Application of salviae miltiorrhizae and flos carthami composition to enhancement of antithrombotic function of aspirin

Abstract

The invention discloses application of a salviae miltiorrhizae and flos carthami composition to enhancement of the antithrombotic function of aspirin. On the basis of the traditional Chinese medicine prescription compatibility theory and a large number of experiments and researches, the salviae miltiorrhizae and flos carthami composition is screened out and can remarkably inhibit the esterase activity of aspirin, the hydrolysis speed of aspirin is reduced, the acting time of aspirin is prolonged, aspirin resistance is inhibited, the antiplatelet function of aspirin is enhanced, the antithrombotic treatment effect can be enhanced by clinically using the salviae miltiorrhizae and flos carthami composition and aspirin, adverse effects are reduced, and application prospects are important.

Description

technical field

[0001] The invention relates to a new application of a traditional Chinese medicine composition, in particular to the application of the Danshen safflower composition in enhancing the antithrombotic effect of aspirin, inhibiting the activity of aspirin esterase and promoting the antiplatelet effect of aspirin. Background technique

[0002] Aspirin is a classic antipyretic, analgesic and anti-inflammatory drug, and is one of the most widely used drugs in the world. The current main use of aspirin is to prevent and treat cardiovascular diseases in small doses.

[0003] During the absorption process, aspirin is partially hydrolyzed into salicylic acid through the first-pass effect of the gastrointestinal tract and the first-pass effect of the liver, and aspirin (50-70%) entering the blood circulation as a prototype is rapidly hydrolyzed into water by aspirin esterase in the liver and blood Salicylic acid. Aspirin can acetylate the COX-1 enzyme active center of ...

Examples

Embodiment 1

[0023] Example 1 Effects of Danshen Safflower Compositions of Different Proportions and Formulations on the Antiplatelet Effect of Low-Dose Aspirin

[0024] 1. Experimental method

[0025] 1.1 Experimental materials

[0026] Salvia safflower composition injection: take different weight ratios of salvia miltiorrhiza and safflower (C1, 3 parts of salvia miltiorrhiza-1 part of safflower; C2, 1 part of salvia miltiorrhiza-1 part of safflower; C3, 1 part of salvia miltiorrhiza-3 parts of safflower ), add water to decoct twice, each time for 60 minutes, filter, combine and concentrate the filtrate to a clear paste with a relative density of 1.20-1.30 (65°C), add ethanol until the alcohol content is 75-80%, refrigerate, and take the supernatant, Recover ethanol and concentrate it into a clear paste with a relative density of 1.20-1.30, add ethanol until the alcohol content is 80-85%, refrigerate, take the supernatant, add about 1% of the input amount of activated carbon, stir for 30...

Embodiment 2

[0034] Example 2 Effect of Danshen Safflower Composition Injection on Aspirin Esterase Activity

[0035] 1. Experimental method

[0036] 1.1 Determination of plasma aspirin esterase activity

[0037]Add 100 μL blank plasma and 10 μL aspirin hydrochloride solution to 890 μL Tris buffer, vortex for 30 s, and incubate in a 37° C. water bath for 20 min. Take 100 μL of reaction solution and add 100 μL of internal standard solution to stop the reaction and precipitate a small amount of protein, centrifuge at 13000×g for 10 min, draw 150 μL of supernatant and inject. The concentration of salicylic acid was determined by UPLC-TQ-MS. The preparation method of the aspirin hydrochloric acid solution is as follows: 1.08 mg of aspirin is dissolved in 6 mL of 0.1 M hydrochloric acid (aspirin concentration is 1 mM). The preparation method of Tris buffer is: mix 0.2423g Tris (Tris) and 2.22g Calcium Chloride (CaCl 2 ) was dissolved in 100mL ultrapure water, and the pH was adjusted to 7.4 ...

technical field

[0001] The invention relates to a new application of a traditional Chinese medicine composition, in particular to the application of the Danshen safflower composition in enhancing the antithrombotic effect of aspirin, inhibiting the activity of aspirin esterase and promoting the antiplatelet effect of aspirin. Background technique

[0002] Aspirin is a classic antipyretic, analgesic and anti-inflammatory drug, and is one of the most widely used drugs in the world. The current main use of aspirin is to prevent and treat cardiovascular diseases in small doses.

[0003] During the absorption process, aspirin is partially hydrolyzed into salicylic acid through the first-pass effect of the gastrointestinal tract and the first-pass effect of the liver, and aspirin (50-70%) entering the blood circulation as a prototype is rapidly hydrolyzed into water by aspirin esterase in the liver and blood Salicylic acid. Aspirin can acetylate the COX-1 enzyme active center of ...

Examples

Embodiment 1

[0023] Example 1 Effects of Danshen Safflower Compositions of Different Proportions and Formulations on the Antiplatelet Effect of Low-Dose Aspirin

[0024] 1. Experimental method

[0025] 1.1 Experimental materials

[0026] Salvia safflower composition injection: take different weight ratios of salvia miltiorrhiza and safflower (C1, 3 parts of salvia miltiorrhiza-1 part of safflower; C2, 1 part of salvia miltiorrhiza-1 part of safflower; C3, 1 part of salvia miltiorrhiza-3 parts of safflower ), add water to decoct twice, each time for 60 minutes, filter, combine and concentrate the filtrate to a clear paste with a relative density of 1.20-1.30 (65°C), add ethanol until the alcohol content is 75-80%, refrigerate, and take the supernatant, Recover ethanol and concentrate it into a clear paste with a relative density of 1.20-1.30, add ethanol until the alcohol content is 80-85%, refrigerate, take the supernatant, add about 1% of the input amount of activated carbon, stir for 30...

Embodiment 2

[0034] Example 2 Effect of Danshen Safflower Composition Injection on Aspirin Esterase Activity

[0035] 1. Experimental method

[0036] 1.1 Determination of plasma aspirin esterase activity

[0037]Add 100 μL blank plasma and 10 μL aspirin hydrochloride solution to 890 μL Tris buffer, vortex for 30 s, and incubate in a 37° C. water bath for 20 min. Take 100 μL of reaction solution and add 100 μL of internal standard solution to stop the reaction and precipitate a small amount of protein, centrifuge at 13000×g for 10 min, draw 150 μL of supernatant and inject. The concentration of salicylic acid was determined by UPLC-TQ-MS. The preparation method of the aspirin hydrochloric acid solution is as follows: 1.08 mg of aspirin is dissolved in 6 mL of 0.1 M hydrochloric acid (aspirin concentration is 1 mM). The preparation method of Tris buffer is: mix 0.2423g Tris (Tris) and 2.22g Calcium Chloride (CaCl 2 ) was dissolved in 100mL ultrapure water, and the pH was adjusted to 7.4 ...

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