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Compound inhalation preparation containing penicillin antibiotic and glucocorticoid

A technology of glucocorticoid and penicillin, applied in the field of inhalation preparations, can solve the problems of inconvenience, poor curative effect, easy decomposition and the like

Inactive Publication Date: 2014-12-17
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The main route of administration of penicillin antibiotics is oral or injection, and can also be used to treat diseases caused by lung bacterial infections through atomized inhalation, but this kind of atomized inhalation has obvious disadvantages. Time, while penicillin antibiotics are placed in water for a long time, which will increase the appearance of allergic substances penicilloic acid and penicillonic acid
The former can be polymerized into a penicillazole acid polymer, which can be combined with a polypeptide or protein to form a penicillazole acid protein, which is an immediate allergen and the main cause of allergic reactions; the latter can also be combined with cysteine ​​in the body. The acid forms a delayed allergen-penicramic acid protein, which is related to serum sickness-like reactions, which will significantly increase the possibility of allergies for users, and secondly, the sprayed mist has a certain pressure, which prevents the air around the mouth from entering the respiratory tract, making the The oxygen partial pressure of the inhaled gas is low. The third is that the lung function of patients with asthma and chronic obstructive pulmonary disease is poor, while the mist inhaled by ultrasonic atomization is low in temperature, which can easily lead to small airway spasm after inhalation, causing chest tightness and dyspnea in patients. Symptoms, the fourth is accurate control of drug particle size after atomization, a large amount of drugs are deposited on the face, oral mucosa and other parts, and less deposited on target parts such as bronchi and lungs, resulting in increased adverse reactions, less drug availability, and easy to decompose , the curative effect is poor, the fifth is inconvenient to use, most of the drugs have bad taste, and the patient's tolerance is poor, so in the daily treatment of antibacterial drugs, especially penicillin antibiotics, generally do not use aerosol inhalation
[0007] Literature reports (observation on the curative effect of azithromycin combined with glucocorticoids in the treatment of mycoplasma pneumonia, Hebei Medicine, July 2012, 2182) Azithromycin combined with glucocorticoids has achieved good clinical results, but the intravenous injection of the two drugs is in the form of intravenous infusion, which is more troublesome to use. The use process is longer, and the patient's compliance is poor. If azithromycin and glucocorticoids are injected in the same container, there will be stability problems. More importantly, the pharmacological effects of penicillins and azithromycin mentioned in the present invention The effects are completely different. Penicillins mainly exert antibacterial effects by inhibiting the formation of bacterial cell walls, while azithromycin is a macrolide antibiotic that exerts antibacterial effects by inhibiting the synthesis of bacterial RNA
[0008] In addition, the U.S. Food and Drug Administration issued a warning on March 12, 2013, saying that antibiotics widely used at present have the risk of causing heart disease. According to the instructions, azithromycin should not be used continuously for more than 6 days, and asthma is a chronic disease that requires long-term medication. , so azithromycin is not suitable for the treatment of asthma and chronic obstructive pneumonia

Method used

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  • Compound inhalation preparation containing penicillin antibiotic and glucocorticoid
  • Compound inhalation preparation containing penicillin antibiotic and glucocorticoid
  • Compound inhalation preparation containing penicillin antibiotic and glucocorticoid

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] According to the following table, the active ingredient is micronized with a flow energy mill. The particle size of D90 is shown in the table below. 8g of anhydrous lactose is micronized with a flow energy mill to an average particle size of 36μm. In 1000 capsules size 3, the active ingredients in each capsule are listed in the table below.

[0045]

Embodiment 2

[0047] According to the table below, the active ingredient is micronized with a flow energy mill. The particle size of D90 is shown in the table below. 8g of anhydrous lactose is micronized with a flow energy mill to an average particle size of 40μm. In 1000 capsules size 3, the active ingredients in each capsule are listed in the table below.

[0048]

Embodiment 3

[0050] According to the table below, the active ingredient is micronized with a flow energy mill. The particle size of D90 is shown in the table below. 8g of anhydrous lactose is micronized with a flow energy mill to an average particle size of 42μm. In 1000 capsules size 3, the active ingredients in each capsule are listed in the table below.

[0051]

[0052] The preparation of aerosol, the active ingredient used is the weight of 1000 dosage units, HFA-134a is 1,1,1,2-tetrafluoroethane, HFA-227 is 1,1,1,2,3,3, 3-Heptafluoropropane.

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Abstract

The invention relates to a compound inhalation preparation containing penicillin antibiotic and glucocorticoid and applications thereof. The preparation is capable of treating pulmonary bacterial infection with less dosage and has a certain curative effect on asthma and chronic obstructive pneumonia. The preparation is made into an dry powder inhalation dosage form, after a long period of preservation, the content of allergic matters namely penicilloic acid and penicillenic acid is not increased, so that the happening rate of allergy is largely reduced, when the preparation is used to treat asthma caused by non-microbial infection and chronic obstructive pneumonia.

Description

Technical field: [0001] The invention relates to a compound inhalation preparation containing penicillin antibiotics and glucocorticoid and its use. Background technique: [0002] Asthma and chronic obstructive pneumonia are airflow limitation diseases caused by respiratory inflammation. In recent years, with the influence of smoking, air pollution and allergens, the incidence rate has increased year by year. It has become an important public health problem affecting human health. At present, the treatment of asthma and chronic obstructive pneumonia is mainly based on inhalants, and compound drugs are mainly based on glucocorticoids and adrenergic β2-receptor agonists. At present, no antibacterial drugs, especially penicillin antibiotics, have been used in the treatment of asthma and chronic obstructive pneumonia caused by non-microbial infections. [0003] Glucocorticoids have anti-inflammatory, anti-allergic, anti-rheumatic, and immunosuppressive effects, and are widely ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K9/12A61K45/06A61P11/00A61P11/06A61P31/04A61K31/43A61K31/431A61K31/58A61K31/573
Inventor 孙亮赵琳
Owner TIANJIN JINYAO GRP
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