Abstract
In this study, the absorption, distribution, metabolism and excretion (ADME) of sodium danshensu (Sodium DL-β-(3, 4-dihydroxyphenyl)lactate), one of the main water-soluble active constituents in Salvia miltiorrhiza, were evaluated in rats. Pharmacokinetic study was evaluated in doses of 15, 30, and 60 mg/kg after intravenous administration of sodium danshensu. Bioavailability study was evaluated by comparing between 30 mg/kg (I.V.) and 180 mg/kg (P.O.) of sodium danshensu. Tissue distribution, metabolism, and excretion were evaluated at 30 mg/kg (I.V.) of sodium danshensu. Following intravenous administration, sodium danshensu exhibited linear pharmacokinetics in the dose range of 15–60 mg/kg. Sodium danshensu appeared to be poorly absorbed after oral administration, with an absolute bioavailability of 13.72%. The primary distribution tissue was kidney, but it was also distributed to lung, stomach, muscle, uterus, heart, etc. Within 96 h after intravenous administration, 46.99% was excreted via urine and 1.16% was excreted via feces as the parent drug. Biliary excretion of sodium danshensu was about 0.83% for 24 h. Metabolites in urine were identified as methylation, sulfation, both methylation and sulfation, and acetylation of danshensu. Sodium danshensu can be developed as an injection because of its poor oral bioavailability. In conclusion, sodium danshensu is widely distributed, mainly phase II metabolized and excreted primarily in urine as an unchanged drug in rats.
Highlights
Salvia miltiorrhiza, named Danshen in Chinese, is one of the most versatile traditional Chinese medicinal herbs
Preclinical ADME of Sodium Danshensu in Rats has been identified from Salvia miltiorrhiza, including diterpenoid quinines, hydrophilic phenolic acids and essential oil constituents (Li et al, 2009)
It is generally known that lipophilic diterpenoid quinines and hydrophilic phenolic acids are the main bioactive components in Salvia miltiorrhiza (Su et al, 2015)
Summary
Salvia miltiorrhiza, named Danshen in Chinese, is one of the most versatile traditional Chinese medicinal herbs. It has been widely used to treat and prevent cardio vascular disease, hyperlipidemia and cerebro vascular disease throughout the world (Cheng 2007; Wang et al, 2017). Preclinical ADME of Sodium Danshensu in Rats has been identified from Salvia miltiorrhiza, including diterpenoid quinines, hydrophilic phenolic acids and essential oil constituents (Li et al, 2009). It is generally known that lipophilic diterpenoid quinines and hydrophilic phenolic acids are the main bioactive components in Salvia miltiorrhiza (Su et al, 2015). Named as salvinanic acid, is the main water-soluble phenolic acids in Salvia miltiorrhiza. It has been reported that danshensu exhibited several pharmacological activities such as cardioprotective effect by inhibiting L-type calcium channels (Song et al, 2016), radioprotective effect by scavenging reactive oxygen species (Guo et al, 2013), protection of vascular endothelial cells by an antioxidative mechanism (Zhao et al, 2012), protection on liver injured by an antioxidative mechanism (Wang et al, 2007), etc
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