阅读说明：本技术 用于减少运动损伤和促进运动损伤修复的组合物 (Composition for reducing athletic injuries and promoting repair of athletic injuries ) 是由 毕思远 解长福 朱志强 于 2020-08-04 设计创作，主要内容包括：本发明公开了一种用于减少运动损伤和促进运动损伤修复的组合物,其特征在于,所述组合物是由3-[5-(苯硫基)吡啶-3-基]-3-[4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基]丙腈三氟乙酸盐、冰片、聚乙烯醇、脱水山梨糖醇单油酸酯、甘油、吐温80、依地酸二钠、乙醇和纯化水制成的涂膜剂。本发明所述的组合物具有优异的减少运动损伤和促进其修复的功能。(The invention discloses a composition for reducing sports injury and promoting sports injury repair, which is characterized by being a film coating agent prepared from 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate, borneol, polyvinyl alcohol, sorbitan monooleate, glycerol, Tween 80, disodium edetate, ethanol and purified water. The composition of the present invention has excellent functions of reducing sports injury and promoting the repair thereof.)

1. A composition for reducing athletic injuries and promoting repair of athletic injuries, wherein the composition is a film coating agent prepared from 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate, borneol, polyvinyl alcohol, sorbitan monooleate, glycerol, Tween 80, disodium edetate, ethanol and purified water.

2. The composition as claimed in claim 1, wherein the weight ratio of 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate, borneol, polyvinyl alcohol, sorbitan monooleate, glycerol, Tween 80, disodium edetate and ethanol is 5-20:3-12:15-60:2.5-10:2.5-10:1-4:0.5-2: 200-.

3. The composition according to claim 2, wherein the weight ratio of 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate, borneol, polyvinyl alcohol, sorbitan monooleate, glycerol, tween 80, disodium edetate and ethanol is 10:6:30:5:5:2:1: 400.

4. The composition of claim 1, wherein the polyvinyl alcohol is a 1:3 weight ratio mixture of PVA05-88 and PVA 17-88.

5. Composition according to any one of claims 1 to 4, characterized in that the preparation process of the composition comprises the following steps:

1) grinding 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate and borneol into fine powder, adding a small amount of ethanol, and uniformly stirring;

2) mixing sorbitan monooleate, tween 80, disodium edetate, glycerol and the balance of ethanol, and stirring;

3) adding polyvinyl alcohol into 5-7 times of purified water for soaking and swelling, then placing the mixture on a water bath at 85-95 ℃ for heating and dissolving, sequentially adding the mixtures obtained in the step 1) and the step 2) while stirring, filtering the obtained mixed solution with a 80-mesh screen when the mixed solution is hot, and naturally cooling; and

4) adding purified water to a sufficient amount, and stirring to obtain the final product.

6. A process for preparing a composition according to any one of claims 1 to 5, characterized in that it comprises the following steps:

1) grinding 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate and borneol into fine powder, adding a small amount of ethanol, and uniformly stirring;

2) mixing sorbitan monooleate, tween 80, disodium edetate, glycerol and the balance of ethanol, and stirring;

3) adding polyvinyl alcohol into 5-7 times of purified water for soaking and swelling, then placing the mixture on a water bath at 85-95 ℃ for heating and dissolving, sequentially adding the mixtures obtained in the step 1) and the step 2) while stirring, filtering the obtained mixed solution with a 80-mesh screen when the mixed solution is hot, and naturally cooling; and

4) adding purified water to a sufficient amount, and stirring to obtain the final product.

Technical Field

The invention relates to the technical field of medicines, in particular to a composition for reducing sports injury and promoting the repair of sports injury.

Background

As the living standard and health consciousness of people are continuously improved, more and more people recognize the importance of exercise for maintaining physical health and actively participate in the exercise. However, due to the reasons of lack of preparation activities or insufficient preparation activities before exercise, insufficient training level, poor physical state, poor flexibility and flexibility, incorrect movements, lack of self-protection ability and the like, people often suffer from various injuries during or after exercise, such as bruise, sprain, contusion, arthralgia, achilles tendon tear and the like, and even severe injuries such as hemorrhage, dislocation, fracture and the like can occur.

Motor Injuries (Athletic injures) refer to the destruction of the anatomical structures of organs or tissues and the disturbance of physiological functions of the human body during and after exercise due to the stimulation of the body by mechanical and physical factors. Generally speaking, sports injuries are common as acute injuries, and the causes of improper treatment of acute injuries or early training can be converted into chronic injuries, thereby seriously affecting the quality of life of patients.

At present, the main nursing modes of sports injury comprise physical treatment such as cold compress, hot compress and the like, external disinfectant such as disinfectant alcohol, iodine tincture, mercurochrome or purple liquid medicine and the like, gauze covering and bandage bandaging, and drug treatment such as Yunnan white drug powder, safflower oil and the like. However, these conventional methods have some limitations because they have slow onset of action, insignificant recovery from sports injuries, and high irritation to wounds. Therefore, it is a problem to be solved by those skilled in the art to overcome the shortcomings of the existing exercise injury care methods and to provide a composition for reducing exercise injury and promoting the repair of exercise injury.

Disclosure of Invention

The technical problem to be solved by the invention is to overcome the defects of the prior art and provide a composition for reducing sports injury and promoting the repair of sports injury.

