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A method of stabilizing carbidopa/levodopa in a biological matrix

A biological matrix and levodopa technology, applied in the biological field, can solve the problems of not being able to truly reflect the drug situation, and achieve the effect of reducing enzymatic reactions, reducing enzymatic reactions, and inhibiting oxidation reactions

Active Publication Date: 2022-06-07
苏州华测生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Previous data reflect that CD / LD has stability problems in biological matrices such as whole blood and plasma. If it cannot be resolved, the test data in the experiment cannot truly reflect the situation of the drug in the body.

Method used

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  • A method of stabilizing carbidopa/levodopa in a biological matrix
  • A method of stabilizing carbidopa/levodopa in a biological matrix
  • A method of stabilizing carbidopa/levodopa in a biological matrix

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Measure 9 mL of sterile water for injection to dissolve completely, and then add 1000 μL of formic acid to obtain stabilizer 10% FA;

[0025] Add 25 μL of stabilizer 10% FA to the pre-cooled EP tube, then add 0.975 mL of plasma, and add 100 μL of 0.03 mg / mL CD / LD after mixing. Take an appropriate amount of the first sample immediately for quantitative detection, the second sample is placed in a wet ice environment for 3 hours for quantitative detection, and the third sample is placed in a wet ice environment for 20 hours for quantitative detection. The results are shown in Table 1 and Table 2.

Embodiment 2

[0027] Take 8 mL of sterile water for injection to dissolve completely, and then add 2000 μL of formic acid to obtain stabilizer 20% FA;

[0028] Add 25 μL of stabilizer 20% FA to the pre-cooled EP tube, then add 0.975 mL of plasma, and add 100 μL of 0.03 mg / mL CD / LD after mixing. Take an appropriate amount of the first sample immediately for quantitative detection, the second sample is placed in a wet ice environment for 3 hours for quantitative detection, and the third sample is placed in a wet ice environment for 20 hours for quantitative detection. The results are shown in Table 1 and Table 2.

Embodiment 3

[0030] Measure 9.5 mL of sterile water for injection, and then add 500 μL of trifluoroacetic acid to obtain stabilizer 5% TFA;

[0031] Add 25 μL of stabilizer 5% TFA to the pre-cooled EP tube, then add 0.975 mL of plasma, and add 100 μL of 0.03 mg / mL CD / LD after mixing. Take an appropriate amount of the first sample immediately for quantitative detection, the second sample is placed in a wet ice environment for 3 hours for quantitative detection, and the third sample is placed in a wet ice environment for 20 hours for quantitative detection. The results are shown in Table 1 and Table 2.

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Abstract

The invention discloses a method for stabilizing carbidopa / levodopa in a biological matrix. A stabilizer is added to the biological matrix, and the stabilizer includes an acidifying agent with a volume fraction of 5% and an antioxidant with a mass fraction of 10%. . The invention is based on adjusting the pH value and adding antioxidants to achieve the purpose of protecting the CD / LD in the biological matrix, and finally enables the biological matrix samples containing the CD / LD to be stored in various environments. Using the present invention, the whole blood sample containing CD / LD can be stored at 2-8°C for 2 hours, the plasma sample at 2-8°C for 20 hours, and the temperature below -60°C for 30 days, Capable of 4 freeze-thaw cycles. It meets the collection, transportation, storage and testing requirements of samples in preclinical / clinical trials of CD / LD, and provides a basis for pharmacokinetic research of CD / LD.

Description

technical field [0001] The present invention relates to a method for stabilizing carbidopa / levodopa in a biological matrix, in particular to a method for meeting the collection, transportation, storage and detection requirements of samples in preclinical / clinical trials of carbidopa / levodopa The method belongs to the field of biotechnology. Background technique [0002] Levodopa (LD) is the most effective drug for the treatment of Parkinson's disease (PD), and it is a prodrug of dopamine (DA). It can pass through the blood-brain barrier and be decarboxylated into DA by Dopa decarboxylase (DDC) in the brain. Because DDC not only exists in the brain, but also widely exists in other organs and vascular wall cells. For example, if LD is used alone, only about 1% of the drugs can enter the center. Therefore, LD combined with peripheral dopa decarboxylase inhibitors is often used clinically ( Dopadecarboxylase inhibitor, DDCI) such as carbidopa (Carbidopa, CD) or benserazide (Be...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A01N1/02
CPCA01N1/0231A01N1/0226
Inventor 冷明红叶双双陆国才夏玉叶宗英胡明文叶爱华刘大伟
Owner 苏州华测生物技术有限公司