Use of stable aqueous silicic acid solution in preparation of product for treating acne

Abstract

The present invention relates to the use of a stable aqueous silicic acid solution in the preparation of a product for treating acne, wherein a mass concentration of the stable aqueous silicic acid solution is 0.5-2%. A product using the stable aqueous silicic acid solution as an active ingredient can be used for treating acne or for preventing and / or treating sebaceous gland dyshomeostasis. At a mass concentration of 0.5-2%, the product can lighten the color of sebaceous gland plaques, thereby achieving an anti-acne effect. Moreover, the stable aqueous silicic acid solution has a low raw material cost, is environmentally friendly and safe, and can thus be used as a highly therapeutically effective alternative to traditional tretinoin drugs.

Description

Use of stabilized silica aqueous solution in the preparation of acne treatment products Technical Field

[0001] This invention relates to the field of biomedical technology, specifically to the use of a stable aqueous silicic acid solution in the preparation of products for treating acne; more specifically, to the use of a stable aqueous silicic acid solution in the preparation of products for preventing and / or treating sebaceous gland homeostasis imbalance, and to products and methods for treating acne or preventing and / or treating sebaceous gland homeostasis imbalance. Background Technology

[0002] Acne is a chronic inflammatory skin disease occurring in the pilosebaceous unit. Initially, it often presents as comedones and inflammatory papules, which progress to inflammation, pustules, nodules, and even persistent scarring. The long course and recurrent flare-ups can leave pigmentation or scarring. It commonly affects areas with high sebum secretion, such as the face, chest, and back, severely impacting patients' physical, psychological, and social lives, and may even lead to depression or suicide. It is one of the most common disfiguring skin diseases in dermatology. Some studies suggest that excessive sebum secretion and altered lipid composition are central to the development and progression of acne, persisting throughout its development. Sebaceous glands are holoseric glands. Androgens stimulate the proliferation and differentiation of newly formed sebaceous gland cells, simultaneously synthesizing lipids and causing them to migrate towards the center of the gland, forming small lipid droplets. When the intracellular lipid droplet content reaches a certain level, the sebaceous gland cells will spontaneously disintegrate and release lipids.

[0003] Currently, the main drugs used in clinical treatment of acne to address sebaceous gland homeostasis imbalance are retinoids. Although they are effective in inhibiting sebum secretion, long-term systemic use of these drugs may cause many adverse reactions such as liver damage, intestinal mucosal damage, cardiovascular disease, birth defects, and mental health problems. Summary of the Invention

[0004] The purpose of this invention is to address the problems with existing drugs that disrupt sebaceous gland homeostasis by proposing an alternative drug that utilizes a stable silica aqueous solution to prepare an acne treatment product, thereby achieving better therapeutic effects.

[0005] To achieve the above objectives, a first aspect of the present invention provides the use of a stabilized silicic acid aqueous solution in the preparation of a product for treating acne, wherein the stabilized silicic acid aqueous solution has a mass concentration of 0.5% to 2%. The stabilized silicic acid aqueous solution of the present invention, as an active ingredient, has anti-acne efficacy at a mass concentration of 0.5% to 2%. Furthermore, the raw materials for the stabilized silicic acid aqueous solution are inexpensive, environmentally friendly, and safe, and can serve as a substitute for traditional retinoids with good efficacy.

[0006] A second aspect of the invention provides the use of a stabilized silica aqueous solution in the preparation of products for the prevention and / or treatment of sebaceous gland homeostasis imbalance, wherein the stabilized silica aqueous solution has a mass concentration of 0.5% to 2%. The stabilized silica aqueous solution of the present invention, as an active ingredient, at a mass concentration of 0.5% to 2%, can reduce the area of ​​sebaceous gland spots in golden hamsters and lighten the color of the sebaceous gland spots. Simultaneously, the stabilized silica aqueous solution is made from inexpensive, environmentally friendly, and safe raw materials, and can serve as a traditional retinoid alternative with good efficacy.

[0007] In some embodiments, the stabilized aqueous silicate solution is dispersed as an active ingredient in an ointment matrix for external application.

[0008] In a third aspect, the present invention provides a product for treating acne or preventing and / or treating sebaceous gland homeostasis imbalance. According to embodiments of this application, the product comprises a stable silicic acid aqueous solution at a mass concentration of 0.5% to 2% as an active ingredient. In the product according to embodiments of the present invention, the stable silicic acid aqueous solution, as the active ingredient, at a mass concentration of 0.5% to 2%, can reduce the area of ​​golden hamster sebaceous gland spots and lighten their color, exhibiting anti-acne efficacy. Simultaneously, the stable silicic acid aqueous solution is inexpensive, environmentally friendly, and safe, and can serve as a traditional retinoid alternative with good efficacy.

