CN112773799B - Use of fexofenadine for preparing medicine for treating acute lung injury - Google Patents
Use of fexofenadine for preparing medicine for treating acute lung injury Download PDFInfo
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- CN112773799B CN112773799B CN202110114203.3A CN202110114203A CN112773799B CN 112773799 B CN112773799 B CN 112773799B CN 202110114203 A CN202110114203 A CN 202110114203A CN 112773799 B CN112773799 B CN 112773799B
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- fexofenadine
- lung injury
- acute lung
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- 206010069351 acute lung injury Diseases 0.000 title claims abstract description 23
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 title claims abstract description 21
- 229960003592 fexofenadine Drugs 0.000 title claims abstract description 21
- 239000003814 drug Substances 0.000 title claims abstract description 17
- 238000002360 preparation method Methods 0.000 claims description 3
- 230000000694 effects Effects 0.000 abstract description 3
- 241000699670 Mus sp. Species 0.000 description 9
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 8
- 229940079593 drug Drugs 0.000 description 7
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- 210000004072 lung Anatomy 0.000 description 6
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- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 4
- 210000001519 tissue Anatomy 0.000 description 4
- 239000003085 diluting agent Substances 0.000 description 3
- 238000010186 staining Methods 0.000 description 3
- 238000011740 C57BL/6 mouse Methods 0.000 description 2
- 206010021143 Hypoxia Diseases 0.000 description 2
- 102000004877 Insulin Human genes 0.000 description 2
- 108090001061 Insulin Proteins 0.000 description 2
- 229930040373 Paraformaldehyde Natural products 0.000 description 2
- QGMRQYFBGABWDR-UHFFFAOYSA-M Pentobarbital sodium Chemical compound [Na+].CCCC(C)C1(CC)C(=O)NC(=O)[N-]C1=O QGMRQYFBGABWDR-UHFFFAOYSA-M 0.000 description 2
- 229920002556 Polyethylene Glycol 300 Polymers 0.000 description 2
- 201000000028 adult respiratory distress syndrome Diseases 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 208000018875 hypoxemia Diseases 0.000 description 2
- 229940125396 insulin Drugs 0.000 description 2
- 235000015110 jellies Nutrition 0.000 description 2
- 239000008274 jelly Substances 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 229920002866 paraformaldehyde Polymers 0.000 description 2
- 230000008506 pathogenesis Effects 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 238000001356 surgical procedure Methods 0.000 description 2
- 210000003437 trachea Anatomy 0.000 description 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 description 1
- 208000035285 Allergic Seasonal Rhinitis Diseases 0.000 description 1
- RRJFVPUCXDGFJB-UHFFFAOYSA-N Fexofenadine hydrochloride Chemical compound Cl.C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RRJFVPUCXDGFJB-UHFFFAOYSA-N 0.000 description 1
- 241000699666 Mus <mouse, genus> Species 0.000 description 1
- 206010029538 Non-cardiogenic pulmonary oedema Diseases 0.000 description 1
- 206010033645 Pancreatitis Diseases 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 description 1
- 208000004756 Respiratory Insufficiency Diseases 0.000 description 1
- 206010038687 Respiratory distress Diseases 0.000 description 1
- 208000036284 Rhinitis seasonal Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 206010052428 Wound Diseases 0.000 description 1
- 208000027418 Wounds and injury Diseases 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 201000010105 allergic rhinitis Diseases 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 208000030949 chronic idiopathic urticaria Diseases 0.000 description 1
- 206010072757 chronic spontaneous urticaria Diseases 0.000 description 1
- 208000024376 chronic urticaria Diseases 0.000 description 1
- 238000007405 data analysis Methods 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 238000003306 harvesting Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000008595 infiltration Effects 0.000 description 1
- 238000001764 infiltration Methods 0.000 description 1
- 210000004969 inflammatory cell Anatomy 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 239000007928 intraperitoneal injection Substances 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 239000010977 jade Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 238000001543 one-way ANOVA Methods 0.000 description 1
- 206010033675 panniculitis Diseases 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 229960001412 pentobarbital Drugs 0.000 description 1
- 229960002275 pentobarbital sodium Drugs 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 201000004193 respiratory failure Diseases 0.000 description 1
- 230000029058 respiratory gaseous exchange Effects 0.000 description 1
- 208000017022 seasonal allergic rhinitis Diseases 0.000 description 1
- 230000035939 shock Effects 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000008354 sodium chloride injection Substances 0.000 description 1
- 210000004304 subcutaneous tissue Anatomy 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 230000002618 waking effect Effects 0.000 description 1
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Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Pulmonology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention discloses an application of fexofenadine in preparing a medicine for treating acute lung injury. The invention discovers that fexofenadine can effectively treat acute lung injury and has a prospect of being developed into a medicament for treating acute lung injury. The prior art does not disclose that fexofenadine has this activity, with outstanding substantive features and significant advances.
