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Method for preparing high-concentration tetralin compound homogeneous stable solution by using sulfobutyl-β-cyclodextrin

A technology of tetralin and cyclodextrin is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc. Simple to use effects

Active Publication Date: 2016-05-25
WUXI APPTEC SUZHOU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Sulfobutyl-β-cyclodextrin (SBECD), as an anionic highly water-soluble cyclodextrin derivative, can be well included with drug molecules to form non-covalent complexes, improving drug stability, water solubility, and safety It can reduce nephrotoxicity, alleviate drug hemolysis, control drug release rate, and mask bad smell. However, there is no literature showing that sulfobutyl-β-cyclodextrin (SBECD) can prepare high-concentration tetralin compound homogeneous and stable solution

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] 1) Dissolve commercially available sulfobutyl-β-cyclodextrin in deionized water to prepare sulfobutyl-β-cyclodextrin with a weight volume (w / v) concentration of 10% (ie 10g / 100mL) solution.

[0024] 2) Weigh 500mg of 8-ring substituted 2-amino-1,2,3,4-tetralin, and dissolve it in 9ml of 10% (w / v) sulfobutyl-β-cyclodextrin solution prepared above In, and dilute to 10ml, the solution is a suspension.

[0025] 3) Dilute the suspension prepared in step 2) to a concentration of 30 mg / ml with 10% (w / v) sulfobutyl-β-cyclodextrin solution to form a semi-clear solution, which has a small amount of precipitation after standing for 10 minutes .

[0026] 4) Dilute the suspension in step 3) to a concentration of 25 mg / ml with 10% (w / v) sulfobutyl-β-cyclodextrin solution to form a homogeneous and clear solution without precipitation after standing for 10 minutes.

[0027] 5) The prepared 25mg / ml 8-ring substituted 2-amino-1,2,3,4-tetralin solution can be directly used in related e...

Embodiment 2

[0029] 1) Dissolve commercially available sulfobutyl-β-cyclodextrin in deionized water to prepare sulfobutyl-β-cyclodextrin with a weight volume (w / v) concentration of 30% (ie 30g / 100mL) solution.

[0030] 2) Weigh 500mg of 8-ring-substituted 2-amino-1,2,3,4-tetralin, and dissolve it in 9ml of 30% (w / v) sulfobutyl-β-cyclodextrin solution prepared above In, and dilute to 10ml, the solution is a suspension.

[0031] 3) Dilute the suspension prepared in step 2) to a concentration of 30 mg / ml with 30% (w / v) sulfobutyl-β-cyclodextrin solution to form a homogeneous and clear solution without precipitation after standing for 10 minutes.

[0032] 4) The prepared 30 mg / ml 8-ring substituted 2-amino-1,2,3,4-tetralin solution can be directly used in related experiments, or diluted to the target concentration for related experiments.

Embodiment 3

[0034] 1) Dissolve commercially available sulfobutyl-β-cyclodextrin in deionized water to prepare sulfobutyl-β-cyclodextrin with a weight volume (w / v) concentration of 50% (50g / 100mL) solution;

[0035] 2) Weigh 500mg of 8-ring substituted 2-amino-1,2,3,4-tetralin, and dissolve it in 9ml of the above prepared 50% (w / v) sulfobutyl-β-cyclodextrin solution In, and dilute to 10ml, the solution is a suspension.

[0036] 3) Dilute the suspension prepared in step 2) to a concentration of 30 mg / ml with 50% (w / v) sulfobutyl-β-cyclodextrin solution to form a uniform and clear solution, which has no precipitation after standing for 10 minutes.

[0037] 4) The prepared 30 mg / ml 8-ring substituted 2-amino-1,2,3,4-tetralin solution can be directly used in related experiments, or diluted to the target concentration for related experiments.

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Abstract

A disclosed method for preparing a high-density tetralin-compound homogeneous stable solution by employing sulfobutyl ether-beta-cyclodextrin comprises the following steps: 1) dissolving sulfobutyl ether-beta-cyclodextrin in water to prepare a sulfobutyl ether-beta-cyclodextrin solution; and 2) weighing a tetralin compound, dissolving into the sulfobutyl ether-beta-cyclodextrin solution, so as to form a homogeneous stable high-density tetralin compound solution. The method is simple in operation and rapid for preparation, helps to solve the problem of bad solubility of tetralin compounds, and is widely applicable to preparation of homogeneous stable high-density solutions of tetralin compounds.

Description

technical field [0001] The invention relates to a method for preparing a uniform and stable solution of high-concentration tetralin compounds, in particular to a method for quickly and easily preparing high-concentration tetralin compounds uniform and stable solutions using sulfobutyl-β-cyclodextrin (SBECD) solution method. Background technique [0002] The tetrahydronaphthalene compound has a novel structure and is a selective 5-HTA receptor antagonist. Recently, it has been found that such compounds have significant antifungal activity in vitro, which is of great development value. At present, the tetrahydronaphthalene compounds already on the market, such as naphthoquine phosphate, have a killing effect on various Plasmodium schizonts and some strains of Plasmodium gametophytes and tissue-stage protozoa, and have a good healing effect on drug-resistant Plasmodium , has a long-term preventive effect on malaria parasites. In addition, 8-ring substituted 2-amino-1,2,3,4-t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K47/48A61K31/015A61K31/136
Inventor 王友红陈秀芳赵宗良陆佳佳王霞
Owner WUXI APPTEC SUZHOU
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