CN114699508A

CN114699508A - Silicone gel and preparation method and application thereof

Info

Publication number: CN114699508A
Application number: CN202210378149.8A
Authority: CN
Inventors: 魏民; 耿伯显; 贾芳
Original assignee: Nanjing Tianlang Pharmaceutical Co ltd
Current assignee: Nanjing Tianlang Pharmaceutical Co ltd
Priority date: 2022-04-12
Filing date: 2022-04-12
Publication date: 2022-07-05

Abstract

The invention discloses a silicone gel and a preparation method and application thereof, and relates to the technical field of external anti-scar drugs. The silicone gel comprises the following components in parts by weight: 10-40 parts of simethicone, 0.01-0.05 part of mussel mucin, 0.5-2 parts of emulsifier, 5-20 parts of humectant, 0.01-0.05 part of preservative, 0.4-2 parts of acid-base regulator and 0.4-2 parts of thickening agent. It can reduce the water evaporation amount on the surface of the scar, and increase the hydration of the scar tissue; the permeability of the mixture of water-soluble protein and various low-molecular water-soluble inflammatory proteins on the surface of the scar is increased, so that the water-soluble protein and products in the interstitium are reduced, the fluid pressure is reduced, and the scar is easy to mature and soften. Can improve the film forming effect of the silicone gel, and simultaneously improve the scar recovery speed and the comfort of the recovery process.

Description

Silicone gel and preparation method and application thereof

Technical Field

The invention relates to the technical field of external scar-resistant medicines, in particular to silicone gel and a preparation method and application thereof.

Background

Along with the rapid growth of domestic economy, the income per capita is increased, the living standard is continuously improved, and the consumption demand of people on health and beauty is also increased. The continuous fire explosion in the markets of shaping, beautifying, body building, health products and cosmetics is the evidence. Data show that the annual composite growth rate of sales income of the novel medical silicone gel industry of China exceeds 30 percent in nearly ten years. The patient not only wants the silicone gel to have the function of repairing the injured part, but also wants to leave no or few capacitive injured traces to achieve wound healing in the cosmetic sense, and modern cosmetic medical products are produced at once.

The silicone gel is applied on the surface of scar, and has effects of protecting scar, inhibiting scar hyperplasia, retaining water, relieving itching and softening scar. After the silicone gel is smeared on the surface of a scar, a thin transparent film can be quickly formed, and the film is breathable and impermeable, so that the normal breathing of the skin can be ensured, the metabolism of scar tissues can be accelerated, the water on the surface of the skin can be kept from being lost, and the effects of softening the scar and eliminating discomfort can be achieved.

The silicone gel belongs to a scar-removing medicine which passes clinical verification and has good clinical effect, but the silicone gel must be used in an early stage. When scars are formed due to scar constitution or chronic inflammatory stimulation, the silicone gel is used immediately after the scar scabs fall off. The silicone gel forms a film to protect the wound, thereby creating a moist environment for collagen fiber repair, and the application time is at least half a year. However, the existing silicone gel has long service time and poor comfort during use.

In view of the above, the present invention is particularly proposed.

Disclosure of Invention

The invention aims to provide a silicone gel and a preparation method and application thereof.

The invention is realized by the following steps:

in a first aspect, the present invention provides a silicone gel, which comprises the following components in parts by weight: 10-40 parts of simethicone, 0.01-0.05 part of mussel mucin, 0.5-2 parts of emulsifier, 5-20 parts of humectant, 0.01-0.05 part of preservative, 0.4-2 parts of acid-base regulator and 0.4-2 parts of thickening agent.

In an alternative embodiment, the dimethylsilicone fluids include a low molecular weight dimethylsilicone fluid and a high molecular weight dimethylsilicone fluid, and the mass ratio of the low molecular weight dimethylsilicone fluid to the high molecular weight dimethylsilicone fluid is 25 to 35: 4-6;

preferably, the low molecular weight dimethylsilicone oil has a molecular weight of 1 to 10 ten thousand;

preferably, the high molecular weight dimethylsilicone fluid has a molecular weight of more than 30 ten thousand.

In alternative embodiments, the concentration of mussel mucin is from 0.1mg/ml to 15 mg/ml.

In alternative embodiments, the emulsifier comprises any one or combination of more of a triglyceride, soy lecithin, polysorbate 80, sodium stearoyl lactylate, sucrose esters, and monoglycerol ester of lauric acid.

In alternative embodiments, the preservative comprises any one or combination of more of ethyl paraben, sorbic acid and its potassium salt, benzoic acid and its sodium salt, calcium propionate, sodium propionate, dehydroacetic acid, and lactic acid.

