CN111514130A - Composition for treating whelk - Google Patents
Composition for treating whelk Download PDFInfo
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- CN111514130A CN111514130A CN202010058294.9A CN202010058294A CN111514130A CN 111514130 A CN111514130 A CN 111514130A CN 202010058294 A CN202010058294 A CN 202010058294A CN 111514130 A CN111514130 A CN 111514130A
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- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
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- A61P17/10—Anti-acne agents
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Abstract
The invention belongs to the field of external medicines and/or cosmetics, and relates to application of arctigenin in preparation of anti-acne medicines and/or cosmetics. When the arctigenin disclosed by the invention is used for removing acnes, the treatment effect is obvious, and the arctigenin is safe and nontoxic and has a good application prospect.
Description
Technical Field
The invention belongs to the field of medicines and/or cosmetics, and particularly relates to application of arctigenin in preparation of anti-acne medicines and/or cosmetics.
Background
Acne, also known as acne, is a common skin disease affecting hair follicles and sebaceous glands and occurs well on the face, chest, back and other parts rich in sebaceous glands. Statistical data of a multinational health monitoring system show that about 85% of people have whelks in the age of 12-24 years, and the incidence rate tends to increase year by year. The pathogenesis of the skin disease is various, and the increase of the secretion of androgens in puberty is generally considered to cause the hyperplasia of sebaceous glands and the increase of sebum secretion, and at the same time, the hair follicles and the ducts of the sebaceous glands are subjected to keratosis embolism, and sebum is accumulated in the hair follicles to form lipid embolism. Under anaerobic environment, a large amount of anaerobic bacteria such as propionibacterium acnes proliferate to generate lysolipase, sebum is separated to generate free fatty acid, hair follicle wall damage is broken, and the free sebum enters into dermis, so that the surrounding degree of hair follicles is unequal.
Aiming at the different pathogenic links, the current acne treatment methods are various and mainly comprise local drug treatment (vitamin cream, benzoyl peroxide, antibiotic preparations and the like), oral drug treatment (antibiotics, antiandrogens, vitamins and the like) and various phototherapies (blue light, red light, photodynamic therapy and the like), but the drugs are still the first method for treating the acne at present. Sebaceous glands are important organs related to the pathogenesis of whelk, and hyperseborrhea caused by the increase of the activity of the sebaceous glands is a main primary factor of whelk, so that the inhibition of the activity of the sebaceous glands and the control of the sebaceous secretion are important ways for effectively treating the whelk. The isovitamin is considered to be the most effective sebaceous gland inhibitor nowadays, can play a role in multiple links of whelk, has the functions of shrinking sebaceous gland tissues, inhibiting sebaceous gland activity, reducing sebum secretion and epithelial cell keratinization and inhibiting propionibacterium acnes, and is considered to be a first-line medicament for acne treatment at present. However, studies have found that long-term systemic application of isotretinoin may cause various side effects such as brain damage, skin barrier dysfunction, intestinal mucosa damage, teratogeny, psychopsychological problems, etc., and thus, the clinical application of isotretinoin has certain limitations. Moreover, the course of acne is long, the recurrence rate of medicine withdrawal is high, and long-term medicine taking treatment is often needed, so that the acne treatment is still a very delicate problem, and the finding of an effective and relatively safe medicine for treating acne has obvious practical significance.
Fructus Arctii is dry mature fruit of Arctium lappa L.of Compositae, named fructus Arctii, fructus Muscovifolii, and fructus fici. The burdock belongs to common traditional Chinese medicines, and the traditional Chinese medicine considers that the traditional Chinese medicine has the effects of dispelling wind and heat, ventilating and smoothing lung, promoting eruption, relieving sore throat, resolving masses, detoxifying and reducing swelling, and is used for treating wind-heat type common cold, cough with excessive phlegm, measles, rubella, sore throat, mumps, erysipelas, carbuncle and sore. The western medicine considers that the traditional Chinese medicine composition has the pharmacological effects of promoting urination, removing food retention, eliminating phlegm, stopping diarrhea and the like, and is also used for food therapy of constipation, hypertension and hypercholesterolemia.
