Butylidenephthalide pharmacokinetic study
AbstractChuanxiong anticonvulsant principal component Butylidenephthalide, referred to as Bdph, the drug has been found against the role of angina pectoris. To further understand the situation of oral
absorption and drug pharmacodynamics and pharmacokinetics of the relationship, we conducted the following experiment. High performance liquid chromatography analysis technique of
intravenous and oral Bdph rabbit concentration. To being filled with the silica gel column (5 μ m, 4 × 250mm) and the hexane and
chloroform (1:1, v / v) mixture composed of, respectively, as
stationary phase and mobile phase. In addition, the UV wavelength of 254 nm and integrator, testing and recording Bdph of peak height.
95% n-hexane and ethanol (49:1, v / v) mixture, then as the extraction of plasma with internal standard dibutylphthalate Bdph of solution.
HPLC analysis of the above methods, measured the blood
concentration of Bdph of 0.01 μ g / ml. Experiments were conducted on rabbits as the target and were given intravenous injection of 10, 30 and 90 mg / kg and oral administration of 60 mg / kg of Bdph, to get Bdph in rabbits pharmacokinetic parameters, this parameter we can learn at home Rabbit for Bdph absorption, distribution and
exclusions. Assumed to be linear pharmacokinetic conditions, the experimental results, Bdph intravenous injection of 90 mg / kg, may have lent pharmacokinetic parameters clearance 780.8 ± 306.9 ml / min, V ss 118638 ± 104153 ml, T 1 / 2 172.4 ± 69.8 min, while the oral
administration of 60 mg / kg, the Bdph the bioavailability of about 17%, clearance 4465.9 ± 1548.3 ml / min, V ss 13.7 × 10 ± 9.5 × 10 ml, T 1 / 2 210.5 ± 145.7 min observed value of Cmax and Tmax was 0.169 ± 0.093 μ g / ml and 101.3 ± 27.5 min. The intravenous injection of 10 and 30 mg / kg dose, because time can not be clearly reflected in the concentration index map rule curve, it can not analyze its kinetic parameters, in order to improve this deficiency, however, await future analysis by gas chromatography to further to improve its sensitivity, to seek our more satisfactory results.