A shrinkage lubricating gel and a preparation method thereof

Abstract

The application relates to a shrinking and lubricating gel, which comprises the following raw materials in percentage by weight: xanthan gum 0.1-2%, trehalose 0.1-2%, carbomer 0.1-3%, glycerol 1-20%, gelatin alginate complex 1-10%, humectant 0.2-4%, disodium edetate 0.01-0.1%, polyethylene glycol 0.1-2%, pH regulator 0.1-3%, royal jelly extract 0-2%, schisandra extract 0-2%, and the balance is water. The application forms a protective biological gel layer on the vaginal wall through the lubricating gel, so as to prevent pathogenic microorganisms from planting, and is suitable for improving itching, erosion, burning, vaginal atrophy, sexual intercourse pain, senile vaginitis, abnormal leucorrhea, urinary urgency, dysuria and other menopausal reproductive urological syndromes.

Description

Technical Field

[0001] This application relates to the field of reproductive health care, and in particular to a vaginal tightening lubricating gel and its preparation method. Background Technology

[0002] Genitourinary syndrome of menopause (GSM) refers to a set of symptoms and signs in women who have entered the menopausal transition or postmenopausal period, caused by decreased levels of estrogen and other sex hormones, including atrophy of the reproductive and urinary tracts and sexual dysfunction. According to foreign data, the prevalence of GSM in women one year after menopause is 64.7%, and the prevalence reaches as high as 84.2% six years after menopause.

[0003] During pregnancy, the enlarged uterus, increased abdominal pressure, and hormonal changes can easily lead to relaxation of the pelvic floor muscles. During childbirth, the extreme dilation of the birth canal causes overstretching and even tearing of the pelvic floor muscles, fascia, and other supporting tissues, resulting in pelvic floor muscle atrophy and fibrosis, thus causing vaginal laxity. After pregnancy and childbirth, as women age and enter the menopausal transition or postmenopausal period, they are prone to menopausal genitourinary syndrome, which exacerbates vaginal laxity. With increasing age, this can lead to vaginal atrophy, painful intercourse, vaginal dryness, and stress urinary incontinence. To alleviate these symptoms, there is an urgent need in this field to provide a lubricating gel for vaginal tightening and its preparation method. Summary of the Invention

[0004] In order to effectively improve the negative effects of menopausal genitourinary syndrome and vaginal laxity caused by other reasons, this application provides a vaginal tightening lubricating gel and its preparation method.

[0005] In a first aspect, this application provides a vaginal tightening lubricating gel, which adopts the following technical solution:

[0006] A vaginal tightening and lubricating gel comprises the following ingredients by weight percentage: xanthan gum 0.1-2%, trehalose 0.1-2%, carbomer 0.1-3%, glycerin 1-20%, gelatin-alginate complex 1-10%, humectant 0.2-4%, disodium edetate 0.01-0.1%, polyethylene glycol 0.1-2%, pH adjuster 0.1-3%, royal jelly extract 0-2%, schisandra extract 0-2%, and the balance being water.

[0007] By employing the above technical solutions, a stable initial gel product is formed using a gelatin-alginate complex, carbomer, and glycerin, which has a physical lifting effect and improves vaginal laxity. Xanthan gum is used as a thickener to prepare a lubricating gel, and the viscosity of the gel is adjusted to be greater than 1000 mPa·s, making its gel properties more stable. Trehalose is a typical stress metabolite that can form a unique protective film on the surface of skin cells under harsh environmental conditions such as high temperature, high cold, high osmotic pressure, and dehydration, physically protecting the biomolecular structure from damage, thereby maintaining the life processes and biological characteristics of the organism. It also prevents reinfection or worsening of the infection by physically shielding the affected area. The moisturizer relieves symptoms such as vaginal dryness and painful intercourse, while also extending the product's shelf life. Disodium edetate, as a pharmaceutical excipient, acts as an antioxidant and increases the stability of the drug. Polyethylene glycol acts as an emulsifier. The pH adjuster neutralizes the polymer gel, adjusting the pH of the lubricating gel to around 4.5, thereby meeting the needs of the vaginal microenvironment and achieving both thickening and moisturizing effects.

[0008] Based on this, royal jelly extract and schisandra extract are added as natural estrogens to synergistically improve the affected area. The supplementation of natural estrogens can regulate the vaginal flora, thereby improving the symptoms of vaginal atrophy and providing certain improvement for the treatment of reproductive and urinary tract symptoms.