The fructus Arctii mainly contains lignanoid compounds, and mainly comprises arctiin and arctigenin. According to experimental research, the arctigenin has stronger physiological activity than arctiin, and the arctiin is decomposed into the arctigenin in vivo to generate a plurality of pharmacological actions. At present, the arctigenin has been reported to have the following pharmacological activities in the literature: 1) antiviral effects, including HIV-1 and influenza virus; 2) inducing apoptosis of tumor cells; 3) nephropathy, diabetes and diabetic complications; 4) inhibition of heat shock response; 5) neuroprotective effect; 6) the function of expanding blood vessels; 7) platelet activating factor antagonism; 8) anti-senile dementia effect; 9) inhibiting K + contracture, etc.
In the prior art, no research report on the treatment effect of arctigenin on whelk exists.
Disclosure of Invention
In order to solve the problems in the prior art, the invention provides the application of arctigenin in preparing medicines and/or cosmetics for removing acnes. The invention discloses that the arctigenin can effectively inhibit the proliferation of sebaceous glands and has a remarkable treatment effect on whelk. When the arctigenin disclosed by the invention is used for removing acnes, the treatment effect is obvious, and the arctigenin is safe and nontoxic and has a good application prospect.
Through a large number of experimental researches, the inventors find that arctigenin has obvious inhibition on sebaceous gland cell proliferation and can improve the tissue morphology of thickened sebaceous glands and tightly-arranged glands of golden-yellow mice. The arctigenin has obvious therapeutic effect on the auricular acne model of the New Zealand rabbit. Clinical tests show that the arctigenin can effectively treat whelk. Therefore, the arctigenin can play an important role in preparing the acne-removing medicine and/or the cosmetic.
The invention relates to application of arctigenin in preparing acne-removing medicines, and the pharmaceutical formulation of the arctigenin is an external preparation.
Preferably, the external preparation is powder, ointment, gel, cream, spray or patch thereof.
Wherein the external preparation is administered in the form of skin.
The arctigenin cosmetics of the invention can be various cosmetics in the field, such as soap, facial cleanser, toner, essence, emulsion or cream.
In the present invention, the content of arctigenin in the medicine and/or cosmetic is 0.0125 to 99.00 wt%, preferably 0.01 to 10 wt%, and more preferably 0.05 to 2 wt%.
The pharmaceutical and/or cosmetic composition of the present invention may further comprise other pharmaceutical ingredients or active ingredients, if necessary, and may further comprise a combination of active ingredients, for example, vitamin E, amino acids, blood circulation promoters, cell activation factors, and the like. These other pharmaceutical ingredients or active ingredients may or may not be used, depending on the preparation requirements.
In the pharmaceutical and/or cosmetic composition of the present invention, and in the pharmaceutical and/or cosmetic composition of the present invention, it is also included to add an auxiliary selected from conventional external pharmaceutical and/or cosmetic agents, such as a gelling agent, a thickener, a surfactant, a preservative, an antioxidant, an emulsifier, a humectant, a lubricant, a humectant, a binder, a preservative, a bactericide, a perfume and the like. These auxiliaries may be used alone or in combination, and the use or not and the use amount thereof depend on the requirements for preparing the dosage form.
Compared with the scheme in the prior art, the arctigenin provided by the invention has the following characteristics and advantages that:
(1) originality of the study: the inventor firstly discovers that the arctigenin has a strong acne removing effect at home and abroad, and the acne removing effect of the arctium fruit and the components thereof is not reported so far. The research result is original.
(2) Innovativeness of the study: the inventor breaks through the conventional process, develops Chinese herbal medicine treasury, and develops the effective, efficient, nontoxic, cheap and high-specificity arctigenin acne-removing medicine and/or cosmetic for external use.
