CN105267866A - Emulsion for treating onychomycosis and preparation method of emulsion for treating onychomycosis - Google Patents

Abstract

The invention discloses an emulsion for treating onychomycosis and a preparation method thereof. The emulsion contains the following substances: eucalyptus oil, turmeric oil, javanica oil, eugenol, self-emulsifying compound emulsifier AC-402, olive emulsifying agent, urea, salicylic acid, camphor, borneol, CMC-Na, sodium alginate, azone, boric acid, glycerin, sodium hydroxypropyl methylcellulose, 1,2-propanediol, fennel, sophora flavescens, 5% nitric acid Parkin ethyl ester propylene glycol solution. The emulsion for treating onychomycosis prepared by the invention has strong functionality, and little toxicity and irritation. Brucea javanica oil can inhibit fungal reproduction and effectively prevent fungal infection. Sophora flavescens extract has anti-inflammatory and antibacterial effects. The ingredients in the formula complement each other. Compared with traditional medicines, the treatment effect is better, the permeability is stronger, and the recurrence is lower, and it fundamentally treats onychomycosis caused by various fungi.

Description

A kind of emulsion for treating onychomycosis and preparation method thereof

technical field

The invention relates to an emulsion for treating onychomycosis and a preparation method thereof, belonging to the field of pharmacy.

Background technique

Onychomycosis caused by fungal infection in real life has become an annoyance to more and more people. For a long time, the diagnosis and treatment methods of onychomycosis are relatively simple, the treatment effect is not satisfactory, and repeated recurrence has become a difficult problem in treatment.

There are three main causes of onychomycosis: personal factors, environmental factors, and disease factors.

1. Personal factors

1. Not paying attention to personal hygiene; 2. Suffering from tinea pedis; 3. Long-term direct contact with water or chemicals; 4. Malnutrition; 5. Trauma or impact on nails may lead to fungal invasion; (onychomycosis) patient contact.

2. Environmental factors

High temperature and high humidity are important conditions for frequent occurrence of ringworm. Therefore, ringworm in summer and rainy season is more and heavier than winter and dry season. The working and living environment of patients cannot be ignored. Ringworm is prone to occur in high-temperature, high-humidity workshops, especially in environments where heavy work clothes must be worn for production and poor ventilation. If there is no bathing equipment or failure to bathe in time, the incidence of ringworm will increase significantly.

3. Disease factors

Certain chronic diseases such as malnutrition, hyperthyroidism, and ringworm in patients with diabetes are common, and the symptoms are also severe. Some severe diseases, such as AIDS and advanced cancer patients, not only have a high incidence of fungal ringworm, but also have a wide distribution of ringworm, which is very stubborn and difficult to heal.

Adding traditional Chinese medicine ingredients with less toxic effect and stronger antifungal ability to the prepared emulsion with stronger penetration will effectively solve the troubles caused by onychomycosis.

Contents of the invention

The object of the present invention is to provide an emulsion for treating onychomycosis with little toxicity, strong antifungal ability and strong permeability and a preparation method thereof.

A kind of emulsion for treating onychomycosis of the present invention, wherein comprises the material of following consumption:

In the above-mentioned emulsion for the treatment of onychomycosis, also comprise the material of following consumption:

In the above-mentioned emulsion for treating onychomycosis, the extract of Sophora flavescens is prepared by the following method: Take 2-15g of Sophora flavescens, grind it into a coarse powder, and extract in three times: add 150-200ml0.1% for the first time Soak in -0.5% hydrochloric acid for 5-30min, extract by reflux extraction for 0.5-2h, collect the extract, add 130-150ml of 0.1%-0.5% hydrochloric acid for the second time, extract for 0.5-2h, collect the extract, and the third time Add 100-120ml of 0.1%-0.5% hydrochloric acid to extract for 0.5-1h, filter each time, combine the three filtrates, mix and concentrate to 10-90ml. Wherein, 0.1%-0.5% hydrochloric acid is the volume concentration.

In the above-mentioned emulsion for treating onychomycosis, the fennel extract is prepared by the following method: take 2-15g of fennel, grind it into a coarse powder, and extract in three times: add 200-300ml of 70%-80% ethanol for the first time Soak for 5-30min, extract by reflux extraction for 0.5-1.5h, collect the extract, add 150-200ml70%-80% ethanol for the second time to extract for 0.2-1h, collect the extract, add 100-150ml70%-80 for the third time Extract with % ethanol for 0.2-1h, filter each time, combine the three filtrates, mix and concentrate to 10-90ml. Wherein, 70%-80% ethanol is the volume concentration.

