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

A technology of phenylethoxy and quinuclidine, which can be used in drug combinations, inactive components of polymer compounds, cardiovascular system diseases, etc., can solve the problems of different enantiomeric activities, unreported, low activity, etc. , to achieve the effect of strong stereoselectivity, avoiding toxic and side effects, and high optical 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, 2'R)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy) quinuclidine hydrochloride and uses thereof
  • Pharmaceutical composition containing (3S, 2'R)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy) quinuclidine hydrochloride and uses thereof
  • Pharmaceutical composition containing (3S, 2'R)-3-(2'-hydroxy-2'-cyclopentyl-2'-phenylethoxy) quinuclidine hydrochloride and uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] An injection preparation containing (3S, 2'R)-3-(2'-hydroxyl 2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride, characterized in that the composition And the weight ratio is:

[0055] Recipe (1)

[0056] (3S,2'R)-3-(2'-Hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride: 0.1g

[0057] Purified water: 1L

[0058] Hydrochloric acid (3mol / L): 10ml

[0059] Prepared into 1000 tubes, unit concentration 0.1mg / ml.

[0060] Recipe (2)

[0061] (3S,2'R)-3-(2'-Hydroxy 2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride: 1g

[0062] Purified water: 1L

[0063] Hydrochloric acid (3mol / L): 10ml

[0064] Prepared into 1000 tubes, unit concentration 1mg / ml.

[0065] Recipe (3)

[0066] (3S,2'R)-3-(2'-Hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride: 10g

[0067] Purified water: 1L

[0068] Hydrochloric acid (3mol / L): 10ml

[0069] Prepare 1000 vials with a unit concentration of 10mg / ml.

[0070] It is used for the treatment of ch...

Embodiment 2

[0072] A tablet containing (3S, 2'R)-3-(2'-hydroxyl-2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride, characterized in that the composition The ingredients and weight ratio are:

[0073] Recipe (4)

[0074] (3S,2'R)-3-(2'-Hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride: 0.1g

[0075] Lactose: 68g

[0076] Sodium carboxymethyl starch: 10g

[0077] Magnesium stearate: 0.35g

[0078] Prepared into 1000 tablets, unit content 0.1mg / tablet, orally, 1 tablet each time, once a day.

[0079] Recipe (5)

[0080] (3S,2'R)-3-(2'-Hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride: 1g

[0081] Lactose: 68g

[0082] Sodium carboxymethyl starch: 10g

[0083] Magnesium stearate: 0.35g

[0084] Prepared into 1000 tablets, unit content 1mg / tablet, orally, 1 tablet each time, once a day.

[0085] Recipe (6)

[0086] (3S,2'R)-3-(2'-Hydroxy 2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride: 0.1g

[0087] Lactose: 520g

[0088] Sodium ca...

Embodiment 3

[0099] An aerosol and spray containing (3S, 2'R)-3-(2'-hydroxyl-2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride, It is characterized in that the composition and weight ratio are:

[0100] Recipe (eight)

[0101] (3S,2'R)-3-(2'-Hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride: 10g

[0102] Absolute ethanol: 1000ml

[0103] HFC-134a: 11.2kg

[0104] Prepare 1000 vials, unit concentration 10mg / bottle.

[0105] For the treatment of chronic obstructive pulmonary disease, various shock diseases.

[0106] Recipe (9)

[0107] (3S,2'R)-3-(2'-Hydroxy-2'-cyclopentyl-2'-phenylethoxy)quinuclidine hydrochloride: 10g

[0108] Purified water: 1000ml

[0109] Prepare 1000 vials, unit concentration 10mg / bottle.

[0110] For the treatment of chronic obstructive pulmonary disease, various shock diseases.

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Abstract

The invention discloses medical composition containing active component of (3S, 2'R)-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 (3S, 2'R)-3-(2'-hydroxyl-2'-cyclopentyl-2'-phenylethoxy)quinine A pharmaceutical composition of naphthenic hydrochloride, 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-anesthesia adjuvant medication. Background technique [0002] The synthesis and research of chiral drugs has become the focus and hotspot in the field of pharmaceutical research in the 21st century. Chiral drugs have been known for more than 150 years, but clinical research has only begun in recent decades. An important reform trend in the current pharmaceutical industry is to focus on using 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. [0003] Am...

Claims

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Application Information

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