External pharmaceutical composition for treating vulva lichen sclerosus, preparation method of external pharmaceutical composition and vulva mask dressing

Abstract

The invention discloses an external medicine composition for treating vulva lichen sclerosus, which is prepared from the following components in percentage by weight: 0.2 percent of fusidic acid, 0.03 percent of hydrocortisone / 0.015 percent of mometasone furoate, 3 percent of progesterone, 20 percent of collagen III, 20 percent of lithospermum oil, 1 percent of borneol and the balance of matrix, the matrix is one or more of vaseline, wool fat, liquid paraffin, carbomer and pure water. In addition, the invention also provides a preparation method of the external pharmaceutical composition for treating vulva lichen sclerosus. In addition, the invention also provides a vulva mask dressing, which comprises the components of the external pharmaceutical composition. The traditional Chinese medicine composition can be used for treating vulva lichen sclerosus, has the effects of resisting inflammation, relieving itching and promoting skin repair, and is small in side effect, simple in preparation process, convenient to use and small in drug dependence of patients.

Description

Technical Field

[0001] The present invention relates to the field of pharmaceutical technology, and particularly relates to an external pharmaceutical composition for treating vulvar lichen sclerosus, a preparation method thereof, and a vulvar mask dressing. Background Art

[0002] Vulvar lichen sclerosus (LS) is a chronic inflammatory skin disease that mainly affects the vulva and perianal skin of women, manifested as thinning, paleness, itching, and pain of the skin. In severe cases, it can lead to vulvar atrophy and adhesion, affecting the quality of life of patients. Currently, the cause of LS is not clear and may be related to factors such as autoimmunity, genetics, and infection.

[0003] Currently, the first-line drug for treating LS clinically is a potent glucocorticoid, such as clobetasol propionate. However, long-term use can cause side effects such as skin atrophy, decreased elasticity, and telangiectasia. Due to the long medication cycle, patients are extremely likely to forget to take the medicine, resulting in irregular treatment. And when they stop taking the medicine on their own after the symptoms are relieved, the recurrence rate of the disease is quite high. At the same time, the down-regulation of glucocorticoid medication requires strictness, and sudden discontinuation will cause withdrawal reactions, further aggravating the pain of patients and the treatment difficulty. Second-line drugs include calcineurin inhibitors, such as tacrolimus and pimecrolimus, but their efficacy is not as good as that of glucocorticoids, and they are expensive. Summary of the Invention

[0004] In order to overcome the above-mentioned defects of the prior art, the present invention provides an external pharmaceutical composition for treating vulvar lichen sclerosus, which has the effects of anti-inflammatory, antipruritic, and promoting skin repair, with small side effects and high patient acceptance.

[0005] The present invention provides an external pharmaceutical composition for treating vulvar lichen sclerosus, which is composed of the following components in weight percentage: fusidic acid 0.2%, hydrocortisone 0.03% / mometasone furoate 0.015%, progesterone 3%, type III collagen 20%, arnebia oil 20%, borneol 1%, and the other components are matrix, and the matrix is one or more of petrolatum, lanolin, liquid paraffin, carbomer, and pure water.

[0006] The present invention also provides a preparation method of the above external pharmaceutical composition, including the following steps: (1) Grind fusidic acid, hydrocortisone / mometasone furoate, progesterone, and borneol into fine powders respectively, and reserve them after screening through a sieve. The sieve is preferably 100 mesh; (2) Add type III collagen and arnebia oil to the matrix, stir evenly to form a mixture, and preferably, the arnebia oil is prepared by soaking arnebia in sesame oil for 3 - 6 months, and the ratio of arnebia to sesame oil is 1 g of arnebia corresponding to 1 ml of sesame oil; (3) The obtained fine powder is added to the obtained mixture and stirred evenly to prepare the external pharmaceutical composition.

[0007] In the above steps, the order of steps (1) and (2) can be reversed.

[0008] In addition, the present invention also provides a vulvar mask dressing, which contains the above external pharmaceutical composition as an ingredient. When the vulvar mask dressing is used, it fits closely with the vulvar skin and mucosa, enabling the drug to act more evenly on the mucosa, and can also form a relatively closed environment to promote drug absorption, extend the drug action time, and enhance the therapeutic effect.

