CN110917132A - Vaginal squamous epithelium repair aqua and preparation method thereof - Google Patents

Vaginal squamous epithelium repair aqua and preparation method thereof Download PDF

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CN110917132A
CN110917132A CN201911314731.2A CN201911314731A CN110917132A CN 110917132 A CN110917132 A CN 110917132A CN 201911314731 A CN201911314731 A CN 201911314731A CN 110917132 A CN110917132 A CN 110917132A
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vaginal
squamous epithelium
estrogen
aqua
vitamin
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徐丽君
张可研
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Zhejiang Inotai Medical Devices Co ltd
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    • A61K9/0034Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • AHUMAN NECESSITIES
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    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
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    • A61K31/47Quinolines; Isoquinolines
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    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
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    • A61K31/726Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728Hyaluronic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
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    • A61K38/18Growth factors; Growth regulators
    • A61K38/1808Epidermal growth factor [EGF] urogastrone
    • AHUMAN NECESSITIES
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    • A61K38/00Medicinal preparations containing peptides
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    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/39Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin, cold insoluble globulin [CIG]
    • AHUMAN NECESSITIES
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    • A61K38/40Transferrins, e.g. lactoferrins, ovotransferrins
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    • A61K9/08Solutions
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
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Abstract

The invention discloses a vaginal squamous epithelium repair water aqua and a preparation method thereof, which solve the problem that the risk of causing gynecological tumor exists because the vaginal dryness and atrophic vaginitis are mainly treated by estrogen at present, and the invention comprises the following components in percentage by mass: l-glutamine: 0.005% -1%; 0.001% -0.5% of epidermal cell growth factor; transferrin: 0.001% -0.5%; 0.005% -1% of vitamin C; hydrolyzing collagen: 0.1% -10%; sodium hyaluronate: 0.1% -1.0%; glycerol: 5% -10%; lactic acid: 0.1% -1.0%; sodium lactate: 0.2% -2.0%; the balance being purified water. The technical scheme can repair the vaginal squamous epithelium layer and recover the barrier function of the vaginal mucosa, does not depend on estrogen, and does not have the risk factor of the estrogen.

