CN115192639A - Medicine for treating eczema and preparation method thereof - Google Patents

Abstract

The invention discloses a medicine for treating eczema and a preparation method thereof, belonging to the field of traditional Chinese medicines. The traditional Chinese medicine is prepared from the following raw material medicines in percentage by mass: alum = 1. For damp-heat syndrome of extreme dampness-heat, skin accumulation and heat in excess of dampness in the acute stage of atopic dermatitis, the skin damage of patients in the stage of atopic dermatitis can be effectively improved and exudation and erosion can be reduced by externally applying medicines which are compatible with coptis chinensis and alum; reduce the content of Th2 cell factor in serum and inhibit the protein expression of TLR4 and p-NF-kappa B.

Description

Medicine for treating eczema and preparation method thereof

Technical Field

The invention relates to the field of traditional Chinese medicines, in particular to a medicine for treating eczema and a preparation method thereof.

Background

Atopic Dermatitis (AD) is a common chronic inflammatory skin disease in clinic, is mainly characterized by pruritus, erythema and severe papule, has repeated attack characteristics, needs long-term treatment and is a huge damage and injury to physical and mental health of patients. AD is an incurable chronic disease at present, drugs for clinical treatment mainly comprise glucocorticoid, and can cause serious side effects after long-term use, so that the search for efficient and safe anti-AD drugs is very important.

Disclosure of Invention

The invention aims to overcome the defects of the prior art and provide a medicine for treating eczema and a preparation method thereof, and the medicine can effectively improve the skin damage of patients in atopic dermatitis attack stage and reduce exudation and erosion.

In order to achieve the purpose, the invention adopts the technical scheme that: the medicine for treating eczema is prepared from the following raw material medicines in parts by weight: alum = 1.

AD belongs to the categories of infantile eczema and blood-wind sore in traditional Chinese medicine, and doctors of different generations believe that the disease is caused by the mutual attack of internal damp-heat, external wind, dampness and heat evil and internal and external pathogenic factors on the skin. In the traditional Chinese medicine, mr. TaidouZhao Zhan, mr. Puhan, believes that the intrinsic damp-heat and the damp-heat exogenous pathogenic factor are mutually struggled and combined, which is the essence of the disease, the damp-heat pathogen runs through all the time, the dampness is heavy and turbid and is difficult to remove, the dampness is stagnated to transform into heat after a long time, and the damp-heat pathogens are caused and caused mutually, so that the persistent and difficult to heal is caused.

The inventor finds that for the damp-heat accumulation, skin accumulation and damp-heat syndrome with heat over dampness in the acute AD stage, coptis chinensis and alum are externally used for matching medicines and generate a synergistic effect on the coptis chinensis and the alum, so that the skin damage performance of a patient in the attack stage of AD can be effectively improved, and exudation and erosion are reduced.

The medicine has effects of clearing heat, eliminating dampness, etc., and can be used for treating atopic dermatitis such as eczema.

The invention is proved by a dinitrochlorobenzene patch test (DNCB) -induced atopic dermatitis model test that the medicament has the effects of remarkably reducing the skin damage area, exudation and other symptoms of mice, can obviously reduce the content of Th2 type cytokines in peripheral blood serum of the mice and inhibit the protein expression of TLR4 and p-NF-kappa B.

Preferably, the medicine is prepared from the following raw material medicines in parts by weight: alum =2 to 5. Within the specific mass ratio range, the medicament has a more obvious inhibiting effect on protein expression of TLR4 and p-NF-kappa B, and can effectively reduce the skin damage area and exudation and other symptoms of mice.

Preferably, the medicine is prepared from the following raw material medicines in parts by weight: alum = 2. The inventor finds that when the mass ratio of the coptis chinensis to the alum is 2.

Preferably, the dosage form of the medicament is an external dosage form.

Preferably, the external preparation is lotion, ointment, gel, paste, coating agent, cataplasm or external aerosol.