(3) The practicability of the invention is as follows: research work of the inventor proves that arctigenin has a strong acne removing effect, and is effective and efficient to use externally and nontoxic.
In conclusion, the research integrates theoretical innovation, application innovation and technical innovation. The innovative project has forward looking, leading and exploratory leading-edge technology in secondary development and research of traditional Chinese medicine, and can create a new approach for treating the whelk.
Detailed Description
The following further illustrates the invention by way of specific examples, but it is to be understood that the examples are not to be construed as limiting the invention in any way.
Example 1 arctigenin cream
The preparation method comprises the following steps: taking stearic acid, glyceryl monostearate and ethylparaben according to the prescription amount, heating and melting in water bath, and preserving heat in water bath at 80 ℃ to prepare an oil phase; mixing triethanolamine, glycerol, ethylparaben and water, and keeping temperature in 80 deg.C water bath to obtain water phase. Slowly adding the oil phase into the water phase, adding arctigenin under stirring, and cooling to room temperature to obtain the final product.
Example 2 arctigenin cream
The preparation method comprises the following steps: taking stearic acid, glyceryl monostearate and ethylparaben according to the prescription amount, heating and melting in water bath, and preserving heat in water bath at 80 ℃ to prepare an oil phase; mixing triethanolamine, glycerol, ethylparaben and water, and keeping temperature in 80 deg.C water bath to obtain water phase. Slowly adding the oil phase into the water phase, adding arctigenin under stirring, and cooling to room temperature to obtain the final product.
Example 3 arctigenin gel
The preparation method comprises the following steps: dissolving carbomer in appropriate amount of purified water, standing for 24 hr for swelling, and adding triethanolamine; adding propylene glycol and glycerol into the swelled carbomer, and mixing to obtain carbomer gel; and finally, adding appropriate amount of purified water into arctigenin, ethylparaben and polyvinylpyrrolidone, heating to dissolve, cooling, adding into the carbomer gel, stirring, adding purified water to full amount, and mixing to obtain the final product.
Example 4 arctigenin gel
The preparation method comprises the following steps: dissolving carbomer in appropriate amount of purified water, standing for 24 hr for swelling, and adding triethanolamine; adding propylene glycol and glycerol into the swelled carbomer, and mixing to obtain carbomer gel; and finally, adding appropriate amount of purified water into arctigenin, ethylparaben and polyvinylpyrrolidone, heating to dissolve, cooling, adding into the carbomer gel, stirring, adding purified water to full amount, and mixing to obtain the final product.
Example 5 Arctiin ointment
The preparation method comprises the following steps: placing octadecanol, white vaseline, and liquid paraffin in a suitable container, and heating to 70 deg.C for melting. Mixing sodium laurylsulfate, ethylparaben, glycerol and purified water, dissolving, and heating to the same temperature. Slowly adding the oil phase into the water phase, adding arctigenin under stirring, and cooling to room temperature to obtain the final product.
Example 6 Arctiin ointment
The preparation method comprises the following steps: placing octadecanol, white vaseline, and liquid paraffin in a suitable container, and heating to 70 deg.C for melting. Mixing sodium laurylsulfate, ethylparaben, glycerol and purified water, dissolving, and heating to the same temperature. Slowly adding the oil phase into the water phase, adding arctigenin under stirring, and cooling to room temperature to obtain the final product.
Example 7 toner
The preparation process comprises the following steps:
1. mixing and heating the components of the phase A to 85 ℃, and fully dissolving and uniformly stirring; c is dissolved in advance;
2. cooling the phase A to 45 ℃, and adding B, C phase;
3. uniformly stirring and discharging, wherein the PH value is controlled to be 5.5-7.0.
