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Application of non-oral berberine

A berberine, non-oral technology, applied in the field of non-oral berberine or its salts, can solve the problems of poor gastrointestinal absorption, buried pharmacological activity, low bioavailability and the like, and achieves less adverse reactions, good effects, The effect of high safety

Pending Publication Date: 2021-07-27
厦门市健康医疗大数据中心
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Berberine is usually administered orally, but its gastrointestinal absorption effect is poor, and its bioavailability is extremely low, resulting in many very good pharmacological activities of berberine being buried. It has been used clinically as an oral treatment for enteritis, dysentery, etc. Drug use in the treatment of gastrointestinal infectious diseases
There are few reports on the use of berberine administered by non-oral route

Method used

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  • Application of non-oral berberine
  • Application of non-oral berberine
  • Application of non-oral berberine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Example 1 Protective effect of berberine atomized inhalation on lung injury in mouse acute pneumonia model

[0039] C57B / 6J mice (Jiangsu Jicui Experimental Animal Co., Ltd.), male, weighing 30±2g, 32 were randomly divided into normal control group (Normal control, NC), acute pneumonia model group (Model control, MC), berberine Nebulized low-dose inhalation group (Berberine inhaled low dose, BIL) and Berberine inhaled high-dose group (Berberine inhaled high dose, BIH), 8 rats in each group.

[0040] The mouse model of acute pneumonia was replicated as follows: the mice were injected intraperitoneally with 45 mg / kg of pentobarbital sodium according to body weight, and after the righting reflex disappeared, the mouth was gently opened, the tongue was pulled out, and 50 μL of LPS solution was sucked with a pipette ( Prepared according to body weight, the administration dose is 5 mg / kg), injected into the oral cavity through the posterior pharyngeal wall, quickly pinched th...

Embodiment 2

[0046] Example 2 Protective Effects of Subcutaneous Injection of Berberine on Lung Injury in Mouse Acute Pneumonia Model

[0047] C57B / 6J mice (Jiangsu Jicui Experimental Animal Co., Ltd.), male, weighing 30±2g, 32 were randomly divided into normal control group (Normal control, NC), acute pneumonia model group (Model control, MC), berberine Subcutaneous injection low dose group (1mg / kg, Berberine low dose, BL) and berberine subcutaneous injection high dose group (2mg / kg, Berberine high dose, BH), 8 rats in each group.

[0048] The mouse acute pneumonia model replication method is the same as in Example 1.

[0049] The experimental scheme is as follows: After the modeling was completed, the BL group was subcutaneously injected with 1 mg / kg berberine hydrochloride via a 3 mm micro-syringe, and the BH group was given 2 mg / kg berberine hydrochloride via a 3 mm micro-injection subcutaneous injection. After 12 hours of modeling, the body weight of mice in each group was recorded, ...

Embodiment 3

[0054] Example 3 Protective effect of berberine subcutaneous injection and aerosol inhalation on ACE2 receptor-associated pneumonia and lung injury

[0055] The method for replicating the acute pneumonia model in mice, the regimen of administration in groups, and the detection methods for related indicators of sample collection are the same as those in Examples 1 and 2.

[0056] In this example, Western blotting was used to detect the expression of ACE2 protein in lung tissue of mice in each group by subcutaneous injection and aerosol inhalation of berberine. The results of the study showed that subcutaneous injection and aerosol inhalation of berberine could significantly inhibit the expression of ACE2 receptor in lung tissue of acute pneumonia (see Figure 4 ). It is suggested that the non-oral route of subcutaneous injection and aerosol inhalation of berberine may produce effects through acting on ACE2 protein.

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Abstract

The invention discloses an application of non-oral berberine. The berberine is used as a main effective component of heat-clearing and detoxifying traditional Chinese medicines such as coptis chinensis and golden cypress, is clinically and widely used for treating gastrointestinal bacterial infection, has main indications of enteritis, dysentery and the like, and is relatively high in safety, few in adverse reaction, low in price and high in acceptability. The invention finds that berberine has a good curative effect on mouse acute pneumonia and lung injury caused by the mouse acute pneumonia in a non-oral administration way, which prompts that berberine is expected to be used for preparing non-oral medicines for preventing and treating lung injury and pneumonia, and can also be used for preparing potential medicines for upper respiratory infection and lung injury caused by the upper respiratory infection. The application is expected to increase the indications of berberine and expand the clinical application range of berberine, has potential application prospects in the fields of traditional Chinese medicine modernization, health, medical treatment and the like, and generates certain social benefits and economic benefits.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to the use of berberine, in particular to the use of non-oral berberine or a salt thereof. Background technique [0002] Berberine is an antibacterial active ingredient extracted from Chinese medicine Coptis chinensis and Cortex Phellodendron by Japanese and German scholars in the early 20th century, and its trade name is berberine. Berberine is an isoquinoline alkaloid with the molecular formula C 20 h 18 NO 4 , molecular weight 336.3, yellow solid, soluble in water, low solubility in organic solvents. The commonly used clinical form is the salt formed by berberine and acid, such as berberine hydrochloride and berberine sulfate. Berberine is a medicinal ingredient derived from plants. It has been used clinically as an antibacterial drug for many years. It has definite curative effect and high safety. Fungi, molds, viruses, protozoa, and nematodes have inhibitory and killing effects, an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4375A61K9/00A61K9/02A61K9/06A61K9/72A61P11/00A61P31/04A61P31/12
CPCA61K31/4375A61K9/0019A61K9/0014A61P11/00A61P31/04A61P31/12A61K9/0073A61K9/02A61K9/0031A61K9/0034A61K9/06A61K9/7007A61K9/0021A61K9/006Y02A50/30
Inventor 许光辉万慧琪罗友华黄亦琦
Owner 厦门市健康医疗大数据中心
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