CN111728975A - Composition for reducing athletic injuries and promoting repair of athletic injuries - Google Patents
Composition for reducing athletic injuries and promoting repair of athletic injuries Download PDFInfo
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- CN111728975A CN111728975A CN202010772579.9A CN202010772579A CN111728975A CN 111728975 A CN111728975 A CN 111728975A CN 202010772579 A CN202010772579 A CN 202010772579A CN 111728975 A CN111728975 A CN 111728975A
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- ethanol
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- polyvinyl alcohol
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- borneol
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- 208000025978 Athletic injury Diseases 0.000 title claims abstract description 26
- 230000008439 repair process Effects 0.000 title claims abstract description 17
- 230000001737 promoting effect Effects 0.000 title claims abstract description 16
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 55
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 48
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 30
- 239000004372 Polyvinyl alcohol Substances 0.000 claims abstract description 29
- 229920002451 polyvinyl alcohol Polymers 0.000 claims abstract description 29
- 235000019422 polyvinyl alcohol Nutrition 0.000 claims abstract description 29
- DTGKSKDOIYIVQL-WEDXCCLWSA-N (+)-borneol Chemical compound C1C[C@@]2(C)[C@@H](O)C[C@@H]1C2(C)C DTGKSKDOIYIVQL-WEDXCCLWSA-N 0.000 claims abstract description 22
- REPVLJRCJUVQFA-UHFFFAOYSA-N (-)-isopinocampheol Natural products C1C(O)C(C)C2C(C)(C)C1C2 REPVLJRCJUVQFA-UHFFFAOYSA-N 0.000 claims abstract description 22
- CKDOCTFBFTVPSN-UHFFFAOYSA-N borneol Natural products C1CC2(C)C(C)CC1C2(C)C CKDOCTFBFTVPSN-UHFFFAOYSA-N 0.000 claims abstract description 22
- 229940116229 borneol Drugs 0.000 claims abstract description 22
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- 239000008213 purified water Substances 0.000 claims abstract description 20
- ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 claims abstract description 16
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims abstract description 16
- 235000011187 glycerol Nutrition 0.000 claims abstract description 16
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims abstract description 16
- 229920000053 polysorbate 80 Polymers 0.000 claims abstract description 16
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- 239000001593 sorbitan monooleate Substances 0.000 claims abstract description 16
- 229940035049 sorbitan monooleate Drugs 0.000 claims abstract description 16
- GNAYMQJAWJVZJT-UHFFFAOYSA-N 3-(5-phenylsulfanylpyridin-3-yl)-3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C1=C(C=2C=3C=CNC=3N=CN=2)C=NN1C(CC#N)C(C=1)=CN=CC=1SC1=CC=CC=C1 GNAYMQJAWJVZJT-UHFFFAOYSA-N 0.000 claims abstract description 15
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 13
- 239000007888 film coating Substances 0.000 claims abstract description 13
- 238000009501 film coating Methods 0.000 claims abstract description 13
- 229960005150 glycerol Drugs 0.000 claims abstract description 6
- 229940068984 polyvinyl alcohol Drugs 0.000 claims abstract description 6
- 238000003756 stirring Methods 0.000 claims description 28
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- 239000007788 liquid Substances 0.000 description 2
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- 239000011118 polyvinyl acetate Substances 0.000 description 2
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- LOGFVTREOLYCPF-KXNHARMFSA-N (2s,3r)-2-[[(2r)-1-[(2s)-2,6-diaminohexanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoic acid Chemical compound C[C@@H](O)[C@@H](C(O)=O)NC(=O)[C@H]1CCCN1C(=O)[C@@H](N)CCCCN LOGFVTREOLYCPF-KXNHARMFSA-N 0.000 description 1
- DSSYKIVIOFKYAU-XCBNKYQSSA-N (R)-camphor Chemical compound C1C[C@@]2(C)C(=O)C[C@@H]1C2(C)C DSSYKIVIOFKYAU-XCBNKYQSSA-N 0.000 description 1
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- XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 description 1
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- 210000001361 achilles tendon Anatomy 0.000 description 1
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- 238000006136 alcoholysis reaction Methods 0.000 description 1
- 210000003484 anatomy Anatomy 0.000 description 1
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- 238000001266 bandaging Methods 0.000 description 1
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- 235000013305 food Nutrition 0.000 description 1
- 230000004054 inflammatory process Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 229940043355 kinase inhibitor Drugs 0.000 description 1
- SQFDQLBYJKFDDO-UHFFFAOYSA-K merbromin Chemical compound [Na+].[Na+].C=12C=C(Br)C(=O)C=C2OC=2C([Hg]O)=C([O-])C(Br)=CC=2C=1C1=CC=CC=C1C([O-])=O SQFDQLBYJKFDDO-UHFFFAOYSA-K 0.000 description 1
- 229940008716 mercurochrome Drugs 0.000 description 1
- 230000000474 nursing effect Effects 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 239000003973 paint Substances 0.000 description 1
- 125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 description 1
- 230000035790 physiological processes and functions Effects 0.000 description 1
- 239000001739 pinus spp. Substances 0.000 description 1
- ZSSCVXMAHNMCPY-UHFFFAOYSA-N propanenitrile 2,2,2-trifluoroacetic acid Chemical compound CCC#N.OC(=O)C(F)(F)F ZSSCVXMAHNMCPY-UHFFFAOYSA-N 0.000 description 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 description 1
- 235000005713 safflower oil Nutrition 0.000 description 1
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7015—Drug-containing film-forming compositions, e.g. spray-on
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
Abstract
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.