[0009] In some embodiments, the product is a cosmetic, a medical device, or a pharmaceutical.

[0010] In some embodiments, the product is a topical preparation.

[0011] In some embodiments, the stable aqueous silicic acid solution comprises one or more of monosilicic acid, metasilicic acid, and hydrogen silicate.

[0012] In a fourth aspect, the present invention provides a method for preparing the product described in the third aspect. According to an embodiment of the present invention, the method includes mixing the stabilized aqueous silicic acid solution with a pharmaceutically acceptable excipient.

[0013] In some embodiments, the mass concentration of the stabilized silica aqueous solution is 0.5% to 2%.

[0014] Additional aspects and advantages of the invention will be set forth in part in the description which follows, and in part will be obvious from the description, or may be learned by practice of the invention. Attached Figure Description

[0015] Figure 1 shows photographs of the appearance of the sebaceous gland spots of golden hamsters in each group in Example 1.

[0016] Figure 2 shows the appearance and size of the sebaceous gland spots of golden hamsters in each group in Example 1.

[0017] Figure 3 shows the histopathological manifestations of sebaceous gland spots in each group after drug administration in Example 1. Detailed Implementation

[0018] The embodiments of the present invention are described in detail below. The embodiments described below are exemplary and are only used to explain the present invention, and should not be construed as limiting the present invention.

[0019] It should be noted that the terms "first" and "second" are used for descriptive purposes only and should not be construed as indicating or implying relative importance or implicitly specifying the number of indicated technical features. Therefore, a feature defined as "first" or "second" may explicitly or implicitly include one or more of that feature. Furthermore, in the description of this invention, unless otherwise stated, "a plurality of" means two or more.

[0020] To facilitate understanding of this invention, certain technical and scientific terms are specifically defined below. Unless otherwise expressly defined elsewhere in this invention, all other technical and scientific terms used herein have the meanings commonly understood by one of ordinary skill in the art to which this invention pertains.

[0021] In this invention, the terms "comprising" or "including" are open-ended expressions, meaning they include the contents specified in this invention but do not exclude other aspects.

[0022] In this document, the term "pharmaceuticalally acceptable excipient" may include any solvent, solid excipient, diluent, or other liquid excipient, etc., suitable for the specific target dosage form. The use of any conventional excipients, except those that are incompatible with the compounds of the present invention, such as any adverse biological effects or harmful interactions with any other component of the pharmaceutically acceptable composition, is also within the scope of this invention.

[0023] In this document, the term "treatment" refers to the administration of a drug or compound to an individual to achieve a desired pharmacological and / or physiological effect. This effect may be preventative in terms of complete or partial prevention of a disease or its symptoms, and / or therapeutic in terms of partial or complete cure of a disease and / or adverse effects caused by the disease. As used herein, "treatment" encompasses diseases in mammals, particularly humans, including: (a) prevention of disease or the onset of a condition in an individual who is susceptible but has not yet been diagnosed with the disease; (b) inhibition of disease, such as blocking disease progression; or (c) relief of disease, such as reducing symptoms associated with the disease. As used herein, "treatment" encompasses any administration of a drug or compound to an individual to treat, cure, relieve, improve, reduce, or inhibit the individual's disease, including but not limited to the administration of a drug containing a compound described herein to an individual in need.

[0024] In this document, the term "administration" refers to the introduction of a predetermined amount of a substance into a patient in a suitable manner. The stable silica aqueous solution of the present invention can be administered via any common route, as long as it can reach the intended tissue. Various routes of administration are foreseeable, including peritoneal, intravenous, intramuscular, subcutaneous, etc., but the present invention is not limited to these exemplified routes of administration. Preferably, the compositions of the present invention are administered via intravenous or subcutaneous injection.

[0025] This invention proposes the use of a stable aqueous silicic acid solution in the preparation of a product for treating acne, the use of a stable aqueous silicic acid solution in the preparation of a product for preventing and / or treating sebaceous gland homeostasis imbalance, a product for treating acne or preventing and / or treating sebaceous gland homeostasis imbalance, and a method for preparing the product described in the third aspect of this invention, which will be described in detail below.

