author(s): Qian T, Cai Z, Wong RN, Jiang ZH
Author(s): Xie HT, Wang GJ, Sun JG, Tucker I, Zhao XC, et al.
Author(s): Jiang L, Zhao S, Ya L, Li J
Author(s): Li XW, Gui MY, Zheng Y, Jin YR, Zhang HQ
Author(s): Xie HT, Wang GJ, Lv H, Sun RW, Jiang XL, et al.