An active drug for pediatric asthma

A technology for children with asthma and drugs, which is applied in the field of acid addition salt pharmaceutical compositions, and can solve problems such as non-synergistic interactions

Active Publication Date: 2022-05-20
青岛山大齐鲁医院(山东大学齐鲁医院(青岛))
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the prior art, there is no report on the above-mentioned combination for the treatment of respiratory diseases, and there is no relevant report on the synergistic interaction

Method used

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  • An active drug for pediatric asthma
  • An active drug for pediatric asthma
  • An active drug for pediatric asthma

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Safety Experiment: Cardiovascular Interaction of Compound A and Compound B

[0027] The post-administration peak changes in blood pressure and heart rate of male rats were determined after compound A and compound B were administered alone or in combination. The study design adopts a random blind method, selects 12 healthy rats with an average body weight of 220g, and divides them into 3 groups, and each group of four rats in the 3 groups is given compound A (4 μg / kg) and compound B (8 μg / kg) respectively. , Compound A (4 μg / kg) + Compound B (8 μg / kg). The primary pharmacokinetic variables measured were systolic blood pressure, diastolic blood pressure, and heart rate using calculated mean blood pressure. No major interactions between the drugs were found through the tests.

Embodiment 2

[0029] Synergistic Effect of Combination Administration of Compound A and Compound B on Reducing Airway Obstruction

[0030] The experiment induced airway obstruction by intravenous administration of bombesin (4 μg / ml) to guinea pigs. Different doses of compound A (1 μg / kg, 2 μg / kg, 4 μg / kg, 8 μg / kg) were administered intravenously alone, and compound A (1 μg / kg, 2 μg / kg, 4 μg / kg, 8 μg / kg) were administered separately Combined with compound B (8 μg / kg), the effect of compound B on reducing airway obstruction of compound A was investigated.

[0031]

[0032] This result provides further evidence that when Compound B can significantly enhance the bronchodilation activity of Compound A.

Embodiment 3

[0034] Synergistic effect of compounds A+B on tracheal rings

[0035] Methods: 200-300g male Wistar rats were sacrificed, the neck was dissected, the trachea was excised 1mm above the tracheal bifurcation and 1mm below the thyroid cartilage, and a 3mm thick trachea was cut in Krebs-Henseleit solution ventilated with 95% oxygen-5% carbon dioxide at room temperature. The rings are divided into 6 groups. Wash twice with Krebs-Henseleit solution aerated with 95% oxygen-5% carbon dioxide, pH 7.0±0.5, apply a 1 g load to each ring, and let stand for 60 minutes.

[0036] Three groups were selected, and 150 μmol / L acetylcholine was added to stimulate the trachea. When the trachea fully contracted, the elution returned to the baseline, and the experiment began after the trachea rested for 30 minutes. 150 μmol / L acetylcholine was stimulated again, and then three groups were added compound A (4 mg), compound B (8 mg) and compound A (4 mg) + compound B (8 mg) dissolved in DMSO respective...

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Abstract

The present invention relates to a compound containing 5-[3-(3-hydroxyphenoxy)azetidine-1-yl]-5-methyl-2,2-diphenylhexanamide or its pharmaceutically acceptable The acid addition salt of and 2-amino-2-[2-(4-octylphenyl) ethyl] propane-1,3-diol or its pharmaceutically acceptable acid addition salt pharmaceutical composition and its Use in the prevention or treatment of asthma in children.

Description

technical field [0001] The present invention relates to a compound containing 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide or its pharmaceutically acceptable Acid addition salt of and 2-amino-2-[2-(4-octylphenyl) ethyl] propane-1,3-diol or its pharmaceutically acceptable acid addition salt pharmaceutical composition and its Use in the prevention or treatment of asthma in children. Background technique [0002] Children's asthma is called bronchial asthma, referred to as asthma, is the most common chronic respiratory disease in childhood. It is a chronic inflammatory disease of the airway in which a variety of cells and cell components participate. This chronic inflammation leads to increased airway responsiveness, usually with extensive and variable reversible airflow limitation, and causes recurrent wheezing, Symptoms such as shortness of breath, chest tightness or coughing, the morbidity and mortality of children with asthma are increasing year b...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/397A61K31/137A61P11/06A61P11/00
CPCA61K31/397A61K31/137A61P11/06A61P11/00A61K2300/00
Inventor 刘艳丽
Owner 青岛山大齐鲁医院(山东大学齐鲁医院(青岛))
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