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Compound for treating acute lung injury as well as preparation method and application thereof

A compound and hydrophobic drug technology, applied in biochemical equipment and methods, medical preparations of non-active ingredients, non-active ingredients of polymer compounds, etc., can solve low drug loading, systemic side effects, and lung retention Short time and other issues, to achieve the effect of prolonging the residence time, improving targeted delivery, and protecting from degradation

Active Publication Date: 2021-07-27
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Micro / nanoparticle drug delivery strategies based on polymers, lipids and other materials have been widely studied for the targeted delivery of drugs to the lungs for the treatment of acute lung injury, but the existing drug delivery systems often have poor stability and drug loading The disadvantages of low dose, insufficient therapeutic effect, poor targeting, short residence time in the lungs, and high toxicity greatly limit its application.
[0004] At the same time, most of the existing therapeutic drugs for the treatment of acute lung injury are single traditional Chinese medicines, Chinese patent medicines, chemical drugs, biological drugs, and mesenchymal stem cells, etc., which are directly administered by oral administration, inhalation, injection, etc., but there is often a single Insufficient efficacy of the drug, systemic side effects and other problems caused by direct administration, the treatment effect is unsatisfactory

Method used

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  • Compound for treating acute lung injury as well as preparation method and application thereof
  • Compound for treating acute lung injury as well as preparation method and application thereof
  • Compound for treating acute lung injury as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Embodiment 1: Indomethacin drug crystal

[0078] (1) The preparation flow chart is as follows figure 1 As shown, the formulation optimization process of indomethacin pharmaceutical crystals is as follows:

[0079] Weigh different indomethacin (5mg, 10mg, 20mg, 30mg) raw materials and dissolve them in 0.2ml acetone as the organic phase; weigh 10mg of cationized β-lactoglobulin and dissolve them in 10ml distilled water as the water phase; Both the organic phase and the aqueous phase were pre-cooled at 4°C; under ice bath conditions, the organic phase was added dropwise to the aqueous phase under the stirring condition of 1500r / min, and the probe was ultrasonicated immediately, and the ultrasonic condition was ultrasonic The power is 360W, the ultrasonic mode is on for 3s and off for 5s, and the total ultrasonic time is 15min. The residual organic solvent acetone is removed by vacuum evaporation to obtain indomethacin drug crystals.

[0080] The particle size and potenti...

Embodiment 2

[0086] Example 2: Indomethacin drug crystal-superoxide dismutase complex

[0087] (1) The formulation optimization process of indomethacin drug crystal-superoxide dismutase complex is as follows:

[0088] The nanorods were selected as indomethacin drug crystals in Example 1 (2), and the antioxidant protein was selected as superoxide dismutase.

[0089] Weigh an appropriate amount of superoxide dismutase, dissolve it with distilled water and dilute it into solutions of different concentrations, so that the mass ratio of cationized β-lactoglobulin to superoxide dismutase is 1.0, 2.0, 4.0, 16.0, 32.0 and 64.0, The indomethacin drug crystals in Example 1 (2) were added dropwise to an equal volume under vortexing conditions, and the indomethacin drug crystals-superoxide dismutase complex was obtained after standing at room temperature for 30 min.

[0090] The particle size and potential results of the prepared indomethacin drug crystal-superoxide dismutase complex are as follows: ...

Embodiment 3

[0094] Example 3: Verification of the formation of indomethacin drug crystal-superoxide dismutase complex by native polyacrylamide gel electrophoresis

[0095] The indomethacin drug crystal-superoxide dismutase complexes with the mass ratios of cationized β-lactoglobulin and superoxide dismutase of 1.0, 2.0, 4.0, 16.0, 32.0 and 64.0 were prepared respectively. Dismutase was used as a control, and was analyzed by non-denaturing polyacrylamide gel electrophoresis. The specific method is as follows: respectively preparing a 3% acrylamide / diacrylamide stacking gel (0.25M Tris-HCl, pH 6.8) and a 12.7% acrylamide / diacrylamide separating gel (0.75M Tris-HCl, pH 8.8), The loading amount of superoxide dismutase in each well was 1 μg. After loading, electrophoresis was carried out at a current of 20 mA. When the band reached the separation gel, the current was increased to 30 mA for electrophoresis separation for 1 h. After electrophoresis, the gel was transferred to Coomassie brillian...

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Abstract

The invention belongs to the field of pharmaceutical preparations, and particularly relates to a compound for treating acute lung injury and a preparation method and application thereof. The drug crystal is prepared by wrapping an anti-inflammatory drug with cationized globulin, and the crystal is positively charged under physiological conditions. The antioxidant protein is acidic protein, is negatively charged under physiological conditions, and can be combined with the drug crystal through electrostatic interaction to form a compound. The prepared compound can be efficiently targeted to endothelial cells, small molecule drugs and protein drugs are simultaneously delivered into the vascular endothelial cells in a non-lysosome way, the effect of asynchronous slow-control drug release is achieved, and the drugs are specifically accumulated in the lung, so that the vascular endothelial cells are better repaired, and inflammation is relieved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a targeting molecule-drug crystal-antioxidant protein complex and its preparation method and application. Background technique [0002] Acute lung injury is an inflammatory disease of the lungs due to sepsis, pneumonia, or other injury that may subsequently develop into acute respiratory distress syndrome and even pulmonary fibrosis. As a life-threatening clinical syndrome, acute lung injury has no specific medicine at present, and the fatality rate is as high as 40%-50%. Clinically, it is mainly based on the treatment of the primary disease, combined with mechanical ventilation, anti-inflammatory and other comprehensive treatment methods. The drugs used in clinical treatment are mainly hormone drugs (such as glucocorticoids), aspirin, ulinastatin, etc. Most of these drugs are administered systemically, and the therapeutic effect is poor and will cause many...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K47/64A61K31/405A61K38/44A61K47/68A61P11/00A61P29/00A61P39/06
CPCA61K47/42A61K47/64A61K31/405A61P11/00A61P29/00A61P39/06A61K47/6835A61K38/446C12Y203/02013A61K2300/00Y02A50/30
Inventor 何伟杨艺
Owner CHINA PHARM UNIV
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