Coumarins

widely existed in Chinese herbal medicine

are important components in the natural medicine. They had shown various pharmacological effects

such as analgesic

anti-inflammatory

anti-tumor

anti-arrhythmic

etc. Coumarins can be quickly absorbed and distributed in human body

and concentrated mostly in the organs with rich blood such as heart

liver

lung

spleen and so on. The pharmacokinetic behavior of coumarins is firstly affected by delivery way in vivo. It is prior to one-compartment model when delivery way is extravascular administration such as oral

intraperitoneal injection and muscle injection and so on. When intravascular administration

such as intravenous injection and intravenous drip

the two-compartment model is primary. Second

it is affected by the distribution rate of coumarins as slow distribution phase are covered by absorption phase. So some drugs performance one-compartment model when oral administration

but it performances two rooms model when intravenous. In addition

the pharmacokinetic behavior of coumarins is also affected by animal species and individual differences in vivo

because of the CYP isoenzymes. The metabolic process of coumarins is complex

but the metabolic processes are similar because they have the same parent nuclear. A large numbers of enzymes are involved the metabolism of coumarins. When coumarins entered the body

phase Ⅰ metabolism occured firstly

such as hydroxylation

dehydrogenation

demethylation

lactone ring open-loop and so on

then phase Ⅱ metabolism reacted with glucuronic acid

sulfuric acid and glutathione etc. generated larger water-soluble compounds

and excreted finally. The author arranged documents on coumarins from recent years

reviewed the documents on biodistribution and metabolic mechanism of coumarins

which would lay the foundation for their development and clinical rational application.