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Anticholinergic pharmaceutical composition

A composition and drug technology, applied in the field of medicine, can solve the problem of no central anticholinergic activity

Active Publication Date: 2014-02-05
HUNAN DONGTING PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Glycopyrronium bromide is a quaternary ammonium anticholinergic drug, which can inhibit the secretion of gastric juice and regulate gastrointestinal peristalsis; this product also has a stronger antisaliva secretion effect than atropine, but has no central anticholinergic activity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0185] Embodiment 1: Preparation of glycopyrronium bromide bulk drug

[0186] Step (1), synthetic formula I compound and enantiomer thereof:

[0187] Make hydroxycyclopentyl mandelic acid methyl ester (MCPM) and N-methylpyrrolidin-3-alcohol (NMP) reaction according to the method in US2956062A to obtain glycopyrrolate base (GP base), then according to CN101133021B specification sheet [0015]- The method contained in section makes glycopyrronium base react with methyl bromide and then carries out recrystallization refining to gained product, obtains glycopyrronium bromide.

[0188] RRT0.89 content=4.63%, RRT1.14 content=1.78%, RRT2.68 content=1.14%.

[0189] Step (2), recrystallization refining:

[0190] At a temperature of 55-60°C, dissolve 1.5 g of the product obtained in step (1) in 10 ml of anhydrous ethanol-ethyl acetate mixed solvent (100:12, v / v), and slowly add 120 ml of methyl ethyl ether dropwise to it , Stand still at 4-5° to allow sufficient precipitation (about ...

Embodiment 2

[0203] Embodiment 2: Preparation of glycopyrronium bromide bulk drug

[0204] Step (1), synthetic formula I compound and enantiomer thereof:

[0205] According to the method of the specific embodiment part of the CN103159659A description, that is, the method set forth in the description [0010] paragraph to the [0013] paragraph 4 line, the crude product of glycopyrronium bromide is prepared. RRT0.89 content=4.76%, RRT1.14 content=1.61%, RRT2.68 content=1.21%.

[0206] Step (2), recrystallization refining:

[0207] The product obtained in the above step (1) was recrystallized according to the method of step (2) of Example 1 of the present invention (recrystallization yield 89.7%).

[0208] RRT0.89 content=0.83%, RRT1.14 content=0.34%, RRT2.68 content=0.20%. In this recrystallization purification, the content of RRT0.89 was reduced by 82%, the content of RRT1.14 was reduced by 79%, and the content of RRT2.68 was reduced by 83%.

[0209] Step (3), recrystallization refining ...

Embodiment 3

[0217] Embodiment 3: Preparation of glycopyrronium bromide bulk drug

[0218] Step (1), synthetic formula I compound and enantiomer thereof:

[0219] Glycopyrronium bromide was prepared according to the method in the specific embodiment part of the CN102627595A description, that is, the method described in paragraphs [0043] to [0046] of the description. RRT0.89 content=4.13%, RRT1.14 content=1.36%, RRT2.68 content=1.03%.

[0220] Step (2), recrystallization refining:

[0221] The product obtained in the above step (1) was recrystallized according to the method of step (2) of Example 1 of the present invention (recrystallization yield 92.4%).

[0222] RRT0.89 content=0.70%, RRT1.14 content=0.24%, RRT2.68 content=0.16%. In this recrystallization purification, the content of RRT0.89 was reduced by 83%, the content of RRT1.14 was reduced by 82%, and the content of RRT2.68 was reduced by 84%.

[0223] Step (3), recrystallization refining again:

[0224] The product obtained ...

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Abstract

The invention relates to an anticholinergic pharmaceutical composition. Specifically, the invention relates to a medicament capable of being used in pharmacy, wherein the,medicament comprises a compound expressed by the following formula. The invention further provides a preparation of the medicament, and the medicament and the preparation are used as an anticholinergic medicament and can be clinically used for anesthesia, peptic ulcer, salivation, etc. The raw material medicament or preparation has the function of inhibiting gastric secretion and regulating gastrointestinal peristalsis; the raw material medicament or preparation has relatively strong salivary secretion resistance than atropine while having no central anticholinergic activity. The anticholinergic pharmaceutical composition is generally used for clinically treating such symptoms as gastric and duodenal ulcer, chronic gastritis and excessive secretion of gastric acid.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to a pharmaceutical composition as an anticholinergic agent, in particular to a pharmaceutical composition containing glycopyrronium bromide as an anticholinergic agent. Background technique [0002] Glycopyrronium bromide, its English name is Glycopyrronium Bromide or Glycopyrrolate, and its typical Chinese chemical name is: (3RS)-3-[(2SR)-(2-cyclopentyl-2-hydroxy-2-phenylacetyl )oxy]-1,1-dimethylpyrrolidinium bromide, the typical English chemical name is: (3RS)-3-[(2SR)-(2-Cyclopentyl-2-hydroxy-2-phenylacetyl)oxy ]-1,1-dimethylpyrrolidinium bromide, whose molecular formula is C 19 h 28 BrNO 3 , the molecular weight is 398.3, and its typical chemical structural formula is: [0003] [0004] That is, the glycopyrronium bromide used as medicine is (3R)-3-[(2S)-(2-cyclopentyl-2-hydroxy-2-phenylacetyl)oxy]-1,1-dimethyl ylpyrrolidinium bromide and (3S)-3-[(2R)-(2-cyclopentyl-2-hyd...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D207/12A61K31/40A61P23/00A61P1/04A61P43/00
CPCA61K31/40C07D207/12
Inventor 李兴惠
Owner HUNAN DONGTING PHARMA
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