Sphaelactone dimethylamine lipidosome atomizing inhalant and application thereof

A dimethylamine ester and liposome technology, applied in the treatment of pulmonary fibrosis, in the field of laughing lactone-containing dimethylamine aerosol inhalation, can solve the problems of pulmonary fibrosis without specific drugs and difficult to cure, etc. The effect of prolonging the action time in vivo, improving the binding rate and changing the pharmacokinetic characteristics

Active Publication Date: 2016-07-06
NANKAI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Pulmonary fibrosis is difficult to heal once it occurs because it is caused by persistent lung damage
There is currently no specific drug for the treatment of pulmonary fibrosis

Method used

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  • Sphaelactone dimethylamine lipidosome atomizing inhalant and application thereof
  • Sphaelactone dimethylamine lipidosome atomizing inhalant and application thereof
  • Sphaelactone dimethylamine lipidosome atomizing inhalant and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Example 1 Preparation of PSMC

[0055] Experimental method and procedure: Dissolve egg yolk lecithin and cholesterol in ethanol at a ratio of 5:1, evaporate under reduced pressure at 50°C on a rotary evaporator, and evaporate the solvent to a uniform film. Dissolve the weighed ACT001 in PBS and preheat it to 60°C, add it to the spun membrane, hydrate the membrane, wash the membrane with a probe, and filter with a microporous membrane to obtain a PSMC ACT001 suspension.

Embodiment 2

[0056] Example 2 Establishment of mouse lung fibrosis model and ACT001 pharmacodynamic test

[0057] Experimental methods and steps:

[0058] 1. Establishment of mouse pulmonary fibrosis model: 25 mice were randomly divided into five groups, blank group, model group (pulmonary fibrosis model group), blank PSMC group (blank PSMC after modeling), ACT001-PBS Group (administer PBS solution after modeling), ACT001-PSMC group (administer PSMC after modeling), 5 animals in each group. In the blank group, 0.15 mL of saline solution was intragastrically administered once; in the other groups, 0.15 mL of bleomycin solution was administered to the lung.

[0059] 2. Administration and treatment of pulmonary fibrosis mice: In the second week after modeling, the mice were given drug treatment. The blank group and the model group were perfused with 0.1mL PBS each time (simulating clinical aerosol inhalation administration form) The blank PSMC group was perfused with 0.1 mL of blank PSMC solution ...

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Abstract

The invention innovatively provides sphaelactone dimethylamine lipidosome.The lipidosome uses a similar surface active substance as the carrier and includes medicine effective components, namely, sphaelactone dimethylamine and derivatives of sphaelactone dimethylamine.The application of the sphaelactone dimethylamine lipidosome in medicine for treating the pulmonary fibrosis is achieved.Compared with the prior art, the sphaelactone dimethylamine lipidosome atomizing inhalant with the PSMC as the carrier and the application of the inhalant in medicine for treating the pulmonary fibrosis have the advantages that through the phospholipid bilayer structure, the same as that of cytomembrane, of PSMC and the lubricating and protecting effects of phospholipids, the combining rate of medicine and alveolar cells is increased, the pharmacokinetics characteristics are changed, the medicine in-vivo acting time is prolonged, and the treatment effect of sphaelactone dimethylamine on the pulmonary fibrosis is remarkably improved.

Description

Technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular to the application of aerosol inhalation of mircolactone dimethylamine (ACT001) with pulmonary surfactant (PSMC) as a carrier in the treatment of pulmonary fibrosis. Background technique [0002] Nebulized inhalation is a common treatment for respiratory diseases, such as asthma, emphysema, bronchiectasis and chronic bronchitis. Mainly because: ①The absorption area of ​​the lungs is huge (about 140m 2 ), and the alveoli are closely connected to the systemic circulatory system; ②The epithelial barrier is thin, and the membrane permeability is high; ③The inhalation method is bioequivalent to arterial injection, and the biocompatibility is good; ④The first pass effect of the liver is avoided And the impact on kidney function. As a kind of inhalant, the aerosol inhaler is applied to lung diseases. It enters through the nose and can be used by anyone anytime and anywhere, e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K31/365A61K47/24A61K47/28A61P11/00
CPCA61K9/0043A61K9/127A61K31/365A61K47/24A61K47/28
Inventor 杨诚周红刚孙涛陈双刘艳荣刘慧娟孙波闫雪琴肖婷李咪咪荆学双秦源仲威龙凌红雷张春红
Owner NANKAI UNIV
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