Study On The Pharmacokinetics And Fingerprint Of Breviscapine

Breviscapine, the flavonoid constituents isolated from Erigerin breviscapus (Vant.)Hand-Mazz, have clear pharmacological effects and have been widely used in thetreatment of cerebral infarction and its sequela. But there is little research on thepharmacokinetics of the breviscapine. In this paper, a method is thus developed todetect its plasma drug concentration, and its pharmacokinetics of ig breviscapine inanimals is investigated and the bioavailability of its phytosomes is determined.Moreover, a HPLC method is exploited to determine the fingerprint of Erigerin bre-viscapus and breviscapine injection. The factors influencing the fingerprint are stud-ied. The results are as follows: 1. The pharmacokinetics of scutellarin in mice. After ig administration of brevis-capine and its phytosomes (100 mg · kg-1), the drug absorbed rapidly and the time cureof plasma concentration of two drugs are both fitted with one-compartment model.The relative bioavailability of breviscapine phytosomes to the breviscapine powder is345% and it indicates that the phytosoems greatly enhance the oral absorption of bre-viscapine in mice. 2. The pharmacokinetics of scutellarin in rats. At high dose (400 mg · kg-1), thepharmacokinetic parameters are different from that of the medium and low dose(100and 50 mg · kg-1). The difference shows that the pharmacokinetics of breviscapine isnonlinear at the high dose. The relative bioavailability of breviscapine phytosomes tothe powder is 274%, while that to the philipid mixtures is 150%. The increase in rela-tive bioavailability shows that the chemical/physical properties of phytosoems may IIIhave been greatly changed. The combination ratio of breviscaipine to the plasma pro-tein is about 24% ~ 26% and it is quite low. About 41.2% of the drug is excreted fromthe dejecta after the rats are ig administration of the breviscapine powder. 3. The fingerprints of Erigerin breviscapus and breviscapine injection. Themethod to determine the fingerprint of Erigerin breviscapus and breviscapine injec-tion is developed. Although the major composition in the fingerprints of breviscapineinjections from different production batch and manufactures is similar, the content ofthe minor compositions are quite different. The growth place influences the finger-print of Erigerin breviscapus, while the extraction technology has more effect on itsfingerprint of Erigerin breviscapus.