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Flumazenil inclusion compound and production method and application thereof

A technology of flumazenil and clathrate, applied in the field of flumazenil clathrate and its preparation, can solve the problems of low bioavailability, limited solubility of flumazenil, etc., achieve improved solubility and simple preparation conditions Effect

Active Publication Date: 2020-06-26
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The present invention solves the current technical problems of limited solubility and low bioavailability of flumazenil, and provides a flumazenil inclusion compound, which has stable properties and greatly improves the flumazenil inclusion compound. Solubility of Ni

Method used

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  • Flumazenil inclusion compound and production method and application thereof
  • Flumazenil inclusion compound and production method and application thereof
  • Flumazenil inclusion compound and production method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-5

[0031] Embodiments 1-5 relate to the preparation of a flumazenil β-cyclodextrin inclusion compound. The specific components in each embodiment are shown in Table 1 below, and the preparation method is as follows:

[0032] Weigh 110 mg of flumazenil, weigh corresponding hydroxypropyl β-cyclodextrin according to Example 1-5 and place it in a round-bottomed flask, then add 9 ml of absolute ethanol and 1 ml of water to the round-bottomed flask. The inclusion of flumazenil and β-cyclodextrin was carried out on a constant temperature magnetic stirrer at 45° C. and a rotational speed of 200 r / min, and the inclusion time was 30 minutes.

[0033] Table 1. Inclusion of flumazenil and hydroxypropyl β-cyclodextrin in different molar ratios

[0034]

[0035] As can be seen from the above Table 1, when the molar ratio of flumazenil to hydroxypropyl β cyclodextrin is 1:1, the inclusion compound of flumazenil β cyclodextrin cannot be completely prepared, and the With the increase of the c...

Embodiment 6-15

[0037] Examples 6-15 relate to the preparation of a flumazenil β-cyclodextrin inclusion compound. The specific components in each example are shown in Table 2 below, and the preparation method is as follows:

[0038] Weigh 110 mg of flumazenil and 1120 mg of hydroxypropyl β-cyclodextrin in a round-bottomed flask, then add corresponding amounts of absolute ethanol and water to the round-bottomed flask according to Examples 6-15, and stir magnetically at a constant temperature The inclusion of flumazenil and β-cyclodextrin was carried out on the machine at 45°C and the rotation speed was 200r / min, and the inclusion time was 30min.

[0039] Table 2. Inclusion of mixed solvents with different ratios of ethanol and water

[0040]

[0041] As can be seen from the above table 2, when the volume fraction of the ethanol solution is 10%, the inclusion compound of flumazenil β-cyclodextrin cannot be completely prepared; as the volume fraction of the ethanol solution increases, the vol...

Embodiment 16-19

[0043] Examples 16-19 relate to the preparation of a flumazenil β-cyclodextrin inclusion compound. The specific components in each example are shown in Table 3 below, and the preparation method is as follows:

[0044] Weigh 110 mg of flumazenil and 1120 mg of hydroxypropyl β-cyclodextrin in a round-bottomed flask, then add 9 ml of absolute ethanol and 1 ml of water to the round-bottomed flask. -19 The inclusion of flumazenil and β-cyclodextrin was carried out at a certain temperature and the rotation speed was 200r / min, and the inclusion time was 30min.

[0045] Table 3. Inclusion of flumazenil and hydroxypropyl β-cyclodextrin at different temperatures

[0046]

[0047] It can be known from the above Table 3 that when the inclusion temperature of flumazenil and hydroxypropyl β-cyclodextrin is 30°C, the inclusion is complete, and the inclusion compound of flumazenil β-cyclodextrin can be prepared. The increase of β-cyclodextrin can still be completely included, so the selec...

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Abstract

The invention discloses a flumazenil inclusion compound. The flumazenil inclusion compound contains flumazenil and beta-cyclodextrin or a derivative of the beta-cyclodextrin, wherein a molar mass ratio of the flumazenil to the beta-cyclodextrin or the derivative of the beta-cyclodextrin ranges from 1:1.5 to 1:4. A production method of the flumazenil inclusion compound is further disclosed. According to the flumazenil inclusion compound, production conditions are simple, the flumazenil inclusion compound is suitable for industrial mass production, the solubility of the flumazenil can be greatlyimproved, and development of novel dosage forms of flumazenil is facilitated, so that the flumazenil inclusion compound has wide application prospects.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a flumazenil inclusion compound and its preparation method and application, the flumazenil inclusion compound can greatly improve the solubility of flumazenil, which is beneficial to flumazenil Development of new dosage forms. Background technique [0002] Flumazenil, molecular formula C 15 h 14 FN 3 o 3 , CAS number: 78755-81-4, chemical name is 8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4] Benzodiazepine-3-carboxylic acid ethyl ester, its structural formula is as follows: [0003] [0004] flumazenil as benzodiazepine (BDZ) receptor antagonist, used to reverse the central sedative effect caused by BDZ drugs: 1. Terminate the general anesthesia induced and maintained by BDZ drugs. 2. As a specific reversal agent for the central action of BDZ drug overdose. 3. For the differential diagnosis of unexplained coma caused by BDZ, other drugs or brain injury. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K31/5517A61P25/26A61P25/08A61P1/16A61P25/00
CPCA61K47/6951A61K31/5517A61P25/26A61P25/08A61P1/16A61P25/00
Inventor 邹豪侯成卢光照高习清韩凌张思悦
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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