CN111437280A

CN111437280A - New application based on tripterine and application thereof

Info

Publication number: CN111437280A
Application number: CN202010356373.8A
Authority: CN
Inventors: 沙莎; 马瑞; 李志平; 刘欢
Original assignee: Chongqing Yanying Biotechnology Co ltd
Current assignee: Chongqing Yanying Biotechnology Co ltd
Priority date: 2020-04-29
Filing date: 2020-04-29
Publication date: 2020-07-24

Abstract

The invention discloses a novel application and an application based on tripterine, wherein the tripterine and a preparation thereof can be orally taken or externally used for preventing or treating alcoholism, and the tripterine and the preparation thereof can be orally taken or externally used for preventing or treating alcoholism and preventing or treating alcoholism, and can be orally taken within 2 hours before drinking or within 1 hour after drinking. Relates to the technical field of tripterine. The novel application and the application based on the tripterine can effectively play a role in preventing alcohol, can effectively treat alcoholism, meet the requirements of oral administration and external administration, meet the requirements of different personnel and improve the application range of the tripterine.

Description

New application based on tripterine and application thereof

Technical Field

The invention relates to the technical field of tripterine, in particular to a new application and an application based on tripterine.

Background

The wine has the effects of promoting blood circulation, dredging channels, invigorating qi and stomach, eliminating dampness and relieving pain. However, with the continuous development of economy and the increase of interpersonal interaction, the proportion of people who drink alcohol increases, diseases and problems caused by alcohol are increasingly serious, and acute alcoholism (commonly called drunkenness, which refers to the process of body injury after a patient drinks a lot) becomes one of the diseases with the highest morbidity in holidays.

Investigations have shown that of patients who drink for a long period of time, about 57.5% of patients have fatty liver and 15% of patients have cirrhosis. The incidence of some digestive system tumors such as gastric cancer, esophageal cancer and liver cancer is also closely related to alcoholism. Alcoholism has become an increasingly serious threat to the health of people. Therefore, people are more and more eagerly hoped that related anti-alcoholism and liver protection medicines can be researched and developed for reducing the occurrence of alcoholism at an early time.

The existing antialcoholic mechanism comprises the functions of reducing the absorption of ethanol, enhancing the decomposition of ethanol, improving the activity of Alcohol Dehydrogenase (ADH) to accelerate the oxidative metabolism of ethanol, improving the activity of acetaldehyde dehydrogenase (A L DH) to accelerate the metabolic transformation of acetaldehyde, protecting liver organs and reducing the liver injury of ethanol metabolism.

Disclosure of Invention

Technical problem to be solved

Aiming at the defects of the prior art, the invention provides a new application based on tripterine and application thereof, and solves the problem of alcoholism.

(II) technical scheme

In order to achieve the purpose, the invention is realized by the following technical scheme: a new use based on tripterine, tripterine and its preparation can be used for preventing or treating alcoholism by oral administration or external use;

has obvious effect of treating and preventing alcoholism, and has no irritation to human body.

Further, tripterine and preparations thereof can be used for preventing or treating alcoholism by oral or external administration.

Further, for preventing or treating alcoholism, tripterine and its preparation can be orally administered within 2 hours before drinking or within 1 hour after drinking.

Further, preventing or treating alcoholism comprises applying the tripterine topical preparation to fat accumulation part within 2 hr before drinking or 1 hr after drinking, wherein the fat accumulation part can be one or more of abdomen, waist, thigh, hip or arm, and the dose of tripterine is 0.1-10 g/time.

Further, the tripterine accounts for 0.05-10% of the preparation by weight.

Further, the content of tripterine in the preparation is preferably 0.05-3% by weight.

Further, the tripterine oral preparation can be tablets, capsules, granules, powder, oral solution, oral suspension and oral emulsion.

Further, the tripterine external preparation can be made into lotion, tincture, emulsion, paste, and gel.

Further, the paste may be a common paste, or a paste formed by mixing with a liquid crystal, a nanocrystal or a liposome

Furthermore, the gel can be a common gel, and can also be a gel formed by mixing liquid crystal, nano-crystal or liposome.

(III) advantageous effects

The invention has the following beneficial effects:

(1) the tripterine and the preparation thereof can be orally or externally used for preventing or treating alcoholism, can also be orally or externally used for preventing or treating alcoholism, can be smeared at a fat accumulation part within 2 hours before drinking or within 1 hour after drinking, can effectively play a role in preventing alcohol, can effectively treat alcoholism, and meet the requirements of oral administration and external administration, thereby meeting the requirements of different personnel and improving the application range of the tripterine.