In the above-mentioned emulsion for the treatment of onychomycosis,

In the above-mentioned emulsion for the treatment of onychomycosis, it is preferred to contain the following materials:

The preparation method of the emulsion for the treatment of onychomycosis of the present invention, comprises the following steps:

a) Weigh sodium alginate, disperse it in 10-15ml distilled water, fully swell into transparent gel A;

b) Weigh carboxymethylcellulose sodium, disperse it in 6-10ml distilled water, fully swell into transparent gel B;

c) Weigh hydroxypropyl methylcellulose, disperse it in 6-10ml distilled water, and fully swell it into a transparent gel C;

d) Weigh eucalyptus oil, zedoary oil, javanica javanica oil, eugenol, self-emulsifying compound emulsifier AC-402, and olive emulsifier in beaker 1, heat in a water bath at 60-90°C, and use it as the oil phase for later use;

e) Measure 1-10ml of distilled water into beaker 2, heat in a water bath at 60-90°C, use it as the water phase, and set aside;

f) Add the distilled water in beaker 2 into beaker 1 in a thin stream, and stir in the same direction while adding to form emulsion matrix a, set aside;

g) adding gel A, gel B, and gel C to emulsion matrix a to form matrix b for later use;

h) Disperse urea, salicylic acid, and boric acid in 1-6ml of distilled water to form a solution a for later use;

i) Disperse camphor and borneol in 1-5ml of 75% ethanol to form solution b, set aside;

j) Add solution a, solution b, azone, glycerol, 1,2-propanediol, fennel extract, Sophora flavescens extract, 5% ethylparaben alcohol solution to matrix b, stir and mix evenly, that is Get a lotion for nail fungus.

The present invention uses self-emulsifying composite emulsifier AC-402 and olive emulsifier as emulsifier, sodium carboxymethyl cellulose, sodium alginate, hydroxypropyl methyl cellulose as emulsification stabilizer, glycerin, 1 , 2-propanediol is a co-emulsifier. The 5% ethylparaben alcohol solution is a weight concentration, wherein the alcohol can be ethanol, propylene glycol, glycerin and the like.

Various compositions among the present invention are as follows:

Eucalyptus oil has an antiviral effect and is the most effective for respiratory diseases. It can relieve inflammation and make the nasal mucosa comfortable. It is especially helpful for sinusitis, influenza, cough, nasal catarrh, asthma and tuberculosis. It has obvious effects on burns, prevents bacteria and fungi from growing and subsequent pus, and promotes the construction of new tissues. Cuts, wounds, ulcers and inflammatory conditions all respond well to eucalyptus.

Brucea javanica oil penetrates deep into the skin and inhibits fungi. Its main component is oleic acid, which can inhibit the activity of topoisomerase (TOPOII), thereby inhibiting the synthesis and growth of cellular DNA, and blocking the proliferation of fungi.

Curcuma oil has a wide antibacterial spectrum, and has antibacterial effects on skin filamentous bacteria, Candida, yeast, black filamentous bacteria, Aspergillus, Penicillium, and actinomycetes. It also has antibacterial activity against some Gram-positive bacteria. Its mechanism of action is to act on the cell membrane of pathogenic bacteria, change its permeability, prevent nutrient uptake, and cause its death.

Eugenol has a strong inhibitory effect on common food contamination bacteria Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Hansenula, Aspergillus niger, Penicillium, etc. A small amount of eugenol is dropped into the cavity of dental caries, in addition to playing a disinfection role, and destroying its nerves, thereby relieving toothache. It can also inhibit epidermis fungi.

Urea is a very useful moisturizing ingredient. It exists in the stratum corneum of the skin and is the main component of the skin's natural moisturizing factor NMF. For the skin, urea has the effect of moisturizing and softening the cutin, thus assisting the penetration of active ingredients.

Salicylic acid can irritate the skin and mucous membranes, and because it can react with proteins in body tissues, it can make the cornea proliferate and then peel off.

Sophora flavescens is rich in matrine, which has anti-pathogen effect and also has inhibitory effect on Mycobacterium tuberculosis.