The dosage form of the drug of the present invention is not particularly limited, and may be any dosage form suitable for external treatment of mammals; preferably, the dosage form may be selected from: liquid preparation for external use, patch, ointment, gel, paste, plastics, cataplasm or aerosol for external use. From the standpoint of ease of preparation and administration, liquid external preparations, particularly solutions and lotions, are preferred.

The composition of the invention can be added with various conventional carriers or auxiliary materials required for preparing different formulations, such as penetration enhancers (such as peppermint and borneol), excipients (such as starch), antioxidants and the like. Can be prepared into any common dosage form such as liquid external preparation, patch, ointment, gel, etc. by conventional Chinese medicinal preparation method.

Preferably, the medicament contains a pharmaceutically acceptable carrier.

As used herein, an ingredient of the term "pharmaceutically acceptable" is one that is suitable for use in humans and/or animals without undue adverse side effects (such as toxicity, irritation, and allergic response), i.e., at a reasonable benefit/risk ratio.

As used herein, the term "pharmaceutically acceptable carrier" refers to a carrier for administration of a therapeutic agent, including various excipients and diluents and the like. The term refers to such pharmaceutical carriers: they are not necessary active ingredients per se and are not excessively toxic after administration. Suitable carriers are well known to those of ordinary skill in the art. A thorough discussion of pharmaceutically acceptable excipients can be found in Remington's pharmaceutical Sciences (Mack pub. Co., n.j.1991). Pharmaceutically acceptable carriers in the compositions may comprise liquids such as water, saline, glycerol and ethanol. In addition, auxiliary substances may also be present in these vectors, including but not limited to: mannitol, sorbitol, sodium metabisulfite, sodium bisulfite, sodium thiosulfate, cysteine hydrochloride, thioglycolic acid, methionine, vitamin C, disodium EDTA, calcium sodium EDTA, monovalent alkali metal carbonates, acetates, phosphates or aqueous solutions thereof, hydrochloric acid, acetic acid, sulfuric acid, phosphoric acid, amino acids, sodium chloride, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivatives, cellulose and derivatives thereof, alginates, gelatin, polyvinylpyrrolidone, glycerol, tween 80, agar, calcium carbonate, calcium bicarbonate, surfactants, polyethylene glycol, cyclodextrin, beta-cyclodextrin, phospholipid-like materials, kaolin, talc, calcium stearate, magnesium stearate. However, it will be appreciated by those skilled in the art that the pharmaceutically acceptable carriers useful in the present invention are not limited to the above types.

In a second aspect, there is also provided a process for the preparation of the medicament, comprising the steps of:

(1) Weighing coptis chinensis and alum according to the weight ratio of 1;

(2) The preparation is prepared by taking the medicinal powder of the raw material medicines or the water extract of the raw material medicines as active ingredients and adding a pharmaceutically acceptable carrier.

Preferably, when the preparation is powder, the preparation method comprises the following steps: (1) Respectively pulverizing Coptidis rhizoma and Alumen into fine powder, mixing at a preferred ratio, and making into powder.

Preferably, when the preparation is a lotion, the preparation method comprises the following steps: (1) Mixing Coptidis rhizoma and Alumen, adding water, decocting for the first time, filtering, adding water to the residue, decocting for the second time, filtering, mixing filtrates, and concentrating to obtain concentrated solution, which is lotion; the concentrated solution has a drug content of 0.05-0.1g/ml.

Preferably, when the preparation is an ointment or a gel, the preparation method comprises (1) respectively crushing coptis chinensis and alum into fine powder, mixing according to a preferred proportion, and adding auxiliary materials to prepare the ointment or the gel.

In a third aspect, the invention also provides application of the medicine in preparing a medicine for treating eczema.

