Hydroxychloroquine sulfate and polyglutamic acid polymer, as well as preparation method and application thereof

A technology of hydroxychloroquine sulfate and polyglutamic acid, which is used in drug combinations, pharmaceutical formulations, medical preparations containing active ingredients, etc., can solve the problem of excessive metabolism, low specificity of drug action, body irritation or pain And other issues

Inactive Publication Date: 2016-09-07
陕西省生物农业研究所
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, the unsatisfactory pharmacokinetic properties affect the absorption of drugs, resulting in low bioavailability, or the metabolic rate is too fast or too slow due to the cha...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] A hydroxychloroquine sulfate polyglutamic acid polymer is a polymer formed by the esterification reaction of hydroxychloroquine sulfate and polyglutamic acid in a weight ratio of 1:1. The hydroxyl group of the hydroxychloroquine sulfate is esterified with the carboxyl group of polyglutamic acid. The content of hydroxychloroquine sulfate in the polymer is in the range of 50% (weight ratio). The molecular weight of the polyglutamic acid is 30000. The polyglutamic acid is gamma-polyglutamic acid.

[0023] The preparation method of this hydroxychloroquine sulfate polyglutamic acid polymer is:

[0024] (1) take hydroxychloroquine sulfate and polyglutamic acid by weight ratio of 1:1, standby;

[0025] (2) dissolving polyglutamic acid in deionized water, stirring magnetically to form a 1 mg / ml polyglutamic acid aqueous solution;

[0026] (3) hydroxychloroquine sulfate is dissolved in deionized water, and magnetically stirred to form a 1mg / ml aqueous solution of hydroxychlo...

Embodiment 2

[0031] A hydroxychloroquine sulfate polyglutamic acid polymer is a polymer formed by the esterification reaction of hydroxychloroquine sulfate and polyglutamic acid in a weight ratio of 1:3.5. The hydroxyl group of the hydroxychloroquine sulfate is esterified with the carboxyl group of polyglutamic acid. The content of hydroxychloroquine sulfate in the polymer is in the range of 22.22% (weight ratio). The molecular weight of the polyglutamic acid is 40000. The polyglutamic acid is gamma-polyglutamic acid.

[0032] The preparation method of this hydroxychloroquine sulfate polyglutamic acid polymer is:

[0033] (1) take hydroxychloroquine sulfate and polyglutamic acid by weight ratio of 1:4.5, standby;

[0034] (2) dissolving polyglutamic acid in deionized water, stirring magnetically to form a 2 mg / ml polyglutamic acid aqueous solution;

[0035] (3) hydroxychloroquine sulfate is dissolved in deionized water, and magnetically stirred to form a 2mg / ml aqueous solution of hydr...

Embodiment 3

[0040] A hydroxychloroquine sulfate polyglutamic acid polymer is a polymer formed by the esterification reaction of hydroxychloroquine sulfate and polyglutamic acid in a weight ratio of 1:6. The hydroxyl group of the hydroxychloroquine sulfate is esterified with the carboxyl group of polyglutamic acid. The content of hydroxychloroquine sulfate in the polymer is in the range of 14.28% (weight ratio). The molecular weight of the polyglutamic acid is 50000. The polyglutamic acid is gamma-polyglutamic acid.

[0041] The preparation method of this hydroxychloroquine sulfate polyglutamic acid polymer is:

[0042] (1) take hydroxychloroquine sulfate and polyglutamic acid by weight ratio of 1:6, standby;

[0043] (2) dissolving polyglutamic acid in deionized water, stirring magnetically to form a 3 mg / ml polyglutamic acid aqueous solution;

[0044] (3) hydroxychloroquine sulfate is dissolved in deionized water, and magnetically stirred to form a 3mg / ml aqueous solution of hydroxyc...

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PUM

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Abstract

The invention discloses a hydroxychloroquine sulfate and polyglutamic acid polymer, as well as a preparation method and application thereof. The hydroxychloroquine sulfate and polyglutamic acid polymer is a polymer formed by carrying out esterification reaction between hydroxychloroquine sulfate and polyglutamic acid according to a weight ratio of 1:(1-6). The hydroxychloroquine sulfate and polyglutamic acid polymer is applied to treatment of discoid lupus erythematosus and systemic lupus erythematosus. The hydroxychloroquine sulfate and the polyglutamic acid are cross-linked to obtain the hydroxychloroquine sulfate and polyglutamic acid polymer, and hydroxyls of the hydroxychloroquine sulfate are modified to change certain original physiochemical properties thereof, improve pharmaceutical activity, enhance curative effects, reduce side effects, improve the sustained release effects of the drug and reduce the medication frequency of a patient; when the hydroxychloroquine sulfate and polyglutamic acid polymer is used for treating discoid lupus erythematosus and systemic lupus erythematosus, the drug can reach a destination lesion location under protection of the polyglutamic acid in a slow degradation process, so that the aim of accurate treatment is fulfilled, and the hydroxychloroquine sulfate and polyglutamic acid polymer has a certain clinical application value.

Description

technical field [0001] The invention relates to the technical field, in particular to a hydroxychloroquine sulfate polyglutamic acid polymer and a preparation method and application thereof. Background technique [0002] Hydroxychloroquine sulfate, medicine, the main component is 2-4-(7-chloro-4-quinolyl) aminopentylethylamino-ethanol sulfate. It is a film-coated tablet, which is white or off-white after the coating is removed. For the treatment of discoid lupus erythematosus and systemic lupus erythematosus. [0003] Hydroxychloroquine sulfate may have the following reactions during long-term treatment, but the adverse reactions of different compounds and their types and incidence may be different. (1) Central nervous system reactions: excitement, nervousness, mood changes, nightmares, psychosis, headache, dizziness, vertigo, tinnitus, nystagmus, nervous deafness, convulsions, ataxia. (2) Neuromuscular reactions: external ophthalmoplegia, skeletal muscle weakness, and de...

Claims

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Application Information

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IPC IPC(8): C08G69/48A61K31/785A61K31/787A61P37/02A61P19/04A61P17/02
CPCA61K31/785A61K31/787C08G69/48
Inventor 陈卫锋孟永宏徐升运秦涛
Owner 陕西省生物农业研究所
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