[0009] In one specific feasible embodiment, the gelatin alginate complex is prepared as follows:

[0010] Gelatin and sodium alginate were added to deionized water and reacted. The mixture was heated and stirred until homogeneous, and then left at room temperature for 20-28 hours to obtain a gelatin-alginate complex.

[0011] By adopting the above technical solution, proteins and polysaccharide biomolecules are combined through electrostatic interactions. The steric hindrance and viscosity of polysaccharides are used to improve the stability of gelatin. Furthermore, the addition of polysaccharides can transform the irregular coiled parts of gelatin into triple helices, thereby improving the texture, strength, and hardness of the gel.

[0012] In one specific implementation, the alginate is grafted with dopamine, and the alginate-dopamine is prepared as follows:

[0013] Sodium alginate was added to distilled water and stirred. Then N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride were added and stirred for 10-20 minutes. Finally, dopamine hydrochloride was added and stirred for 20-28 hours. After dialysis, the mixture was freeze-dried.

[0014] By adopting the above technical solution and selecting mild reaction conditions, dopamine is grafted onto alginate. Dopamine is a natural catecholamine formed by the decarboxylation of dehydroxyphenylalanine. Its catecholamine can greatly help the female urinary system, thereby improving menopausal genitourinary syndrome such as urinary urgency and difficulty in urination.

[0015] In one specific embodiment, the humectant comprises a coconut oil derivative, 1,2-hexanediol, and 1,3-propanediol, wherein the mass ratio of the coconut oil derivative, 1,2-hexanediol, and 1,3-propanediol is 1:(5-7):(12-14).

[0016] In one specific possible implementation, the coconut oil derivative is capryloyl hydroxamic acid.

[0017] By adopting the above technical solution, capryloyl hydroxamic acid, 1,2-hexanediol and 1,3-propanediol are selected as a common preservative. Among them, capryloyl hydroxamic acid, as a coconut oil derivative, enables the gel to have antibacterial effects while moisturizing, thereby extending its shelf life. 1,2-hexanediol and 1,3-propanediol are both small molecule moisturizing ingredients, and also have antibacterial effects, thereby extending their shelf life.

[0018] In one specific implementation, the pH adjuster is triethanolamine.

[0019] By adopting the above technical solution, triethanolamine is selected as the pH adjuster for acidic polymer gels. Triethanolamine neutralizes the carboxyl group of carbomer to form a stable polymer structure, so that the pH value of the product reaches between 4.0 and 7.5, which meets the needs of the vaginal microenvironment, while achieving the application effects of thickening and moisturizing.

[0020] In one specific implementation, the royal jelly extract comprises 0.01-2% by weight and the schisandra extract comprises 0.05-2% by weight.

[0021] In one specific implementation, the royal jelly extract is a royal jelly fatty acid extract; the preparation of the royal jelly fatty acid extract is as follows:

[0022] Ethyl acetate was added to the freeze-dried royal jelly powder, stirred and dissolved, and the ethyl acetate in the solution was extracted. Then ethyl acetate was added to the extracted powder, stirred and dissolved, and the ethyl acetate in the solution was extracted again. Subsequently, the ethyl acetate solution obtained from the two extractions was concentrated and freeze-dried to obtain the royal jelly fatty acid extract.

[0023] By adopting the above technical solution, fatty acids in royal jelly are extracted using the ethyl acetate method. This is because royal jelly fatty acid extract contains substances that can exert estrogen-like effects. By extracting royal jelly fatty acid extract, the natural estrogen can be further supplemented.

[0024] In one specific implementation, the Schisandra chinensis extract is a Schisandra lignan extract, which is prepared as follows:

[0025] Ethanol solution was added to Schisandra chinensis, heated to reflux, filtered, and then heated to reflux again. The filtrates were combined after the two filtrations and the ethanol was evaporated by rotary evaporation. After concentration, Schisandra chinensis lignan extract was obtained.

[0026] By adopting the above technical solution, lignans in Schisandra chinensis are extracted using the reflux method. This is mainly because lignans are phytoestrogens and can be the main substances in Schisandra chinensis that can exert estrogen-like effects, thus promoting the secretion of estrogen in women.

[0027] Secondly, this application provides a method for preparing a vaginal tightening lubricating gel, which adopts the following technical solution:

[0028] A method for preparing a vaginal tightening and lubricating gel involves weighing the raw materials according to the weight percentage, mixing water, glycerin, trehalose, gelatin alginate complex, humectant, disodium edetate, and polyethylene glycol, then adding carbomer and xanthan gum and stirring. After stirring and cooling, royal jelly extract and schisandra extract are added, and finally, a pH adjuster is added to adjust the pH to 4.0-7.5. After stirring evenly, the mixture is left to stand for 20-28 hours to obtain the final product.

