Pharmaceutical composition for preventing or treating inflammatory skin diseases and application
The topical formulation prepared by combining astaxanthin and p-toluenesulfonamide solves the adverse reactions and tolerability problems of existing treatments, achieving highly effective and safe treatment of inflammatory skin diseases. It is suitable for a variety of skin diseases and promotes skin repair.
Patent Information
- Application Number
- CN202511953473.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-12-23
- Publication Date
- 2026-01-27
AI Technical Summary
Existing treatments for inflammatory skin diseases have risks such as adverse reactions from long-term use of topical corticosteroids, poor tolerance in some patients, and risks associated with systemic drugs. Furthermore, there is a lack of topical preparations that synergistically enhance anti-inflammatory effects and promote skin repair.
Astaxanthin and its derivatives are combined with p-toluenesulfonamide and its derivatives as excipients to prepare various topical dosage forms such as gels and ointments, which are applied to inflamed skin to synergistically inhibit skin inflammation and promote barrier repair.
It significantly inhibits skin inflammation, accelerates wound healing, provides highly effective and safe treatment, is suitable for a variety of inflammatory skin diseases, avoids systemic adverse reactions, and improves medication adherence.
Smart Images
Figure CN121401246A_ABST
Abstract
Description
Technical Field
[0001] This invention relates to the field of skin medicine technology, specifically to a pharmaceutical composition and its application for the prevention or treatment of inflammatory skin diseases. Background Technology
[0002] Inflammatory skin diseases are common in dermatology, with diverse clinical manifestations, ranging from occasional itching, erythema, and rashes to chronic conditions such as urticaria, eczema (e.g., atopic dermatitis, neurodermatitis, nummular eczema), and psoriasis. All are closely related to skin inflammation. These diseases are often accompanied by significant pain, itching, and skin lesions, severely impacting patients' quality of life.
[0003] Currently, treatments for this type of disease mainly include moisturizers, emollients, topical corticosteroids, calcineurin inhibitors, and systemic immunomodulatory drugs. However, existing therapies still have many limitations: long-term use of topical corticosteroids may cause adverse reactions such as skin atrophy and telangiectasia; some patients do not respond adequately to current treatments or develop tolerance; and systemic drugs may pose risks such as liver and kidney damage and immunosuppression. Therefore, there is an urgent clinical need for a topical treatment regimen that is safe, well-tolerated, and can effectively relieve inflammation and promote skin repair.
[0004] Astaxanthin, a potent natural antioxidant, has been proven to possess significant anti-inflammatory and antioxidant activities, and can alleviate skin inflammation by inhibiting inflammatory pathways such as NF-κB. Toluenesulfonamide has certain local analgesic, anti-irritant, and penetration-enhancing effects. However, there are currently no reports on combining astaxanthin and toluenesulfonamide in topical formulations to synergistically enhance anti-inflammatory effects, promote skin barrier repair, and promote wound healing. Summary of the Invention
[0005] The purpose of this invention is to at least solve one of the technical problems existing in the prior art, and to provide a pharmaceutical composition and its application for the prevention or treatment of inflammatory skin diseases.
[0006] To achieve the above objectives, the technical solution adopted by the present invention is as follows: a pharmaceutical composition for the prevention or treatment of inflammatory skin diseases, comprising astaxanthin and its derivatives, p-toluenesulfonamide and its derivatives, and excipients, wherein the structure of the astaxanthin is shown below: ; The astaxanthin and its derivatives include one or more astaxanthin, astaxanthin isomers, and pharmaceutically acceptable salts of astaxanthin; the p-toluenesulfonamide and its derivatives include one or more p-toluenesulfonamide, p-toluenesulfonamide isomers, and pharmaceutically acceptable salts of p-toluenesulfonamide.
[0007] Furthermore, the weight percentage of astaxanthin and its derivatives is 0.0001%-10%; the weight percentage of p-toluenesulfonamide and its derivatives is 1%-40%.
[0008] Furthermore, the excipients comprise 60%-99% by weight.
[0009] Furthermore, excipients include one or more of the following: preservatives, lubricants, suspending agents, wetting agents, flavoring agents, thickeners, biocompatible solvents, surfactants, and complexing agents.
