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Varenicline pharmaceutical composition capable of reducing generation of nitrosamine impurities, and preparation and application of varenicline pharmaceutical composition

A technology of varenicline and its composition, which is applied in the field of varenicline pharmaceutical composition, can solve problems such as excessive content of nitrosamine impurities, achieve the effects of reducing the generation of nitrosamine impurities, ensuring drug safety, and improving stability

Pending Publication Date: 2022-01-11
SHANDONG WEIZHI ZHONGKE PHARM CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] For varenicline or its pharmaceutically acceptable salts, crystalline forms, solvates, compositions, preparations, and other pharmaceutical compounds, there may also be problems with excessive levels of nitrosamine impurities

Method used

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  • Varenicline pharmaceutical composition capable of reducing generation of nitrosamine impurities, and preparation and application of varenicline pharmaceutical composition
  • Varenicline pharmaceutical composition capable of reducing generation of nitrosamine impurities, and preparation and application of varenicline pharmaceutical composition
  • Varenicline pharmaceutical composition capable of reducing generation of nitrosamine impurities, and preparation and application of varenicline pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0163] Table 1. Components and contents of formula A (specification 1 mg)

[0164]

[0165] in,

[0166] 1.71mg / tablet of varenicline tartrate can be converted into 1mg / tablet of varenicline, that is, each tablet contains 1mg of active ingredient (varenicline), which can also be expressed as: 1mg plain tablet (or 1mg coated tablet, etc.) . And the 0.5mg tablet is that the amount of each component is reduced to half on the basis of the 1mg tablet. In the above formulation, microcrystalline cellulose and anhydrous calcium hydrogen phosphate were used as diluents, partially pregelatinized corn starch was used as a disintegrant, colloidal silicon dioxide was used as a glidant, and stearic acid was used as a lubricant , L-(+)-tartaric acid is used as an acidity regulator (or called a pH regulator), and purified water is used as a coating solvent.

[0167] The preparation method (every batch of 130,000 pieces) comprises the following steps:

[0168] ⑴ Screening and mixing

...

Embodiment 2

[0187] Formula B (specification 1 mg): change the dosage of L-(+)-tartaric acid to 1.71 mg / tablet, and keep other conditions unchanged. According to the same preparation method as in Example 1, 1 mg plain tablet B, 1 mg white coated tablet B and 1 mg blue coated tablet B can be prepared.

Embodiment 3

[0189] Formula Y (specification 1mg): L-(+)-tartaric acid is not added to the tablet, and other conditions remain unchanged. According to the same preparation method as in Example 1, 1 mg plain tablet Y, 1 mg white coated tablet Y and 1 mg blue coated tablet Y can be prepared.

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Abstract

The invention discloses a varenicline pharmaceutical composition capable of reducing generation of nitrosamine impurities, and preparation and application of the varenicline pharmaceutical composition. According to the pharmaceutical composition disclosed by the invention, pharmaceutically acceptable acid is added into a secondary amine compound or the composition thereof, the generation of nitrosamine impurities can be effectively inhibited and reduced, the stability of the secondary amine compound or the composition thereof is improved, the content of nitrosamine genotoxic impurities is controlled at a relatively low level, and the safety requirement is met.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a varenicline pharmaceutical composition capable of reducing the formation of nitrosamine impurities and its preparation and application. Background technique [0002] Varenicline, an aryl-fused azapolycyclic compound that modulates cholinergic activity, is sold as the tartrate salt under the trade name or It can bind to neuronal nicotinic acetylcholine specific receptor sites and can be used for the following diseases: [0003] Treatment of inflammatory bowel disease (including but not limited to: ulcerative colitis, pyoderma gangrenosum, and Crohn's disease), irritable bowel syndrome, spastic dystonia, chronic pain, acute pain, Celiac sprue, pouchitis, vasoconstriction, anxiety, panic disorder, depression, bipolar disorder, autism, sleep disturbance, jet lag, muscular Atrophic lateral sclerosis (ALS), cognitive impairment, drug / toxin-induced cognitive impairment (eg, d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/28A61K31/55A61K47/38A61K47/36A61K47/02A61K47/04A61K47/12A61P1/00A61P1/04A61P1/12A61P9/12A61P25/06A61P25/08A61P25/16A61P25/18A61P25/22A61P25/28A61P25/32A61P25/34A61P25/36
CPCA61K31/55A61K9/2059A61K9/2054A61K9/2009A61P1/00A61P1/04A61P1/12A61P25/22A61P25/28A61P25/32A61P25/34A61P25/06A61P25/16A61P9/12A61P25/18A61P25/08A61K9/2013A61K9/2866A61P21/00A61P29/00A61P17/00A61P25/24A61P25/20A61P31/18A61P1/14A61P3/04A61P9/06A61P35/00A61P25/14
Inventor 魏彦君巴萨瓦拉杰·希达贡纳瓦孙中亚裴慧刘希望邢艳平徐青景刘艳胡青燕
Owner SHANDONG WEIZHI ZHONGKE PHARM CO LTD
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