Description
Technical Field
The invention belongs to the field of medicines, and particularly relates to application of fexofenadine in preparation of a medicine for treating acute lung injury.
Background
Acute Lung Injury (ALI) is a life-threatening disease that may be associated with severe infection, shock, trauma, acute severe pancreatitis, or burns, characterized by non-cardiogenic pulmonary edema, respiratory distress, hypoxemia, and the like. Severe ALI can lead to acute respiratory distress syndrome manifested as refractory hypoxemia, decreased lung compliance, respiratory failure, and the like. In recent years, the definition, pathogenesis and diagnosis and treatment of ALI have been studied, but the pathogenesis is still not completely understood, and thus treatment is still difficult.
Fexofenadine is a drug used to alleviate the symptoms caused by seasonal allergic rhinitis and chronic idiopathic urticaria. At present, the application of fexofenadine in the treatment of acute lung injury is not seen.
Disclosure of Invention
The invention aims to provide the application of fexofenadine in preparing a medicament for treating acute lung injury.
The above purpose of the invention is realized by the following technical scheme:
use of fexofenadine for the preparation of a medicament for the treatment of acute lung injury.
A pharmaceutical preparation for treating acute lung injury contains fexofenadine as active ingredient.
Preferably, the pharmaceutical preparation further comprises pharmaceutically acceptable auxiliary materials, and is prepared into pharmaceutically acceptable dosage forms.
More preferably, the dosage form includes, but is not limited to, tablets, capsules, injections, oral liquids.
Has the advantages that:
the invention discovers that fexofenadine can effectively treat acute lung injury and has a prospect of being developed into a medicament for treating acute lung injury. The prior art does not disclose that fexofenadine has this activity, with outstanding substantive features and significant advances.
Drawings
FIG. 1 shows the results of BAFF cell counting;
FIG. 2 shows H & E staining results of lung tissues.
Detailed Description
The following detailed description of the present invention is provided in connection with the accompanying drawings and examples, but not intended to limit the scope of the invention.
First, experimental material
C57BL/6 mouse, 20-22g, Male, Beijing Huafukang Biotech GmbH
Lipopolysaccharide (LPS, L2880, Sigma-Aldrich)
Fexofenadine (FFD, HY-B0801A, MCE)
Plastic feeding tubes,20ga × 38mm (T-001, Jade research apparatus)
Cell counting plate (707-03021-00, RWD)
Cell counter (C100, RWD)
Disposable insulin needle (328421, Shurui)
PBS，1X(G4202，Servicebio)
1.5mL EP tube (BS-15-MF, Biosharp)
Disposable injector (10mL, BB000931, KDL)
Absorbable surgical suture (YY1116-2010, PGA)
Disposable venous transfusion needle (No. 7, HD)
Paraformaldehyde stationary liquid (neutral) (G1101, Servicebio)
Desk type high speed refrigerated centrifuge (5424R, Eppendorf)
Experimental full-nutrition jelly for big mouse (J10001 Ruidi biotechnology)
Dimethyl sulfoxide (DMSO, D2650, SIGMA)
Sodium chloride injection (L120031609, Sichuan Kelun pharmaceutical Co., Ltd.)