The medicament of the present invention can be directly used for treating atopic dermatitis. The amount of the drug of the present invention to be used may vary depending on the mode of administration, the dosage form and the severity of the disease to be treated. For example, a single dose may be administered several times separately per day, or the dose may be reduced proportionally as required by the condition being treated. Of course, the particular dosage will also take into account such factors as the mode of administration, the physical condition of the subject, and the like, which are within the skill of the art.

Compared with the prior art, the invention has the following beneficial effects: the medicine has the effects of clearing heat, eliminating dampness and the like, can be used for treating atopic dermatitis, and has an obvious effect on typical symptoms caused by the atopic dermatitis, such as pruritus, erythema or serious pimple. The medicine takes common traditional Chinese medicinal materials as raw materials, exerts the advantage of low toxic and side effects of the traditional Chinese medicines, and has clinical application value of safety, effectiveness, low price and easy wide popularization.

Drawings

FIG. 1 is a graph showing the effect of the drug of the present invention on skin lesions of atopic dermatitis model mice;

FIG. 2 is a graph showing the effect of the drug of the present invention on the number of scratching of atopic dermatitis model mice;

FIG. 3 is a graph showing the effect of the drug of the present invention on serum inflammatory factor levels in mice model of atopic dermatitis;

FIG. 4 shows the effect of the drugs of the present invention on TLR 4/NF-. Kappa.B pathway protein in atopic dermatitis model mice.

Detailed Description

To better illustrate the objects, aspects and advantages of the present invention, the present invention is further illustrated by the following examples and the accompanying drawings. It is apparent that the following examples are only a part of the embodiments of the present invention, and not all of them. It should be understood that the embodiments of the present invention are only for illustrating the technical effects of the present invention, and are not intended to limit the scope of the present invention.

Example 1

The embodiment provides a preparation method of a lotion of a medicine, which comprises the following raw material medicines in percentage by mass: coptis root: alum = 20.

The preparation method of the lotion comprises the following steps: (1) Mixing coptis chinensis and alum, adding water with the volume of 8 times that of the raw materials, decocting for the first time, filtering, adding water with the volume of 6 times that of the filter residue into the filter residue, decocting for the second time, filtering, combining the two filtrates, concentrating the filtrate to obtain a concentrated solution, namely a lotion, wherein the medicine content of the lotion is 0.0525g/ml.

Example 2

The embodiment provides a preparation method of a lotion of a medicine, which comprises the following raw material medicines in percentage by mass: coptis chinensis: alum = 10.

The preparation method of the lotion comprises the following steps: (1) Mixing rhizoma Coptidis and Alumen, adding 8 times of water, decocting for the first time, filtering, adding 6 times of water to the residue, decocting for the second time, filtering, mixing the two filtrates, and concentrating the filtrate to obtain concentrated solution as lotion with a dosage of 0.055g/ml.

Example 3

The embodiment provides a preparation method of a lotion of a medicine, which comprises the following raw material medicines in percentage by mass: coptis chinensis: alum = 5.

The preparation method of the lotion comprises the following steps: (1) Mixing rhizoma Coptidis and Alumen, adding water 8 times the volume of the raw materials, decocting for the first time, filtering, adding water 6 times the volume of the residue into the residue, decocting for the second time, filtering, mixing the two filtrates, concentrating the filtrate to obtain concentrated solution as lotion, wherein the dosage of the lotion is 0.06g/ml.

Example 4

The embodiment provides a preparation method of a lotion of a medicine, which comprises the following raw material medicines in percentage by mass: coptis chinensis: alum = 2.

The preparation method of the lotion comprises the following steps: (1) Mixing rhizoma Coptidis and Alumen, adding water 8 times the volume of the raw materials, decocting for the first time, filtering, adding water 6 times the volume of the residue into the residue, decocting for the second time, filtering, mixing the two filtrates, concentrating the filtrate to obtain concentrated solution as lotion, wherein the content of the lotion is 0.075g/ml.

Example 5

The embodiment provides a preparation method of a lotion of a medicine, which comprises the following raw material medicines in percentage by mass: coptis chinensis: alum = 1.