Example 8 skin lotion
The preparation process comprises the following steps:
1. dispersing carbomer 941 in glycerol, dispersing in water while heating to 85 deg.C, adding other components of phase B, and stirring;
2. completely dissolving the phase A at 85 ℃, and uniformly stirring;
3. adding the phase A into the phase B, stirring and homogenizing (about 4 minutes), defoaming and cooling to 45 ℃;
4. adding the C phase components, stirring uniformly and discharging. The pH value is controlled to be 5.5-7.0.
Example 9 Effect of arctigenin of the present invention on growth and proliferation of sebaceous gland cells
Preparing the medicine: dissolving arctigenin in DMSO to obtain final concentration of 0.8, 1.6, 3.125, 6.25, 12.5, 25, 50 umol/L. The culture medium containing 0.2% DMSO and no test drug was used as a negative control.
And inoculating SZ95 cells into a 96-well plate at the density of 2000 cells/well, culturing for 24 hours, adding arctigenin with different concentrations and negative control, culturing for 72 hours and 96 hours, and adding MTT (methyl thiazolyl tetrazolium) to detect the growth and proliferation conditions of the cells. The absorbance values (A values) were determined on an enzyme-linked immunosorbent assay at 490 nm.
As shown in table 1, the arctigenin exhibited time-and dose-dependence on the inhibition of SZ95 cell proliferation. After the arctigenin acts for 72 hours and 96 hours, the arctigenin has obvious inhibition effect on the proliferation of SZ95 cells.
Table 1 effect of arctigenin on SZ95 cell proliferation (a value, n ═ 6)
| Drug concentration (umol/L) | 72h | 96h |
| 0.8 | 0.521±0.045 | 0.691±0.043 |
| 1.6 | 0.516±0.049 | 0.751±0.051 |
| 3.125 | 0.498±0.052 | 0.513±0.039＊＊ |
| 6.25 | 0.384±0.051＊ | 0.395±0.037＊＊ |
| 12.5 | 0.361±0.019＊＊ | 0.346±0.023＊＊ |
| 25 | 0.285±0.026＊＊ | 0.371±0.031＊＊ |
| 50 | 0.234±0.020＊＊ | 0.196±0.026＊＊ |
| Negative control group | 0.495±0.077 | 0.751±0.067 |
Compared with the negative control group, the test results show that,＊P<0.05，＊＊P<0.01。
example 10 Effect of Arctiin on the morphology of sebaceous gland speckle tissue of golden hamster
The golden hamster lateral sebaceous gland plaques contain important structures such as hair follicles, a large number of sebaceous glands and melanin lumps, are similar to human beings in anatomical characteristics and response to hormone stimulation, and are an ideal animal model for screening and researching the anti-sebaceous gland proliferation activity of the drug at present. Research shows that the numerical change of the maximal transverse Diameter (DT) multiplied by the maximal longitudinal Diameter (DL) of the sebaceous glands of the back of the golden hamster is in positive correlation with the real volume change of the sebaceous gland plaques, so the experimental method selects the sebaceous gland plaques of the back of the golden hamster as an animal model.
Adult male golden hamster 56, body mass (100 + -20) g, golden hamster randomly divided into 7 groups of 8 mice each. The experiment was started 3 days after acclimatization. After the golden hamster was anesthetized with ether at the start of the experiment on day 4, the hairs of the back of the golden hamster were shaved off with a shaver, and the maximum transverse Diameter (DT) and the maximum longitudinal Diameter (DL) of the plaque on the right side of the back were measured with a vernier caliper. Grouping and administration were as follows:
arctigenin high dose group: example 1 arctigenin cream, concentration 3%;
arctigenin low dose group: example 3 arctigenin gel, concentration 1%;
diclofenac groups: diclofenac sodium gel with concentration of 1%;
ketoprofen group: ketoprofen gel, concentration 2.5%;
piroxicam group: piroxicam ointment, concentration is 1%;
indomethacin group: indomethacin gel, concentration 1%.