[0029] By adopting the above technical solution, a lubricating gel with good biocompatibility is prepared. This lubricating gel can form a protective biogel layer on the vaginal wall, preventing the colonization of pathogenic microorganisms. It is suitable for improving cervical and vaginal itching, erosion, burning, vaginal atrophy, painful intercourse, senile vaginitis, and effectively improving vaginal laxity, vaginal dryness, stress urinary incontinence and restoring vaginal elasticity, as well as reducing abnormal leukorrhea, urinary urgency, difficulty urinating and other postmenopausal genitourinary syndrome.

[0030] In summary, this application includes at least one of the following beneficial technical effects:

[0031] 1. The lubricating gel of this application can form a protective biogel layer on the vaginal wall, thereby preventing the colonization of pathogenic microorganisms. It is suitable for improving cervical and vaginal itching, erosion, burning, vaginal atrophy, painful intercourse, senile vaginitis, as well as abnormal leukorrhea, urinary urgency, difficulty urinating and other postmenopausal genitourinary syndrome.

[0032] 2. This application utilizes dopamine grafted onto alginate to improve and regulate the female urinary system by utilizing the catecholamines in the dopamine system, thereby producing a better therapeutic effect on urinary tract symptoms.

[0033] 3. This application uses royal jelly extract and schisandra extract as natural estrogens to synergistically supplement estrogen therapy, which can increase the thickness and elasticity of the vaginal mucosa to a certain extent, improve atrophy symptoms, relieve dyspareunia, and promote the increase of vaginal secretions, thereby improving vaginal symptoms caused by GSM. Detailed Implementation

[0034] In this application, the carbomer was purchased from Shanghai Yuanye Biotechnology Co., Ltd., model number Carbomer 934; the royal jelly freeze-dried powder was purchased from Jiangsu Daosimai Biotechnology Co., Ltd.; the polyethylene glycol was purchased from Merck Electronic Materials, model number Polyethylene Glycol 4000; and other raw materials were all available commercially.

[0035] Preparation Example

[0036] Preparation Example 1

[0037] Sodium alginate was added to distilled water and stirred for 12 hours to prepare a 1% sodium alginate solution. Then, N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride were added to make the mass ratio of the three components 1:1:1. The mixture was stirred for 10 minutes. Finally, dopamine hydrochloride was added to make the molar ratio of dopamine hydrochloride to sodium alginate 1:1. The mixture was stirred for 22 hours. The resulting solution was dialyzed through a dialysis bag for 3 days and then freeze-dried to obtain dopamine-grafted alginate.

[0038] Preparation Example 2

[0039] Sodium alginate was added to distilled water and stirred for 12 hours to prepare a 2% sodium alginate solution. Then, equal amounts of N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride were added to make the mass ratio of the three components 1:1:1. The mixture was stirred for 20 minutes. Finally, dopamine hydrochloride was added to make the molar ratio of dopamine hydrochloride to sodium alginate 2:1. The mixture was stirred for 26 hours. The resulting solution was dialyzed through a dialysis bag for 3 days and then freeze-dried to obtain dopamine-grafted alginate.

[0040] Preparation Example 3

[0041] Weigh gelatin and sodium alginate in a mass ratio of 1:4, add them to deionized water to prepare a 2wt% mixed solution, stir at 50°C to make it uniform, and let it stand at room temperature for 20 hours to obtain a gelatin-alginate complex.

[0042] Preparation Example 4

[0043] Weigh gelatin and sodium alginate in a mass ratio of 1:1, add them to deionized water to prepare a 2wt% mixed solution, stir at 50℃ to make it uniform, and let it stand at room temperature for 24 hours to obtain a gelatin-alginate complex.

[0044] Preparation Example 5

[0045] Weigh gelatin and sodium alginate in a mass ratio of 1:4, add them to deionized water to prepare a 2wt% mixed solution, stir at 50°C to make it uniform, and let it stand at room temperature for 28 hours to obtain a gelatin-alginate complex.

[0046] Preparation Example 6

[0047] Weigh gelatin and alginate-dopamine prepared in Preparation Example 1 at a mass ratio of 1:4, add them to deionized water to prepare a mixed solution with a concentration of 2wt%, stir at 50°C to make it uniform, and let it stand at room temperature for 20 hours to obtain gelatin alginate-dopamine complex.