[0010] Furthermore, the biocompatible solvent is one or more of polyethylene glycol, propylene glycol, glycerol, sorbitol, ethanol, dimethyl sulfoxide, N-methyl-2-pyrrolidone, N,N-dimethylacetamide, tetrahydrofuran polyethylene glycol ether, acetone, isopropanol, triglycerides, benzyl benzoate, benzyl alcohol, and acetone glyceryl chloride.
[0011] Furthermore, the surfactant is one or more of the following: lecithin, polyethylene glycol-15-hydroxystearate, polyoxyethylene alkyl ether, polyoxyethylene castor oil, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene stearate, polyoxyglycerol ester, sorbitan ester, and tocopherol polyethylene glycol succinate.
[0012] Furthermore, the complexing agent is polyvinylpyrrolidone or cyclodextrin.
[0013] Furthermore, the pharmaceutical composition may be in the form of a gel, soft gel, lotion, ointment, paste, emulsion, cream, slurry, patch, film, cream, or aerosol.
[0014] Application of a pharmaceutical composition for the prevention or treatment of inflammatory skin diseases, wherein the pharmaceutical composition described above is applied to inflamed skin.
[0015] Compared with the prior art, the technical solution of this application has the following beneficial effects: 1. Synergistic enhancement of anti-inflammatory and repair effects: Astaxanthin and its derivatives have strong antioxidant and anti-inflammatory properties. Combined with the auxiliary analgesic and penetration-promoting effects of p-toluenesulfonamide and its derivatives, they can significantly inhibit skin inflammatory responses, accelerate barrier repair and wound healing, and provide highly effective treatment for inflammatory skin diseases and skin injuries.
[0016] 2. Flexible dosage form and convenient use: The composition can be adapted to a variety of topical dosage forms (such as gel, cream, spray, etc.), which can be selected according to clinical needs and patient preferences, thereby improving medication adherence.
[0017] 3. Wide range of indications and good safety: It is suitable for a variety of inflammatory skin diseases such as atopic dermatitis, eczema, and psoriasis. It can effectively relieve symptoms such as itching, erythema, and skin lesions. Moreover, topical application is unlikely to cause systemic adverse reactions, and it has a high safety profile.
[0018] 4. Overcoming the shortcomings of existing treatments: Compared with traditional hormone drugs, this composition avoids side effects such as skin atrophy caused by long-term use, providing patients with a safer and more tolerable topical treatment option. Attached Figure Description
[0019] Figure 1 Image A shows the skin of an acne patient before use, and image B shows the skin of an acne patient after use. Figure 2 Image A shows the affected area of a patient with atopic dermatitis before use, and image B shows the affected area of a patient with atopic dermatitis before use. Figure 3 Image A shows the affected area of autoimmune dermatitis before use, and image B shows the affected area of autoimmune dermatitis after use. Figure 4 Image A shows the wound before use, and image B shows the wound after use. Detailed Implementation
[0020] The technical solutions of the present invention will be clearly and completely described below with reference to the accompanying drawings of the embodiments of the present invention. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments.
[0021] As used herein, the term "an effective amount" refers to the active dose that, when administered to a subject, achieves a clinical effect. For example, when the active agent of this disclosure is administered to a subject suffering from eczema, beneficial "clinical effects" include reduction of rash and redness, reduction of itching, reduction of scaly plaques, reduction of eczema-related symptoms, and / or improvement in the overall health of the subject. Effective doses may vary depending on the route of administration, excipient use, the possibility of combination with other treatments, and the condition being treated, as is recognized by those skilled in the art.
[0022] As used herein, the term "preventing / prevention" refers to measures to prevent or avoid a disease, or its symptoms or conditions, including but not limited to the administration of one or more active agents to a patient who has not been diagnosed with the disease but may be susceptible or at risk of developing it. The preventive measures provided in this disclosure are intended to avoid, prevent, or delay the occurrence of a disease, or its symptoms or conditions.