Of course, it is not necessary for any product to practice the invention to achieve all of the above-described advantages simultaneously

Drawings

FIG. 1 is a schematic structural diagram of a mixing device provided by the present invention;

FIG. 2 is an external view of the present invention shown in FIG. 1.

In the figure, 1-base, 2-shell, 3-partition board, 4-motor, 5-mixing shaft, 6-stirring blade, 7-auxiliary blade, 8-feeding mouth, 9-movable box, 10-filtering board, 11-discharging pipe, 12-operating rod, 13-T-shaped board, 14-sealing pad and 15-box door.

Detailed Description

The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the drawings in the embodiments of the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.

In the description of the present invention, it is to be understood that the terms "opening," "upper," "lower," "thickness," "top," "middle," "length," "inner," "peripheral," and the like are used in an orientation or positional relationship that is merely for convenience in describing and simplifying the description, and do not indicate or imply that the referenced component or element must have a particular orientation, be constructed and operated in a particular orientation, and thus should not be considered as limiting the present invention.

First embodiment

The embodiment of the invention provides a technical scheme that: a new use based on tripterine, tripterine and its preparation can be used for preventing or treating alcoholism by oral administration or external use;

The tripterine and the preparation thereof can be used for preventing or treating alcoholism by oral administration or external application.

Preventing or treating alcoholism, and can be orally administered with tripterine and its preparation within 2 hr before drinking or 1 hr after drinking.

Preventing or treating alcoholism by applying the tripterine topical preparation to fat accumulation part (one or more parts of abdomen, waist, thigh, hip or arm) within 2 hr before drinking or 1 hr after drinking, wherein the tripterine content is 0.1-10 g/time.

The tripterine accounts for 0.05-10% of the preparation by weight.

The content of tripterine in the preparation is preferably 0.05-3% by weight.

The tripterine oral preparation can be tablet, capsule, granule, powder, oral solution, oral suspension, or oral emulsion.

The tripterine external preparation can be in the forms of lotion, tincture, emulsion, paste, and gel.

The paste can be common paste, or paste formed by mixing with liquid crystal, nanocrystal or liposome

The gel can be common gel, or gel formed by mixing with liquid crystal, nanocrystal or liposome.

The mixing device comprises a base 1, a shell 2 is arranged at the top of the base 1, a partition plate 3 is arranged between two sides of the inner wall of the shell 2, a motor 4 is arranged at the top of the shell 2 through a support frame, an output shaft of the motor 4 is fixedly connected with a mixing shaft 5, the bottom end of the mixing shaft 5 penetrates through the shell 2 and extends into the shell 2, one end of the mixing shaft 5, which extends into the shell 2, is rotatably connected to the top of the partition plate 3, stirring blades 6 are arranged at two sides of the mixing shaft 5, and auxiliary blades 7 are rotatably connected to the tops of the stirring blades 6;

the motor 4 is connected with an external power supply and a control switch and is used for driving the mixing shaft to rotate so as to drive the stirring blades to rotate, the raw materials in the shell are mixed through the stirring blades, and the mixing effect of the raw materials can be improved through the arrangement of the auxiliary blades 7;

the two sides of the top of the shell 2 are both provided with feeding nozzles 8, and the bottoms of the two feeding nozzles 8 are communicated with the inside of the shell 2;

two feeding nozzles 8 are arranged, so that feeding of two different raw materials is facilitated, and the feeding effect is improved;

a movable box 9 is arranged at the bottom of the inner wall of the shell 2, a filter plate 10 is arranged between two sides of the inner wall of the movable box 9, one side of the inner wall of the movable box 9 is communicated with a discharge pipe 11, one end of the discharge pipe 11 penetrates through the shell 2 and extends to the outside of the shell 2, the top of one side of the movable box 9 is movably connected with an operating rod 12, one end of the operating rod 12 is fixedly connected with a T-shaped plate 13, a sealing gasket 14 is arranged at the top of the T-shaped plate 13, the top of the T-shaped plate 13 is slidably connected to the top of the inner wall of the movable box 9, the inside of the movable box 9 is communicated with the top of the partition plate 3 through a through pipe, and the front of the shell 2 is;

the setting of filter 10, be convenient for filter the tripterine solution after the preparation, can effectively filter the residual in the tripterine solution, and through the setting of sealed pad 14, can block up the bottom of siphunculus, so that mix processing, and through the motion about action bars 12, can drive T template 13 and sealed 14 side-to-side motion of filling up, be convenient for control the siphunculus, guarantee that the staff can the ration be unloaded, and the action bars 12 adopts the seal cover to be connected with the position that movable box 9 runs through, guarantee its leakproofness.