[0026] use

[0027] A first aspect of the present invention provides the use of a stabilized silicic acid aqueous solution in the preparation of a product for treating acne, wherein the mass concentration of the stabilized silicic acid aqueous solution is 0.5% to 2%, for example, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1.0%, 1.1%, 1.2%, 1.3%, 1.4%, 1.5%, 1.6%, 1.7%, 1.8%, 1.9%, 2.0%, or a range between both, 0.6% to 2% or 0.7% to 2%. The stabilized silicic acid aqueous solution according to the present invention, as an active ingredient, has anti-acne efficacy at a mass concentration of 0.5% to 2%. Furthermore, the raw materials for the stabilized silicic acid aqueous solution are inexpensive, environmentally friendly, and safe, and can serve as a substitute for traditional retinoids with good efficacy.

[0028] It should be noted that the stable silicic acid aqueous solution described in this invention is a stable stable silicic acid aqueous solution, which refers to a solution in a stable state where polymerization has not occurred. Its main components include monosilicic acid (H4SiO4), metasilicic acid (H2SiO3), and hydrogen silicate (HSiO3). - In this invention, a mass concentration of 0.5% to 2% refers to a total concentration of the main components of 0.5% to 2%.

[0029] use

[0030] A second aspect of the invention provides the use of a stabilized silicic acid aqueous solution in the preparation of a product for the prevention and / or treatment of sebaceous gland homeostasis imbalance, wherein the mass concentration of the stabilized silicic acid aqueous solution is 0.5% to 2%, for example, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1.0%, 1.1%, 1.2%, 1.3%, 1.4%, 1.5%, 1.6%, 1.7%, 1.8%, 1.9%, 2.0%, or a range between both, 0.6% to 2% or 0.7% to 2%. The stabilized silicic acid aqueous solution of the present invention, as an active ingredient, at a mass concentration of 0.5% to 2%, can reduce the area of ​​sebaceous gland spots in golden hamsters and lighten the color of the sebaceous gland spots. Simultaneously, the raw materials for the stabilized silicic acid aqueous solution are inexpensive, environmentally friendly, and safe, and can serve as a traditional retinoid alternative with good efficacy.

[0031] In some embodiments, the stabilized aqueous silicate solution is dispersed as an active ingredient in an ointment matrix for external application.

[0032] It should be explained that since acne is essentially a manifestation of sebaceous gland homeostasis imbalance, the stable silica aqueous solution of the present invention can also be used in the preparation of products for the prevention and / or treatment of sebaceous gland homeostasis imbalance, wherein the mass concentration of the stable silica aqueous solution is 0.5% to 2%.

[0033] product

[0034] In a third aspect, the present invention provides a product for treating acne or preventing and / or treating sebaceous gland homeostasis imbalance. According to embodiments of this application, the product comprises a stable silicic acid aqueous solution with a mass concentration of 0.5% to 2% as an active ingredient. The mass concentration can be, for example, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1.0%, 1.1%, 1.2%, 1.3%, 1.4%, 1.5%, 1.6%, 1.7%, 1.8%, 1.9%, 2.0%, or a range between both, 0.6% to 2% or 0.7% to 2%. According to the product of the embodiments of the present invention, the stable silicic acid aqueous solution as the active ingredient, at a mass concentration of 0.5% to 2%, can reduce the area of ​​golden hamster sebaceous gland spots and lighten the color of the sebaceous gland spots, exhibiting anti-acne efficacy. Simultaneously, the stable silicic acid aqueous solution has low raw material costs and is environmentally friendly and safe, and can serve as a traditional retinoid alternative with good efficacy.

[0035] In some embodiments, the product is a cosmetic, a medical device, or a pharmaceutical.

[0036] In some embodiments, the product is a topical preparation.

[0037] In some embodiments, the stable aqueous silicic acid solution comprises one or more of monosilicic acid, metasilicic acid, and hydrogen silicate.

[0038] method

[0039] In a fourth aspect, the present invention provides a method for preparing the product described in the third aspect. According to an embodiment of the present invention, the method includes mixing the stabilized aqueous silicic acid solution with a pharmaceutically acceptable excipient.

[0040] In some embodiments, the mass concentration of the stabilized silicic acid aqueous solution is 0.5% to 2%, for example, it can be 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1.0%, 1.1%, 1.2%, 1.3%, 1.4%, 1.5%, 1.6%, 1.7%, 1.8%, 1.9%, 2.0%, or a range between both, such as 0.6% to 2% or 0.7% to 2%.

[0041] The present invention will be explained below with reference to embodiments. Those skilled in the art will understand that the following embodiments are for illustrative purposes only and should not be considered as limiting the scope of the invention. Where specific techniques or conditions are not specified in the embodiments, they are performed according to the techniques or conditions described in the literature in the field or according to the product instructions. Reagents or instruments whose manufacturers are not specified are all conventional products that can be obtained commercially.