In alternative embodiments, the moisturizer comprises any one or combination of glycerin, petrolatum, propylene glycol, polyethylene glycol 800, and polyethylene glycol.

In alternative embodiments, the thickening agent comprises any one or combination of guar gum, xanthan gum, locust bean gum, pectin, alginates, carbomers, agar, gelatin, and acacia.

In a second aspect, the present invention provides a method of preparing a silicone gel comprising mixing the components of the silicone gel according to any one of the preceding embodiments to homogeneity;

preferably, the humectant and the preservative are mixed and dissolved, then the simethicone, the thickener and the emulsifier are sequentially added, the mussel mucin is added after homogenization, and the pH regulator is added after uniform mixing, so that the mussel adhesive is obtained.

In a third aspect, the present invention provides the use of a silicone gel as described in any one of the preceding embodiments in the manufacture of a medicament for ameliorating or preventing pathological scarring of the skin;

preferably, the scars include keloid scars, hypertrophic scars, contracture scars, acne scars, and surgical scars.

In a fourth aspect, the present invention provides a scar gel comprising a polyethylene hose and a silicone gel as described in any one of the preceding embodiments, the silicone gel being filled in the polyethylene hose.

The invention has the following beneficial effects:

the silicone gel provided by the application is prepared by compounding the dimeticone and the mussel mucin according to a specific weight ratio, and silicone oil molecules in the dimeticone have an inhibitory effect on fibroblasts, so that division and proliferation of the fibroblasts are reduced, and a large amount of secretion of extracellular matrix is reduced. The mussel mucin forms a microcosmic discontinuous nano-scale protective film on the local part, so that the wound surface or the skin mucosa are effectively protected, and the efficacy of relieving itching is achieved. After the prepared silicone gel is used, the evaporation capacity of water on the surface of the scar can be reduced, and the hydration effect of the scar tissue is increased; the permeability of the mixture of the water-soluble protein on the surface of the scar and various low-molecular water-soluble inflammatory proteins is increased, so that the scar can be diffused on the surface of the skin, the water-soluble proteins and products in the interstitium are reduced, the fluid pressure is reduced, the scar is easy to mature and soften, and the scar has the effects of protecting the wound surface and relieving itching under the action of mussel mucin. The combination of dimethicone and mussel mucin can improve the film forming effect of silicone gel, and simultaneously improve the speed of scar recovery and the comfort of the recovery process. The silicone gel can be widely applied to the preparation of medicines for improving or preventing the pathological scar formation of skin.

Detailed Description

In order to make the objects, technical solutions and advantages of the embodiments of the present invention clearer, the technical solutions in the embodiments of the present invention will be clearly and completely described below. The examples, in which specific conditions are not specified, were conducted under conventional conditions or conditions recommended by the manufacturer. The reagents or instruments used are not indicated by the manufacturer, and are all conventional products available commercially.

Wherein the dimethyl silicone oil comprises low molecular weight dimethyl silicone oil and high molecular weight dimethyl silicone oil, and the mass ratio of the low molecular weight dimethyl silicone oil to the high molecular weight dimethyl silicone oil is 25-35: 4-6; preferably, the low molecular weight dimethylsilicone fluid has a molecular weight of 1 to 10 ten thousand; the molecular weight of the high molecular weight dimethylsilicone fluid is greater than 30 ten thousand.

The silicone oil molecules in the simethicone have the inhibition effect on fibroblasts, so that the division and proliferation of the fibroblasts are reduced, and the massive secretion of extracellular matrix is reduced. Through the compounded low molecular weight and high molecular weight dimethyl silicone oil in the application, the viscosity of the low molecular weight dimethyl silicone oil is lower, the viscosity of the high molecular weight dimethyl silicone oil is higher, the two are compounded to obtain a product with proper viscosity, the coating comfort level is good, the excessively greasy feeling can not occur, the film forming effect is better, and the film has excellent toughness.

The concentration of the added mussel mucin is 0.1-15 mg/ml, and the mussel mucin can effectively protect the wound surface or the skin mucosa by forming a micro discontinuous nano-scale protective film on the local part and has the effect of relieving itching.

According to the application, the simethicone and the mussel mucin are compounded according to a specific weight ratio, so that after the prepared silicone gel is used, the water evaporation amount on the surface of a scar can be reduced, and the hydration effect of the scar tissue is increased; the permeability of the mixture of the water-soluble protein on the surface of the scar and various low-molecular water-soluble inflammatory proteins is increased, so that the scar can be diffused on the surface of the skin, the water-soluble proteins and products in the interstitium are reduced, the fluid pressure is reduced, the scar is easy to mature and soften, and the scar has the effects of protecting the wound surface and relieving itching under the action of mussel mucin. The combination of dimethicone and mussel mucin can improve the film forming effect of the silicone gel, as well as the speed of scar recovery and the comfort of the recovery process.