Second embodiment

Preparing tripterine oral capsule.

Table 1 prescription composition of tripterine oral capsules:

taking the raw and auxiliary materials, respectively sieving with a 60-mesh sieve, then weighing the raw and auxiliary materials (except magnesium stearate) according to the prescription amount, mixing by an equivalent progressive method, then adding a proper amount of water, mixing, granulating by a 20-mesh sieve, drying overnight for about 12 hours in a 40 ℃ oven, granulating by a 18-mesh sieve, adding the magnesium stearate according to the prescription amount, mixing, and encapsulating.

Third embodiment

Preparing tripterine aqueous solution.

Table 2 prescription composition of tripterine aqueous solution:

weighing tripterine according to the prescription amount, adding ethanol according to the prescription amount, stirring and dissolving for later use; and respectively weighing the propylene glycol, the glycerol, the phenoxyethanol and the VC according to the prescription amount, adding the water according to the prescription amount, stirring and dissolving, and then uniformly stirring and mixing with the ethanol solution of the tripterine to obtain the tripterine aqueous solution.

Fourth embodiment

Preparing tripterine gel.

Table 3 prescription composition of tripterine gel:

weighing carbomer according to a prescription amount, adding the carbomer into 250ml of water for dissolving, weighing sodium hydroxide according to the prescription amount, adding an appropriate amount of water to prepare a 1M solution, adding the solution into the carbomer solution, uniformly mixing to obtain a gel for later use, weighing propylene glycol, glycerin, phenoxyethanol, sodium hyaluronate, VC and VE according to the prescription amount respectively, adding L M of water according to the prescription amount, stirring for dissolving to obtain an auxiliary material solution for later use, weighing tripterine according to the prescription amount, adding ethanol according to the prescription amount, stirring for dissolving, then adding the auxiliary material solution, uniformly mixing, then adding carbomer gel, and uniformly mixing.

Fifth embodiment

And (3) preparing tripterine liquid crystal.

Table 4 prescription composition of tripterine liquid crystal:

weighing a proper amount of purified water, placing the purified water in a proper container, respectively adding the phenoxyethanol and the glycerol according to the prescription amount, heating and stirring the materials under the water bath condition of 65 ℃ until the materials are dissolved to obtain a water phase for later use; weighing tripterine, glyceryl monooleate, poloxamer-407 and ethylparaben according to the prescription amount, weighing ethanol according to the prescription amount, mixing, placing in a constant-temperature water bath kettle at 65 ℃, heating until completely dissolved to obtain an oil phase for later use; weighing carbomer according to the prescription amount, placing the carbomer into a proper container, adding a proper amount of distilled water, uniformly mixing, swelling, adding sodium hydroxide according to the prescription amount for neutralization after complete swelling, and uniformly stirring to obtain carbomer transparent gel; dripping the oil phase into the water phase under temperature maintaining condition, stirring at high speed, emulsifying for more than 30min, homogenizing under high pressure, and preparing liquid crystal; and uniformly stirring the obtained liquid crystal and carbomer gel to obtain a final product.

Sixth embodiment

Preparing tripterine nanoemulsion.

Table 5 prescription composition of tripterine nanoemulsion:

weighing tripterine according to the prescription amount, adding ethanol according to the prescription amount, stirring for dissolving, then respectively adding poloxamer 188, tween 80 and a proper amount of water according to the prescription amount, and uniformly mixing for later use; and taking another container, respectively weighing ethylparaben and phenoxyethanol according to the prescription amount, adding glycerol according to the prescription amount, dissolving and uniformly mixing, then adding the mixture into a solution containing tripterine, stirring and uniformly mixing, and stirring at the temperature of 60 ℃ and the speed of 1000rpm for later use.