[0042] Example 1:

[0043] To illustrate the use and effectiveness of stabilized silicic acid aqueous solution in the preparation of acne treatment products, this example uses sebaceous gland spots from golden hamsters to simulate human acne.

[0044] The Syrian hamster, also known as the golden hamster, has sebaceous patches on its back, primarily composed of hair follicles, sebaceous glands, and melanin clusters; these are androgen-dependent organs. Anatomically similar to humans and physiologically responding to hormones, it is an ideal animal model for studying abnormal sebum metabolism in acne. Therefore, the Syrian hamster is frequently used as an animal model for dermatological research, particularly in the field of acne (pimples). Sebaceous patches are small lumps that form when sebaceous glands are overactive; they are particularly common on the flanks of the Syrian hamster and can be used to simulate the pathological process of human acne.

[0045] Experimental animals: 0.5%, 1%, and 2% stable silicic acid aqueous solutions were used as the active ingredient, dispersed in a commercially available water-in-oil ointment base as the test drug for ease of use; retinoic acid; 30 SPF-grade male golden hamsters, 6-7 weeks old, weighing 110±10g. They were housed separately in an SPF-grade animal room at a constant temperature of 22±2℃ with 12 hours of day and night, and fed with golden hamster-specific feed.

[0046] Experimental grouping: Thirty golden hamsters were acclimatized for 10 days before the experiment began. The animals were randomly divided into six groups of five each: a control group, a substrate group, a test drug group (0.5%), a test drug group (1.0%), a test drug group (2.0%), and a positive control group (0.1% retinoic acid cream). Each group was housed in two cages.

[0047] Model establishment test index: Sebaceous gland patch area measurement. On day 0 of drug administration, the size of the sebaceous gland patches on the back of golden hamsters was measured with vernier calipers under natural light. The area was expressed as the maximum transverse diameter × the maximum longitudinal diameter, and the sebaceous gland patch area was calculated. The size of the sebaceous gland patches was measured every 3 days, and photos were taken for archiving.

[0048] Pathological examination: HE staining of skin tissue was used to observe the histopathological changes of sebaceous gland patches. On day 25 of drug administration, skin tissue from sebaceous gland patches on the backs of golden hamsters was collected, fixed in 4% formaldehyde for 24 hours, and then dehydrated, embedded in paraffin, sectioned, and stained with HE to observe the thickness, area, number of lobes, number of overlapping layers, and degree of looseness of the sebaceous glands. HE staining procedure:

[0049] (1) Dehydration: Place the fixed skin tissue in a dehydration box and immerse it in a gradient of ethanol from low to high (75% ethanol, 90% ethanol, 90% ethanol, 100% ethanol I, 100% ethanol II, 100% ethanol III for 1 hour each).

[0050] (2) Transparency: Xylene I, Xylene II, and Xylene III were each made transparent for 45 minutes.

[0051] (3) Wax impregnation: Paraffin I, Paraffin II, and Paraffin III, 1 hour each.

[0052] (4) Embedding: After the skin tissue is immersed in wax, it is placed vertically in the embedding frame and liquid paraffin is slowly poured into the frame. After the paraffin solidifies, the embedded wax block is removed and corrected and marked.

[0053] (5) Sectioning: First, remove excess wax from the surface of the wax block. When the tissue is about to be exposed, place it in a microtome and cut it into 5μm sections. Then, gently place the specimen in 42℃ warm water to flatten it. Use a glass slide to lift it out and dry it at 60℃.

[0054] (6) Dewaxing and hydration: Place the slices in a 60°C oven and dry for 1 hour. Immerse the slices in xylene I and xylene II for 15 minutes each, and in 100% alcohol, 95% alcohol, 90% alcohol, 80% alcohol and 70% alcohol for 5 minutes each. Then put them in distilled water for 3 minutes.

[0055] (7) Staining: Hematoxylin staining solution for 5 minutes.

[0056] (8) Washing: Rinse with running tap water for about 15 minutes to turn the slices blue (or place them in alkaline water), but be careful not to let the water flow too strong to prevent the slices from falling off.

[0057] (9) Differentiation: Place the slices in 1% hydrochloric acid ethanol solution to decolorize for about 2 seconds. The slices are ready when they turn red and the color is light.

[0058] (10) Rinse: Place the slices in running tap water to restore their blue color.

[0059] (11) Dehydration I: Slices are placed in 50% ethanol → 70% ethanol → 80% ethanol for 3-5 minutes each.

[0060] (12) Counterstaining: Use 0.5% eosin ethanol solution for 1 min as a contrast stain.

