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Pharmacokinetics (ADME)

June 08, 2020

Pharmacokinetics (ADME) by Pubmed.gov

 

Evaluation of the intramuscular and intravenous pharmacokinetics of a dry extract of Panax notoginseng root in humans showed unchanged saponins were the major circulating forms after intramuscular administration, while their metabolites were poorly detected. Zhang 2020

Ginsenoside F1, ginsenoside Rh2, ginsenoside compound K, and protopanaxatriol, metabolites found in Panax notoginseng, were detected in rat plasma while they could not be determined in germ-free rat plasma, indicating that the microbiome may play a role in bioavailability of P. notoginseng saponins. Guo 2019

The pharmacokinetics and glycosylation end products of Panax notoginseng leaves administered to germ-free and normal microbiome rats were evaluated; in pseudo germ-free rats, glycosidase activities were significantly decreased, and no obvious degradation occurred. Ju 2019

The saponins NR1, GRg1, and GRb1 from a Panax notoginseng Traditioal Chinese Medicine formula were quantified in human plasma via LC-MS/MS after oral administration. Li 2019

Metabolite profiles of ginsenosides Rk3 and Rh4 from steamed Panax notoginseng in zebrafish were qualitatively determined by ultraperformance liquid chromatography/quadrupole -time-of-flight mass spectrometry. Chen 2015

After oral and intravenous administration, notoginsenoside Fc exhibited dose-independent pharmacokinetic behaviors in rats with a t1/2 of >22h and oral bioavailability of 0.10-0.14%; deglycosylation was found to be the major metabolic pathway. He 2015

The distribution of notoginsenoside R1, ginsenosides Rg1, Rb1, Re, and Rd, and the saponin fraction from Panax notoginseng were measured in the rat cortex, striatum, hypothalamus, medulla oblongata, hippocampus, and olfactory bulb. Guo 2014

Intravenous administration of Panax notoginseng saponins decreased the elimination rate of the Radix Scutellariae flavonoid baicalin from rat plasma, promoted the penetration of baicalin into the rat brain, and slowed the elimination of baicalin from the rat brain. Yang 2014

 

20(R)-25-OCH3-PPD, a saponin from Panax notoginseng, was found to be extensively metabolized in mammalian species. CYP3A4-catalyzed oxygenation metabolism played an important role in the disposition of 25(R)-OCH3-PPD, especially at the C-20 hydroxyl group. Zhang 2014

 

Borneol was found to enhance intestinal absorption, increase distribution, and inhibit metabolism of notoginsenoside R1 and ginsenosides Rg1 and Re in rabbit plasma. The underlying mechanism may be attributed to loosening of the intercellular tight junction. Wang 2013

 

Panax notoginseng saponins was found to upregulate the protein expression of CYP1A2 in rats; however, no significant changes in CYP2C9, 2D6, or 3A4 activities were observed. Liu 2012

 

A dynamic microdialysis sampling method using liquid chromatography-quadrupole time-of-flight mass spectrometry was developed for rapid and sensitive analysis of the metabolite profile of Panax notoginseng extract in rat bile. Wen 2012

 

In an investigation of pharmacokinetics of marker compounds after oral administration ofPanax notoginseng extract and combinations of herbs in Fufang Danshen showed herb-herb interactions may account for different pharmacokinetics of active constituents administered in compounds vs single-herbs. Yang 2012

 

The distribution and pharmacokinetics of ginsenoside Rb1, ginsenoside Rg1, and sanchinoside R1 after intratympanic administration or intravenous administration of Panax notoginseng saponins in guinea pigs was evaluated, with significant differences found. [Article in Chinese] Chen 2011

 

High performance liquid chromatography-electrospray mass spectrometry (HPLC-ESI-MS) was used to evaluate the metabolism of notoginsenoside R1, ginsenoside Rg1 and ginsenoside Rb1, saponins isolated from Panax notoginseng in a zebrafish model. Wei 2011

 

LC-MS/MS method was used to determine the pharmacokinetics of ginsenosides Rg1, an active saponin from Panax notoginseng, and its metabolites in rat plasma after oral and intravenous administration. [Article in Chinese] Feng 2010

 