Fennel contains volatile oils, organic acids, flavonoids, anisole, anisaldehyde and other active ingredients, which have a good inhibitory effect on Escherichia coli and Shigella. It can help kill harmful bacteria in the gastrointestinal tract and epidermis, and promote the healing of inflammation and ulcers.

Camphor has mild stimulation and antiseptic effect when applied to the skin. Rubbing vigorously has a reddening effect; lightly applying it is like mint. Camphor also has inhibitory effect on common pathogenic fungi, can improve local blood circulation, and can promote mucous membrane secretion.

Borneol can inhibit or kill common clinical bacteria such as Staphylococcus aureus, beta-hemolytic streptococcus, and Streptococcus viridans. Borneol also has antibacterial effects on five common fungi such as rubrum rubrum. , causing cell membrane damage, destruction and changes in its permeability.

The emulsion for treating onychomycosis prepared by the invention has strong functionality and little toxicity and irritation. Brucea javanica oil can inhibit fungal reproduction and effectively prevent fungal infection. Sophora flavescens extract has anti-inflammatory and antibacterial effects. The ingredients in the formula complement each other. Compared with traditional medicines, the treatment effect is better, the permeability is stronger, and the recurrence is lower, and it fundamentally treats onychomycosis caused by various fungi.

detailed description

The following examples are a further description of the content of the present invention as an explanation of the technical content of the present invention, but the essential content of the present invention is not limited to the following examples, those of ordinary skill in the art can and should know any Simple changes or replacements of the essential spirit of the invention shall fall within the scope of protection required by the present invention.

1 Preparation of fennel extract

Take 15g of Sophora flavescens, crush it into a coarse powder, and extract it three times: add 200ml of 0.2% hydrochloric acid for the first time, soak for 30 minutes, extract by reflux extraction for 2 hours, collect the extract by filtration, and add 150ml of 0.2% hydrochloric acid to the filter residue for the second time Extract for 2 hours, collect the extract by filtration, add 120 ml of 0.2% hydrochloric acid to the filter residue for the third time to extract for 1 hour, combine the three filtrates, mix and concentrate to 90 ml.

2 Preparation of Sophora flavescens extract

Take 15g of fennel, crush it into a coarse powder, and extract it three times: first add 300ml of 75% ethanol to soak for 30min, use reflux extraction for 1.5h, collect the extract, add 200ml of 75% ethanol to the filter residue for 1h, collect and extract liquid, add 150ml of 75% ethanol to the filter residue for the third time to extract for 1h, filter each time, combine the three filtrates, mix and concentrate to 90ml.

Example 1

The preparation method of treating onychomycosis emulsion

a) Weigh 0.04g of sodium alginate, disperse it in 10ml of distilled water, and fully swell into a transparent gel A:

b) Weigh 0.05g of sodium carboxymethylcellulose, disperse it in 6ml of distilled water, and fully swell into a transparent gel B:

c) Weigh 0.06g of hydroxypropyl methylcellulose, disperse it in 6ml of distilled water, and fully swell into a transparent gel C:

d) Weigh 1.0g of eucalyptus oil, 0.7g of zedoary oil, 0.6g of javanica javanica oil, 1.0g of self-emulsifying compound emulsifier AC-402, and 0.5g of olive emulsifier in beaker 1, and heat it in a water bath at 90°C to be used as oil Phase, standby;

e) Measure 8ml of distilled water in beaker 2, heat it in a water bath at 90°C, and use it as the water phase for later use;

f) When the oil phase and the water phase reach the same temperature, add the distilled water in the beaker 2 into the beaker 1 in a trickle, and stir in the same direction while adding to form the emulsion matrix a, set aside;

g) adding gel A, gel B, and gel C to emulsion matrix a to form matrix b for later use;

h) Disperse 0.5g of urea, 0.3g of salicylic acid and 0.2g of boric acid in 6ml of distilled water to form a solution a for later use;

i) Disperse 0.5g camphor and 0.5g borneol in 5ml75% ethanol to form solution b, set aside;

j) Add solution a, solution b, azone 0.1g, glycerol 5ml, 1,2-propanediol 5ml, fennel extract 5ml, Sophora flavescens extract 5ml, 5% ethylparaben propylene glycol solution to matrix b 4ml, stir and mix evenly to get the emulsion for treating onychomycosis.