The preparation method of the lotion comprises the following steps: (1) Mixing rhizoma Coptidis and Alumen, adding water 8 times the volume of the raw materials, decocting for the first time, filtering, adding water 6 times the volume of the residue into the residue, decocting for the second time, filtering, mixing the two filtrates, concentrating the filtrate to obtain concentrated solution as lotion, wherein the dosage of the lotion is 0.1g/ml.

Example 6

The embodiment provides a preparation method of a medicinal ointment, which comprises the following raw material medicines in percentage by mass: coptis root: alum = 1.

The preparation method of the ointment comprises the following steps: respectively pulverizing Coptidis rhizoma and Alumen into fine powder, mixing at a certain proportion, adding Cera flava and yellow Vaseline, stirring at 50 deg.C for 1h, and cooling to obtain ointment.

Example 7

The embodiment provides a preparation method of a gel of a medicine, which comprises the following steps: adding carbomer into glycerol, grinding to moisten, adding small amount of distilled water, grinding, transferring into a measuring cup, dissolving triethanolamine, ethylparaben and distilled water, stirring to obtain gel, adding distilled water, and stirring; adding the concentrated solution obtained in the example 4, and grinding uniformly to obtain the gel.

Example 8

Effects of the drug of the present invention on atopic dermatitis model mice.

1. Test methods and groups:

BALB/c male mice, 6-8 weeks old, were taken and all animal experiments were performed in a pathogen-free environment and in accordance with the Chinese animal welfare method. DNCB animal models are respectively established, experiments are divided into 5 groups, and the models are randomly divided into a normal control group, a model group, a drug low, medium and high dose group, and each group is provided with 10 drugs.

Except for the normal control group, the other groups were molded by the following method: on the day of shaving (day 1) and day 4, 200uL of 1-percent DNCB solution was applied to the shaved area, the allergic period was induced, and 200uL of 0.5-percent DNCB solution was administered 3 times per week (fixed days 1, 3, 5) starting at week 2-5. The normal group is given the mixture of acetone and olive oil (the mass ratio of acetone to olive oil is 1.

After the molding is successful, the rat is placed on a fixed frame, and the affected part of the rat is dipped in physiological saline at 40 ℃ for 10min by a cotton swab in a normal control group (Con); diluting the lotion obtained in example 4 into a low drug (L), a medium drug (M) and a high drug (H) group respectively, wherein the drug content of the low drug (L) group is 0.000974g/ml, the drug content of the medium drug (M) group is 0.001948g/ml, and the drug content of the high drug (H) group is 0.003896g/ml, dipping the low drug (L), the medium drug (M) and the high drug (H) groups with a cotton swab at 40 ℃, and dipping affected parts of mice for 10min; the Model set (Model) does not process. 1 time per day for a total of 28 days.

2. Observation of indices

2.1 general case and behavior Observation: weighing the weight of the mouse every other day and recording the general condition of the mouse; the mice were individually placed on the 1d, 7d, 14d, 21d and 28d, and the behavior was recorded by a mobile phone for 10min, and the number and duration of front-paw scratching and scratching of the head and ears and rear-paw scratching of the trunk and back of the mouse were counted within 10min, and the number of continuous scratching was counted as 1.

2.2 skin lesion inflammation degree score: the dynamic changes of the skin lesions on the back of the mice were recorded by taking pictures with a camera every other day, and scored at the 1 st, 7 th, 14 th and 21 st days of the start of the experiment with reference to the clinical atopic dermatitis Score (SCORAD) index, the scoring criteria including 4 points of erythema/hemorrhage, edema/exudation, dryness/desquamation, epidermal exfoliation, divided into four grades of none (0), mild (1), moderate (2) and severe (3), 4 symptoms added up to the final score, the score being between 0 and 12.

