| The dried flower of the Safflower plant, Carthamus tinctorius L. hasbeen used extensively in traditional Chinese medicine (TCM) to treatcoronary heart disease, hypertention and cerebrovascular disease. Intraditional Chinese medicinal prescription safflower is mainly taken asdecoction. Saffior yellow (SY) is the main constituents in water-solubleextract of safflower, and hydroxysaffior yellow A (HSYA) is the main activecomponent of SY. In recent years, some pharmacokinetic studies on HSYAhave been performed only after intravenous administration of SY or pureHSYA on animals. The study is to investigate the difference of absorptionand distribution after oral administration of safflower extract and SY in rats.In the present work a simple and reproducible HPLC method forquantification of HSYA in rat plasma and tissues after oral administration ofsafflower extract or SY was developed. Sample preparation was achievedby protein precipitation of plasma and tissue homogenates with threevolumes of methanol, p-Hydroxybenzaldehyde was used as the internalstandard (IS). HSYA and IS were separated on a Hypersil BDS-C18 columnwith a gradient elution system which composed of acetonitrile and aqueousacetic acid. UV detection was used at 320 nm. The calibration curves werelinear in all tested matrices (r＞0.999) with the concentration range of0.51-101.36μg/mL for plasma, 12.27-2454.46μg/g for intestines and 0.96-192.20μg/g for lung, respectively. The intra-day and inter-dayprecision were all less than 12.5％, and the extract recovery was in the rangeof 64.1％to 103.7％with RSD less than 15.6％for HSYA in all testedmatrices.The method was successfully used to quantify the contents of HSYA inrat plasma, tissues and gastrointestine, the results were as follows:1. The mean plasma concentration-time profile of HSYA showed theabsorption of HSYA was rapid, with peak concentrations occurring at 10min for safflower extract and 20 min for SY after oral administration. Theprimary pharmacokinetic parameters were calculated by non-compartmentanalysis using WinNonlin 5.0.1 program, these parameters indicated thatHSYA was absorbed better from safflower extract than SY, the AUC wasgreater after oral administration of safflower extract than SY.2. It was shown that the distribution of HSYA in rats was abroad, butonly the HSYA in intestines after oral administration of safflower extractand SY, and in lung after oral administration of safflower extract were overthe limit of quantification. The concentration of HSYA in small intestineafter oral administration of safflower extract was almost close to that of SY,but in caecum and large intestine the concentration was higher after oraladministration of safflower extract. It could be included that HSYA wasabsorbed mostly by small intestine because the concentration of HSYA insmall intestine was much higher than that in caecum and large intestine. And the difference of absorption between safflower extract and SY wasprobably because of the difference of absorption in caecum and largeintestine.3. It was investigated that the concentration of HSYA in gastric contentsafter oral administration of safflower extract was higher than that of SY, butit was reversed in small intestinal contents, the possible reason was that instomach the SY was emptied more quickly and safflower extract wasabsorbed better in small intestine. Much HSYA was measured in smallintestinal contents, it could be inferred that HSYA was mainly excretedthrough feces.The results provide scientific data for the further study of safflower anduseful references for the modern pharmacokinetic study of traditionalChinese medicine. |
