WHO monographs on selected medicinal plants - travolekar.ru

Cortex Berberidis
The pharmacokinetics of berberine were assessed by high-performance
liquid chromatography coupled to microdialysis to determine the concentration
of unbound berberine in rat blood, liver and bile (68). Microdialysis
probes were simultaneously inserted into the jugular vein towards
the right atrium, the median lobe of the liver and the bile duct of rats for
biological fluid sampling after administration of berberine, at a dose of
10 mg/kg bw, through the femoral vein. A linear concentration–response
relationship was observed over the concentration range 0.05–50.0 μg/ml.
The results demonstrated that the disposition of berberine occurred in the
blood, liver and bile fluid. These data indicate that berberine is metabolized
in the liver and undergoes hepatobiliary excretion (68).
The structures of the unknown metabolites of berberine were determined
after isolation of the compounds from the urine of five volunteers.
Each of the volunteers was given an oral dose of berberine chloride, 0.9 g
per day, for 3 days. Metabolites in urine samples were isolated and purified
by polyporous resin column chromatography and identified by electrospray
ionization mass spectroscopy and proton nuclear magnetic resonance
spectroscopy. The three major unknown metabolites (M1, M2 and
M3) were isolated and identified as jatrorrhizine-3-sulfate, demethyleneberberine-2-sulfate
and thalifendine-10-sulfate (50).
Toxicology and overdose
Following accidental ingestion by humans of more than 500 mg of berberine,
lethargy, nosebleeds, dyspnoea, and skin and eye irritation may
occur. In addition, kidney irritation, nephritis and lethal poisoning have
been reported. Disturbances of the gastrointestinal tract with nausea,
vomiting and diarrhoea have also been observed (69).
Adverse reactions
No information found.
Contraindications
Cortex Berberidis is contraindicated in patients with hypersensitivity or
allergy to the plant material.
Warnings
Exposure of patients to sunlight or artificial light sources emitting UVA
should be avoided when topical preparations derived from the crude drug
or berberine are applied (70).
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