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Compound and pharmaceutical composition for treating nasal oversecreation and chronic obstructive pulmonary disease

A composition and drug technology, applied in the field of pharmaceutical compounds, can solve the problems of short half-life, etc., and achieve the effect of long half-life, long glandular secretion inhibition function, and no toxic and side effects

Active Publication Date: 2010-10-06
YINGU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, nasal sprays and aerosols of ipropyl atropine are currently the first-choice drugs for the treatment of various types of nasal hypersecretion and chronic obstructive pulmonary disease, but the short half-life (only 1.6h) is the shortcoming of this compound

Method used

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  • Compound and pharmaceutical composition for treating nasal oversecreation and chronic obstructive pulmonary disease
  • Compound and pharmaceutical composition for treating nasal oversecreation and chronic obstructive pulmonary disease
  • Compound and pharmaceutical composition for treating nasal oversecreation and chronic obstructive pulmonary disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] 1. Preparation of intermediate product: 9.3 g of 1-phenyl-1-cyclopentyl oxirane was dissolved in DMSO. Take 6.35g of quinine alcohol, dissolve it in 64ml of DMSO, add 2.5g of sodium hydride, stir for 1 hour, cool to room temperature, add dropwise phenylcyclopentyl oxirane-DMSO solution, and stir for another 3 hours. Cool to room temperature, extract with ether, extract the ether layer with 6N HCl, alkalinize the acidic aqueous layer with 20% NaOH, extract with ether, and dry over anhydrous sodium sulfate. The solvent was evaporated, and the product was purified by distillation to obtain the intermediate product 3-quinuclidinyl-(2'-phenyl-2'-cyclopentyl-2'-hydroxy)ethyl ether (yield 54%);

[0053] 2. Preparation of compound α: Dissolve the intermediate product in absolute ethanol, pass through excess methyl bromide, and react overnight. After distilling off the solvent, recrystallize with acetone to obtain a white solid which is compound α (yield 75%).

[0054] 1 HNMR...

Embodiment 2

[0067] 1. Unilateral nasal drops

[0068] The composition of nasal drops consists of the following elements

[0069] Compound V

12mg

Benzalkonium chloride

3mg

h 2 o

10ml

[0070] Under 100,000-level production conditions, the active ingredient (compound V) and bacteriostatic agent (benzalkonium chloride) were dissolved in H 2 In O, it is filled in a small brown bottle with a spindle-shaped cap, which can be used for nasal drops.

[0071] The unilateral nasal drop can dissolve 2.0-25mg of the compound V in every 10ml of water, and can be prepared into nasal drops with different concentrations;

[0072] Single nasal drops 2-3 drops (0.1ml-0.15ml) / nostril each time, about 20-300μg / nostril dosage.

[0073] 2. Compound nasal drops

[0074] Compound II

2.5mg

Fenoterol

10mg

Benzalkonium chloride

5mg

h 2 o

10ml

[0075] Under 100,000-level production conditions, active ingredien...

Embodiment 3

[0102] Beagle dogs were used in the experiment, and each 1 mg of compound α, I, II, III, IV, and V was given nasal spray for pharmacokinetic test, and the blood drug concentration was determined by GC-MS / SIM analysis method. Analyze the drug-time curve in blood and calculate the corresponding pharmacokinetic parameters. The results show that the absorption rates of the six compounds after nasal spray are 19.8±1.2%, 20.5±3.2%, 22.1±3.3%, and 20.7±4.3%. , 19.5±2.7%, 21.6±3.4%, 15min after administration, the given compound can be detected in all dog blood, 30min blood drug concentration reaches a higher level, 30-40min reaches a peak. After 2 hours, the blood drug concentration decreased slowly, and the blood drug concentration maintained a considerable concentration for at least 48 hours. The drug-time fitting curves of each compound in the blood after nasal spray administration all conform to the first-order absorption two-compartment model, and the basic kinetic parameter t ...

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Abstract

The invention discloses the drug of treating the nasal over-secretion and chronic obstructive emphysema, at the mean time, provides the drug compositions of treating the nasal over-secretion and chronic obstructive emphysema, which are aerosol, powder cloud agent, naristillae and spray. In the invention, the compositions, which are introduced quaternary ammonium group on the basis of penehyclidine hydrochloride, can't permeate membrane and enter into the circulatory system and central, so it can be used in treating the chronic obstructive emphysema. Besides, due to the low absorptivity in themucous membrane position, the said new compositions are extended the resistance time at local, so it can be used in treating the chronic obstructive emphysema and coryza.

Description

Technical field: [0001] The invention relates to a pharmaceutical compound, in particular to a novel pharmaceutical compound and pharmaceutical composition for treating nasal cavity hypersecretion and chronic obstructive pulmonary disease. Background technique: [0002] For nasal hypersecretion (commonly known as runny nose) and COPD, a variety of active ingredients are now used in the treatment, but the results are not satisfactory. For example, use vasoconstrictor aminoethanol or imidazolines, but you have to face strong dry mouth and rebound phenomenon. [0003] Alternatively, disodium glycinate (DSCG) or steroidal cortisones such as beclomethasone dipropionate are used, but they only relieve the symptoms of perennial allergic rhinitis-hay fever. What's more, long-term use of these preparations has to face some special toxic side effects such as fungal disease, bone mineral loss, blood sugar increase, and mucosal atrophy. [0004] Treatment of various types of nasal hyp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/08A61K31/439A61K9/12A61P11/00A61P11/02
CPCC07D453/02A61K9/008A61K9/0043A61K9/0075A61P11/00A61P11/02
Inventor 陈小平赵书强曹霞张洁清齐涛
Owner YINGU PHARMA
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