Normal control group: the concentration of the solvent is 1%. The normal control group is smeared with solvent, and the other groups are respectively smeared with corresponding medicine at sebaceous gland macula of golden hamster for 2 times per day for 28 days.
Materials were collected on day 31 of the experiment, fasted for 24h before material collection, and golden hamsters were sacrificed by cervical dislocation and dorsal right plaques DT and DL were measured with a vernier caliper. Then, sebaceous gland speckle tissues are cut off and put into a glass bottle filled with a fixing liquid for fixation. The specimens were sectioned to a thickness of 6 μm and examined histologically under a light microscope for sebaceous gland plaques.
Observation indexes are as follows: (1) sebaceous gland area, expressed as maximum transverse Diameter (DT) x maximum longitudinal Diameter (DL);
(2) the thickness of sebaceous gland plaques is less than 2, and the overlapping gland leaves are thin; 2 or more than or equal to the overlapping gland leaf <4 is middle; the overlapping glandular lobes are greater than or equal to 4 thick.
The results were t-tested using the SPSS 15.0 software package.
The experimental results are as follows:
(1) comparison of the areas of sebaceous gland plaques on the back of golden hamster
Compared with the area of sebaceous gland macula on the back of the mice before treatment, the difference has no statistical significance (P is more than 0.05); after the experiment is finished, compared with a control group, the areas of the sebaceous glands of the golden yellow hamsters in the arctigenin low-dose group and the golden yellow hamsters in the high-dose group are obviously reduced (P is less than 0.01), and the differences of the other groups are not statistically significant (P is more than 0.05) compared with the control group, which is shown in table 2.
TABLE 2 comparison of arctigenin for the area of sebaceous gland macula on the back of golden-yellow hamster
Compared with the normal control group,*P＜0.05，**P＜0.01。
(2) comparison of thickness of sebaceous gland plaques on the back of golden hamster
The thickness of the back sebaceous gland plaques of the rats of the low dose group and the high dose group of the arctigenin is thinner than that of the control group (P is less than 0.01), and the difference between the other groups and the control group has no statistical significance (P is more than 0.05), which is shown in table 3.
TABLE 3 comparison of arctigenin for thickness of sebaceous gland macula on back of golden-yellow hamster
| Group of | n | Thick (only) | Middle (only) | Thin (only) |
| Normal control group | 8 | 5 | 2 | 1 |
| Arctigenin low dose group | 8 | 3 | 2 | 3** |
| Arctigenin high dose group | 8 | 3 | 1 | 4** |
| Diclofenac group | 8 | 5 | 1 | 2 |
| Ketoprofen group | 8 | 5 | 2 | 1 |
| Piroxicam group | 8 | 4 | 2 | 2 |
| Indometacin group | 8 | 4 | 3 | 1 |
Compared with the normal control group,*P＜0.05，**P＜0.01。
(3) histological observation
Under a light microscope, the thickness of the sebaceous glands of the arctigenin low-dose group and arctigenin high-dose group golden yellow hamster is smaller, the thickness is 1-2 layers mostly, the sebaceous glands are loosely arranged, the glandular leaves are smaller, and the number of formed liquefied vesicles is large. The sebaceous glands of the golden hamster in the control group are distributed in a lobular manner, are arranged more tightly and thickly (the number of overlapping glandular leaves is more than or equal to 4), and partial glandular leaves are large and full.
In conclusion, arctigenin has inhibitory effect on sebaceous gland secretion, and can improve the tissue morphology of thickened sebaceous glands and tightly arranged glands.
Example 11 Effect of arctigenin of the present invention on Rabbit auricular acne model
And establishing a rabbit ear acne model caused by the oleic acid/propionibacterium acnes. 48 New Zealand rabbits were selected as a building set of 42 rabbits and a normal control group of 6 rabbits by weight after adaptive rearing for 1 week. Making a model of 42 New Zealand rabbits: preparing skin at the opening of an ear canal on the inner side face of the right ear of a New Zealand rabbit within the range of 2cm multiplied by 2cm, smearing oleic acid for 1 time and 0.5 mL/time every day for 2 weeks continuously, injecting 200 mu L of Propionibacterium acnes stock solution into the auricle skin on the 12 th day after smearing the oleic acid, taking 2 New Zealand rabbits at a model making position on the 3 rd day after injection for skin biopsy and pathological section observation, and determining the formation of a model.