[0061] (13) Dehydration II: Wash away excess red color by immersing the slices in 95% ethanol, then immerse them in anhydrous ethanol for 3-5 minutes. Finally, blot away excess ethanol with absorbent paper.

[0062] (14) Transparency: Place the slices in xylene I and II for 3-5 minutes each.

[0063] (15) Sealing: Seal with neutral resin.

[0064] This embodiment uses golden hamsters to investigate the effects of different concentrations of the test drug on sebaceous gland plaques, and the following results were obtained:

[0065] The effects of different concentrations of the test drug applied topically on reducing the area of ​​sebaceous gland patches in golden hamsters and lightening the color of the patches.

[0066] During the experiment, no obvious abnormalities were observed in the living conditions of the golden hamsters in each group, and no obvious adverse reactions were observed in the whole body or in the local area. As the drug administration time was prolonged, the sebaceous gland patches in the control group and the matrix group became darker in color and larger in area.

[0067] Compared with the control group and the matrix group, the sebaceous gland patches of mice in different concentrations of the test drug and the positive control group all showed varying degrees of lightening in color and reduction in area. However, there was no significant difference between the different concentrations of the test drug groups, nor was there a significant difference between the test drug groups and the positive control group, as shown in Figures 1 and 2.

[0068] Histopathological examination of sebaceous gland patches in different experimental groups of mice was conducted. After HE staining, microscopic examination revealed that the sebaceous glands of the golden hamsters in the control group had intact structures, numerous lobes, a lobulated distribution, large and plump lobes, and multiple overlapping layers (mostly three layers) arranged tightly. Compared with the control group, the sebaceous gland structure in the matrix group showed no significant changes. Compared with the control group, the 0.5% test drug, 1.0% test drug, and 2.0% test drug groups showed a relative decrease in the number of glands and the number of overlapping lobes, with the glands arranged in a relatively loose manner, similar to the results of the positive drug group (Figure 3). This suggests potential as a traditional retinoid alternative with good efficacy.

[0069] Animal experiments showed that different concentrations of the test drug had an effect on a mouse model of skin acne (acne vulgaris, a chronic inflammatory skin disease of the pilosebaceous unit): stable silicic acid aqueous solution as the active ingredient, at a mass concentration of 0.5% to 2%, could reduce the area of ​​sebaceous gland spots in golden hamsters and lighten the color of the sebaceous gland spots, thus having an anti-acne effect.

[0070] In the description of this specification, the references to terms such as "one embodiment," "some embodiments," "example," "specific example," or "some examples," etc., refer to specific features, structures, materials, or characteristics described in connection with that embodiment or example, which are included in at least one embodiment or example of the present invention. In this specification, the illustrative expressions of the above terms do not necessarily refer to the same embodiment or example. Furthermore, the specific features, structures, materials, or characteristics described may be combined in any suitable manner in one or more embodiments or examples. Moreover, without contradiction, those skilled in the art can combine and integrate the different embodiments or examples described in this specification, as well as the features of different embodiments or examples.

[0071] Although embodiments of the present invention have been shown and described above, it is understood that the above embodiments are exemplary and should not be construed as limiting the present invention. Those skilled in the art can make changes, modifications, substitutions and variations to the above embodiments within the scope of the present invention.

Claims

1. Use of a stable aqueous silicic acid solution having a mass concentration of 0.5 to 2% for the preparation of a product for the treatment of acne.

2. Use of a stable aqueous solution of silicic acid for the manufacture of a product for the prevention and / or treatment of an imbalance of sebaceous gland homeostasis, characterized in that, The stable aqueous silicic acid solution has a mass concentration of 0.5 to 2%.

3. Use according to claim 1 or 2, characterized in that, The stable aqueous silicic acid solution is dispersed as an active ingredient in an ointment base for external use.

4. A product for treating acne or preventing and / or treating sebaceous homeostasis imbalance, characterized in that, The product comprises a stable aqueous silicic acid solution having a mass concentration of 0.5 to 2% as an active ingredient.

5. The product of claim 4, wherein, The product is a cosmetic, a medical device or a pharmaceutical.

6. The product according to claim 4 or 5, characterized in that, The product is an external preparation.

7. The product of claim 6, wherein, The external preparation is an ointment, a cream, a gel or a patch.

8. The product of claim 4, wherein, The stable aqueous silicic acid solution comprises one or more of monosilicic acid, metasilicic acid and bisilicate.

9. A method of making a product as claimed in any one of claims 4 to 8, characterised in that, The mixing of the stable aqueous silicic acid solution with pharmaceutically acceptable excipients is included.

10. The method according to claim 9, the stable aqueous silicic acid solution having a mass concentration of 0.5 to 2%.

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