With the increase of the administered dose, the elimination half-life (Ti/2ß) of the drug decreases sequentially to (11.80,10.37,4.6hr), the distribution half-life increases sequentially to (0.53,0.64,0.67hr), and it passes the blood-brain barrier with a plasma protein-binding rate of 24.60%. From urine respectively. Excretion in stool and bile. Widely distributed in the body, fast elimination, not easy to accumulate. Low toxicity, no obvious side effects. In mice, the LD of Puerarin was 634.3mg/kg when injected intravenously and 1412.2mg/kg when injected intraperitoneally. In rats, Puerarin was injected intraperitoneally at 150,100,50mg/kg for 5 consecutive weeks, with no accumulation toxicity, and no obvious toxicity to organs such as the heart, liver, lungs, spleen, kidneys, adrenal glands, and intestines. Dogs were injected intravenously with Puerarin 50,30,15mg/kg daily for 5 weeks and then observed for 70 days, with no significant effect on urinary and fecal routines, blood counts, SGPT,BUN and blood glucose. . In healthy adult SD rats, the dose of 50,150mg/kg had no teratogenic effect on female rat embryos and male rat germ cells. . Mutagenicity test showed that Pueraria Mirifica has no potential carcinogenic and mutagenic risk.
Effects of Puerarin on the liver system: Puerarin contains saponin compounds, which are protective against immune damage to liver tissue, and the C-29 hydroxyl group and C-5" oxygen-containing group can enhance the hepatoprotective activity. Puerarin can protect liver injury through gastric absorption, induce apoptosis of activated hepatic stellate cells, effectively reverse chemically induced hepatic fibrosis, and also protect against carbon tetrachloride-induced acute liver injury, as well as possessing multifaceted physiological activities.
Effects of Puerarin on cardiovascular system: The total flavonoids in Pueraria Mirifica can increase the blood flow of brain and coronary arteries. Puerarin has a significant promotion effect on cerebral circulation as well as peripheral circulation in animals and humans. The total flavonoids in Pueraria Mirifica have a mild promoting effect in improving cerebral vascular tone, elasticity, and the supply of mobility in patients with hypertension and coronary artery disease. Pueraria Mirifica not only improves normal cerebral microcirculation in human body, but also has obvious improvement effect on microcirculation disorders, which is mainly manifested in the increase of local microvascular blood flow and amplitude of movement. Puerarin also has an improvement effect on the microcirculation of the nail folds in patients with sudden deafness, which can accelerate the microvascular blood flow rate, clear the vascular collaterals of stagnant blood, and improve the patient's hearing. Puerarin has a protective effect on hypoxic myocardium, Puerarin can significantly reduce the oxygen consumption of ischemic myocardium and protect the heart from ultrastructural damage caused by ischemia and re-port perfusion.
Gergenin is a single component flavonoid glycoside extracted from the legume Pueraria lobata root, which has the effects of activating blood circulation, improving microcirculation, expanding coronary arteries and cerebral blood vessels, and lowering myocardial oxygen consumption, etc. Its preparation, gergenin injection, is used in clinical practice for the treatment of cardio-cerebral vascular diseases and retinal vascular diseases, fundopathy, and sudden deafness. With the widespread use of Puerarin in the clinic, reports of adverse reactions have been increasing. Monitoring found that Puerarin injection can cause the occurrence of acute intravascular hemolysis, prone to drug accumulation, toxicity, damage to the liver and kidney. The hemolytic reaction caused by Puerarin injection mostly occurs when the drug is used again, and the drug is used continuously for more than 7 days, especially for those who have had allergic phenomena such as skin rashes in the past, and the drug is used again, and the extremely serious adverse reactions often occur within a very short period of time or even within 10 minutes. Therefore, the use of Puerarin injection should be asked in detail about the patient's history of use of the drug, patients allergic to the drug should be avoided re-use.
In order to ensure the clinical safety of Puerarin injection, the State Food and Drug Administration requires manufacturers to revise and replace the instructions to increase the contraindications and other instructions; strengthen the management of Puerarin injection, take the initiative to follow up on the safety of clinical use of the product, according to the provisions of the collection of adverse reactions and timely reporting.