Polyethylene glycol (PEG300, P815612, MACKLIN)
Tween-80(1716ML100，Biofroxx)
Sodium pentobarbital (P3761, SIGMA)
Second, Experimental methods
1. Grouping, establishing an ALI model, and dosing and index determination:
20-22g Male C57BL/6 mice were labeled and grouped into Sham (Sham), model (ALI), fexofenadine Low concentration (FFD2, 2mg/kg), and fexofenadine high concentration (FFD10, 10mg/kg) groups of 12 mice each. The drug is administrated by gastric lavage, the volume of each time is 100 mu L, the drug is administrated once on the day before the model is built and the day of modeling, the drug is prepared by drug diluent (the diluent is prepared by 10% DMSO + 40% PEG300 + 5% Tween-80+ 45% saline), and the drug diluent is administrated by the model group. After mice were anesthetized with pentobarbital sodium (0.3%, 0.1mL/10g) by intraperitoneal injection, the laryngeal skin was incised with a scalpel, the subcutaneous tissue was bluntly separated with forceps, the trachea was exposed, 50 μ L LPS (1mg/kg) was injected with an insulin needle after the trachea was fixed with the forceps, the respiration was observed, the mice were returned to the cages, the wounds were sutured with sutures until the mice had a sign of waking with a warm light, and the mice were returned to the cages and given nutritional jelly. 24 hours post-surgery, mice were sacrificed and 6 mice per group were treated with 1.5mL sterile PBS in 10mL syringes and attached to intravenous needles to irrigate the lungs and recover alveolar lavage fluid (BAFF), centrifuged at 3000rmp for 5 min, and resuspended in 200. mu.L sterile PBS for cell counting. 24 hours post-surgery, mice were sacrificed and 6 mice per group were used for lung tissue harvest, paraformaldehyde fixation, paraffin embedding, sectioning (5 μ M), H & E staining.
2. Data processing
Data were plotted using Prism6 software and data analysis using SPSS software, and differences between groups and pairwise comparisons were analyzed by one-way ANOVA and Bonferroni methods. P <0.05 is statistically significant, P <0.05, P <0.01, P <0.001, P < 0.0001.
Third, experimental results
Fig. 1 shows the results of BAFF cell counting, from which it can be seen that: fexofenadine was effective in reducing the number of cells in alveolar lavage fluid in the acute lung injury model induced by LPS, and was dose dependent.
Fig. 2 is the result of H & E staining of lung tissue, from which it can be seen that: fexofenadine reduced inflammatory cell infiltration in lung tissue in the LPS-induced acute lung injury model.
Therefore, the fexofenadine can effectively treat acute lung injury and has a prospect of being developed into a medicament for treating acute lung injury. The prior art does not disclose that fexofenadine has this activity, with outstanding substantive features and significant advances.
The above-described embodiments are intended to be illustrative of the nature of the invention, but those skilled in the art will recognize that the scope of the invention is not limited to the specific embodiments.
Claims (1)
1. Use of fexofenadine for the preparation of a medicament for the treatment of acute lung injury.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110114203.3A CN112773799B (en) | 2021-01-27 | 2021-01-27 | Use of fexofenadine for preparing medicine for treating acute lung injury |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202110114203.3A CN112773799B (en) | 2021-01-27 | 2021-01-27 | Use of fexofenadine for preparing medicine for treating acute lung injury |
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| Publication Number | Publication Date |
|---|---|
| CN112773799A CN112773799A (en) | 2021-05-11 |
| CN112773799B true CN112773799B (en) | 2022-02-11 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202110114203.3A Active CN112773799B (en) | 2021-01-27 | 2021-01-27 | Use of fexofenadine for preparing medicine for treating acute lung injury |
Country Status (1)
| Country | Link |
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| CN (1) | CN112773799B (en) |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101103980A (en) * | 2006-07-14 | 2008-01-16 | 海南盛科生命科学研究院 | Fexofenadine medicinal composition |
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- 2021-01-27 CN CN202110114203.3A patent/CN112773799B/en active Active
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