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Carboxylesterase Inhibitor Preparations for Drug Metabolism Testing

A carboxylesterase and drug technology, applied in the field of carboxylesterase inhibitor preparations for drug metabolism detection, can solve the problems of drug test results distortion, reduction, large sample size, etc., to facilitate animal experiment process and clinical Simplify the experimental process, the blood collection process, and ensure the effect of the inhibitory effect

Active Publication Date: 2021-12-24
ZHEJIANG LONGCHUAN BIOMEDICAL TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] When the applicant was conducting drug metabolism research, he found that adding bis(p-nitrophenyl) phosphate (BNPP) to inhibit carboxylesterase to preserve blood samples when using commonly used heparin and EDTA anticoagulant blood collection tubes would greatly reduce the Reduce the inhibitory effect of carboxylesterase (the inhibitory effect is reduced by about 50%), resulting in serious distortion of the corresponding drug detection results in the sample
Instead of using anticoagulant blood collection tubes, you must complete the series of work of adding BNPP, mixing, centrifuging, and plasma collection for each sample within 10 minutes, which is no problem when processing a small amount of samples under laboratory conditions , but when the sample size is large, especially when a large number of samples need to be processed under poor conditions (such as experimental animal breeding places, hospitalized patients / patients with reduced mobility), it brings great difficulties to the experimental organization
However, other existing carboxylesterase inhibitors such as phenylmethylsulfonyl fluoride, sodium fluoride, prazosin, and thienoyltrifluoroacetone are not suitable for this type of detection due to their inhibition rate and interference with subsequent detection.

Method used

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  • Carboxylesterase Inhibitor Preparations for Drug Metabolism Testing
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  • Carboxylesterase Inhibitor Preparations for Drug Metabolism Testing

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1 anticoagulant is to the discovery of carboxylesterase inhibitor inhibitory effect interference

[0035] The applicant found a common phenomenon in the drug metabolism research of an existing camptothecin class (for reasons of confidentiality, its specific name and experimental protocol will not be disclosed). , using heparin blood collection tubes plus BNPP post-treatment to save the plasma concentration for 8-10 hours, compared with the blood concentration of blood collection directly after adding BNPP post-treatment (several minutes) to take plasma detection immediately (a few minutes) is only 50-70 %.

Embodiment 2

[0036] Embodiment 2 The interference of different anticoagulants to the inhibitory effect of carboxylesterase inhibitors

[0037] Get the fresh blood sample of SD rat, carry out different following processing (each processing is repeated three times):

[0038] Processing method 1

[0039]Use a blood collection tube without anticoagulant, add irinotecan standard acetonitrile solution to make about 245ng·mL -1 The blood samples were directly centrifuged to obtain plasma, stored at minus 70 degrees Celsius for 72 hours and then tested;

[0040] Processing method 2

[0041] Use a blood collection tube without anticoagulant, add irinotecan standard acetonitrile solution to make about 245ng·mL -1 For blood samples, add BNPP 5mg·mL -1 , directly centrifuge to take plasma, store it at minus 70 degrees Celsius for 72 hours, and then test it;

[0042] Processing method 3

[0043] Use anticoagulant blood collection tube 1, add irinotecan standard acetonitrile solution to make about...

Embodiment 3

[0070] Embodiment 3 The actual application effect of the carboxylesterase inhibitor preparation / blood preservation agent of the present application

[0071] The carboxylesterase inhibitor preparation / blood preservation agent of the present application was actually used in the blood drug concentration experiment of irinotecan and symnotecan in rats. Obtained the result that is basically similar to the plasma detection immediately after adding BNPP. Take a representative individual for each test and the results are as follows:

[0072] Table 3 Preservatives of this application are used for irinotecan and ximintecan rat blood drug concentration experiments

[0073]

[0074] The results in multiple individuals are similar to Table 3, and the results show that the blood preservation agent of the present application can effectively anticoagulate and inhibit carboxylesterase activity in the detection of multiple camptothecin drugs, after 8-12 hours (basically Satisfying the coll...

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Abstract

The application provides a carboxylesterase inhibitor preparation for drug metabolism detection, the carboxylesterase inhibitor preparation is composed of phenylmethylsulfonyl fluoride and calcium chloride, the carboxylesterase inhibitor preparation It has a high inhibition rate and is not affected by the anticoagulant heparin, and can be combined with heparin to make a blood preservation agent.

Description

technical field [0001] The application belongs to the field of drug metabolism and the field of biological blood sample detection. Specifically, the application provides a carboxylesterase inhibitor preparation for drug metabolism detection. The carboxylesterase inhibitor preparation is composed of phenylmethylsulfonate Composed of acid fluoride and calcium chloride, the carboxylesterase inhibitor preparation has a high inhibition rate and is not affected by the anticoagulant heparin, and can be combined with heparin to make a blood preservation agent. Background technique [0002] Carboxylesterase (CES) belongs to the B family of esterases and is widely distributed in various organisms. Carboxylesterases in animals can be divided into five families, CES1-CES5, with the highest content in the liver, intestine and lung. . [0003] Carboxylesterase is a hydrolase that can catalyze the breakage of ester bond, amide bond and thioester bond. It has a wide range of substrates (th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): G01N30/02G01N30/06G01N33/86
CPCG01N30/02G01N30/06G01N33/86G01N2030/027G01N2030/062
Inventor 范敏华徐怀友蔡卫东章莹
Owner ZHEJIANG LONGCHUAN BIOMEDICAL TECH CO LTD
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