Description
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
Example 1
Film coating agent 1
[ FORMULATION ]
Note: the polyvinyl alcohol is a mixture of PVA05-88 and PVA17-88 in a weight ratio of 1: 3.
[ PREPARATION METHOD ]
1) Grinding the compound and borneol into fine powder, adding 160g 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 180g of purified water, soaking and swelling, then placing the mixture on a water bath at 90 ℃ for heating and dissolving, adding the mixture obtained in the step 1) and the step 2) in turn under 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.
Example 2
Film coating agent 2
[ FORMULATION ]
Note: the polyvinyl alcohol is a mixture of PVA05-88 and PVA17-88 in a weight ratio of 1: 3.
[ PREPARATION METHOD ]
1) Grinding the compound and borneol into fine powder, adding 160g 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 180g of purified water, soaking and swelling, then placing the mixture on a water bath at 90 ℃ for heating and dissolving, adding the mixture obtained in the step 1) and the step 2) in turn under 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.
Example 3
Film coating agent 3
[ FORMULATION ]
Note: the polyvinyl alcohol is a mixture of PVA05-88 and PVA17-88 in a weight ratio of 1: 3.
[ PREPARATION METHOD ]
1) Grinding the compound and borneol into fine powder, adding 160g 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 180g of purified water, soaking and swelling, then placing the mixture on a water bath at 90 ℃ for heating and dissolving, adding the mixture obtained in the step 1) and the step 2) in turn under 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.
Comparative example 1
Film coatings were prepared in a similar manner to example 2, except that the compound ingredients of the present invention were omitted.
Comparative example 2
A film coating agent was prepared in a similar manner to example 2, except that the borneol component was omitted.
Examples of the experiments
The purpose of this experimental example was to examine whether the film coating agent prepared by the method of the present invention has excellent functions of reducing sports injuries and promoting the repair thereof.
1. Experimental methods
Wistar rats with a body weight of 280g +/-20 g and an age of about 10 weeks are adopted in the experiment. Animals were housed for two days at 23 ℃ room temperature, 50% relative humidity and 12 hours light/12 hours dark conditions for acclimatization. Animals are free to ingest clean food and drinking water.
On the day of the experiment, Wistar rats with no statistical significance in body weight difference were randomly divided into 4 groups, i.e., a blank group, example 2 group, comparative example 1 group and comparative example 2 group, each of which was 8 rats. All rats were subjected to a treadmill experiment (ZH-PT type animal experiment treadmill, purchased from Anhui Zhenghua biological instruments, Inc.) in which the inclination angle of the treadmill was set at-15 degrees and the speed was set at 20 m/min. Each rat was trained daily for 1 hour for 8 consecutive weeks. After the experiment, the test article was applied to the four limbs of the rat 1 time a day for 3 consecutive days, wherein purified water was applied to the blank group, and the coating agents shown were administered to the remaining groups. 24 hours after the last administration, the rats were decapitated and fresh blood was taken and the serum creatine kinase and interleukin 1. beta. content in synovial fluid were measured.
2. Results of the experiment
The results of this experiment are seen in table 1 below.
TABLE 1 serum creatine kinase and Interleukin 1. beta. content in synovial fluid of rats of each experimental group
The above values are the average of the results for each experimental group. The statistical significance of the differences between the results of the groups was examined using Student's t test, and the results showed that the differences between the example 2 group and the blank, comparative example 1 and comparative example 2 groups were statistically significant (p-value <0.05) for both parameters.
5. Discussion of the related Art
The above results prove the unexpected findings of the inventors: the film coating agent prepared by matching 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 be used for reducing sports injury and promoting sports injury repair with borneol and prepared by adding auxiliary materials such as polyvinyl alcohol, sorbitan monooleate, glycerol, Tween 80, disodium edetate, ethanol, purified water and the like can remarkably reduce the content of serum creatine kinase and interleukin 1 beta in synovial fluid of rats after a period of high-intensity strenuous exercise, and the effect is better than that of 3- [5- (phenylthio) pyridin-3-yl ] -3- [4- (7H-pyrrolo [2 ], comparative example 1 group of 3-d ] pyrimidin-4-yl) -1H-pyrazol-1-yl ] propionitrile trifluoroacetate and comparative example 2 group with the omission of borneol. The above results suggest that the film coating agent prepared by the method of the present invention can reduce skeletal muscle damage caused by exercise and shorten the recovery period of osteoarticular damage, i.e., has excellent functions of reducing exercise damage and promoting repair thereof.
Claims (6)
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.
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| DE3107895A1 (en) * | 1981-03-02 | 1982-10-07 | Schweiger Hubert | Diterpenes in synergistic combinations with alpha -keto acids and their esters and use of these plant active substance combinations as bioactive agents in pharmaceutical and cosmetic compositions |
| US20130137681A1 (en) * | 2005-12-13 | 2013-05-30 | Incyte Corporation | HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS |
| CN103214484A (en) * | 2005-12-13 | 2013-07-24 | 因塞特公司 | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors |
| CN106902105A (en) * | 2017-03-13 | 2017-06-30 | 牡丹江医学院 | A kind of method for injury gained in sports protection |
| CN110664756A (en) * | 2019-10-09 | 2020-01-10 | 吉林大学 | Trauma spray for children and preparation method thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| DE3107895A1 (en) * | 1981-03-02 | 1982-10-07 | Schweiger Hubert | Diterpenes in synergistic combinations with alpha -keto acids and their esters and use of these plant active substance combinations as bioactive agents in pharmaceutical and cosmetic compositions |
| US20130137681A1 (en) * | 2005-12-13 | 2013-05-30 | Incyte Corporation | HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS |
| CN103214484A (en) * | 2005-12-13 | 2013-07-24 | 因塞特公司 | Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors |
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