The pharmacokinetic study of butylphthalide by intravenous injection in rats showed that butylphthalide was rapidly eliminated in rats, and the elimination process showed first-order kinetic characteristics. The excretion of the prototype drug through urine and feces within 48 hours after administration only accounts for 3. 16% of the total amount of administration.
The experimental results of oral administration and intravenous injection of racemic butylphthalide in beagle dogs show that there are differences in the absorption of levobutylphthalide and dextrobutylphthalide in beagle dogs, and dextrobutylphthalide may be absorbed faster, but there is no obvious difference in elimination in beagle dogs, and no obvious mutual transformation of butylphthalide optical isomers is found in beagle dogs.
2. Pharmacokinetics of butylphthalide in human body.
Taking healthy adult males in China as the research object, the peak time of plasma NBP in the oral butyl 100mg phthalein Ding An soft capsule group was tmax = 0.82 0.37 h; Cmax = 7 1.52 37. 12, AUC0-t is 70.7129.9726 (ng/m1min); Under the condition of continuous intravenous infusion of 50 mg butylphthalide, the peak concentration of plasma NBP was Cmax = 326.49130.03 and AUC0-t was 522.81.145.26 (ng/m1.min). T 1/2 is 6.39 2. 1lh.
Third, the transformation products of butylphthalide in animals
Butylphthalide is completely absorbed by gastrointestinal tract in animal experiments, and its elimination process is rapid in vivo. About 70% of butylphthalide is excreted through the kidney or intestine as a metabolite. The reason for the rapid elimination process may be that the polarity of most butylphthalide products is enhanced after biotransformation in vivo, and the solubility in water phase is increased, which is excreted with urine. Studies have also shown that the main metabolic pathway of butylphthalide in animals is hydroxylation of fat side chains.