Weighing white oil, Span80 and VE according to the prescription amount, mixing, stirring and mixing uniformly, heating to 60 ℃, then slowly adding into a water solution containing tripterine, poloxamer, tween, ethylparaben, phenoxyethanol, glycerol and the like which is stirred at a high speed, adding VC, continuously stirring for 20 minutes, adding water to a constant volume of 1L, and then homogenizing at a high pressure (500bar for 5 cycles) to obtain the tripterine nanoemulsion.

Seventh embodiment

Guinea pig acute skin irritation test of tripterine external preparation:

in order to examine the acute irritation of the tripterine external preparation to the skin, 5 guinea pigs are selected to carry out experimental animals in each group, the experimental temperature is 20-24 ℃, the relative humidity is 60-70%, the two sides of the spinal column at the back of the guinea pigs are cut off within 3cm and 3cm before the experiment within 24h, the hair removal range is 2.5cm, the application area is 2.5cm and 2.5 cm., 0.5m L of a tested substance is applied to the skin at one side, blank solvent water is applied to the other side as a control, the blank solvent water is applied for 3 times every day, the application is carried out for 14 days continuously, the hair is cut before each application from the next day, the residual tested substance is removed by water or a non-irritant solvent, the results are observed after one hour, the irritation reaction evaluation is carried out according to the regulation of the cosmetic hygiene regulations (2007 edition), and the evaluation results are shown:

table 6 acute skin irritation response of tripterine external preparations:

as can be seen from the results, no acute skin irritation was observed in the tripterine external preparations prepared in examples 2 to 5.

Eighth embodiment

Experiments on the in vivo effectiveness of tripterine in preventing and treating alcoholism of animals;

(1) determination of an intoxicated dose

40 Kunming mice are taken, after adaptive feeding for 1 week, the Kunming mice are randomly divided into 4 groups, 10 mice in each group are fasted for 12 hours, each group is respectively irrigated with 56% (V/V)

Hongxing Erguotou

13, 14, 15 and 16m L/kg. according to the body weight to record the drunkenness rate and the death rate of the mice, the drunkenness dose with the highest drunkenness rate and the lowest death rate is selected, the drunkenness is determined when the righting reflex disappears, and the drunkenness is not determined otherwise.

The results show that the intoxication rate of the mice reaches 90% at the maximum and the mortality rate is only 10% when the gavage dose is 14m L/kg, and the dose is selected to be the optimal dose for the subsequent acute alcoholism test of the mice compared with other dose groups.

(2) Drunkenness treatment test

100 Kunming mice were adaptively fed for 1 week, and then were randomly divided into 10 groups of 10 mice each, 10 mice were fasted without water deprivation for 12 hours before treatment, each group of mice was gavaged with 56% (V/V) Hongxing Erguotou at a weight of 14m L/kg, and then administered with physiological saline of equal volume (blank control group), oral treatment group (example 1, three low, medium and high dose groups of 1mg/kg, 10mg/kg and 35 mg/kg), external treatment group 1 (example 3, three low, medium and high dose groups of 1.5mg/kg, 15mg/kg and 50 mg/kg), and external treatment group 2 (example 4, three low dose groups of 1.5mg/kg, 15mg/kg and 50 mg/kg), before the test, the mice in each group were weighed, labeled and recorded.

The inebriation latency period is the turning reflection disappearance time-drinking time;

the sleep time is the righting reflex recovery time-righting reflex disappearance time;

sobering-up time is the righting recovery time-drinking time.

The specific results are as follows:

table 7 effects of oral and topical preparations of tripterine on the treatment of mouse intoxication;

note: indicates significant differences (P <0.05) compared to the same row of blank control groups.

The above results show that the use of the formulations of examples 3 and 4 can significantly shorten the sleep time and the sobering time of mice and significantly prolong the intoxication latency of mice, compared to the model group, indicating that it has the anti-hangover effect.

(3) Drunkenness prevention test

100 Kunming mice are adaptively fed for 1 week, and then are randomly divided into 10 groups, 10 mice are kept in a fasting state for 12 hours before treatment, each group of mice is respectively subjected to constant volume physiological saline 30min before alcohol gavage (blank control group), oral treatment group (example 1, three low, medium and high dose groups of 1mg/kg, 10mg/kg and 35 mg/kg), external treatment group 1 (example 3, three low, medium and high dose groups of 1.5mg/kg, 15mg/kg and 50 mg/kg) and external treatment group 2 (example 4, three low, medium and high dose groups of 1.5mg/kg, 15mg/kg and 50 mg/kg), and then are subjected to stomach filling 56% (V/V) of Hongxing Erguotou according to the weight of 14m L/kg, and then the activity of each group of mice is observed, and the drunkenness number, death time, righting reflex disappearance time, sleep time and sobering time are recorded according to the formula.