[0048] Preparation Example 7

[0049] Weigh gelatin and alginate-dopamine prepared in Preparation Example 2 at a mass ratio of 1:4, add them to deionized water to prepare a mixed solution with a concentration of 2wt%, stir at 50°C to make it uniform, and let it stand at room temperature for 20 hours to obtain gelatin alginate-dopamine complex.

[0050] Preparation Example 8

[0051] Ethyl acetate was added to the freeze-dried royal jelly powder to prepare a mixed solution with a mass ratio of 5:3. After stirring and dissolving for 8 minutes, the ethyl acetate in the solution was extracted. Then, an equal mass of ethyl acetate was added to the extracted powder, stirred and dissolved for 8 minutes, and the ethyl acetate in the solution was extracted again. Subsequently, the ethyl acetate solution obtained from the two extractions was concentrated and freeze-dried to obtain the royal jelly fatty acid extract.

[0052] Preparation Example 9

[0053] A 90wt% ethanol solution was added to Schisandra chinensis to prepare a mixed solution with a mass ratio of 8:1. The solution was heated under reflux for 2 hours, filtered, and then heated under reflux again. After two filtrations, the filtrates were combined and the ethanol was rotary evaporated and concentrated to obtain Schisandra chinensis lignan extract.

[0054] Example

[0055] Example 1

[0056] A vaginal tightening and lubricating gel is prepared from the following raw materials: 1g xanthan gum, 1g trehalose, 1g carbomer, 10g glycerin, 10g gelatin alginate complex, 2g humectant, 0.1g disodium edetate, 1g polyethylene glycol, 1g triethanolamine, and 972.9g water; wherein the gelatin alginate complex is obtained from Preparation Example 3; the humectant includes capryloyl hydroxamic acid, 1,2-hexanediol, and 1,3-propanediol, with a mass ratio of 1:5:12.

[0057] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenize. After stirring until homogeneous, cool to 40°C. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0058] Example 2

[0059] A vaginal tightening and lubricating gel is prepared from the following raw materials: 10g xanthan gum, 10g trehalose, 15g carbomer, 100g glycerin, 50g gelatin alginate complex, 20g humectant, 0.5g disodium edetate, 10g polyethylene glycol, 15g triethanolamine, and 769.5g water; wherein the gelatin alginate complex is obtained from Preparation Example 3; the humectant includes capryloyl hydroxamic acid, 1,2-hexanediol, and 1,3-propanediol, with a mass ratio of 1:5:12.

[0060] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenize. After stirring until homogeneous, cool to 40°C. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0061] Example 3

[0062] A vaginal tightening and lubricating gel is prepared from the following raw materials: 20g xanthan gum, 20g trehalose, 30g carbomer, 200g glycerin, 100g gelatin alginate complex, 40g humectant, 1g disodium edetate, 20g polyethylene glycol, 30g triethanolamine, and 539g water; wherein the gelatin alginate complex is obtained from Preparation Example 3; the humectant includes capryloyl hydroxamic acid, 1,2-hexanediol, and 1,3-propanediol, with a mass ratio of 1:5:12.

[0063] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenize. After stirring until homogeneous, cool to 40°C. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0064] Example 4

[0065] A vaginal tightening and lubricating gel is prepared from the following raw materials: 1g xanthan gum, 1g trehalose, 1g carbomer, 10g glycerin, 10g gelatin alginate complex, 2g humectant, 0.1g disodium edetate, 1g polyethylene glycol, 1g triethanolamine, and 972.9g water; wherein the gelatin alginate complex is obtained from Preparation Example 4; the humectant includes capryloyl hydroxamic acid, 1,2-hexanediol, and 1,3-propanediol, with a mass ratio of 1:5:12.

[0066] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenize. After stirring until homogeneous, cool to 40°C. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0067] Example 5

[0068] A vaginal tightening and lubricating gel is prepared from the following raw materials: 1g xanthan gum, 1g trehalose, 1g carbomer, 10g glycerin, 10g gelatin alginate complex, 2g humectant, 0.1g disodium edetate, 1g polyethylene glycol, 1g triethanolamine, and 972.9g water; wherein the gelatin alginate complex is obtained from Preparation Example 5; the humectant includes capryloyl hydroxamic acid, 1,2-hexanediol, and 1,3-propanediol, with a mass ratio of 1:5:12.

