动物造模 z-bio 2022-09-24 385

　　Objective To study the effect of 7 active components of pinoresinol diglucoside, geniposide chlorogenic acid, protocatechuic acid, neochlorogenic acid, cryptochlorogenic acid and pinoresinol monoglucoside after repeated administration of Eucommia ulmoides extract in normal conditions. Pharmacokinetic differences between rats and spontaneously hypertensive rats.

　　Methods Normal rats and spontaneously hypertensive rats were used as experimental subjects, and the Eucommia ulmoides extract was administered by gavage at a dose of 5.4 g/kg, once a day for 7 days. Differences in pharmacokinetics and tissue accumulation between rats and SHR models.

　　Results The results of pharmacokinetic study showed that the pharmacokinetic parameters of CCA and NCA in the SHR model were not significantly different from those in the normal group. In the SHR model group, the T1/2 of PDG was 0.26 times that of the normal group; the T1/2, Tmax, and AUC0-t of GA in the SHR model group were 2.20, 0.04, and 0.50 times that of the normal group, respectively; PCG was in the SHR model group. The T1/2 in vivo was 0.55 times that of the normal group; the T1/2 of PCA in the SHR model group was 2.04 times that of the normal group; the T1/2 and AUC0-t of CA were 1.93 and 0.64 times that of the normal group, respectively. The accumulation experiment found that 7 active ingredients including GA were mainly distributed in the stomach, small intestine, heart, liver and lung. Except for CCA, CA, NCA, PCA, GA, PDG and PG in the SHR model compared with the normal group, the number of tissues and organs with significant differences ranged from 2 to 7, respectively.

　　Conclusion The body in the pathological state of spontaneous hypertension can significantly change the pharmacokinetic behavior of the antihypertensive active components of Eucommia ulmoides in plasma and the accumulation in tissues. For hypertensive patients who need long-term medication, the pharmacokinetics of the drug in vivo Behavior is particularly important, and this study can provide some reference for the long-term clinical dose adjustment of Eucommia ulmoides.