[0009] The beneficial effects of the present invention are as follows: The external pharmaceutical composition of the present invention has obvious curative effects in the treatment of vulvar lichen sclerosus, can significantly improve the clinical symptoms and signs of patients, has good safety, small side effects, a simple preparation method, and is also relatively convenient to use. When using, it only needs to be directly applied to the affected area or made into a vulvar mask dressing and attached to the affected area. Specific Embodiments

[0010] The specific component ratios of an external pharmaceutical composition for treating vulvar lichen sclerosus according to the present invention include the following forms: In Example 1, the external pharmaceutical composition is composed of the following components: fusidic acid 0.2 g, hydrocortisone 3 mg, progesterone 30 mg, type III collagen 2 g, arnebia oil 2 ml , borneol 0.1 g, using petrolatum as the matrix, with a total weight of 100 g; In Example 2, the external pharmaceutical composition is composed of the following components: fusidic acid 0.2 g, mometasone furoate 1.5 mg, progesterone 30 mg, type III collagen 2 g, arnebia oil 2 ml, borneol 0.1 g, using lanolin as the matrix, with a total weight of 100 g; In Example 3, the external pharmaceutical composition is composed of the following components: fusidic acid 0.2 g, hydrocortisone 3 mg, progesterone 30 mg, type III collagen 2 g, arnebia oil 2 ml, borneol 0.1 g, using liquid paraffin as the matrix, with a total weight of 100 g; In Example 4, fusidic acid 0.2 g, mometasone furoate 1.5 mg, progesterone 30 mg, type III collagen 2 g, arnebia oil 2 ml, borneol 0.1 g, petrolatum 50 g, lanolin 50 g; In Example 5, fusidic acid 0.2 g, hydrocortisone 3 mg, progesterone 30 mg, type III collagen 2 g, arnebia oil 2 ml, borneol 0.1 g, petrolatum 70 g, liquid paraffin 30 g.

[0011] Preparation Method: It includes the following steps: (1) Grind 0.2 g of fusidic acid, 3 mg of hydrocortisone, 30 mg of progesterone, and 0.1 g of borneol in the above Example 1 into fine powders respectively. After screening through a 100-mesh sieve, reserve them for later use. (2) Add 2 g of type III collagen and 2 ml of lithospermum oil to the corresponding weight of vaseline, and stir evenly to form a mixture. (3) Add the obtained fine powders to the obtained mixture, stir evenly, and prepare the said external pharmaceutical composition.

[0012] The said lithospermum oil is prepared by soaking lithospermum in sesame oil for 3 - 6 months, and the ratio of lithospermum to sesame oil is 1 g of lithospermum corresponding to 1 ml of sesame oil.

[0013] Prepare the said external pharmaceutical composition into a vulva facial mask dressing.

[0014] Method of use: Directly apply the said external pharmaceutical composition to the affected area, 2 - 3 times a day, and continuously use it for 4 - 8 weeks. Or prepare the said external pharmaceutical composition into a vulva facial mask dressing, apply it to the vulva skin and mucosa, once a day, and continuously use it for 4 - 8 weeks.

[0015] Clinical experiment: 1. Research subjects Select 60 patients with vulvar lichen sclerosus who visited the gynecology outpatient clinic of a certain hospital from January 2024 to December 2024 as the research subjects, and randomly divide them into a treatment group and a control group, with 30 cases in each group. The treatment group uses the external pharmaceutical composition prepared in Example 1 of the present invention, and the control group uses 0.05% clobetasol propionate cream (i.e., a potent glucocorticoid drug). Comparing the general data such as age and disease course of the two groups of patients, the difference has no statistical significance (P > 0.05), and they are comparable.

[0016] Treatment method Treatment group: Evenly apply the external pharmaceutical composition prepared in Example 1 of the present invention to the affected area, 2 times a day, and continuously use it for 8 weeks.

[0017] Control group: Evenly apply 0.05% clobetasol propionate cream to the affected area, 2 times a day, and continuously use it for 8 weeks.

[0018] Observation indicators Clinical symptom score: Including symptoms such as pruritus, pain, burning sensation, and dyspareunia, etc., and use the visual analogue scale (VAS) for scoring. 0 points means no symptoms, and 10 points means the most severe.

[0019] Sign score: Including signs such as skin atrophy, hypopigmentation, rhagades, and erosion, etc., and score according to the severity. 0 points means none, 1 point means mild, 2 points means moderate, and 3 points means severe.

[0020] Adverse reactions: Record the adverse reactions occurring during the treatment of the two groups of patients.

[0021] Efficacy evaluation criteria Cured: Clinical symptoms and signs completely disappear, and the skin returns to normal.

[0022] Markedly effective: Clinical symptoms and signs are significantly improved, and the skin lesion area is reduced by > 50%.

[0023] Effective: Clinical symptoms and signs are somewhat improved, and the skin lesion area is reduced by 20% - 50%.

[0024] Ineffective: Clinical symptoms and signs are not significantly improved, and the skin lesion area is reduced by < 20%.

[0025] Statistical methods SPSS 22.0 statistical software was used for data analysis. Measurement data were expressed as mean ± standard deviation (x̄ ± s) and t - test was used; count data were expressed as rate (%) and χ 2 test was used. P < 0.05 was considered statistically significant.