[0069] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenize. After stirring until homogeneous, cool to 40°C. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0070] Example 6

[0071] A vaginal tightening and lubricating gel is prepared from the following raw materials: 1g xanthan gum, 1g trehalose, 1g carbomer, 10g glycerin, 10g gelatin alginate-dopamine complex, 2g humectant, 0.1g disodium edetate, 1g polyethylene glycol, 1g triethanolamine, and 972.9g water; wherein the gelatin alginate-dopamine complex is obtained from Preparation Example 6; the humectant includes capryloyl hydroxamic acid, 1,2-hexanediol, and 1,3-propanediol, with a mass ratio of 1:5:12.

[0072] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenize. After stirring until homogeneous, cool to 40°C. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0073] Example 7

[0074] A vaginal tightening and lubricating gel is prepared from the following raw materials: 1g xanthan gum, 1g trehalose, 1g carbomer, 10g glycerin, 10g gelatin alginate-dopamine complex, 2g humectant, 0.1g disodium edetate, 1g polyethylene glycol, 1g triethanolamine, and 972.9g water; wherein the gelatin alginate-dopamine complex is obtained in Example 7; the humectant includes capryloyl hydroxamic acid, 1,2-hexanediol, and 1,3-propanediol, with a mass ratio of 1:5:12.

[0075] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenize. After stirring until homogeneous, cool to 40°C. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0076] Example 8

[0077] The only difference between this embodiment and Example 1 is that the moisturizer includes capryloyl hydroxamic acid, 1,2-hexanediol and 1,3-propanediol, with a mass ratio of 1:6:13.

[0078] Example 9

[0079] The only difference between this embodiment and Example 1 is that the moisturizer includes capryloyl hydroxamic acid, 1,2-hexanediol and 1,3-propanediol, with a mass ratio of 1:7:14.

[0080] Example 10

[0081] The only difference between this embodiment and Example 1 is that the raw materials used in this embodiment also include: 0.1g of royal jelly extract from Example 8 and 972.8g of water.

[0082] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. The solution system is stirred evenly at 2400 rpm at 70°C. Then, add carbomer and xanthan gum and stir homogenously. After stirring evenly, cool to 40°C, add royal jelly extract, stir evenly and cool. Finally, add triethanolamine, stir evenly and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0083] Example 11

[0084] The only difference between this embodiment and Example 1 is that the raw materials used in this embodiment also include: 0.5g of Schisandra chinensis extract from Example 9, and 972.4g of water.

[0085] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenize. After stirring until homogeneous, cool to 40°C, add Schisandra chinensis extract, stir until homogeneous, and cool. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0086] Example 12

[0087] The only difference between this embodiment and Example 1 is that the raw materials used in this embodiment include: 0.1g of royal jelly extract from Example 8, 0.5g of schisandra extract from Example 9, and 972.3g of water.

[0088] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. The solution system is stirred evenly at 2400 rpm at 70°C. Then, add carbomer and xanthan gum and stir homogenously. After stirring evenly, cool to 40°C, add royal jelly extract and schisandra extract, stir evenly and cool. Finally, add triethanolamine, stir evenly and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0089] Example 13

[0090] The only difference between this embodiment and Example 1 is that the raw materials used in this embodiment also include: 10g of royal jelly extract as in Example 8, and 962.9g of water.

[0091] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. The solution system is stirred evenly at 2400 rpm at 70°C. Then, add carbomer and xanthan gum and stir homogenously. After stirring evenly, cool to 40°C, add royal jelly extract, stir evenly and cool. Finally, add triethanolamine, stir evenly and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0092] Example 14

[0093] The only difference between this embodiment and Example 1 is that the raw materials used in this embodiment also include: 20g of royal jelly extract as in Example 8, and 952.9g of water.

[0094] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenously. After stirring until homogeneous, cool to 40°C, add royal jelly freeze-dried powder, stir until homogeneous, and cool. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0095] Example 15

[0096] The only difference between this embodiment and Embodiment 1 is that the raw materials used in the preparation also include: 20g of freeze-dried royal jelly powder and 952.9g of water.

[0097] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenously. After stirring until homogeneous, cool to 40°C, add royal jelly freeze-dried powder, stir until homogeneous, and cool. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0098] Example 16

[0099] The only difference between this embodiment and Example 1 is that the raw materials used in this embodiment also include: 10g of Schisandra chinensis extract from Example 9, and 962.9g of water.

[0100] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenize. After stirring until homogeneous, cool to 40°C, add Schisandra chinensis extract, stir until homogeneous, and cool. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0101] Example 17

[0102] The only difference between this embodiment and Example 1 is that the raw materials used in this embodiment also include: 20g of Schisandra chinensis extract from Example 9, and 952.9g of water.