The 42 new zealand rabbit models were randomly divided into 7 groups. The grouping and administration of the drugs are as follows,
model control group: the concentration of the solvent is 1 percent;
arctigenin high dose group: example 1 arctigenin cream, concentration 3%;
arctigenin low dose group: example 3 arctigenin gel, concentration 1%;
diclofenac groups: diclofenac sodium gel with concentration of 1%;
ketoprofen group: ketoprofen gel, concentration 2.5%;
piroxicam group: piroxicam ointment, concentration is 1%;
indomethacin group: indomethacin gel, concentration 1%.
Normal control group: the concentration of the solvent is 1%. The normal control group and the model control group are smeared with a solvent, and the other groups are respectively smeared with the corresponding medicines on the right external auditory canal of the rabbit for 2 times a day and for 14 days continuously.
The rabbits were sacrificed 18h after the last drug treatment, skin tissue biopsies were taken from the right ear of the rabbit coated with oleic acid and the same site of the control group of rabbit ears, fixed with 10% neutral formaldehyde, paraffin embedded, sectioned, HE stained, and histological changes were observed under light microscopy.
The hair follicle expansion degree, the quantity of keratinized substances and pathological changes thereof are classified into 4 grades:
grade 0, no obvious pathological changes are found on the surface layer of the skin, sebaceous glands, hair follicles and dermis, namely 0 point;
+ grade, thickening of stratified squamous epithelium on skin surface, vasodilatation, inflammatory cell infiltration, i.e. 1 point;
grade + 2, the stratified squamous epithelium on the skin surface is obviously thickened, the dermis is formed with abscess, the peripheral tube of the abscess is dilated, hyperemia and collagen fiber hyperplasia are caused, and a large amount of inflammatory cells are infiltrated, namely 2 points are formed;
grade +++ with obvious thickening of the stratified squamous epithelium on the skin surface, abscess formation in the dermis, ulceration on the skin surface, dilation of the periempyema, hyperemia, collagen fiber hyperplasia, and massive inflammatory cell infiltration, i.e., 3 points.
The results were t-tested using the SPSS 15.0 software package.
The experimental results are as follows:
no obvious lesions are found on the auricle epidermis, muscle, sebaceous gland and cartilage of the new Zealand rabbits in the normal control group. The model control group has excessive epidermis keratinization, the granular layer of the epidermis and the hair follicle epithelium is thickened, the spinous layer is thickened, adjacent expanded hair follicles are mutually fused, the hair follicle opening and the funnel part are filled with keratinization substances, a plurality of abscesses are formed under the skin, capillary vessels of surrounding tissues are expanded, hyperemia and exudation are caused, the tissue edema is obvious, the muscle degeneration is broken, and the like.
TABLE 4 comparison of arctigenin for the histopathological grading of rabbit auricular acne models
Compared with the model control group,*P＜0.05，**P＜0.01。
as can be seen from Table 4, compared with the model control group, the pathological scores of the rabbit ears in the arctigenin high and low dose groups are obviously reduced, and the significant difference is significant (P is less than 0.01). The research shows that the arctigenin has obvious therapeutic action on a new zealand rabbit auricle acne model caused by the oleic acid/propionibacterium acnes.
Compared with the control group, the pathological scores of the rabbit ears are not significantly different in the diclofenac group, the ketoprofen group, the piroxicam group and the indomethacin group.
