Study On Pharmacokinetics Of Safflor Yellow Powder Injection

The dried flower of the Safflower plant, Carthamus tinctorius L has been used extensively in traditional Chinese medieine (TCM) to treat coronary heart disease, hypertention and cerebrovascular disease.In traditional Chinese medicinal prescription safflower is mainly taken as decoction.Safflor yellow (SY) is the main constituents in water-soluble extract of safflower, and hydroxysafflor yellow A (HSYA) is the main active component of SY. In recent years, some pharmacokinetic studies on HSYA have been performed after intravenous administration of SY or pure HSYA on animals. The purposes of the experiment are to study the pharmacokinetics (PK) of hydroxysafflor yellow A (HSY A) after intravenous injection the powder injection of Honghua yellow pigment in rabbits.To study the plasma protein binding rate of HSY A in rabbits.To study the distribution of HSY A after intravenous injection the powder injection of Honghua yellow pigment in mice.All of the researches will provide data for clinic prescription.In the present work a HPLC method for quantification of HSYA in rabbit's plasma after intravenous injection the powder injection of Honghua yellow pigment. Sample preparation was achieved by protein precipitation of plasma with four volumes of methanol. HSYA were separated on a DiamonsilTMP C18 column with a elution system which composed of methanol, acetonitrile and phosphoric acid (the concentration is 0.2%).The proportion is 35:2:63.UV detection was used at 403 nm. The flow rate is lml/min and the temperature of the column is 40℃.In the study on pharmacokinetics, the concentration of the drug in blood for different time was determined after administering to ear side vein of rabbits. The all pharmacokinetics parameters were taken with calculating the data by DAS2.1.1 pharmacokinetical software. To get rid of the plasma protein with ultra-filtration and to determine the plasma concentration of HSY A by HPLC after injecting through intravenous for low, medium and high-dose.30 mice were divided into 5 groups and 6 per one. Their blood, hearts, livers, spleens, lungs, kidneys and brains were taken in different times after tail intravenous injection the powder injection of Honghua yellow pigment. The content was determined by HPLC. The pharmacokinetics parameters were calculated by DAS2.1.1.The method was successfully used to quantify the contents of HSYA in plasma and tissues, there sults were as follows:(1)The HSY A in the powder injection of Honghua yellow pigment displayed for 3 compartment model in rabbit body, and the main parameters were t1/2αas18.396min, t1/2βas 49.532min, t1/2γas 107.211min, AUC (0-∞) as 8388.797 mg/L·min.The results show that HSYA has a faster absorption and a higher concentration in blood of rabbits after intravenous injection the powder injection of Honghua yellow pigment.The half time is longer.(2)The plasma protein binding rate of HSYA at different doses were 77.22%,78.31%,78.10% respectively. The average of the plasma protein binding rate is 77.88%.The results show that the plasma protein binding rate of HSY A is higher(3)The distribution of HSY A in the powder injection of Honghua yellow pigment was extensive in body of the mouse. The AUC from large to small is blood, kidney, liver, lung, heart, spleen, and the HSY A in brain was not determined under the examination limits.