Emulsifiers include, but are not limited to, any one or combination of triglycerides, soy phospholipids, polysorbate 80, sodium stearoyl lactylate, sucrose esters, and monoglycerides of lauric acid.

Preservatives include, but are not limited to, ethyl paraben, sorbic acid and its potassium salt, benzoic acid and its sodium salt, calcium propionate, sodium propionate, dehydroacetic acid, and lactic acid, either alone or in combination.

Humectants include, but are not limited to, any one or combination of glycols, glycerin, petrolatum, propylene glycol, polyethylene glycol 800, and polyethylene glycol.

Thickeners include, but are not limited to, guar gum, xanthan gum, locust bean gum, pectin, alginates, carbomers, agar, gelatin, and combinations of any one or more of the acacia.

In addition, the application also provides a preparation method of the silicone gel, which comprises the steps of uniformly mixing the components of the silicone gel;

Specifically, the humectant of the prescription amount is accurately weighed, and is slowly added into the accurately weighed preservative (50 ℃ water bath) while stirring, and the stirring is carried out for about 15 minutes to dissolve the preservative; adding the dimethyl silicone oil with the prescription amount after the preservative is dissolved, stirring for about 5 minutes, adding the thickening agent with the prescription amount, stirring for about 10 minutes, adding the emulsifier with the prescription amount, stirring for about 5 minutes, adding purified water (2% of the water is remained) with the temperature of 70 ℃, stirring for 5 minutes, homogenizing for 15 minutes (keeping the temperature at 60 ℃) by a homogenizer with the temperature of 3.5Kr/min, cooling to 25 ℃, adding mussel mucin (dissolving the mussel mucin with the 1% of the purified water and then adding the mussel mucin) and homogenizing and stirring for about 15 minutes; the acid-base modifier (e.g., triethanolamine) is added in the prescribed amount with stirring (the remainder being rinsed with 1% purified water) and stirred for about 15 minutes.

The silicone gel prepared by the method can improve the film forming effect of the silicone gel, and can improve the scar recovery speed and the comfort of the recovery process. The silicone gel can be widely applied to the preparation of medicines for improving or preventing the pathological scar formation of skin; preferably, the scars include keloid scars, hypertrophic scars, contractures, acne scars, and surgical scars.

In addition, the invention also provides scar gel which comprises a polyethylene hose and silicone gel, wherein the silicone gel is filled in the polyethylene hose.

The features and properties of the present invention are described in further detail below with reference to examples.

Example 1

The embodiment provides a silicone gel, which comprises the following components in percentage by mass: 35% of dimethicone with the molecular weight of 1.2 ten thousand, 0.03% of mussel mucin, 1% of polysorbate 80 (emulsifier), 14% of propylene glycol (humectant), 0.02% of ethylparaben (preservative), 0.48% of triethanolamine (acid-base regulator), 0.6% of carbomer (thickener) and the balance of water.

The preparation method comprises the following steps: accurately weighing the propylene glycol according to the prescription amount, slowly adding the accurately weighed ethylparaben (50 ℃ water bath) while stirring, stirring for about 15 minutes to dissolve the ethylparaben, adding the dimethicone according to the prescription amount after dissolving the ethylparaben, stirring for about 5 minutes, adding the carbomer 0.4% -2% according to the prescription amount, stirring for about 10 minutes, adding the polysorbate 80 according to the prescription amount, stirring for about 5 minutes, adding the purified water (2% of water is reserved) at 70 ℃ for stirring for 5 minutes, homogenizing for 15 minutes (keeping the temperature at 60 ℃) by using a homogenizer 3.5Kr/min, cooling to 25 ℃, adding the mussel mucin according to the prescription amount (dissolving the remaining 1% of purified water and adding), stirring for about 15 minutes, adding the triethanolamine according to the prescription amount (washing with the remaining 1% of purified water and adding), stirring for about 15 minutes, filling and packaging to obtain the mussel mucoprotein.

Example 2

The embodiment provides a silicone gel, which comprises the following components in percentage by mass: 30% of dimethyl silicone oil with the molecular weight of 1.2 ten thousand, 5% of dimethyl silicone oil with the molecular weight of 50 ten thousand, 0.03% of mussel mucin, 1% of polysorbate 80 (emulsifier), 14% of propylene glycol (humectant), 0.02% of ethylparaben (preservative), 0.48% of triethanolamine (acid-base regulator), 0.6% of carbomer (thickener) and the balance of water.