Example 12 clinical trial of arctigenin of the present invention for treatment of whelk
1. General data
A total of 240 patients with whelk seen at clinic visits are collected between 1 month and 10 months in 2016, and the patients are randomly divided into 6 groups: arctigenin 1 group, arctigenin 2 group, diclofenac group, ketoprofen group, piroxicam group, and indomethacin group.
Arctigenin 1 group: 40 of 24 men and 16 women, aged 14-28 years, with an average of (21.7 + -2.4 years) and a course of disease of 1-4 years, with an average of (2.5 + -1.4) years.
Arctigenin 2 group: 40 of 25 men and 15 women, aged 15-29 years, with an average age of (22.4 + -2.3 years) and a course of disease of 2-5 years, with an average age of (2.7 + -1.4 years).
Diclofenac groups: 40 of 22 men and 18 women aged 16-27 years, with an average age of (23.5 + -2.2 years) and a course of 2-5 years, with an average age of (2.6 + -1.2 years).
Ketoprofen group: 40 of 25 men and 15 women, aged 15-27 years, with an average age of (22.3 + -2.1) years and a course of disease of 2-5 years, with an average age of (2.5 + -1.3) years.
Piroxicam group: 40 of 24 men and 16 women, aged 14-28 years, with an average of (21.5 + -2.3 years) and a course of disease of 1-4 years, with an average of (2.4 + -1.1) years.
Indomethacin group: 40 of 23 men and 17 women, aged 15-28 years, with an average age of (23.7 + -2.1) years and a course of 2-5 years, with an average age of (2.6 + -1.2) years.
The 6 groups of patients have no significant difference in age, sex, disease course and the like and are comparable.
2. Test method
Arctigenin gel (prepared according to the invention in example 3, the concentration of arctigenin is 1%) is applied to the affected part of the arctigenin group 1, and 2 times a day. The treatment course is 4 weeks.
The arctigenin skin-moistening milk (prepared according to the invention in the embodiment 8, the concentration of the arctigenin is 2%) is smeared on the affected parts of the arctigenin group 2, and the skin-moistening milk is applied 2 times a day. The treatment course is 4 weeks.
Diclofenac sodium gel is applied to affected part of diclofenac group with concentration of 1%, 2 times daily. The treatment course is 4 weeks.
Ketoprofen gel is applied to affected part of ketoprofen group at a concentration of 2.5% for 2 times a day. The treatment course is 4 weeks.
Piroxicam ointment is applied to affected part of piroxicam group with concentration of 1%, and 2 times daily. The treatment course is 4 weeks.
Indometacin gel is applied to affected part of the group of indomethacin at a concentration of 1% 2 times daily. The treatment course is 4 weeks.
The treatment can be stopped after the patient is cured for one treatment course, the patient is continuously observed for 3 months after the medicine is stopped, and the relapse condition is recorded.
Relapse rate was 100% relapse/cure.
3. Standard of therapeutic effect and therapeutic result
3.1 therapeutic criteria
And (3) curing: the patient's symptoms disappear, more than 95% of the skin lesions subside, or there is no skin lesion left with only pigmentation;
the effect is shown: the symptoms of the patients are obviously relieved, 70 to 95 percent of skin damage disappears, and pigmentation is caused;
the method has the following advantages: the symptoms of the patient are improved to a certain extent compared with the symptoms before treatment, 50-70 percent of skin damage disappears, and pigmentation is caused;
and (4) invalidation: the clinical symptoms of the patients did not change significantly compared to those before treatment, and only less than 50% of the lesions resolved with colored pigmentation.
3.2 treatment statistics are shown in Table 5.
