阅读说明：本技术 格列苯脲在制备抗炎药物中的应用 (Application of glibenclamide in preparing anti-inflammatory medicine ) 是由 叶少剑 罗艳丽 王文立 谢怡 张慧娟 韦春梅 于 2019-12-24 设计创作，主要内容包括：本发明公开了格列苯脲在制备抗炎药物中的应用；本发明人发现了格列苯脲的新用途,能够改善毛细血管质量,降低其通透性,预防性减轻致炎因素二甲苯导致的炎症反应程度；优选地,所述格列苯脲给药剂量为40～60mg/kg(格列苯脲的用量与小鼠体重的比值)。最为优选地,所述格列苯脲给药剂量为50mg/kg。(The invention discloses an application of glibenclamide in preparing anti-inflammatory drugs; the inventor finds the new application of the glibenclamide, can improve the quality of capillary vessels, reduce the permeability of the capillary vessels, and preventively reduce the inflammatory reaction degree caused by an inflammation factor xylene; preferably, the dosage of the glyburide is 40-60 mg/kg (the ratio of the dosage of the glyburide to the body weight of the mouse). Most preferably, the glyburide is administered at a dose of 50 mg/kg.)

1. Application of glibenclamide in preparing anti-inflammatory medicine is provided.

2. The use of claim 1, wherein the anti-inflammatory agent is one that is caused by increased capillary permeability due to p-xylene.

3. The use of claim 1, wherein said administration comprises one of gavage, oral, intravenous injection.

4. The use of claim 1, wherein the capillaries comprise mouse capillaries.

5. The use of claim 1, wherein the glyburide is administered at a dose of 40 to 60 mg/kg.

6. The use of claim 1, wherein the glyburide is administered at a dose of 50 mg/kg.

7. The use of claim 1, wherein the medicament for inhibiting capillary permeability comprises glyburide, or a pharmaceutically acceptable salt, hydrate, or combination thereof, and an excipient.

8. The use of claim 1, wherein: the medicine for inhibiting the capillary permeability is prepared into any one or a composition of more than two of tablets, capsules, oral liquid preparations, sprays and injection.

Technical Field

The invention belongs to the technical field of medicines, and particularly relates to application of glibenclamide in preparation of anti-inflammatory medicines.

Background

Many diseases result in increased capillary permeability, are prone to oozing and swelling, and may result in capillary rupture or bleeding. The increased exudation caused by the increased permeability of capillary vessels leads to the manifestation of edema, pain, itch and the like at the diseased region, which is the common symptom of various inflammatory reactions. At present, the inflammation symptoms are mainly controlled clinically by steroidal (glucocorticoid) or non-steroidal (aspirin and the like) anti-inflammatory drugs.

Glibenclamide is an oral hypoglycemic drug, and is mainly used for treating type II diabetes. Glibenclamide inhibits hepatic glycogenolysis and gluconeogenesis and decreases hepatic production and output glucose by increasing portal insulin levels or acting directly on the liver; the oral administration has quick absorption, the protein combination rate is high and is 95 percent, the blood concentration reaches the peak value 2 to 5 hours after the oral administration, and the continuous action lasts for 24 hours. T1/2 was 10 hours. Metabolized in the liver, being excreted by the liver and kidneys in about 50% each. At present, the relation between glibenclamide and inflammation caused by capillary permeability is not reported at home and abroad.

Disclosure of Invention

The invention aims to provide application of glibenclamide in preparing anti-inflammatory drugs. The inventor finds a new application of the glibenclamide, can improve the quality of capillary vessels, reduce the permeability of the capillary vessels, and preventively reduce the inflammatory reaction degree caused by an inflammation factor xylene.

Experiments prove that the glibenclamide can preventively reduce the inflammatory reaction degree caused by the inflammation factor xylene; and preferably, the dosage of the glyburide is 40-60 mg/kg (the ratio of the dosage of the glyburide to the body weight of the mouse). Most preferably, the glyburide is administered at a dose of 50 mg/kg.

The invention has the following beneficial effects:

the invention discovers that glibenclamide has obvious effects of inhibiting inflammation caused by capillary permeability and resisting inflammation, and the detailed description is provided in the embodiment.

Detailed Description

1. The experimental method comprises the following steps:

(1) the glyburide administration stage: healthy adult mice of Kunming species, male and female were divided into experimental group and control group randomly, 9 mice in each group. The test group 1 (glibenclamide 50mg/kg), the test group 2 (glibenclamide 40mg/kg) and the test group 3 (glibenclamide 60mg/kg) were each subjected to a gastric lavage pretreatment for 30 minutes. The control group was performed simultaneously with equal volumes of distilled water for intragastric gavage.

(2) In the inflammation-causing stage: the right auricle of the mouse was coated with xylene. After 1 hour, the cervical vertebrae were cut off, the auricles on both sides were cut off, the auricles on both ears were punched out with a 9mm punch, and the weight difference between the right auricle and the left auricle was used as the edema value.

(3) The effect of preventing inflammatory response is shown in table 1:

TABLE 1

Group of	Left ear weight (mg)	Weight of the right ear (mg)	Edema value
				Control group	19.1±1.73	37.2±7.41	18.1±8.32
Experimental group 1	19.1±2.39	26.1±5.49	6.9±4.10
				Experimental group 2	19.1±2.06	26.8±5.49	7.7±4.14
Experimental group 3	19.1±2.21	27.2±5.04	8.1±4.02

As can be seen from Table 1, the weight of the right ear of the control group significantly exceeded that of the left ear (37.2. + -. 7.41vs 19.1. + -. 1.73, p <0.001), and the difference was statistically significant, indicating that the inflammation model was successful;

the weight values of the right ears of the experimental groups 1-3 are 26.1 +/-5.49, the weight values of the left ears are 19.1 +/-2.39, compared with the control group, the weights of the left ears of the two groups are similar, and the weight of the right ear of the experimental group is obviously smaller than that of the right ear of the model group (p < 0.005);

the results show that the edema value of the experimental group is obviously lower than that of the control group, the difference has obvious significance, and the glibenclamide has good preventive inhibition effect on the obvious anti-inflammatory effect caused by the increase of the capillary permeability caused by the dimethylbenzene. And the dose of the glibenclamide is 40-60 mg/kg (the ratio of the dose of the glibenclamide to the body weight of the mouse). Most preferably, the glyburide is administered at a dose of 50 mg/kg.

The invention is not to be considered as limited to the particular embodiments shown, but is to be accorded the widest scope consistent with the principles and novel features disclosed herein.