Example 3

The embodiment provides a silicone gel, which comprises the following components in percentage by mass: 7% of dimethyl silicone oil with the molecular weight of 1.2 ten thousand, 3% of dimethyl silicone oil with the molecular weight of 50 ten thousand, 0.01% of mussel mucin, 0.5% of sodium stearyl lactate (emulsifier), 15% of propylene glycol (humectant), 0.03% of lactic acid (preservative), 1% of triethanolamine (acid-base regulator), 0.4% of alginate (thickener) and the balance of water.

Example 4

The embodiment provides a silicone gel, which comprises the following components in percentage by mass: 35% of dimethyl silicone oil with the molecular weight of 5 ten thousand, 5% of dimethyl silicone oil with the molecular weight of 30 ten thousand, 0.05% of mussel mucin, 0.5% of sodium stearoyl lactylate (emulsifier), 10% of polyethylene glycol 800 (humectant), 0.05% of sodium propionate (preservative), 2% of triethanolamine (acid-base regulator), 1% of alginate (thickener) and the balance of water.

Comparative example 1

This comparative example is essentially the same as example 2, except that the component in this comparative example omits mussel mucin 0.03% and water is used to make up the corresponding amount.

Comparative example 2

This comparative example is essentially the same as example 2 except that 35% of the simethicone is omitted from the composition and water is used to make up the corresponding amount.

Comparative example 3

This comparative example is essentially the same as example 2 except that 25% dimethicone with a molecular weight of 1.2 ten thousand, 5% dimethicone with a molecular weight of 50 ten thousand, and 0.1% mussel mucin are present in this comparative example, the corresponding amounts being made up with water.

Comparative example 4

This comparative example is essentially the same as example 2 except that it has 40% dimethicone with a molecular weight of 1.2 ten thousand, 10% dimethicone with a molecular weight of 50 ten thousand, and 0.05% mussel mucin.

Comparative example 5

This comparative example is essentially the same as example 2, except that in this comparative example, 20% of dimethicone having a molecular weight of 1.2 ten thousand, and 15% of dimethicone having a molecular weight of 50 ten thousand.

Comparative example 6

This comparative example is essentially the same as example 2, except that in this comparative example, 6% of dimethicone having a molecular weight of 1.2 ten thousand, and 1% of dimethicone having a molecular weight of 50 ten thousand.

Test examples

The test method comprises the following steps: 72 subjects with mild and moderate scars are selected and divided into 6 groups on average, 12 subjects in each group continuously use the products provided by the examples 1-2 and the comparative examples 1-4 for 1 month, and the clinical treatment effect of the invention is evaluated by inspecting the compliance (including oil smell, greasy degree and comfort degree after use) and the treatment effect (scar size, scar color depth, overall effect and the like) of the subjects.

Subject subjects inclusion criteria: the subject is a patient with mild and moderate scars, is not limited by men and women, and is 18-65 years old.

Subject exclusion criteria for subjects: 1. pregnant or lactating women, allergic constitution or those allergic to the product; 2. other subjects with discomfort.

The using method comprises the following steps: the scar area is cleaned and allowed to dry. The product is applied to the scar. 2 times daily, 1 time each in the morning and evening.

And (4) counting results: the compliance and efficacy of the subjects were analyzed after one month of continuous use.

Subject compliance: after investigation by the subject for odor, greasiness, and after-use comfort, the results of the investigation are shown in the following table:

as can be seen from the above table, the comfort level of the sample application is closely related to the ratio and molecular weight of dimethicone, wherein the greater the ratio of dimethicone, the lower compliance, the higher molecular weight of dimethicone, the greater the viscosity, and the lower compliance, the less compliance is related to the amount of mussel mucin.

The curative effect is as follows: after investigation according to the size, color and depth of scars and the overall effect of the tested person, the investigation result is shown as the following table:

as can be seen from the comparison of the data of example 1 and example 2, the application of the dimethicone with high molecular weight and low molecular weight can have better curative effect, and examples 3 and 4 change the dosage of high molecular weight and low molecular weight, which mainly changes the viscosity feeling used by users, and the effective rate is basically consistent with that of example 2. Whereas in the present application, mussel mucin was omitted in comparative example 1, it can be seen that the effect is reduced compared to example 2, whereas in comparative example 2, the effect is significantly reduced or even no effect is obtained by omitting dimethicone. In comparative example 3, the amount of simethicone was decreased, and the amount of mussel mucin was increased, but still no good effect was obtained, whereas in comparative example 4, the increase in the amount of simethicone failed to obtain a better effect or even a lower effective rate than in example 2. In the comparative example 5, due to the fact that the high-molecular-weight dimethyl silicone oil is too large in using amount, viscosity is increased, and effective coating cannot be conducted, and meanwhile in the comparative example 6, due to the fact that the whole using amount of the dimethyl silicone oil is small, gel is thin, and a film is difficult to form or the film forming time is too long, and experiments cannot be conducted. As can be seen from the table above, the dimethicone has a main effect on improving the scar effect, and the mussel mucin increasing effect can play a synergistic effect.