[0023] According to this disclosure, the terms “treatment / treating” and similar terms as used herein generally refer to achieving a desired pharmacological or physiological effect. This effect may be preventative, such as completely or partially preventing a condition, manifestation, disease, or symptom, and / or therapeutic, such as partially or completely curing a condition and / or the adverse effects caused by the condition or disease. The term “treatment” as used herein covers any treatment of a condition, disease, or undesirable manifestation in a mammal (such as a human), including: (a) suppressing a disease, condition, or symptom, i.e., resulting in the resolution of the condition or symptom; and (b) alleviating a disease, condition, or symptom, i.e., resulting in the relief of the condition or symptom.
[0024] The numerical ranges used in this article are inclusive and composable. Any value falling within the numerical range of this article can be used as a maximum or minimum value to derive subranges. For example, the numerical range "1% to 60%" should be understood to include any subrange between the minimum value of 1% and the maximum value of 60%, such as subranges from 1% to 50%, from 10% to 60%, from 20.5% to 40.5%, etc.
[0025] As used herein, the term "about" in exponential values indicates a range of variation including ±20%, ±10%, ±5%, ±1%, ±0.5%, or ±0.1% of that value. Such variations may be due to factors such as experimental errors, measurement or operational errors in the preparation of compounds, compositions, concentrates, or formulations, differences in the source, manufacture, or purity of raw materials or ingredients used in this disclosure, etc.
[0026] As used herein, “subject” can encompass any vertebrate, including but not limited to mammals, reptiles, amphibians, and / or fish. However, preferred subjects are mammals, such as humans, or animal mammals, such as domesticated mammals (e.g., dogs, cats, horses, etc.), or productive mammals (e.g., cattle, sheep, pigs, etc.).
[0027] This disclosure provides a method for preventing or treating inflammatory skin diseases, comprising administering an effective amount of a composition to a subject in need, wherein the composition comprises astaxanthin and p-toluenesulfonamide and pharmaceutically or cosmetically acceptable excipients thereof.
[0028] As used herein, the term "an inflammatory skin disease" refers to a condition that causes symptoms ranging from an occasional rash accompanied by itching and redness to chronic symptoms. In at least one embodiment of this disclosure, an inflammatory skin disease includes herpes simplex, herpes zoster, eczema (such as atopic dermatitis), psoriasis, urticaria, atopic dermatitis, or any combination thereof, but this disclosure is not limited thereto. In some embodiments, an inflammatory skin disease is eczema (such as atopic dermatitis), psoriasis, atopic dermatitis, or any combination thereof. In some embodiments, an inflammatory skin disease does not include acne and / or other inflammatory skin diseases caused by bacteria. In some embodiments of this disclosure, symptoms of an inflammatory skin disease may occur on any body surface of the subject, such as the wrists, fingers, or face.
[0029] In at least one embodiment of this disclosure, astaxanthin is represented by the following formula (I): ; Or its pharmaceutically acceptable salt.
[0030] In at least one embodiment of this disclosure, p-toluenesulfonamide is represented by the following formula (II): ; Or its isomers or pharmaceutically acceptable salts thereof.
[0031] In at least one embodiment of this disclosure, the composition is administered to a subject topically or via nebulization. In some embodiments, the composition is administered to a subject topically.
[0032] In at least one embodiment of this disclosure, the pharmaceutically or cosmetically acceptable excipient may be a group consisting of preservatives, lubricants, suspending agents, wetting agents, flavoring agents, thickeners, biocompatible solvents, surfactants, complexing agents, or any combination thereof.
[0033] As used herein, the term "biocompatible" refers to materials that do not produce significant adverse host responses for their intended use. For example, biocompatible materials are non-toxic for their intended use. Therefore, for human use, biocompatibility is more preferably non-toxic to humans or human tissues.
[0034] In at least one embodiment of this disclosure, the biocompatible solvent may be the group consisting of polyethylene glycol, propylene glycol, glycerol, sorbitol, ethanol, dimethyl sulfoxide, N-methyl-2-pyrrolidone (NMP), N,N-dimethylacetamide (DMA), glycofurol, acetone, isopropyl alcohol (IPA), triglycerides, benzyl benzoate, benzyl alcohol, acetone glyceryl chloride, or any combination thereof.
