Method for preparing homogeneous and stable solution of tetrahydronaphthalene compounds by using hydroxypropyl-β-cyclodextrin

A technology of tetralin and cyclodextrin, which is applied in the direction of non-active ingredients of polymer compounds, medical preparations containing active ingredients, and pharmaceutical formulas, to achieve the effects of rapid preparation, accelerated development, and simple operation

Active Publication Date: 2015-12-09
WUXI APPTEC SUZHOU
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Hydroxypropyl-β-cyclodextrin (HP-β-CD), as an anionic highly water-soluble cyclodextrin derivative, can be well included with drug molecules to form non-covalent complexes, improving drug stability, Water-soluble, safe, reduce nephrotoxicity, alleviate drug hemolysis, control drug release rate, mask bad smell, but there is no literature to disclose that hydroxypropyl-β-cyclodextrin can prepare tetralin compound homogeneous and stable solution report

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0024] 2) Weigh 250mg of 8-ring-substituted 2-amino-1,2,3,4-tetralin, and dissolve it in 9ml of the above prepared 10% (w / v) hydroxypropyl-β-cyclodextrin solution In, and dilute to 10ml, the solution is a suspension.

[0025] 3) Dilute the suspension prepared in step 2) to a concentration of 20 mg / ml with 10% (w / v) hydroxypropyl-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 12.5 mg / ml with 10% (w / v) hydroxypropyl-β-cyclodextrin solution to form a homogeneous and clear solution without precipitation after standing for 10 minutes.

[0027] 5) The prepared 12.5 mg / ml 8-ring substituted 2-amino-1,2,3,4-tetrahydronaphthalene solut...

Embodiment 2

[0029] 1) Dissolve commercially available hydroxypropyl-β-cyclodextrin in deionized water to prepare hydroxypropyl-β-cyclodextrin with a weight volume (w / v) concentration of 20% (ie 20g / 100mL) solution;

[0030] 2) Weigh 250mg of 8-ring-substituted 2-amino-1,2,3,4-tetralin, and dissolve it in 9ml of the above prepared 20% (w / v) hydroxypropyl-β-cyclodextrin solution In, and dilute to 10ml, the solution is a suspension.

[0031] 3) Dilute the suspension prepared in step 2) to a concentration of 15 mg / ml with 20% (w / v) hydroxypropyl-β-cyclodextrin solution to form a uniform and clear solution, and there is no precipitation after standing for 10 minutes.

[0032] 4) The prepared 15 mg / ml 8-ring substituted 2-amino-1,2,3,4-tetrahydronaphthalene solution can be directly used in related experiments, or diluted to the target concentration for related experiments.

Embodiment 3

[0034] 1) Dissolve commercially available hydroxypropyl-β-cyclodextrin in deionized water to prepare hydroxypropyl-β-cyclodextrin with a weight volume (w / v) concentration of 30% (ie 30g / 100mL) solution;

[0035] 2) Weigh 250mg of 8-ring substituted 2-amino-1,2,3,4-tetralin and dissolve it in 9ml of the above-prepared 30% (w / v) hydroxypropyl-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 15 mg / ml with 30% (w / v) hydroxypropyl-β-cyclodextrin solution to form a uniform and clear solution, which has no precipitation after standing for 10 minutes.

[0037] 4) The prepared 15 mg / ml 8-ring substituted 2-amino-1,2,3,4-tetrahydronaphthalene solution can be directly used in related experiments, or diluted to the target concentration for related experiments.

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PUM

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Abstract

A disclosed method for preparing a tetralin-compound homogeneous stable solution by employing hydroxypropyl-beta-cyclodextrin comprises the following steps: 1) dissolving hydroxypropyl-beta-cyclodextrin in water to prepare a hydroxypropyl-beta-cyclodextrin solution; and 2) weighing a tetralin compound, dissolving into the hydroxypropyl-beta-cyclodextrin solution, so as to form the homogeneous stable 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 tetralin-compound solutions.

Description

technical field [0001] The invention relates to a method for preparing a uniform and stable solution of tetralin compounds, in particular to a method for preparing a uniform and stable solution of tetralin compounds quickly and easily by using hydroxypropyl-β-cyclodextrin (HP-β-CD). 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. Tetralin compounds currently on the market, such as naphthoquine phosphate, have killing effects 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-tetrahydronaphthalene and other tetralin compounds have...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/135A61K9/08A61K47/40A61P31/10A61P33/06
Inventor 王友红陈秀芳赵宗良陆佳佳王霞
Owner WUXI APPTEC SUZHOU
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