TABLE 5 comparison of therapeutic effects of the groups
| Group of | n | Cure of disease | Show effect | Is effective | Invalidation | Total effective rate (%) | Recurrence example |
| Arctiin 1 group | 40 | 22 | 14 | 2 | 2 | 95％ | 1(5％) |
| Arctiin 2 group | 40 | 20 | 16 | 1 | 3 | 92.5％ | 2(10％) |
| Diclofenac group | 40 | 0 | 2 | 3 | 35 | 12.5％ | - |
| Ketoprofen group | 40 | 0 | 1 | 2 | 37 | 7.5％ | - |
| Piroxicam group | 40 | 0 | 1 | 3 | 36 | 10％ | - |
| Indometacin group | 40 | 0 | 2 | 3 | 35 | 12.5％ | - |
As can be seen from the data in Table 5, the arctigenin of the present invention can effectively treat acne with low recurrence rate after healing.
The arctigenin disclosed by the invention is high in safety for external use and few in adverse reaction.
Table 6 comparison of adverse reactions in each group
| Group of | n | Adverse reactions example |
| Arctiin 1 group | 40 | 2 cases erythema |
| Arctiin 2 group | 40 | 0 |
| Diclofenac group | 40 | 5 cases (2 cases of dermatitis, 3 cases of erythema with pruritus) |
| Ketoprofen group | 40 | 7 examples (3. erythema, 4 examples Dry) |
| Piroxicam group | 40 | 5 cases (2 cases of dermatitis, 3 cases of photosensitivity) |
| Indometacin group | 40 | 6 cases (3 cases of erythema with pruritus and 3 cases of dermatitis) |
The drug application parts of patients of the diclofenac group, the ketoprofen group, the piroxicam group and the indomethacin group have adverse reactions such as erythema, pruritus, dryness, photosensitivity, dermatitis and the like. The arctigenin external application group of the invention only causes very slight erythema on individual patients, and the safety is higher.
Claims (7)
1. Use of arctigenin in preparing medicine and/or cosmetic for preventing or treating acne is provided.
2. The use according to claim 1, wherein the medicament is in the form of an arctigenin external preparation.
3. The use according to claim 2, wherein the external preparation is a powder, ointment, gel, cream, spray or patch, and the external preparation is administered through the skin.
4. The use according to claim 1, wherein the cosmetic is a soap, a facial cleanser, a toner, an essence, a lotion or a cream.
5. The use according to claim 1, wherein the content of arctigenin in the medicament and/or cosmetic is 0.0125 to 99.00 wt%.
6. The use as claimed in claim 5, wherein the arctigenin is contained in the pharmaceutical and/or cosmetic in an amount of 0.01-10 wt%.
7. The use as claimed in claim 6, wherein the arctigenin is contained in the drug and/or cosmetic in an amount of 0.05-2 wt%.
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US20070166255A1 (en) * | 2004-11-22 | 2007-07-19 | Gupta Shyam K | Treatment of Topical Discomforts Including Acne, Sunburn, Diaper Rash, Wound, Wrinkles and Dandruff/Hair Loss by Natural Lignans via Fatty Acid Desaturase Inhibition |
| CN108601762A (en) * | 2016-02-08 | 2018-09-28 | 客乐谐控股株式会社 | Inflammatory body activates inhibitor |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070166255A1 (en) * | 2004-11-22 | 2007-07-19 | Gupta Shyam K | Treatment of Topical Discomforts Including Acne, Sunburn, Diaper Rash, Wound, Wrinkles and Dandruff/Hair Loss by Natural Lignans via Fatty Acid Desaturase Inhibition |
| CN108601762A (en) * | 2016-02-08 | 2018-09-28 | 客乐谐控股株式会社 | Inflammatory body activates inhibitor |
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| Title |
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| HIROMI TOHNO等: "Evaluation of estrogen receptor Beta binding of pruni cortex and its constituents", 《YAKUGAKU ZASSHI》 * |
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Effective date of registration: 20210823 Address after: 273400 Shandong city of Linyi province Feixian County North Ring Road No. 1 Applicant after: LUNAN NEW TIME BIO-TECH Co.,Ltd. Address before: 276006 No. 209 Hongqi Road, Shandong, Linyi Applicant before: Lunan Pharmaceutical Group Corp. |
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Application publication date: 20200811 |