[0035] In at least one embodiment of this disclosure, the surfactant is a group consisting of lecithin, macrogol 15-hydroxystearate, polyoxyethylene alkyl ether, polyoxyethylene castor oil, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene stearate, polyoxyglycerol ester, sorbitan ester, tocopheryl polyethylene glycol succinate (TPGS), or any combination thereof.
[0036] In at least one embodiment of this disclosure, the complexing agent may be polyvinylpyrrolidone or cyclodextrin.
[0037] In at least one embodiment of this disclosure, the astaxanthin content ranges from about 0.0001% to about 10% by weight; the content of the benzylsulfonamide derivative ranges from about 1% to about 50% by weight. In some embodiments of this disclosure, the astaxanthin is used in combination with p-toluenesulfonamide in a content ranging from about 1% to about 50% by weight.
[0038] In at least one embodiment of this disclosure, the pharmaceutically or cosmetically acceptable excipient ranges from about 30% to about 99% by weight. In some embodiments of this disclosure, the pharmaceutically or cosmetically acceptable excipient ranges from about 40% to about 90% by weight. In another embodiment of this disclosure, the pharmaceutically or cosmetically acceptable excipient ranges from about 50% to about 85% by weight. In yet another embodiment of this disclosure, the pharmaceutically or cosmetically acceptable excipient ranges from about 60% to about 75% by weight.
[0039] In at least one embodiment of this disclosure, the topical formulation is in a form suitable for external application. In another embodiment of this disclosure, the topical formulation may be in the form of a gel, soft gel, lotion, ointment, paste, lotion, cream, slurry, patch, film, cream, or aerosol.
[0040] In some implementations, the topical formulation may be used as a pharmaceutical or cosmetic product.
[0041] In at least one embodiment of this disclosure, the composition is applied to the subject 7 to 70 times per week or 1 to 10 times per day. In some embodiments, the composition containing a benzylsulfonamide derivative is applied topically to the inflamed area of the subject's skin once or twice a day or as needed to treat the subject's inflammatory skin condition. In some embodiments, the composition is continuously applied to the subject for at least 1 week, 2 weeks, or 4 weeks.
[0042] This disclosure also provides the use of a composition in the preparation of a medicament or cosmetic for the prevention or treatment of inflammatory skin diseases, the composition comprising the benzylsulfonamide derivative as described above and pharmaceutically acceptable excipients thereof. This disclosure further provides a pharmaceutical composition for the prevention or treatment of inflammatory skin diseases, the pharmaceutical composition comprising the benzylsulfonamide derivative as described above and pharmaceutically or cosmetically acceptable excipients thereof.
[0043] The following implementation schemes will further demonstrate the effectiveness of this disclosure, but do not limit the scope of this disclosure.
[0044] This disclosure has been described through exemplary embodiments. However, it should be understood that the scope of this disclosure is not limited to the disclosed embodiments. Rather, this disclosure is intended to cover various modifications and similar rearrangements. Therefore, the claims should be interpreted in the broadest possible sense to encompass all such modifications and similar rearrangements.
[0045] Clinical Case I: like Figure 1 As shown in Figure A, the subject had acne on their back, with obvious redness and swelling. Figure 4 B showed that after applying an appropriate amount of a topical formulation combination (Skin-H101) gel containing 0.0001% astaxanthin and 10% p-toluenesulfonamide evenly to the affected area on the back of the subjects once a day for one week, the severity of acne was significantly reduced. Furthermore, Skin-H101 gel did not cause skin irritation.
[0046] Clinical Case II: like Figure 2 As shown in Figure A, the subject had atopic dermatitis on their thigh, and Figure 2 B showed that after applying an appropriate amount of Skin-H101 gel evenly to the thighs of the subjects twice daily for one week, the severity of atopic dermatitis was significantly reduced. Furthermore, Skin-H101 gel did not cause skin irritation.
[0047] Clinical Case III: like Figure 3As shown in Figure A, a subject with autoimmune dermatitis had a rash on the affected area. Figure 3 B showed that after applying an appropriate amount of Skin-H101 gel evenly to the affected area twice daily for 15 days, the severity of rash and itching was significantly reduced. Furthermore, Skin-H101 gel did not cause skin irritation.