[0103] Accurately weigh the raw materials, and add water, glycerin, trehalose, gelatin alginate complex, capryloyl hydroxamic acid, 1,2-hexanediol, 1,3-propanediol, disodium edetate, and polyethylene glycol to an emulsifying pot. Stir the solution system at 2400 rpm at 70°C until homogeneous. Then add carbomer and xanthan gum and stir homogenize. After stirring until homogeneous, cool to 40°C, add Schisandra chinensis extract, stir until homogeneous, and cool. Finally, add triethanolamine, stir until homogeneous, and let stand for 24 hours to obtain a vaginal tightening and lubricating gel.

[0104] Comparative Example 1

[0105] The only difference between this embodiment and Embodiment 1 is that the raw materials used in this embodiment do not include trehalose.

[0106] Comparative Example 2

[0107] The only difference between this embodiment and Example 1 is that the raw materials used in the preparation do not include xanthan gum.

[0108] Comparative Example 3

[0109] The only difference between this embodiment and Example 1 is that the raw materials used in the preparation include 1g xanthan gum, 1g trehalose, 1g carbomer, 20g glycerin, 2g humectant, 0.1g disodium edetate, 1g polyethylene glycol, 1g triethanolamine, and 972.9g water.

[0110] Comparative Example 4

[0111] The only difference between this embodiment and Example 1 is that the raw materials used in this embodiment do not include a humectant.

[0112] Comparative Example 5

[0113] The only difference between this embodiment and Example 1 is that the raw materials used in the preparation include: 1g xanthan gum, 1g trehalose, 11g glycerin, 10g gelatin alginate complex, 2g humectant, 0.1g disodium edetate, 1g polyethylene glycol, 1g triethanolamine, and 972.9g water.

[0114] Comparative Example 6

[0115] The only difference between this embodiment and Example 1 is that the raw materials used in the preparation include: 1g xanthan gum, 1g trehalose, 1g carbomer, 20g gelatin alginate complex, 2g humectant, 0.1g disodium edetate, 1g polyethylene glycol, 1g triethanolamine, and 972.9g water.

[0116] Performance testing

[0117] Mucosal irritation test assessment: According to the WHO-recognized test method and evaluation criteria for vaginal mucosal irritation, healthy, nascent adult female rabbits of the same breed were randomly divided into 3 groups with the same number of rabbits in each group. Each group was given 2.5 ml of the drug once a day via the vagina, with physiological saline as a blank control. The drug was administered for 10 consecutive days. On the 11th day, the vaginal tissue of the rabbits was taken out, fixed and embedded in 10% formalin, and sectioned for pathological histological examination.

[0118] The severity of four lesions in the vaginal mucosa—edema, hyperemia, leukocyte infiltration, and epithelial ulceration—is recorded on a scale of 1-4, for a total of 16 points. A total score <1 indicates no vaginal mucosal irritation; 1-<5 indicates very mild irritation; 5-<9 indicates mild irritation; 9-<12 indicates moderate irritation; and ≥12 indicates severe irritation.

[0119] Evaluation of the antibacterial performance of the lubricating gel: Based on the analysis of vaginal secretions and drug sensitivity in patients with senile vaginitis in relevant literature, the main pathogens in this type of disease are, in descending order, coagulase-negative staphylococci, Staphylococcus aureus, and Escherichia coli. Inhibiting these pathogens can effectively improve vaginitis and postmenopausal genitourinary syndrome in women. Therefore, coagulase-negative staphylococci, Staphylococcus aureus, and Escherichia coli were used as experimental strains to test the antibacterial effect of this product. The antibacterial effect was calculated using the broth dilution method, and the minimum inhibitory concentration (MIC) and the diameter of the inhibition zone were used as standards to measure the effectiveness of the antibacterial effect. When the inhibition rate is ≥50% to 90%, it is considered to have an antibacterial effect; when the inhibition rate is ≥90%, it is considered to have a strong antibacterial effect; when the diameter of the inhibition zone is ≥20mm, it is considered extremely strong; when the diameter of the inhibition zone is 15-20mm, it is considered high; when the diameter of the inhibition zone is 10-15mm, it is considered medium; and when the diameter of the inhibition zone is ≤10mm, it is considered low.

