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Preparation method of desloratadine medicine and desloratadine preparation

A technology of desloratadine and loratadine, which is applied in the field of medicine to achieve the effects of ensuring stability, improving stability, and solving process impurities

Active Publication Date: 2020-01-03
深圳市贝美药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Based on this, it is necessary to provide a preparation method of desloratadine medicine, the related substances of desloratadine medicine prepared by the method are fully qualified, and long-term storage, the stability is greatly improved, and there is no abnormal increase in impurities. This method not only solves the problem of process impurities, but also ensures the improvement of the stability of the drug

Method used

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  • Preparation method of desloratadine medicine and desloratadine preparation
  • Preparation method of desloratadine medicine and desloratadine preparation
  • Preparation method of desloratadine medicine and desloratadine preparation

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preparation example Construction

[0043] The preparation method of desloratadine medicine of one embodiment, the method comprises the following steps:

[0044] S1: Add the organic acid salt to a co-solvent to dissolve, and then add the raw drug desloratadine for a mixed reaction;

[0045] The chemical name of desloratadine in this embodiment is 8-chloro-6,11-dihydro-11-(4-azicyclylidene)-5H-benzene-[5,6]-cyclohepta[1, 2-b]pyridine, molecular formula C 19 h 19 ClN 2 , the bulk drug can be a commercially available product, the structural formula is as follows:

[0046]

[0047] In one of the embodiments, S1 includes adding the organic acid salt into the organic co-solvent, dissolving, then adding the raw drug desloratadine, and diluting with water;

[0048]Specifically, add the organic acid salt into the organic co-solvent at room temperature, stir at a speed of 50r / min to 150r / min to completely dissolve, slowly add the raw drug desloratadine to completely dissolve, and add purified water to dilute ; The...

Embodiment 1

[0082] The preparation method of the desloratadine medicine of the present embodiment comprises the following steps:

[0083] 1) Add 100g of propylene glycol into the concentrated preparation tank at room temperature, add 1.2g of sodium citrate, stir at a speed of 100r / min to completely dissolve, slowly add 0.5g of the raw material desloratadine to completely dissolve, and add Dilute with 200mL purified water;

[0084] 2) Add 500mL of purified water to the main liquid mixing tank at room temperature, stir at a speed of 100r / min, and add 7g of hypromellose in batches. After it is completely dissolved, add 150g of sorbitol and 0.45g of citric acid 1. Edetate disodium 0.25g, stirred until completely dissolved;

[0085] 3) Transfer the solution in the medium concentration mixing tank of step (1) to the main liquid mixing tank of step (2), stir at room temperature for 5 minutes at a speed of 100 r / min, add 2 g of sucralose and 5 g of strawberry flavor essence , after stirring for...

Embodiment 2

[0091] The preparation method of the desloratadine medicine of the present embodiment comprises the following steps:

[0092] 1) Add 100g of polyethylene glycol into the concentrated preparation tank at room temperature, add 1.2g of organic carboxylate sodium citrate, stir at a speed of 100r / min to completely dissolve, and slowly add the raw drug desloratadine 0.5g to dissolve completely, and add 200mL purified water to dilute;

[0093] 2) Add 500mL of purified water to the main liquid mixing tank at room temperature, stir at a speed of 100r / min, and add 7g of hydroxyethyl cellulose in batches. After it is completely dissolved, add 150g of xylitol and 0.45g of citric acid g. 0.25 g of disodium edetate, an ion regulator, was stirred until completely dissolved.

[0094] 3) Transfer the solution in the medium-concentration mixing tank of step 1) to the main mixing tank of step 2). After stirring for 5 minutes at a speed of 100 r / min at room temperature, add 2 g of sweetener sucr...

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Abstract

The invention relates to a preparation method of a desloratadine medicine and a desloratadine preparation. The preparation method comprises the following steps of adding a solubilizer to organic acidsalt, performing dissolving, then adding a raw material medicine namely desloratadine, and performing a mixing reaction; and dissolving medicinal auxiliary materials to a main solvent, and mixing thedissolved medical auxiliary materials with mixed liquor after the reaction to obtain the desloratadine medicine. According to the preparation method disclosed by the invention, in the preparation process of the desloratadine preparation, firstly high-activity organic polybasic carboxylate is added for performing occupied protection on active sites of the desloratadine, the experiment proves that orally-taken solution related substances prepared in the manner are completely qualified and can be kept and stored for a long time, the stability is greatly improved, and the situation that impuritiesare abnormally enlarged does not exist. Through the adoption of the method, the problem of impurities in the technology is solved, and the stability of medicines is also guaranteed.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of desloratadine and a preparation thereof. Background technique [0002] Desloratadine is the active metabolite of loratadine from ethyl formate in vivo. Desloratadine is a new third-generation antihistamine with strong anti-allergic effect, fast onset and long-lasting effect. Many clinical trials have also confirmed the efficacy and safety of desloratadine for adults or children with allergic rhinitis (AR) and chronic idiopathic urticaria (CIU), and has a good application prospect. [0003] Sunovion Pharmaceuticals (formerly known as Sepracor) discovered the compound in 1997 and owns the patent right of the compound. US Patent US4659716 first described desloratadine in detail, and in December 1997 exclusively authorized Schering-Plough (Schering-Plough) , Registered in Europe on January 17, 2001, the indication is seasonal allergic rhinitis, added indica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/12A61K31/4545A61P37/08C07D401/04
CPCA61K9/0095A61K31/4545A61K47/12A61P37/08C07D401/04
Inventor 吴光美任鹏李红组唐邦忠
Owner 深圳市贝美药业有限公司
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