The specific results are shown in the following table.

TABLE 8 oral and topical preparations of tripterine for preventing drunkenness of mice

The above results show that the use of the formulations of examples 3 and 4 can significantly shorten the sleep time and the sober-up time of mice and significantly prolong the intoxication latency of mice, compared to the model group, indicating that it has the effect of preventing alcoholism.

Ninth embodiment

The effectiveness test and the human body irritation test of the tripterine for treating the alcoholism;

the experimental method comprises the following steps:

the subjects were divided into 4 groups of 10 persons, wherein 1 group was a control group and the fat deposition site (abdomen) was applied with physiological saline, the other 3 groups were experimental groups and the fat deposition sites (abdomen or waist) were applied with 5g of the preparations of examples 3, 4 and 5, respectively, and after 30min of administration treatment, the subjects drunk 100m L56% (V/V) of Hongxing Erguotou respectively and drunk 0min after 20 min.

Detection indexes are as follows:

observing whether abnormal phenomena such as erythema edema exist at the smearing part 30min, 60min and 90min after smearing, and inspecting the skin irritation of the product; meanwhile, the blood ethanol content BAC of the study object is measured 20min, 40 min and 60min after drinking (expired gas alcohol content detector Mr. Black-02: Shenzhen McLimited).

The experimental results are as follows:

table 9 acute skin irritation response of tripterine external preparations:

table 10 ethanol concentration in blood of subjects after using tripterine external preparations:

This study showed that: within 90min after the product is used, the abnormal phenomena of erythema, edema and the like are all seen at the smearing part, which shows that the product has no obvious skin irritation; the product can be applied before drinking to significantly reduce the content of ethanol (BAC) in blood and increase the ethanol removal rate.

It is noted that, herein, relational terms such as first and second, and the like may be used solely to distinguish one entity or action from another entity or action without necessarily requiring or implying any actual such relationship or order between such entities or actions. Also, the terms "comprises," "comprising," or any other variation thereof, are intended to cover a non-exclusive inclusion, such that a process, method, article, or apparatus that comprises a list of elements does not include only those elements but may include other elements not expressly listed or inherent to such process, method, article, or apparatus.

The preferred embodiments of the invention disclosed above are intended to be illustrative only. The preferred embodiments are not intended to be exhaustive or to limit the invention to the precise embodiments disclosed. Obviously, many modifications and variations are possible in light of the above teaching. The embodiments were chosen and described in order to best explain the principles of the invention and the practical application, to thereby enable others skilled in the art to best utilize the invention. The invention is limited only by the claims and their full scope and equivalents.

Claims

1. A new use based on tripterine is characterized in that: the tripterine and the preparation thereof can be used for preventing or treating alcoholism by oral administration or external application.

2. The new use of tripterine according to claim 1, wherein: the tripterine and the preparation thereof can be used for preventing or treating alcoholism by oral administration or external application.

3. The new use of tripterine according to claim 2, wherein: preventing or treating alcoholism, and can be orally administered with tripterine and its preparation within 2 hr before drinking or 1 hr after drinking.

4. The new use of tripterine according to claim 2, wherein: preventing or treating alcoholism by applying the tripterine topical preparation to fat accumulation part (one or more parts of abdomen, waist, thigh, hip or arm) within 2 hr before drinking or 1 hr after drinking, wherein the tripterine content is 0.1-10 g/time.

5. The new use of tripterine according to claim 1, wherein: the tripterine accounts for 0.05-10% of the preparation by weight.

6. The new use of tripterine according to claim 5, wherein: the content of tripterine in the preparation is preferably 0.05-3% by weight.

7. The new use of tripterine according to claim 3, wherein: the tripterine oral preparation can be tablet, capsule, granule, powder, oral solution, oral suspension, or oral emulsion.

8. The new use of tripterine according to claim 4, wherein: the tripterine external preparation can be in the forms of lotion, tincture, emulsion, paste, and gel.

9. The new use of tripterine according to claim 8, wherein: the paste can be common paste, or paste formed by mixing with liquid crystal, nanocrystal or liposome.

10. The new use of tripterine according to claim 8, wherein: the gel can be common gel, or gel formed by mixing with liquid crystal, nanocrystal or liposome.