Metabolism of notoginsenoside R1 (NGR1), an active saponin from Panax notoginseng, was evaluated using human intestinal bacteria and liver subcellular fractions with results showing a determinant role of intestinal bacteria in overall disposition and potential bioactivity of NGR1. Ruan 2010

 

LC-MS/MS was used to simultaneously determine pharmacokinetics of 3 bioactive Panax notoginseng saponins (notoginsenoside R1, ginsenoside Rg1, and Rb1) in dog plasma after a single oral administration of Danshen formula tablets. Song 2010

 

In a study of panaxatrol disodium citrate from Panax notoginseng administered to healthy subjects, effect of dose level on single-dose pharmacokinetics was not significant. No accumulation was observed with exposure to 100 mg·m⁻² in a 30-day continuous intravenous injection. Yan 2010

 

Plasma concentration-time profiles of danshensu, tanshinone II(A), cryptotanshinone, notoginsenoside R1, ginsenoside Rg1, and Rb1 were analyzed by LC-MS/MS after administration of Panax notoginseng in combination with Salvia miltiorrhiza to dogs. [Article in Chinese] Zhang 2010

 

A systematic investigation of the absorption and deposition of Ra, Rb, Rd, Re, Rg, and notoginsenoside R after oral administration of Panax notoginseng in rats identified plasma ginsenosides Ra, Rb, and Rd as pharmacokinetic markers for indicating systemic exposure to Sanqi extract. Liu 2009

 

The effect of oral co-administration of Shuxiong and Panax notogiseng on pharmacokinetics was evaluated in rat plasma concluding some parameters of active ingredients are significantly changed but bioavailability is improved only when Chuanxiong volatile oil is co-administered. [Article in Chinese] Qi 2009

 

The relative oral bioavailability of ginsenoside Rg1 and Rb1 from Panax notoginseng in rats was shown to be enhanced by mixing with medium chain fatty glycerides to create a lipid-based formulation. Xiong 2008

 

The bioavaliabliltiy and pharmacokinetics of ginsenosides Rg1 and Rb1 from Panax notoginseng, including intestinal absorption, bile excretion, plasma protein binding, and elimination, were evaluated after iv and ig administration. [Article in Chinese] Han 2007

 

The pharmacokinetics and absolute bioavailability of total saponins from Panax notoginseng after oral or intravenous administration in rats was evaluated with absolute bioavailability of R1, Rg1, Rd, Re, and Rb1 shown to be 9.29%, 6.06%, 2.36%, 7.06%, and 1.18%, respectively. Li 2007

 

Elimination in the stomach, large intestine, and liver was shown to contribute to the low oral bioavailability of ginsenoside Rg1, but low membrane permeability might be a more important factor in determining the extent of absorption. Han 2006

 

Results of CaCo-2 in vitro and oral administration studies in rats show that elimination in the stomach, large intestine, and liver contribute to low bioavailability of Panax notoginseng saponins; however, low membrane permeability may be a more important factor in absorption. [Article in Chinese] Han 2006

 

A high-performance liquid chromatography method was developed for the determination of ginsenoside Rg1, Rb1, Rd, and notoginsenoside R1 from Panax notoginseng in rat feces following oral and intravenous administration of the total saponins. Li 2005

 

The optimal absorption site for sanchinoside R1 and ginsenoside Rg1 from orally administered Panax notoginseng was was found to be the duodenum in rats, indicating relatively low bioavaliability; carbomer and borneol enhanced the permeability of R1 and Rg1 on the intestinal wall. Liang 2005

 

Four major active ginsenosides (i.e. Rg1, Rb1, Rd, and notoginsenoside R1) were identified in rat urine after oral and intravenous administration of total Panax notoginseng saponins. Li 2004

 

Using a simple and sensitive high-performance chromatographic method, ginsenosides Rg1, Rb1, Rd, and notoginsenoside R1 from Panax notoginseng were identified in rat serum after oral and intravenous administration. Li 2004

 

The pharmacokinetics and bioavailability of ginsenoside Rb1 and Rg1 from Panax notoginseng in rats was evaluated with low oral bioavailability of Rb1 and rapid reduction of Rg1 in blood found. Xu 2003

 

Panax notoginseng saponins were better absorbed when administered intranasally in rabbits than through other routes; formulations including microcrystalline cellulose gave high bioavailability and low irritation. [Article in Chinese] Xu 2003