[0048] Clinical Case IV: like Figure 4 As shown in Figure A, after using Skin-H101 once daily for seven days, the wound on the patient's heel showed significant improvement. Figure 4 B).
[0049] As can be clearly seen from the above clinical cases I to IV, the Skin-H101 topical formulation containing astaxanthin and p-toluenesulfonamide can effectively treat inflammatory skin diseases in the subjects, including eczema and atopic dermatitis, and promote wound healing without causing skin irritation.
[0050] Without causing conflict, those skilled in the art can freely combine and use the above-mentioned additional technical features.
[0051] It is understood that the present invention has been described through some embodiments, and those skilled in the art will recognize that various changes or equivalent substitutions can be made to these features and embodiments without departing from the spirit and scope of the invention. Furthermore, under the teachings of the present invention, these features and embodiments can be modified to adapt to specific situations and materials without departing from the spirit and scope of the invention. Therefore, the present invention is not limited to the specific embodiments disclosed herein, and all embodiments falling within the scope of the claims of this application are within the protection scope of the present invention.
Claims
1. A pharmaceutical composition for the prevention or treatment of inflammatory skin diseases, characterized in that: Including astaxanthin and its derivatives, p-toluenesulfonamide and its derivatives, and excipients, the structure of said astaxanthin is shown below:
2. The astaxanthin and its derivatives include one or more of astaxanthin, astaxanthin isomers, and pharmaceutically acceptable salts of astaxanthin; the p-toluenesulfonamide and its derivatives include one or more of p-toluenesulfonamide, p-toluenesulfonamide isomers, and pharmaceutically acceptable salts of p-toluenesulfonamide.
3. The pharmaceutical composition for the prevention or treatment of inflammatory skin diseases according to claim 1, characterized in that: The weight percentage of astaxanthin and its derivatives is 0.0001%-10%; the weight percentage of p-toluenesulfonamide and its derivatives is 1%-40%.
4. The pharmaceutical composition for the prevention or treatment of inflammatory skin diseases according to claim 1, characterized in that: The excipients are 60%-99% by weight.
5. The pharmaceutical composition for the prevention or treatment of inflammatory skin diseases according to claim 1, characterized in that: The excipients include one or more of the following: preservatives, lubricants, suspending agents, wetting agents, flavoring agents, thickeners, biocompatible solvents, surfactants, and complexing agents.
6. The pharmaceutical composition for the prevention or treatment of inflammatory skin diseases according to claim 4, characterized in that: The biocompatible solvent is one or more of the following: polyethylene glycol, propylene glycol, glycerol, sorbitol, ethanol, dimethyl sulfoxide, N-methyl-2-pyrrolidone, N,N-dimethylacetamide, tetrahydrofuran polyethylene glycol ether, acetone, isopropanol, triglycerides, benzyl benzoate, benzyl alcohol, and acetone glyceryl chloride.
7. The pharmaceutical composition for the prevention or treatment of inflammatory skin diseases according to claim 4, characterized in that: The surfactant is one or more of the following: lecithin, polyethylene glycol-15-hydroxystearate, polyoxyethylene alkyl ether, polyoxyethylene castor oil, polyoxyethylene sorbitan fatty acid ester, polyoxyethylene stearate, polyoxyglycerol ester, sorbitan ester, and tocopherol polyethylene glycol succinate.
8. The pharmaceutical composition for the prevention or treatment of inflammatory skin diseases according to claim 4, characterized in that: The complexing agent is polyvinylpyrrolidone or cyclodextrin.
9. The pharmaceutical composition for the prevention or treatment of inflammatory skin diseases according to claim 1, characterized in that: The pharmaceutical composition is in the form of a gel, soft gel, lotion, ointment, paste, emulsion, cream, slurry, patch, film, cream, or aerosol.
10. The use of a pharmaceutical composition for the prevention or treatment of inflammatory skin diseases, characterized in that: Apply the pharmaceutical composition according to any one of claims 1-8 for the prevention or treatment of inflammatory skin diseases to the inflamed skin.