| Safflower injection is made from the composite safflower by water extraction and alcohol precipitation.It has the pharmacological effects of activating blood circulation and removing blood stasis,anti-oxidation,anti-inflammation,lowering blood pressure and blood lipid and so on.Clinically,it is mostly used to prevent and treat coronary heart disease,occlusive cardiovascular and cerebrovascular diseases,and the effect is significant.At present,there are many pharmacological and clinical studies on Safflower injection.However,there are few reports on the active ingredients of safflower injection,especially on the traceability.Basic the requirement for Quality Markers,the migration and transformation of the HSYA in the production of safflower injection was studied in this paper.Taking the inhibition of platelet aggregation and anticoagulation in vitro as index,the biological activity of safflower injection was investigated with the migration and transformation of active ingredient HSYA.The research contents of this paper are as follows:1.In order to investigate the effect of the key steps of the production process of safflower injection on the quality of safflower injection,the activity of key links intermediates which include extraction,concentration,twice alcohol precipitation,water sedimentation,and two sterilizations was determined by prolonging activated partial thromboplastin time(APTT)and ADP-induced platelet aggregation in vitro.And the content of main chemical components in intermediates was determined by HPLC.The results showed that the inhibition of ADP-induced platelet aggregation rate in vitro of intermediates decreased gradually,and the trend of prolonging APTT activity decreased first and then increased with the preparation process of safflower injection.Meanwhile,the content of HSYA was gradually lowered,the content of p-Hydroxy-cinnamic acid was increased,and a new chemical component,p-Hydroxybenzaldehyde,was produced.In addition,the researchresults also showed that,sterilization plays a key role in the HSYA content and biological activity of safflower injection in the key steps of production process of safflower injection,which should be more valued and controlled.2.According to important factors in the key process of safflower injection production,such as temperature,time and p H,HSYA was heated at a high temperature,the p H of HSYA was adjusted and then was treated by moist heat sterilization.The stability and content of HSYA were measured during this process,and the degradation products were analyzed.The results showed that the content of HSYA was reduced by 18% after heating at 100?for 1 h.Then after adjusting the p H to 8.0 and wet heat sterilization at 115?for 40 min twice,the content was reduced to 23%.Chromatographic analysis of HSYA degradation produced a new chemical composition;compared with the standard product,the degradation products were p-hydroxybenzaldehyde and p-hydroxycinnamic acid.The above results indicated that HSYA was unstable to heat and alkali,and a part of p-hydroxybenzaldehyde and p-hydroxycinnamic acid in safflower injection was degraded and converted by HSYA.3.APTT,PT,TT and platelet aggregation induced by ADP were used as four indicators of biological activities.The changes of biological activity of HSYA before and after high temperature,alkali adjustment and sterilization treatment were compared and analyzed.The result showed that HSYA did not prolong the activity of APTT.The samples with degraded HSYA showed a significant prolongation of APTT activity with the increase of system concentration,and showed a dose-effect positive correlation.HSYA and samples with degraded HSYA prolonged PT and TT with the increase of system concentration;HSYA and samples with degraded HSYA had a strong inhibitory effect on platelet aggregation,and both showed a dose-effect positive correlation.The results also showed that HSYA degraded samples enhanced the activity of APTT,PT and TT,but reduced the inhibition of platelet aggregation. |
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