[0120] Table 1 Performance Test Results

[0121]

[0122]

[0123] Referring to Table 1, compared with Comparative Examples 1 to 6, the lubricating gels in Examples 1-3 exhibited good vaginal mucosal irritation and antibacterial properties. This is because the hydrogel polymer has good biocompatibility. By preparing a lubricating gel with good biocompatibility, the gel polymer absorbs a large amount of water and fills the polymer network, thereby extending the cross-linked macromolecular chains to a greater extent, giving the entire material a fluid property. Its soft, wettable surface and affinity to tissues greatly reduce irritation to the affected area. When the gel is applied to the affected area, it can stably adhere to the vaginal wall after ten minutes, forming a protective film that physically shields the affected area. The active ingredients in the lubricating gel can inhibit pathogens in the affected area and effectively improve vaginitis and menopausal genitourinary syndrome by inhibiting coagulase-negative staphylococci, Staphylococcus aureus, Escherichia coli, and other pathogens. This allows the lubricating gel to effectively inhibit and fight common vaginal infections.

[0124] Compared with Comparative Examples 3 and 5-6, and based on Examples 1 and 4-5, it is evident that the gelatin-alginate complex is of significant importance and can be combined with glycerin and carbomer to improve vaginal laxity. The combination of glycerin, carbomer, and the gelatin-alginate complex forms a stable initial gel product, where glycerin primarily acts as a lubricant. Compared to the initial gel products formed by combining glycerin and carbomer or carbomer and gelatin-alginate complex, this product exhibits better stability and lubrication properties, thereby enhancing the viscosity and elasticity of the lubricating gel.

[0125] Gelatin-alginate complexes can also improve the performance of lubricating gels. When gelatin is used as a single component, its stability is poor. Combining proteins and polysaccharides allows alginate and gelatin to form a complex through intermolecular electrostatic and hydrogen bonding interactions, which helps improve the stability of the single component and thus improves the mechanical properties of the lubricating gel.

[0126] According to Examples 1 and 4-5, the changes in vaginal mucosal irritation were minimal when the mass ratio of sodium alginate to gelatin was adjusted, due to the good biocompatibility of both sodium alginate and gelatin. However, as the sodium alginate content increased, the mechanical properties of the product changed slightly, indicating that the addition of sodium alginate had a certain impact on the formation of the gel structure. This may be because the interaction between proteins and polysaccharides can affect the formation of the gel network. When the mass ratio of sodium alginate to gelatin was 4:1, the particle size of the complex reached its maximum; when the mass ratio of sodium alginate to gelatin was 1:4, the mechanical properties of the complex were maximized.

[0127] As shown in Examples 1 and 6-7, dopamine is a natural catecholamine formed by the decarboxylation of dehydroxyphenylalanine. By grafting dopamine onto alginate, this natural catecholamine can greatly benefit the female urinary system, effectively improving symptoms such as urinary urgency and difficulty urinating associated with postmenopausal genitourinary syndrome. Dopamine and its polymers can modify hydrogels, thereby improving their self-healing ability, adsorption capacity, and biocompatibility. Furthermore, by applying the lubricating gel to the affected area, it can inhibit the growth and reproduction of pathogenic bacteria, thus achieving the antibacterial properties of the lubricating gel.

[0128] According to Examples 1, 8-9, when the mass ratio of coconut oil derivative, 1,2-hexanediol and 1,3-propanediol in the moisturizer is 1:(5-7):(12-14), the three components in the moisturizer achieve an optimal ratio. All three components—coconut oil derivative, 1,2-hexanediol and 1,3-propanediol—possess moisturizing and antibacterial properties. When the mass ratio of coconut oil derivative, 1,2-hexanediol and 1,3-propanediol in the moisturizer is 1:7:14, its gelling properties and antibacterial effect are optimal.

[0129] As shown in Examples 1, 10-17, by adding royal jelly extract and Schisandra chinensis extract to the lubricating gel as natural estrogens, natural estrogen can be supplemented to the affected area, thereby improving the vaginal flora and inhibiting pathogenic strains. This is because royal jelly can competitively bind to ER-α and ER-β with estradiol, thus regulating the expression of estrogen-sensitive genes. Furthermore, royal jelly contains royal jelly main protein, various active peptides, and the unique 10-hydroxy-2-decenoic acid, all of which have good antibacterial activity. Fatty acids extracted from royal jelly are the main substances that exert estrogen-like effects. Schisandra chinensis refers to the dried fruit of Schisandra chinensis or Schisandra chinensis of the Magnoliaceae family. It has strong antioxidant properties and contains a large amount of lignans, which are phytoestrogens. Its extract is the main substance in Schisandra chinensis that exerts estrogen-like effects, promoting the secretion of estrogen in women.