2.3 histopathological evaluation: after the experiment is finished, the back skin of each group of mice is taken, dehydrated, fixed and embedded in paraffin to prepare paraffin sections, the histological characteristics of the skin lesions of the mice are observed by adopting hematoxylin-eosin staining, the thickening condition of the epidermis is analyzed by image analysis software, 5 sections are selected for each tissue, 5 visual fields are selected for each section, the vertical distance from the cuticle layer to the basal layer of the epidermis is measured, and the vertical distance is compared.

3. Results of the experiment

3.1 Effect of the drugs of the present invention on general conditions and scratching behavior of DNCB model mice

After the normal control group mice are smeared with the mixture of acetone olive oil, no obvious inflammatory damage exists on the back/ear skin; compared with a normal group, after the model group mice are coated with DNCB for the first time, the skin firstly has acute inflammatory reactions such as obvious edema, exudation and the like, and with the increase of the coating times, chronic changes such as erythema, erosion and the like begin to appear, and the skin is dry and desquamation, so that tawny dementia gradually forms on the surface of the skin, hairs at the scab position are sparse and lusterless, animals have scratching, AD-like dermatitis symptoms appear, and the clinical manifestations of the AD-like dermatitis are consistent with those of atopic dermatitis. As can be seen from the graphs in fig. 1 and fig. 2, when the coptidis rhizome and alum water decoction is applied to the skin lesion parts of mice, erythema, erosion and scab are gradually removed, and the scratching times are obviously reduced compared with the model group, which shows that the coptidis rhizome and alum water decoction has obvious inhibition effect on AD-like dermatitis of mice induced by DNCB. ( Note: # p <0.001 compared to normal control group; compared to model group, p <0.001, p <0.01, p <0.05. )

3.2 Effect of the inventive Agents on Th2 cytokines IL-4, IL-6 and IL-10 in serum

As can be seen from FIG. 3, the levels of IL-4, IL-6 and IL-10 in the model group were significantly increased as compared with the normal group; compared with the model group, the administration group can obviously inhibit the increase of IL-4, IL-6 and IL-10. ( Note: # p <0.001, compared to the normal control group; compared to model group, p <0.001, p <0.01, p <0.05. )

3.3 the expression action of the drug of the invention on TLR 4/NF-kB pathway protein in skin protein

As can be seen from FIG. 4, the expression of TLR4 and p-NF-kB in the model group is obviously increased compared with that in the normal group; compared with the model group, the protein expression is obviously reduced after the administration.

Finally, it should be noted that the above embodiments are intended to illustrate the technical solutions of the present invention and not to limit the scope of the present invention, and although the present invention has been described in detail with reference to the preferred embodiments, it should be understood by those skilled in the art that modifications and equivalent substitutions can be made to the technical solutions of the present invention without departing from the spirit and scope of the technical solutions of the present invention.

Claims (8)

1. The medicine for treating eczema is characterized by being prepared from the following raw material medicines in parts by weight: alum = 1.

2. The medicine of claim 1, wherein the medicine is prepared from the following raw material medicines in parts by weight: alum =2 to 5.

3. The medicine of claim 1, wherein the medicine is prepared from the following raw material medicines in parts by weight: alum = 2.

4. The medicament of claim 1, wherein the medicament is in a form for external use.

5. The medicament of claim 4, wherein the external dosage form is a lotion, paste, gel, paste, film, cataplasm or external aerosol.

6. The medicament of claim 5, wherein the medicament comprises a pharmaceutically acceptable carrier.

7. A process for the preparation of a medicament as claimed in any one of claims 1 to 6, comprising the steps of:

(1) Weighing coptis chinensis and alum according to the weight ratio of 1;

(2) The preparation is prepared by taking the medicinal powder of the raw material medicines or the water extract of the raw material medicines as active ingredients and adding a pharmaceutically acceptable carrier.

8. Use of a medicament as claimed in any one of claims 1 to 6 in the manufacture of a medicament for the treatment of eczema.

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