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Inhibitor or promoter of uridinediphosphate glucuronosyltransferase 2B (UGT2B)

A technology based on uridine diphosphate and aldehyde acid groups, which is applied in the field of effective UGT2B inhibitors and UGT2B accelerators, and can solve the problem of low clearance rate

Active Publication Date: 2009-12-23
INT EDUCATION FOUND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the clearance rate in the body is significantly lower than more than 2 times

Method used

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  • Inhibitor or promoter of uridinediphosphate glucuronosyltransferase 2B (UGT2B)
  • Inhibitor or promoter of uridinediphosphate glucuronosyltransferase 2B (UGT2B)
  • Inhibitor or promoter of uridinediphosphate glucuronosyltransferase 2B (UGT2B)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Example 1. In Vitro Experiments of UGT 2B Inhibitors

[0070] Materials and Methods:

[0071] 1. Preparation of UGT2B inhibitors

[0072] In the following experiments, the present invention uses 27 kinds of traditional Chinese medicine medicines and 10 kinds of excipients as UGT2B inhibitors, wherein the Chinese medicine medicines are all commercial pure compounds, purchased from Sigma Chemical Co., Nacalai Tesque (Kyoto, Japan) and INDOFINE Chemical Co., Inc. (Somerville, New Jersey). The types, names, crude drug sources and chemical formulas of these traditional Chinese medicines are listed in Table 1 below. These traditional Chinese medicines were formulated with ethanol to concentrations of 1, 10, and 100 μM, respectively, for subsequent experiments.

[0073] In addition, the excipients are all commercial pure compounds. PEG (Polyethyleneglycol) 400, PEG 2000, PEG 4000, Tween 20, Tween 60, Tween 80, 58. 76. F68, F127. These excipients were formulated w...

Embodiment 2

[0118] Example 2 In Vitro Experiment of UGT 2B Accelerators

[0119] This example is carried out with the same procedure as that described in Example 1, but 40 kinds of traditional Chinese medicine medicines adopted in the following list 5 are used as UGT2B accelerators, and these Chinese medicine medicines are all commercialized pure Compounds were purchased from Sigma Chemical Co., Nacalai Tesque (Kyoto, Japan) and INDOFINE Chemical Co., Inc. (Somerville, New Jersey), respectively. The types, names, crude drug sources and chemical formulas of these traditional Chinese medicines are listed in Table 5 below.

[0120] Table 5 The types, names, sources and chemical formulas of UGT2B accelerators

[0121]

[0122]

[0123]

[0124]

[0125]

[0126] result:

[0127] The results of the above experiments are shown in Table 6. Orthoguaic acid has the best promoting effect on liver microsomal metabolism of nalbuphine, which can reach -188.09 (±16.566)% inhibition ...

Embodiment 3

[0131]The impact of embodiment 3 UGT 2B inhibitor on the concentration of oral nalbuphine

[0132] Materials and Methods:

[0133] 1. Experimental animals

[0134] The source of animals is the Sprague-Dawley strain of male rats used in experiments, mainly healthy rats with a body weight of 500-600 g, purchased from the National Laboratory Animal Breeding and Research Center, Taiwan. After the purchase, the animals were given an adaptation period of one week, and were reared at a fixed temperature (25±1° C.), humidity and photoperiod (12 hours of light per day). Fast for about 12-16 hours before the experiment. The experimental method is to evaluate drug absorption in an oral way.

[0135] 2. Preparation of UGT2B inhibitor and nalbuphine

[0136] The standard solution of nalbuphine is prepared in water, and the inhibitor is prepared in alcohol.

[0137] 3. Experimental method:

[0138] i. After intraperitoneal injection (I.P.) of 3-5mg / 100g body weight of pentobarbital (p...

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Abstract

The present invention provides a UGT2B inhibitor that can increase the bioavailability of drugs, which is one of the compounds selected from capillarisin, isorhamnetin, and β-naphthoflavone. Or combined in the form of free base or pharmaceutically acceptable salts; the present invention also provides a UGT2B accelerator that can promote the liver detoxification function of the individual, the accelerator is selected from the group consisting of nordihydroguaiaretic acid, One or a combination of compounds such as wogonin and trans-cinnamic acid are in the form of free base or pharmaceutically acceptable salts.

Description

technical field [0001] The present invention relates to the field of biology, in particular to an effective UGT2B inhibitor to increase the bioavailability of a drug (drug bioavability); the present invention also specifically relates to a UGT2B accelerator to promote the detoxification function of an individual. Background technique [0002] The process of drug metabolism in the human body, especially for highly fat-soluble drugs, can basically be divided into two stages of biotransformation: the first phase reaction (phase Ireaction) is the conversion of the original lipid Soluble molecules are added with functional groups to make them polar molecules; the second phase reaction (phase II reaction) produces highly polar products through conjugation to rapidly metabolize the drug, while the self- Eliminated in urine or feces. [0003] The most common and important conjugation is glucuronidation via uridine diphosphate(UDP)-glucuronosyl trans-ferases (abbreviated as UGTs; EC...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K31/704A61K31/7048A61K31/045A61K31/366A61K31/56A61K31/215A61K31/01A61K31/11A61K31/485A61K45/00A61P1/16
CPCA61K31/352A61P1/16A61P25/04A61P35/00A61P43/00
Inventor 胡幼圃熊正辉王媺婷鲍力恒
Owner INT EDUCATION FOUND
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