Example 2

The preparation method of treating onychomycosis emulsion

a) Weigh 0.05 g of sodium alginate, disperse it in 12 ml of distilled water, and fully swell to form a transparent gel A.

b) Weigh 0.10 g of sodium carboxymethyl cellulose, disperse it in 10 ml of distilled water, and fully swell into a transparent gel B;

c) Weigh 0.12 g of hydroxypropyl methylcellulose, disperse it in 10 ml of distilled water, and fully swell it into a transparent gel C;

d) Weigh 0.8g of eucalyptus oil, 0.6g of zedoary oil, 0.6g of javanica javanica oil, 1.0g of self-emulsifying compound emulsifier AC-402, and 0.4g of olive emulsifier in beaker 1, and heat it in a water bath at 80°C as oil Phase, standby;

e) Measure 10ml of distilled water in beaker 2, heat it in a water bath at 80°C, and use it as the water phase for later use;

f) When the oil phase and the water phase reach the same temperature, add the distilled water in the beaker 2 into the beaker 1 in a trickle, and stir in the same direction while adding to form the emulsion matrix a, set aside;

g) adding gel A, gel B, and gel C to emulsion matrix a to form matrix b for later use;

h) Disperse 0.4g of urea, 0.2g of salicylic acid, and 0.1g of boric acid in 5ml of distilled water to form solution a for later use;

i) Disperse 1g of camphor and 0.5g of borneol in 5ml of 75% ethanol to form solution b for subsequent use;

j) Add solution a, solution b, azone 0.05g, glycerol 4ml, 1,2-propanediol 4ml, fennel extract 4ml, Sophora flavescens extract 4ml, 5% ethylparaben propylene glycol solution to matrix b 3ml, stir and mix evenly to get the emulsion for treating onychomycosis.

Example 3

The preparation method of treating onychomycosis emulsion

a) Weigh 0.06g of sodium alginate, disperse it in 15ml of distilled water, and fully swell into a transparent gel A;

b) Weigh 0.07g of sodium carboxymethylcellulose, disperse it in 10ml of distilled water, and fully swell into a transparent gel B;

c) Weigh 0.12 g of hydroxypropyl methylcellulose, disperse it in 10 ml of distilled water, and fully swell it into a transparent gel C;

d) Weigh 1.0g of eucalyptus oil, 0.7g of zedoary oil, 0.6g of javanica javanica oil, 0.8g of self-emulsifying compound emulsifier AC-402, and 0.5g of olive emulsifier in beaker 1, and heat it in a water bath at 90°C to be used as oil Phase, standby;

e) Measure 8ml of distilled water in beaker 2, heat it in a water bath at 90°C, and use it as the water phase for later use;

f) When the oil phase and the water phase reach the same temperature, add the distilled water in the beaker 2 into the beaker 1 in a trickle, and stir in the same direction while adding to form the emulsion matrix a, set aside;

g) adding gel A, gel B, and gel C to emulsion matrix a to form matrix b for later use;

h) Disperse 0.4 g of urea, 0.2 g of salicylic acid, and 0.2 g of boric acid in 6 ml of distilled water to form solution a, which is set aside;

i) Disperse 0.5g camphor and 0.5g borneol in 5ml75% ethanol to form solution b, set aside;

j) Add solution a, solution b, azone 0.1g, glycerol 5ml, 1,2-propanediol 3ml, fennel extract 3ml, Sophora flavescens extract 3ml, 5% ethylparaben propylene glycol solution to matrix b 4ml, stir and mix evenly to get the emulsion for treating onychomycosis.

Test example 1

The physicochemical index of embodiment 1-3 gained emulsion is as follows:

1 character

This product is a light brownish-yellow emulsion with a relatively thin, fine and uniform consistency and good spreadability.

2pH check

Take this product and measure it with a pH meter, and the measured pH value is between 6.8-7.0.

3 hot and cold test

The emulsion was packaged in a transparent emulsion bottle and refrigerated in a refrigerator at 4°C for one month to observe no delamination. Put it in a constant temperature box at 55°C for 24 hours, and the emulsion has no delamination and odor change.

4 Centrifugal test

The emulsion was packaged in a stoppered test tube and centrifuged at 3000r/min for 20min, without stratification.

5 Placement experiment at room temperature

The embodiment emulsion is placed in the emulsion bottle, and the room temperature is left to stand for 6 months, and there is no delamination phenomenon, and there is no change in the feeling after use, and the smell does not change.

6 irritation test, allergy test

The hair on the back of the mouse was cut off, and the emulsion prepared according to the embodiment was applied to the cut off area respectively, and compared with the uncoated area, the results showed no irritation and allergic reaction.