[0130] Natural estrogen supplementation not only regulates vaginal flora but also improves urinary tract symptoms, thereby alleviating cervical and vaginal itching, erosion, burning, vaginal atrophy, dyspareunia, senile vaginitis, and effectively improving vaginal laxity, vaginal dryness, stress urinary incontinence, and restoring vaginal elasticity. It also reduces abnormal vaginal discharge, urinary urgency, and difficulty urinating, characteristic of postmenopausal genitourinary syndrome. Therefore, when lubricating gels contain royal jelly extract or Schisandra chinensis extract, their test results are higher than those without.

[0131] Comparing Examples 10-12, it is evident that when royal jelly extract and Schisandra chinensis extract are added together to the lubricating gel, their synergistic effect can significantly improve the vaginal flora at the affected area, thereby better alleviating the symptoms of vaginal atrophy. However, when royal jelly extract or Schisandra chinensis extract is added to the lubricating gel individually, the effect is not as good as when both are added together. According to Examples 10-11, 13-14, and 16-17, the amount of royal jelly extract or Schisandra chinensis extract added to the lubricating gel has a significant impact on its antibacterial properties. This is because when the amount of royal jelly extract or Schisandra chinensis extract added is too small, the extract cannot fully exert its regulatory effect on estrogen, resulting in a lower effect than the results measured in Examples 14 or 17. According to Example 15, adding freeze-dried royal jelly powder to the lubricating gel can also promote the secretion of estrogen in women, but the effect is relatively lower than that of royal jelly extract.

[0132] The above are all preferred embodiments of this application, and are not intended to limit the scope of protection of this application. Therefore, all equivalent changes made in accordance with the structure, shape and principle of this application should be covered within the scope of protection of this application.

Claims

1. A vaginal tightening lubricating gel, characterized in that, It is composed of the following ingredients by weight percentage: xanthan gum 0.1-2%, trehalose 0.1-2%, carbomer 0.1-3%, glycerin 1-20%, gelatin-alginate complex 1-10%, humectant 0.2-4%, disodium edetate 0.01-0.1%, polyethylene glycol 0.1-2%, pH adjuster 0.1-3%, royal jelly extract 0.01-2%, schisandra extract 0.05-2%, and the balance being water; The moisturizer comprises a coconut oil derivative, 1,2-hexanediol, and 1,3-propanediol, wherein the mass ratio of the coconut oil derivative, 1,2-hexanediol, and 1,3-propanediol is 1:(5-7):(12-14). The coconut oil derivative is capryloyl hydroxamic acid; The pH adjuster is triethanolamine.

2. The vaginal tightening lubricating gel according to claim 1, characterized in that: The gelatin-alginate complex is prepared as follows: Gelatin and alginate were added to deionized water and reacted. The mixture was heated and stirred until homogeneous, and then left at room temperature for 20-28 hours to obtain a gelatin-alginate complex.

3. The vaginal tightening lubricating gel according to claim 2, characterized in that: The alginate grafted with dopamine is prepared as follows: Add alginate to distilled water and stir. Then add N-hydroxysuccinimide and 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and stir for 10-20 min. Finally, add dopamine hydrochloride and stir for 20-28 h. After dialysis, freeze dry.

4. The vaginal tightening lubricating gel according to claim 1, characterized in that: The royal jelly extract is a royal jelly fatty acid extract; the preparation of the royal jelly fatty acid extract is as follows: Ethyl acetate was added to the freeze-dried royal jelly powder, stirred and dissolved, and the ethyl acetate in the solution was extracted. Then ethyl acetate was added to the extracted powder, stirred and dissolved, and the ethyl acetate in the solution was extracted again. The ethyl acetate solution obtained from the two extractions was then concentrated and freeze-dried to obtain the royal jelly fatty acid extract.

5. The vaginal tightening lubricating gel according to claim 1, characterized in that: The schisandra extract is a schisandra lignan extract, and the preparation of the schisandra lignan extract is as follows: Ethanol solution was added to Schisandra chinensis, heated to reflux, filtered, and then heated to reflux again and filtered. The filtrates were combined after the two filtrations and the ethanol was evaporated by rotary evaporation. After concentration, Schisandra chinensis lignan extract was obtained.

6. A method for preparing a vaginal tightening lubricating gel according to any one of claims 1-5, characterized in that: Weigh the raw materials according to the weight percentage, mix water, glycerin, trehalose, gelatin alginate complex, humectant, disodium edetate and polyethylene glycol, then add carbomer and xanthan gum and stir. After stirring and cooling, add royal jelly extract and schisandra extract, and finally add pH adjuster to adjust the pH to 4.0-7.

5. Stir evenly and let stand for 20-28 hours to obtain the final product.

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