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Preparation method of escitalopram oxalate inclusion compound oral liquid

A technology of escitalopram oxalate and inclusion compound is applied in the field of preparation of escitalopram oxalate inclusion compound oral liquid, and can solve the problem of masking the bitterness, astringency, poor medication compliance, Swallowing requirements are low and other problems, to achieve the effect of good taste, improve quality, and improve medication compliance

Inactive Publication Date: 2020-02-14
BEIJING VENTUREPHARM BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the published patents and clinical applications of escitalopram oxalate mainly include ordinary tablets, orally disintegrating tablets, effervescent tablets, and oral liquids. However, the medication compliance of swallowing air crash population is poor; orally disintegrating tablets have low requirements for swallowing, and are not suitable for patients with poor medication compliance; effervescent tablets and oral liquids greatly improve patients’ medication compliance compared with ordinary tablets, but traditional The flavoring method cannot completely cover the bitter and astringent taste of escitalopram oxalate itself

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] prescription:

[0029] Escitalopram Oxalate 1.28g

[0030] β-cyclodextrin 7.68g

[0031] Glycerin 350.0 g

[0032] Sorbitol 150.0g

[0033] Propylene glycol 10.0g

[0034] Citric acid 2.0g

[0035] Sodium citrate 4.0g

[0036] Propylparaben 0.5g

[0037] Menthol 0.1g

[0038] Add purified water to 1000ml

[0039] Preparation Process:

[0040] 1. Grind menthol, propylparaben, etc. through a 60-mesh sieve for later use;

[0041] Take an appropriate amount of purified water to boil, degas, and let cool for later use.

[0042] 2. Add escitalopram oxalate and β-cyclodextrin to purified water in a weight ratio of 1:6, and then remove the water to form an inclusion compound;

[0043] 3. Take the prescribed amount of escitalopram oxalate inclusion compound, add an appropriate amount of purified water and heat it in a water bath to dissolve.

[0044] 4. Take about 200g of purified water, add the prescribed amount of citric acid and sodium citrate into it, and stir t...

Embodiment 2

[0049] prescription:

[0050] Escitalopram Oxalate 1.28g

[0051] Hydroxypropyl-β-cyclodextrin 10.24g

[0052] Glycerin 300.0 g

[0053] Propylene glycol 30.0 g

[0054] Sorbitol 280.0g

[0055] Citric acid 2.0g

[0056] Sodium citrate 6.0 g

[0057] Methylparaben 0.5g

[0058] Propylparaben 1.5g

[0059] Sucrose 1.0g

[0060] Menthol 0.15g

[0061] Apple essence 0.05g

[0062] Add purified water to 1000ml

[0063] Preparation Process:

[0064] 1. Grind menthol, methylparaben, propylparaben, etc. through a 60-mesh sieve for later use;

[0065] Take an appropriate amount of purified water to boil, degas, and let cool for later use.

[0066] 2. Add escitalopram oxalate and hydroxypropyl-β-cyclodextrin to purified water in a weight ratio of 1:8, and then remove the purified water to form an inclusion compound;

[0067] 3. Take the prescribed amount of escitalopram oxalate inclusion compound, add an appropriate amount of purified water and heat it in a water bath to...

Embodiment 3

[0073] prescription:

[0074] Escitalopram Oxalate 1.28g

[0075]β-cyclodextrin 12.8g

[0076] Glycerin 150.0 g

[0077] Propylene glycol 175.0 g

[0078] Sorbitol 150.0g

[0079] Citric acid 3.5g

[0080] Sodium citrate 6.5 g

[0081] Methylparaben 1.0g

[0082] Propylparaben 0.1g

[0083] Aspartame 1.5g

[0084] Menthol 0.15g

[0085] Sweet orange essence 0.05g

[0086] Add purified water to 1000ml

[0087] Preparation Process:

[0088] 1. Grind menthol, methylparaben, propylparaben, etc. through a 60-mesh sieve for later use;

[0089] Take an appropriate amount of purified water to boil, degas, and let cool for later use.

[0090] 2. Add escitalopram oxalate and β-cyclodextrin to purified water at a weight ratio of 1:10, then remove the purified water to form an inclusion compound;

[0091] 3. Take the prescribed amount of escitalopram oxalate inclusion compound, add an appropriate amount of purified water and heat it in a water bath to dissolve.

[0092] 4....

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Abstract

The invention discloses escitalopram oxalate inclusion compound oral liquid and a preparation method of the escitalopram oxalate inclusion compound oral liquid. In order to overcome the defect of a conventional flavor correction process of escitalopram oxalate, the preparation method disclosed by the invention has the advantages that the flavor is corrected commonly by adopting an inclusion technology and a flavor correction agent, so that a bitter taste of the escitalopram oxalate is covered, and an oral liquid preparation having an appropriate mouth feel is developed, and thus, the medicineapplication compliance of patients is improved.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a preparation method of an escitalopram oxalate inclusion compound oral liquid. Background technique [0002] Depression seriously endangers human physical and mental health. The World Health Organization predicts that depression will become the second leading cause of abnormal death and disability by 2020. Currently, the first-line clinical antidepressants mainly include selective serotonin reuptake inhibitors (SSRI, representative drugs fluoxetine, paroxetine, sertraline, fluvoxamine, citalopram and escitalopram) , serotonin and norepinephrine reuptake inhibitors (SNRIs, representing the drugs venlafaxine and duloxetine), norepinephrine and specific serotonergic antidepressants (NaSSA, representing the drugs mirtazapine equality. [0003] Escitalopram oxalate is clinically used for the treatment of major depressive disorder and panic disorder with or without agoraphobia. ...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K9/08A61K31/343A61P25/24
CPCA61K47/6949A61K47/6951A61K9/0095A61K31/343A61P25/24
Inventor 赵宇巍王宇杰
Owner BEIJING VENTUREPHARM BIOTECH
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