阅读说明：本技术 雷公藤内酯酮的应用 (Application of triptonide ) 是由 周泉生 曹志飞 于 2018-06-15 设计创作，主要内容包括：本发明涉及医药技术领域,公开了雷公藤内酯酮的应用。本发明发现中草药单体雷公藤内酯酮预防或者治疗给药后能显著地降低高脂饮食肥胖小鼠的血糖水平,此外,还能降低C57-ApoE敲除的高脂饮食肥胖模型小鼠的血糖含量。这表明雷公藤内酯酮对高血糖症具有预防和治疗作用。由于高血糖症是高血糖型糖尿病的主因,故其还可以应用到高血糖型糖尿病的相关药物制备中。(The invention relates to the technical field of medicines, and discloses application of triptonide. The invention discovers that Chinese herbal medicine monomer triptolide ketone can obviously reduce the blood sugar level of a high-fat diet obese mouse after being taken for prevention or treatment, and can also reduce the blood sugar content of a C57-ApoE knockout high-fat diet obese model mouse. This indicates that triptonide has preventive and therapeutic effects on hyperglycemia. Since hyperglycemia is the main cause of hyperglycemia-type diabetes, it can also be applied to the preparation of related medicines for hyperglycemia-type diabetes.)

1. Application of triptonide or pharmaceutically acceptable salt thereof in preparing medicines for preventing and/or treating hyperglycemia is provided.

2. The use according to claim 1, wherein the medicament is a capsule, a microcapsule, a tablet, a granule, a pill, a dispersion powder, an injection, a liposome or an oral liquid.

3. A medicine for treating hyperglycemia or hyperglycemia diabetes is characterized by comprising effective dose of triptonide or pharmaceutically acceptable salt thereof and pharmaceutically acceptable medicinal auxiliary materials.

4. The drug according to claim 3, wherein the drug adjuvant is one or more selected from the group consisting of solvents, propellants, solubilizers, solubilizing agents, emulsifiers, colorants, adhesives, disintegrants, fillers, lubricants, wetting agents, tonicity adjusting agents, stabilizers, glidants, flavoring agents, preservatives, suspending agents, coating materials, fragrances, anti-adhesives, integration agents, penetration enhancers, pH adjusting agents, buffers, plasticizers, surfactants, foaming agents, antifoaming agents, thickening agents, encapsulation agents, humectants, absorbents, diluents, flocculants, deflocculants, filter aids, and release retardants.

5. The medicament of claim 3, wherein the triptonide or the pharmaceutically acceptable salt thereof accounts for 0.05 wt% to 90 wt% of the total weight of the medicament.

6. The medicament of claim 3 or 5, wherein the triptonide or the pharmaceutically acceptable salt thereof accounts for 15 wt% to 60 wt% of the total weight of the medicament.

7. Application of triptonide or pharmaceutically acceptable salt thereof in preparing medicine for preventing and/or treating hyperglycemia diabetes is provided.

Technical Field

The invention relates to the technical field of medicines, in particular to application of triptonide.

Background

The sugar in the blood is called blood Glucose, and is mostly Glucose (Glucose). Most of the energy required for the cellular activities of tissues in the body comes from glucose, so blood glucose must be maintained at a certain level to maintain the needs of organs and tissues in the body. The normal fasting blood glucose concentration is 3.6-6.2 mmol/L. A fasting blood glucose concentration above 7.0mmol/L is called hyperglycemia, and a fasting blood glucose concentration below 3.6mmol/L is called hypoglycemia.

In critical illness, many factors can lead to hyperglycemia, which can cause fluid imbalance, reduce immune function, and increase infection. In vitro experiments show that hyperglycemia can cause abnormal leukocyte function, and the performance of these abnormalities can be improved along with blood sugar control. Hyperglycemia can also impair complement activity, and sugars are glycated by complement and compete with the complement for binding by microorganisms, inhibiting opsonization. In addition, studies have found that the mortality rate of patients with non-diabetic ischemic stroke is increased by 3 times when the blood glucose level exceeds 6.0-8.0mmol/L, and the disability rate of stroke patients is increased, suggesting that hyperglycemia may have a direct toxic effect on ischemic brain tissue. In addition, hyperglycemia-type diabetes has gradually attracted extensive attention in the social and medical community due to its increasing prevalence and higher disability and mortality rates. At present, great progress has been made in controlling blood glucose levels, but there is still an urgent need to develop new blood glucose level-controlling drugs against the associated adverse symptoms caused thereby.

Disclosure of Invention

In view of the above, the present invention aims to provide an application of Triptonide (TN) or a pharmaceutically acceptable salt thereof in the preparation of a medicament for preventing and/or treating hyperglycemia.

Tripterygium wilfordii lactone (TN) is a monomer substance extracted from the whole plant or peeled xylem of Tripterygium wilfordii hook F.H. Chen et S.F. Chen of Celastraceae, with purity up to 98%, and has the following structure:

tripterygium wilfordii lactone ketone has been reported to have the effects of male antifertility, leukemia resistance and malignant tumor resistance, but has not been reported at home and abroad in the aspect of hyperglycemia.