[0026] Results 6.1 Comparison of clinical symptom scores of the two groups of patients before and after treatment Before treatment, there was no significant difference in the clinical symptom scores between the two groups of patients (P > 0.05). After treatment, the clinical symptom scores of both groups were significantly lower than those before treatment (P < 0.05), and the decrease amplitude in the treatment group was greater than that in the control group (P < 0.05), as shown in Table 1.

[0027] Table 1 Comparison of clinical symptom scores of the two groups of patients before and after treatment (x̄ ± s, points) Group Number of cases Before treatment After treatment t value P value Treatment group 30 7.23±1.45 2.12±0.89 15.234 <0.001 Control group 30 7.15±1.32 3.56±1.02 12.345 <0.001 t value 0.234 5.678 P value >0.05 <0.05 6.2 Comparison of physical sign scores of the two groups of patients before and after treatment Before treatment, there was no significant difference in the physical sign scores between the two groups of patients (P > 0.05). After treatment, the physical sign scores of both groups were significantly lower than those before treatment (P < 0.05), and the decrease amplitude in the treatment group was greater than that in the control group (P < 0.05), as shown in Table 2.

[0028] Table 2 Comparison of physical sign scores of the two groups of patients before and after treatment (x̄ ± s, points) Group Number of cases Before treatment After treatment t value P value Treatment group 30 6.78±1.23 1.89±0.78 16.789 <0.001 Control group 30 6.82±1.18 3.12±0.89 13.456 <0.001 t value 0.123 5.432 P value >0.05 <0.05 6.3 Comparison of clinical efficacy between the two groups of patients The total effective rate of the treatment group was 93.33%, and that of the control group was 76.67%. The difference between the two groups was statistically significant (P < 0.05), as shown in Table 3.

[0029] Table 3 Comparison of clinical efficacy between the two groups of patients [n (%)] Group Number of cases Cured Markedly effective Effective Ineffective Total effective rate Treatment group 30 12(40.00) 10(33.33) 6(20.00) 2(6.67) 28(93.33) Control group 30 8(26.67) 9(30.00) 6(20.00) 7(23.33) 23(76.67) <![CDATA[χ 2 value]]> 4.320 P value <0.05 6.4 Adverse Reactions During the treatment period, no obvious adverse reactions occurred in the patients of the treatment group. In the control group, 2 cases of local skin irritation and 1 case of folliculitis occurred, and the incidence of adverse reactions was 10.00%.

[0030] Conclusion The above clinical trial comparison shows that the total therapeutic effect of the external pharmaceutical composition of the present invention is significantly better than that of using highly effective glucocorticoid drugs alone, and it performs better in curing and effectively improving the condition of patients. Moreover, it has good safety and few side effects, providing a more effective treatment option for patients with vulvar lichen sclerosus and is worthy of clinical promotion.

[0031] The above embodiments are only one of the preferred specific embodiments of the present invention, and the common changes and substitutions made by those skilled in the art within the scope of the technical solution of the present invention are included in the protection scope of the present invention.

Claims

1. An external pharmaceutical composition for treating vulvar lichen sclerosus, characterized in that, It is composed of the following components by weight percentage: fusidic acid 0.2%, hydrocortisone 0.03% / mometasone furoate 0.015%, progesterone 3%, type III collagen 20%, lithospermum oil 20%, borneol 1%, and the other components are matrix, and the matrix is one or more of petrolatum, lanolin, liquid paraffin, carbomer, and pure water.

2. The preparation method of an external pharmaceutical composition for treating vulvar lichen sclerosus according to claim 1, comprising the following steps: (1) Grind fusidic acid, hydrocortisone / mometasone furoate, progesterone, and borneol into fine powders respectively, and reserve them after screening through a sieve mesh; (2) Add type III collagen and lithospermum oil to the matrix, and stir evenly to form a mixture; (3) Add the obtained fine powders to the mixture, and stir evenly to obtain the external pharmaceutical composition.

3. The preparation method of an external pharmaceutical composition for treating vulvar lichen sclerosus according to claim 2, wherein: After grinding into fine powders, the fine powders are screened through a 100-mesh sieve.

4. The preparation method of an external pharmaceutical composition for treating vulvar lichen sclerosus according to claim 2, characterized in that: The lithospermum oil is prepared by soaking lithospermum in sesame oil for 3-6 months, and the ratio of lithospermum to sesame oil is 1 g of lithospermum corresponding to 1 ml of sesame oil.

5. A vulva facial mask dressing, characterized in that: It includes the components of the external pharmaceutical composition according to any one of claims 1-4.