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Pharmaceutical composition containing (3S, 2í»S)-3-(2í»-hydroxy-2í»-cyclopentyl-2í»-phenylethoxy) quinuclidine hydrochloride and uses thereof

A technology of phenylethoxy and quinuclidane, which is applied in the field of pharmaceutical compositions, can solve the problems of different enantiomeric activities, unreported, low activity, etc., achieve strong stereoselectivity, avoid toxic side effects, optical The effect of high purity

Inactive Publication Date: 2008-08-06
CHENGDU LIST PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] (1) Only one of the enantiomers in the racemate is active, and the activity of the other enantiomer is very low or inactive, or the activity of the enantiomers is qualitatively different, such as the total blood concentration of the racemate cannot be true respond to the concentration of the enantiomer that exerts the effect;
[0005] (2) A specific toxicity of certain drugs is mainly attributable to one of the enantiomers;
[0018] At present, there have been no reports on the use of 4 chiral compounds of penehyclidine hydrochloride for pharmaceutical compositions.

Method used

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  • Pharmaceutical composition containing (3S, 2í»S)-3-(2í»-hydroxy-2í»-cyclopentyl-2í»-phenylethoxy) quinuclidine hydrochloride and uses thereof
  • Pharmaceutical composition containing (3S, 2í»S)-3-(2í»-hydroxy-2í»-cyclopentyl-2í»-phenylethoxy) quinuclidine hydrochloride and uses thereof
  • Pharmaceutical composition containing (3S, 2í»S)-3-(2í»-hydroxy-2í»-cyclopentyl-2í»-phenylethoxy) quinuclidine hydrochloride and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] An injection preparation containing (3S, 2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidin hydrochloride, which is characterized by composition and The weight ratio is:

[0054] Recipe (1)

[0055] (3S,2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidinine hydrochloride: 0.1g

[0056] Purified water: 1L

[0057] Hydrochloric acid (3mol / L): 10ml

[0058] Prepared into 1000, the unit concentration is 0.1mg / ml.

[0059] Formula (2)

[0060] (3S, 2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidinone hydrochloride: 1g

[0061] Purified water: 1L

[0062]Hydrochloric acid (3mol / L): 10ml

[0063] Prepared into 1000, the unit concentration is 1mg / ml.

[0064] Formula (3)

[0065] (3S, 2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidinone hydrochloride: 10g

[0066] Purified water: 1L

[0067] Hydrochloric acid (3mol / L): 10ml

[0068] Prepared into 1000 bottles with a unit concentration of 10mg / ml.

[0069] It is used to treat chronic obst...

Embodiment 2

[0071] A tablet containing (3S, 2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidinine hydrochloride, which is characterized by composition and The weight ratio is:

[0072] Recipe (four)

[0073] (3S,2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidinine hydrochloride: 0.1g

[0074] Lactose: 68g

[0075] Sodium carboxymethyl starch: 10g

[0076] Magnesium stearate: 0.35g

[0077] Prepare 1000 tablets with a unit content of 0.1 mg / tablet, orally, 1 tablet each time, once a day.

[0078] Formula (5)

[0079] (3S, 2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidinone hydrochloride: 1g

[0080] Lactose: 68g

[0081] Sodium carboxymethyl starch: 10g

[0082] Magnesium stearate: 0.35g

[0083] Prepared into 1000 tablets, with a unit content of 1 mg / tablet, orally, 1 tablet each time, once a day.

[0084] Recipe (6)

[0085] (3S,2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidinine hydrochloride: 0.1g

[0086] Lactose: 520g

[0087] Sodium carbo...

Embodiment 3

[0098] An aerosol or spray containing (3S, 2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidin hydrochloride, its characteristics The composition and weight ratio are:

[0099] Recipe (8)

[0100] (3S, 2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidinone hydrochloride: 10g

[0101] Anhydrous ethanol: 1000ml

[0102] HFC-134a: 11.2kg

[0103] Prepare 1000 bottles with a unit concentration of 10mg / bottle.

[0104] It is used to treat chronic obstructive pulmonary disease and various shock diseases.

[0105] Recipe (9)

[0106] (3S, 2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidinone hydrochloride: 10g

[0107] Purified water: 1000ml

[0108] Prepare 1000 bottles with a unit concentration of 10mg / bottle.

[0109] It is used to treat chronic obstructive pulmonary disease and various shock diseases.

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Abstract

The invention discloses medical composition containing active component of (3S, 2' S)-3-(2'-hydroxyl-2'-cyclopentyl-2'-phenylethoxy) quinine quinuclidine chloride and application of the medical composition in preparing drugs for treating chronic obstructive lung disease, incontinentia urinae, diversified shock diseases and preparing adjuvant drugs used before anaesthesia. The active component of the medical composition of the invention has high optical purity, strong stereoselectivity in vivo process, definite curative effects and high pertinency to the disease, thus effectively avoiding generation of toxic and side effects.

Description

Technical field [0001] The present invention relates to a pharmaceutical composition. Specifically, the present invention relates to containing (3S, 2'S)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidin The pharmaceutical composition of the hydrochloride salt, and the application of the composition in the preparation of drugs for the treatment of chronic obstructive pulmonary disease, urinary incontinence disease, shock disease and pre-anaesthesia auxiliary medication. Background technique [0002] The synthesis and research of chiral drugs has become the focus and hot spot in the field of pharmaceutical research in the 21st century. Chiral drugs have been known for more than 150 years, and clinical research has only begun in recent decades. At present, an important trend in the pharmaceutical industry is to focus on the use of a single optical isomer with high optical purity as a specific drug. In the future, most chiral innovative drugs will focus on a single enantiomer...

Claims

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Application Information

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IPC IPC(8): A61K31/439A61K47/36A61K47/38A61K47/40A61P11/00A61P9/02A61P13/00A61P43/00
Inventor 朱登军
Owner CHENGDU LIST PHARMA
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