The invention researches the effect of triptolide in a high-fat diet obese mouse, and proves that the triptolide can obviously reduce the blood sugar level of the high-fat diet obese mouse after the administration for prevention or treatment, and can also reduce the blood sugar content of a C57-ApoE knockout high-fat diet obese model mouse. This indicates that triptonide has preventive and therapeutic effects on hyperglycemia. Since hyperglycemia is the main cause of hyperglycemia-type diabetes, triptonide or pharmaceutically acceptable salts thereof can be used for preventing and/or treating hyperglycemia-type diabetes and can be applied to the preparation of drugs for the disease.

The triptonide can be an artificial extract, such as an extract obtained by extracting the whole plant or peeled xylem part of tripterygium wilfordii; or artificial chemical synthesis substances, such as synthesis according to the existing chemical synthesis process.

The invention provides application of triptolide or pharmaceutically acceptable salts thereof in preparing medicaments for preventing and/or treating hyperglycemia or hyperglycemia diabetes, and the medicaments can be any suitable dosage form in the field of medicaments, such as capsules, microcapsules, tablets, granules, pills, dispersion powder, injections, liposomes or oral liquids.

According to related applications, the invention also provides a medicament for preventing and/or treating hyperglycemia or hyperglycemia diabetes, which comprises effective amount of triptonide or pharmaceutically acceptable salts thereof and pharmaceutically acceptable medicinal auxiliary materials; or consists of effective dose of triptolide or pharmaceutically acceptable salt thereof and pharmaceutically acceptable pharmaceutical excipients.

Preferably, the pharmaceutical excipients are selected from the pharmaceutical excipients generally used in the art according to the dosage form to be prepared, such as one or more selected from solvents, propellants, solubilizers, solubilizing agents, emulsifiers, colorants, binders, disintegrants, fillers, lubricants, wetting agents, tonicity adjusting agents, stabilizers, glidants, flavoring agents, preservatives, suspending agents, coating materials, fragrances, anti-adhesives, integration agents, permeation enhancers, pH adjusting agents, buffers, plasticizers, surfactants, foaming agents, antifoaming agents, thickening agents, encapsulation agents, humectants, absorbents, diluents, flocculants, deflocculants, filter aids, and release retardants.

Preferably, the triptonide or the pharmaceutically acceptable salt thereof accounts for 0.05-90 wt% of the total weight of the medicine; further, the triptonide or the pharmaceutically acceptable salt thereof accounts for 15 wt% -60 wt% of the total weight of the medicine.

The medicament of the present invention may be administered by any suitable means of: oral, rectal, nasal, topical, buccal, sublingual, parenteral such as subcutaneous, intravenous, intramuscular, intraperitoneal, intrathecal, intraventricular, intrasternal or intracranial injection or infusion, or via an explanted reservoir.

The dosage and method of administration of the drug of the present invention will depend on a variety of factors including the age, weight, sex, physical condition, nutritional status, the activity intensity of the compound, time of administration, metabolic rate, severity of the course of disease, and the subjective judgment of the treating physician. The dosage and method of use can be readily determined by one skilled in the art based on the factors described above.

According to the technical scheme, the invention finds that the Chinese herbal medicine monomer triptolide ketone can obviously reduce the blood sugar level of a high-fat diet obese mouse after being administered for prevention or treatment, and can also reduce the blood sugar content of a C57-ApoE knockout high-fat diet obese model mouse. This indicates that triptonide has preventive and therapeutic effects on hyperglycemia. Since hyperglycemia is the main cause of hyperglycemia-type diabetes, it can also be applied to the preparation of related medicines for hyperglycemia-type diabetes.

Drawings

FIG. 1 shows the results of statistical analysis of the effect of triptonide on blood glucose in mice with high-fat diet; wherein, the high fat diet group (HFD-TN), the normal diet group (ND), and the triptonide treatment group (HFD + TN);

FIG. 2 shows the results of statistical analysis of the effect of triptonide on blood glucose in mice with high-fat diet; wherein, the high fat diet group (HFD-TN) and the triptonide treatment group (HFD + TN) have 40, 95, 104 and 114 days for each node;

FIG. 3 shows the results of statistical analysis of the effect of triptonide on blood glucose in high-fat high-cholesterol model C57-ApoE knockout mice; among them, high-fat high-cholesterol group (HFD-TN), normal diet group (ND), and triptonide treatment group (HFD + TN).

Detailed Description

The invention discloses application of triptonide, and can be realized by appropriately improving process parameters by referring to the content. It is expressly intended that all such similar substitutes and modifications which would be obvious to one skilled in the art are deemed to be included in the invention. While the invention has been described in terms of embodiments, it will be apparent to those skilled in the art that the technology can be practiced and applied by modifying or appropriately combining the embodiments described herein without departing from the spirit and scope of the invention.

In the specific embodiment of the invention, the comparison test is involved, and the test environment, the raw materials and the like are consistent except for the difference of each test group.

The triptolide provided by the present invention is further described below.