Clinical tests prove that the product is suitable for assisting in improving pathological scars of skin and assisting in preventing the formation of the pathological scars of skin.

In summary, the silicone gel provided by the application adopts the compounding of the dimeticone and the mussel mucin according to a specific weight ratio, and silicone oil molecules in the dimeticone have an inhibitory effect on fibroblasts, so that the division and proliferation of the fibroblasts are reduced, and the massive secretion of extracellular matrix is reduced. The mussel mucin can effectively protect the wound surface or the skin mucosa by locally forming a micro non-continuous nano-scale protective film, and has the effect of relieving itching. After the prepared silicone gel is used, the evaporation capacity of water on the surface of the scar can be reduced, and the hydration effect of the scar tissue is increased; the permeability of the mixture of the water-soluble protein on the surface of the scar and various low-molecular water-soluble inflammatory proteins is increased, so that the scar can be diffused on the surface of the skin, the water-soluble proteins and products in the interstitium are reduced, the fluid pressure is reduced, the scar is easy to mature and soften, and the scar has the effects of protecting the wound surface and relieving itching under the action of mussel mucin. The combination of dimethicone and mussel mucin can improve the film forming effect of the silicone gel, as well as the speed of scar recovery and the comfort of the recovery process. The silicone gel can be widely applied to the preparation of medicines for improving or preventing the pathological scar formation of skin.

The above description is only a preferred embodiment of the present invention and is not intended to limit the present invention, and various modifications and changes may be made by those skilled in the art. Any modification, equivalent replacement, or improvement made within the spirit and principle of the present invention should be included in the protection scope of the present invention.

Claims

1. The silicone gel is characterized by comprising the following components in parts by weight: 10-40 parts of simethicone, 0.01-0.05 part of mussel mucin, 0.5-2 parts of emulsifier, 5-20 parts of humectant, 0.01-0.05 part of preservative, 0.4-2 parts of acid-base regulator and 0.4-2 parts of thickening agent.

2. The silicone gel according to claim 1, wherein the dimethicone comprises a low molecular weight dimethicone and a high molecular weight dimethicone, the mass ratio of the low molecular weight dimethicone to the high molecular weight dimethicone being from 25 to 35: 4-6;

preferably, the low molecular weight dimethylsilicone fluid has a molecular weight of 1 to 10 ten thousand;

3. The silicone gel of claim 1, wherein the concentration of mussel mucin is from 0.1mg/ml to 15 mg/ml.

4. The silicone gel of claim 1, wherein the emulsifier comprises any one or a combination of triglycerol esters, soy lecithin, polysorbate 80, sodium stearoyl lactylate, sucrose esters, and monoglycerol ester of lauric acid.

5. The silicone gel of claim 1, wherein the preservative comprises any one or a combination of ethyl paraben, sorbic acid and its potassium salt, benzoic acid and its sodium salt, calcium propionate, sodium propionate, dehydroacetic acid and lactic acid.

6. The silicone gel of claim 1, wherein the humectant comprises any one or a combination of glycerin, petrolatum, propylene glycol, polyethylene glycol 800, and polyethylene glycol.

7. The silicone gel of claim 1, wherein the thickener comprises any one or a combination of guar gum, xanthan gum, locust bean gum, pectin, alginate, carbomer, agar, gelatin, and acacia.

8. A method for preparing a silicone gel, comprising mixing the components of the silicone gel according to any one of claims 1 to 7;

preferably, the humectant and the preservative are mixed and dissolved, then the dimeticone, the thickener and the emulsifier are sequentially added, the mussel mucin is added after homogenization, and the acid-base regulator is added after uniform mixing, so that the mussel mucin-containing composition is obtained.

9. Use of a silicone gel as claimed in any one of claims 1 to 7 in the manufacture of a medicament for ameliorating or preventing pathological scarring of the skin;

10. A scar gel, characterized in that it comprises a polyethylene hose and a silicone gel as claimed in any one of claims 1 to 7, which is filled in the polyethylene hose.