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Novel probe medicament combination and preparation method and application thereof

A probe and drug technology, which is applied in the new probe drug combination, preparation and application fields, can solve the problem of not being able to specifically reflect the drug metabolism ability of the liver and the like

Inactive Publication Date: 2015-02-04
娄建石
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although there are many clinical indicators used to check liver function, they cannot specifically reflect the drug metabolism ability of the liver. Therefore, the "cocktail" method is used to quantitatively measure the activity of metabolic enzymes in the body to study the effect of liver disease status on the activity of drug metabolism enzymes. It can estimate the possible toxic reaction caused by the traditional drug dose, adjust the clinical drug regimen, and has important significance in alleviating the adverse drug reaction and guiding clinical rational drug use.

Method used

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  • Novel probe medicament combination and preparation method and application thereof
  • Novel probe medicament combination and preparation method and application thereof
  • Novel probe medicament combination and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0236] Accurately weigh 5mg of probe drug caffeine and 20mg of metoprolol dissolved in 6ml of normal saline, weigh 10mg of chlorzoxazone and 5mg of tolbutamide and dissolve in 2ml of absolute ethanol, slowly add absolute ethanol to the normal saline Then, accurately draw 2ml (10mg) of midazolam injection and add to the above mixture to prepare a "cocktail" probe solution. The solution was prepared freshly before administration and used immediately after preparation.

Embodiment 2

[0238] Accurately weigh 5mg of probe drug caffeine and 50mg of metoprolol dissolved in 6ml of normal saline, weigh 30mg of chlorzoxazone and 5mg of tolbutamide and dissolve in 2ml of absolute ethanol, slowly add absolute ethanol to the normal saline Then, accurately draw 2ml (10mg) of midazolam injection and add to the above mixture to prepare a "cocktail" probe solution. The solution was prepared freshly before administration and used immediately after preparation.

Embodiment 3

[0240] Accurately weigh 15mg of probe drug caffeine and 20mg of metoprolol dissolved in 6ml of normal saline, weigh 20mg of chlorzoxazone and 15mg of tolbutamide and dissolve in 2ml of absolute ethanol, slowly add absolute ethanol to the normal saline Then, accurately draw 30 mg of midazolam injection and add it to the above mixture to prepare a "cocktail" probe solution. The solution was prepared freshly before administration and used immediately after preparation.

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Abstract

The invention relates to a novel cocktail probe medicament combination comprising caffeine, metoprolol, chlorzoxazone, tolbutamide and midazolam. The influence of hepatic ischemia preconditioning and hepatic ischemia-reperfu-sion injury on medicament metabolism activity of rat CYP1A2, CYP2C9, CYP2E1, CYP2D6, and CYP3A4 in vivo is evaluated through the change of pharmacokinetics parameters of the combination.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a new "cocktail" probe pharmaceutical composition, which can be used to evaluate the effects of hepatic ischemia preconditioning and hepatic ischemia-reperfusion injury on CYP subtypes of rats through changes in its pharmacokinetic parameters. Effects of CYP1A2, CYP2C9, CYP2E1, CYP2D6 and CYP3A4 on drug metabolism activity in vivo. Background technique [0002] Many exogenous substances (xenobiotics) need to undergo biotransformation process in the body, and the liver is the main place for the human body to carry out the phase I reaction of biotransformation. Enzymes involved in biotransformation are cytochrome P450-dependent mixed-function oxidase systems encoded and regulated by a huge gene family, the main component of which is cytochrome P450 (CYP) enzyme system. CYP is divided into 17 gene families, 42 subfamilies, and 64 enzymes in humans. The functional enzymes closely related to...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K49/00
Inventor 娄建石刘颖焦建杰张才丽
Owner 娄建石
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