The technical scheme adopted by the invention is as follows: a composition for reducing exercise damage and promoting repair of exercise damage, which is a film coating agent made of 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate (abbreviated as "the compound of the present invention" in the examples section), borneol, polyvinyl alcohol, sorbitan monooleate, glycerol, tween 80, disodium edetate, ethanol and purified water. The composition has excellent functions of reducing sports injury and promoting the repair thereof.

The "film-forming agent (Paints)" refers to a liquid preparation for external use in which a drug is dissolved or dispersed in a solvent containing a film-forming material (e.g., polyvinyl alcohol) and applied to the affected part to form a thin film. When in use, the film coating agent is applied to the affected part, the organic solvent is volatilized rapidly, and a film is formed on the affected part to gradually release the contained medicine, thereby playing the therapeutic effect.

The polyvinyl alcohol is a high molecular material which is obtained by carrying out condensation reaction on vinyl acetate in a methanol solvent to generate polyvinyl acetate and finally carrying out alcoholysis reaction on the polyvinyl acetate and methanol, and is white or yellowish white powder. Polyvinyl alcohol has various specifications such as PVA05-88, PVA17-88 and the like. The average polymerization degree of PVA05-88 is 500-600 (molecular weight is 22000-26400), the water solubility is larger, the flexibility is slightly poor, the average polymerization degree of PVA17-88 is 1700-1800 (molecular weight is 74800-79200), the water solubility is smaller, and the flexibility is better. The two kinds of polyvinyl alcohol are used in a proper proportion, so that the advantages of the polyvinyl alcohol with two specifications can be combined, and the deficiency of the polyvinyl alcohol can be compensated.

In one aspect, the 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate, borneol, polyvinyl alcohol, sorbitan monooleate, glycerol, Tween 80, disodium edetate and ethanol are in a weight ratio of 5-20:3-12:15-60:2.5-10:2.5-10:1-4:0.5-2: 200-.

Preferably, the weight ratio of the 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate to borneol to polyvinyl alcohol to sorbitan monooleate to glycerol to Tween 80 to disodium edetate to ethanol is 10:6:30:5:5:2:1: 400.

Preferably, the polyvinyl alcohol is a 1:3 weight ratio mixture of PVA05-88 and PVA 17-88.

In one aspect, the method of making the composition comprises the steps of:

1) grinding 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate and borneol into fine powder, adding a small amount of ethanol (for example, 30-50% of ethanol based on the total weight of ethanol) and stirring uniformly;

2) mixing sorbitan monooleate, tween 80, disodium edetate, glycerol and the balance of ethanol, and stirring;

3) adding polyvinyl alcohol into 5-7 times of purified water for soaking and swelling, then placing the mixture on a water bath at 85-95 ℃ for heating and dissolving, sequentially adding the mixtures obtained in the step 1) and the step 2) while stirring, filtering the obtained mixed solution with a 80-mesh screen when the mixed solution is hot, and naturally cooling; and

4) adding purified water to a sufficient amount, and stirring to obtain the final product.

In one aspect, the present invention also provides a method for preparing the composition for reducing and promoting repair of sports injuries according to the present invention, characterized in that the method comprises the steps of:

1) grinding 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate and borneol into fine powder, adding a small amount of ethanol (for example, 30-50% of ethanol based on the total weight of ethanol) and stirring uniformly;

2) mixing sorbitan monooleate, tween 80, disodium edetate, glycerol and the balance of ethanol, and stirring;

3) adding polyvinyl alcohol into 5-7 times of purified water for soaking and swelling, then placing the mixture on a water bath at 85-95 ℃ for heating and dissolving, sequentially adding the mixtures obtained in the step 1) and the step 2) while stirring, filtering the obtained mixed solution with a 80-mesh screen when the mixed solution is hot, and naturally cooling; and

4) adding purified water to a sufficient amount, and stirring to obtain the final product.

One of the active ingredients in the composition for reducing sports injuries and promoting the repair of sports injuries according to the present invention is 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate, having the following structural formula:

3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate salt was originally disclosed as a bisnerve kinase inhibitor compound for use in the treatment of diseases associated with the activity of Janus kinases (Janus kinases), such as immune-related diseases, skin diseases, myeloproliferative diseases, cancer and other diseases in International patent publication No. WO2007/070514A1 (see example 488).

Borneol, also called borneol, is colorless transparent or white semitransparent flaky crisp crystal obtained by distilling branches and leaves of borneol camphor of Lauraceae or stems and leaves of blumea balsamifera of Compositae with water vapor and recrystallizing or obtained by performing a series of chemical processes on turpentine. The borneol has faint scent, pungent and cool taste, and has the functions of resisting bacteria, diminishing inflammation, improving eyesight and removing nebula.

The inventors surprisingly found that a film coating agent prepared by compounding 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2,3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate, which is not known to reduce sports injury and promote sports injury repair, with borneol and adding auxiliary materials such as polyvinyl alcohol, sorbitan monooleate, glycerol, Tween 80, disodium edetate, ethanol, purified water and the like has excellent functions of reducing sports injury and promoting repair.

In order to further clarify the spirit and gist of the present invention, preferred embodiments of the present invention and effects thereof will be described below with reference to specific embodiments. It should be understood, however, that the description of these preferred embodiments is intended to further illustrate the features and advantages of the present invention, and not to limit in any way the claims of the present invention.

Detailed Description