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Preparation method, detection method and application of probe drug composition for determination of metabolic activity of cytochrome P450

A metabolic activity and cytochrome technology, which is applied to the preparation, detection and application fields of a probe pharmaceutical composition for measuring the metabolic activity of cytochrome P450, can solve the problems of inability to accurately determine low concentration drugs and low recovery rate.

Inactive Publication Date: 2012-08-29
TIANJIN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method lacks CYP2C19, an important CYP450 subtype, and the detection method uses a single-wavelength HPLC method, which has a low recovery rate and cannot accurately determine low-concentration drugs

Method used

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  • Preparation method, detection method and application of probe drug composition for determination of metabolic activity of cytochrome P450
  • Preparation method, detection method and application of probe drug composition for determination of metabolic activity of cytochrome P450
  • Preparation method, detection method and application of probe drug composition for determination of metabolic activity of cytochrome P450

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Preparation of the probe drug composition of the present invention:

[0052]Accurately weigh 10 mg of chlorzoxazone and 5 mg of tolbutamide, dissolve them in 2 ml of absolute ethanol, and set aside; accurately weigh 5 mg of caffeine, 20 mg of metoprolol, and 35 mg of omeprazole, dissolve them in 6 ml of normal saline, and dissolve the above The water ethanol solution was added to the physiological saline solution, and then 2ml (10mg) of midazolam injection was accurately absorbed and added to the above mixed solution to prepare a "cocktail" probe liquid. The concentration of each probe drug was caffeine 0.5mg / ml, metoprolol 2mg / ml, omeprazole 3.5mg / ml, chlorzoxazone 1mg / ml, tolbutamide 0.5mg / ml, Dazolam 1mg / ml. The solution was prepared freshly before administration and used immediately after preparation.

Embodiment 2

[0054] Preparation of the probe drug composition of the present invention:

[0055] Accurately weigh 10 mg of chlorzoxazone and 3 mg of tolbutamide, dissolve them in 2 ml of absolute ethanol, and set aside; accurately weigh 12 mg of caffeine, 35 mg of metoprolol, and 18 mg of omeprazole, dissolve them in 6 ml of normal saline, and dissolve the above The water ethanol solution was added to the physiological saline solution, and then 2ml (10mg) of midazolam injection was accurately absorbed and added to the above mixed solution to prepare a "cocktail" probe liquid. The concentration of each probe drug is caffeine 1.2mg / ml, metoprolol 3.5mg / ml, omeprazole 1.8mg / ml, chlorzoxazone 1mg / ml, tolbutamide 0.3mg / ml, Midazolam 1mg / ml. The solution was prepared freshly before administration and used immediately after preparation.

Embodiment 3

[0057] Preparation of the probe drug composition of the present invention:

[0058] Accurately weigh 20 mg of chlorzoxazone and 10 mg of tolbutamide, dissolve them in 2 ml of absolute ethanol, and set aside; accurately weigh 3 mg of caffeine, 18 mg of metoprolol, and 18 mg of omeprazole, and dissolve them in 5 ml of normal saline. The water ethanol solution was added to the physiological saline solution, and then 3ml (15 mg) of midazolam injection was accurately absorbed and added to the above mixed solution to prepare a "cocktail" probe liquid. The concentration of each probe drug was caffeine 0.3mg / ml, metoprolol 1.8mg / ml, omeprazole 1.8mg / ml, chlorzoxazone 2mg / ml, tolbutamide 1mg / ml, Dazolam 1.5mg / ml. The solution was prepared freshly before administration and used immediately after preparation.

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Abstract

The invention relates to a preparation method, a detection method and application of a probe drug composition for determination of metabolic activity of cytochrome P450. The composition mainly comprises a preparation made with a specific probe with major isoforms of CYP450, i.e. CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4, as an active component. Cocktail probe drug solution is prepared, the probe drug composition is injected into an animal or liver microsomes for in vitro co-incubation, and the concentration of each probe drug is determined to assess the metabolic activity of the CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4. In the early stage of research and development of new drugs, the effects of the drugs on the activity of each isoform of the cytochrome P450 are screened in a high-throughput way, and the interactions of the drugs can be predicted. In the stage of clinical research, the testing can be performed with the probe drug composition in an in-vivo probe method, and the effects of the drugs on the in-vivo metabolic activity of different isoforms of the human liver CYP450 can be examined.

Description

technical field [0001] The present invention relates to the field of medicine, and more specifically relates to a new "cocktail" probe pharmaceutical composition for measuring the metabolic activity of cytochrome P450, and evaluates the effect of the drug on rat CYP450 subtype CYP1A2 by changing its pharmacokinetic parameters. , CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 metabolic activities in vivo and in vitro. Background technique [0002] Cytochrome P450 oxidase (cytochrome P450, CYP450) is the most important enzyme in the oxidative metabolism of drugs in the human body, of which CYP1A2, CYP2C9, CYP2C19, CYP2D6, CYP2E1 and CYP3A4 are the most important subtypes, accounting for about the total amount of CYP450 in the liver More than 80% of the drugs metabolized by the liver, and more than 90% of the drugs metabolized by the liver are metabolized by these 6 subtypes. [0003] Many factors such as genetic factors, age, gender, disease, and environment can affect the activi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N30/02A61K49/00
Inventor 李芹娄建石焦建杰刘洁汪云张才丽
Owner TIANJIN MEDICAL UNIV
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