Appropriate amount of the example was applied to the hands of volunteers (16-50 years old, 80 people), observed after 30 minutes, no redness, rash, and blistering occurred.

Test example 2

The comprehensive effect investigation of the treatment of onychomycosis emulsion obtained in embodiment 1-3 of the present invention.

The efficacy of the treatment of onychomycosis emulsion that embodiment 1-3 manufactures is evaluated below by curative effect. Using the public opinion survey scoring method, 120 patients aged 20-60 were selected as the trial objects. Arbitrarily divide into three groups, apply on the affected part with the treatment of onychomycosis emulsion that embodiment 1,2,3 manufactures respectively. Use twice a day for three months. The total score of each effect is 5: 5 is the highest score, which means very good and very satisfied; 4 is good; 3 is acceptable; below 3 is bad and unacceptable. Below are the average scores for each category. The results are shown in Table 1:

Table 1 Comprehensive effect investigation

To sum up, this product has a good smell, is delicate and even, and has a good effect on treating onychomycosis with little irritation.

Claims (5)

1. treat an Emulsion for tinea unguium, wherein include the material of following consumption:

2. the Emulsion for the treatment of tinea unguium according to claim 1, is characterized in that, also includes the material of following dosage:

3. the Emulsion for the treatment of tinea unguium according to claim 1, it is characterized in that, described Radix Sophorae Flavescentis extractive liquid prepares by the following method: get Radix Sophorae Flavescentis 2-15g, be ground into coarse powder, divide and extract for three times: the soak with hydrochloric acid 5-30min adding 150-200ml0.1%-0.5% for the first time, 0.5-2h is extracted with reflux extraction, collect extracting solution, second time adds the hydrochloric acid extraction 0.5-2h of 130-150ml0.1%-0.5%, collect extracting solution, add the hydrochloric acid extraction 0.5-1h of 100-120ml0.1%-0.5% for the third time, each filtration, merge three filtrates, mixing is concentrated into 10-90ml.

4. the Emulsion for the treatment of tinea unguium according to claim 1, it is characterized in that, described Fructus Foeniculi extracting solution prepares by the following method: get Fructus Foeniculi 2-15g, be ground into coarse powder, divide and extract for three times: first time adds 200-300ml70%-80% soak with ethanol 5-30min, 0.5-1.5h is extracted with reflux extraction, collect extracting solution, second time adds 150-200ml70%-80% ethanol extraction 0.2-1h, collect extracting solution, third time adds 100-150ml70%-80% ethanol extraction 0.2-1h, each filtration, merge three filtrates, mixing is concentrated into 10-90ml.

5. the preparation method of the Emulsion of the treatment tinea unguium described in any one of claim 2-4, comprises the steps:

A) take sodium alginate, be scattered in 10-15ml distilled water, be fully swelled into transparent gel A;

B) take sodium carboxymethyl cellulose, be scattered in 6-10ml distilled water, be fully swelled into transparent gel B;

C) take hydroxypropyl emthylcellulose, be scattered in 6-10ml distilled water, be fully swelled into transparent gel C;

D) eucalyptus oil, Oleum Curcumae, Oleum Fructus Bruceae, eugenol, self emulsifying mixed emulsifier AC-402, Fructus Canarii albi emulsifying agent is taken in beaker 1,60-90 DEG C of heating in water bath, as oil phase, for subsequent use;

E) distilled water 1-10ml is measured in beaker 2,60-90 DEG C of heating in water bath, as aqueous phase, for subsequent use;

F) be that thread shape adds in beaker 1 by the distilled water in beaker 2, limit edged stirs towards same direction, forms emulsion bases a, for subsequent use;

G) in emulsion bases a, add gel A, gel B, gel C, form substrate b, for subsequent use;

H) carbamide, salicylic acid, boric acid are scattered in 1-6ml distilled water, form solution a, for subsequent use;

I) Camphora, Borneolum Syntheticum are scattered in 1-5ml75% ethanol, form solution b, for subsequent use;

J) in substrate b, add solution a, solution b, azone, glycerol, 1,2-PD, Fructus Foeniculi extracting solution, Radix Sophorae Flavescentis extractive liquid, 5% ethyl hydroxybenzoate alcoholic solution, be uniformly mixed, the Emulsion of tinea unguium must be treated.