Description

Vaginal squamous epithelium repair aqua and preparation method thereof
Technical Field
The invention relates to the field of biological medicines, and particularly relates to a vaginal squamous epithelium repair aqua and a preparation method thereof.
Background
Vaginal dryness and atrophic vaginitis are caused by atrophy, incompleteness or disappearance of the squamous epithelial layer of the vagina after a decrease in estrogen levels. The vaginal mucosa consists of non-keratinized stratified squamous epithelium rich in glycogen and basement membrane rich in fiber. The stratified squamous epithelium is rich in glycogen and moist and elastic in vaginal mucosa when the female is in the second and third years of age. As the estrogen is reduced, the epithelium is atrophied, the squamous cell layer disappears, only basal layer cells and accessory basal layer cells which are poor in nutrition and easy to fall villi are reserved, and in the case, the discomfort such as dryness or stabbing pain can be caused, and the infection is easily caused by the formation of small lacerations; secondly, the vaginal suppository is easy to be infected by bacteria and permeated by toxic metabolites to generate atrophic vaginitis. At present, estrogen medicines are commonly used in clinic to relieve symptoms, but the use of estrogen is double-edged sword, so that the risk of gynecological tumor is caused, and the use of estrogen for people with uterine fibroids and breast cancer history is strictly limited.
Disclosure of Invention
The invention aims to solve the defects and provides the vaginal squamous epithelium repairing aqua and the preparation method thereof.
The above object of the present invention is achieved by the following technical means: the vaginal squamous epithelium repairing water aqua is characterized by comprising the following components in percentage by mass:
l-glutamine: 0.005% -1%;
0.001% -0.5% of Epidermal Growth Factor (EGF);
transferrin: 0.001% -0.5%;
0.005% -1% of vitamin C;
hydrolyzing collagen: 0.1% -10%;
sodium hyaluronate: 0.1% -1.0%;
glycerol: 5% -10%;
lactic acid: 0.1% -1.0%;
sodium lactate: 0.2% -2.0%;
the balance being purified water.
Since the shrinking and weakening of the squamous epithelial layer and the disappearance of damage are the speed of the proliferation and the regeneration of the squamous epithelial cells cannot catch up with the speed of apoptosis, the efficacy of the product formula mainly aims at promoting the growth and the proliferation of cells and controlling the speed of apoptosis.
The L-glutamine is a main energy source and a nitrogen source for cell growth, is essential amino acid for synthesizing purine, pyrimidine, protein and polypeptide in cells, and is added to ensure a nutrient source for epithelial cell growth so as to avoid poor cell growth. The EGF can accelerate the transition of cells from interphase to interphase, shorten the multiplication time of cell proliferation and promote the cell proliferation and division. Transferrin and small molecule hydrolyzed collagen provide energy and nutrition for cell growth and proliferation. Free radicals generated in the process of cell physiological metabolism are gathered on cell membranes to promote cell membrane fusion to cause apoptosis, vitamin C has strong effects of resisting oxidation and removing free radicals, and the apoptosis speed is controlled after the vitamin C is added. The sodium hyaluronate and the glycerin have good moisturizing effect, and can quickly replenish water to relieve uncomfortable symptoms such as dryness and the like after being used. Lactic acid and sodium lactate are buffer systems, so that the pH value of the product is in a stable weak acid state, and the product is suitable for the vaginal environment.
Preferably, the components and the formula thereof are as follows by mass percent:
l-glutamine 0.01%;
epidermal growth factor 0.02%;
transferrin is 0.02%;
vitamin C is 0.05%;
the hydrolyzed collagen is 2%;
0.2% of sodium hyaluronate;
5% of glycerin;
0.5 percent of lactic acid;
sodium lactate is 1 percent;
the purified water was 91.2%.
A preparation method of a vaginal squamous epithelium repairing water aqua comprises the steps of dissolving hydrolyzed collagen, sodium hyaluronate, glycerol, lactic acid and sodium lactate in purified water, heating to 80 ℃, keeping the temperature at 80 ℃ for 20 minutes, then cooling, adding L-glutamine, epidermal growth factor, transferrin and vitamin C when the temperature of the system is reduced to be within 40 ℃, and stirring uniformly to obtain the vaginal squamous epithelium repairing water aqua.
Furthermore, the prepared aqueous solution is subpackaged in a trunk tube spray bottle, the front half section of the trunk tube wall of the spray bottle is provided with a plurality of uniformly arranged small holes, and when the spray bottle is used, the trunk tube of the spray bottle is deeply inserted into a vagina and is pressed to spray liquid to the vaginal wall.
A vagina squamous epithelium repair aqua and a preparation method thereof, the product formula emphasizes various nutrients and energy substances required by the growth and proliferation of epithelial cells, functional components for promoting the division of the epithelial cells and removing free radicals to reduce apoptosis are added, simultaneously, the uncomfortable symptoms of vagina dryness and atrophic vaginitis can be rapidly relieved, and the formula system is also suitable for the vaginal tissue environment; the preparation method greatly retains the biological activity of each component, and the compounding performance of each component is good.
Detailed Description
The present invention will be described in more detail with reference to examples.
Example 1
A vaginal squamous epithelium repairing aqua is prepared by dissolving hydrolyzed collagen, sodium hyaluronate, glycerol, lactic acid and sodium lactate in purified water, heating to 80 deg.C, holding at 80 deg.C for 20 min, cooling, adding L-glutamine, EGF, transferrin and vitamin C when the temperature of the system is reduced to below 40 deg.C, stirring, and packaging in a nasal tube spray bottle with uniformly arranged pores at the front half section of nasal tube wall. When in use, the trunk catheter is rotated by 90 degrees to penetrate into the vagina, and the liquid is sprayed to the wall of the vagina by pressing.
The prepared components have the following mass percentages:
l-glutamine: 0.005% -1%;
0.001% -0.5% of Epidermal Growth Factor (EGF);
transferrin: 0.001% -0.5%;
0.005% -1% of vitamin C;
hydrolyzing collagen: 0.1% -10%;
sodium hyaluronate: 0.1% -1.0%;
glycerol: 5% -10%;
lactic acid: 0.1% -1.0%;
sodium lactate: 0.2% -2.0%;
the balance being purified water.
The selection of the components and the selection of the weight ratio in the technical scheme can be freely proportioned according to the range described in the claims, and the selection is not exemplified here.
In order to verify the therapeutic effect of the product, one of the formulations was used for a control test.
The water aqua used in the test comprises the following components in parts by weight:
0.01 percent of L-glutamine;
EGF 0.02%;
0.02% of transferrin;
0.05% of vitamin C;
hydrolyzed collagen 2%
0.2 percent of sodium hyaluronate
5 percent of glycerin
0.5 percent of lactic acid;
sodium lactate 1 percent;
purified water 91.2%.
Evaluation of action of vaginal squamous epithelium repair water agent on vaginal dryness and atrophic vaginitis
In order to verify the effect of the invention, 60 cases of patients with vaginal dryness and atrophic vaginitis are clinically selected, 30 cases of test groups of 2 patients are randomly extracted to carry out treatment and observation on vaginal squamous epithelium repair aqua (called squamous aqua for short later), and 30 cases of control groups of 2 patients are carried out treatment and observation on estrogen (Hongli combined with estrogen cream, Xinjiang attitude source biological pharmacy Limited liability company).
The main symptoms of vaginal dryness are as follows: vaginal dryness, dyspareunia, with low vaginal health score (see table 1 below) and vaginal atrophy index (table 2). The patients in the test group applied the scaly aqua after cleaning private parts every night, the dosage of the scaly aqua is about 3ml each time, the treatment effect is evaluated according to clinical grading standard after the scaly aqua is continuously used for 14 days. The control group patients applied estrogen after cleaning private parts every night, the dosage of the estrogen is about 0.5g each time, the estrogen is used once a day, and the treatment effect is evaluated according to clinical grading standards after the estrogen is continuously used for 14 days. Evaluation criteria of treatment results of vaginal dryness: 1) the effect is shown: the main symptoms such as vaginal dryness and dyspareunia disappear, the vagina health score after the administration-before administration vagina health score is more than or equal to 2, and the vagina atrophy index after the administration-before administration vagina atrophy index is more than or equal to 2; 2) the method has the following advantages: relieving main symptoms such as vaginal dryness and dyspareunia, wherein the vaginal health score after administration-before administration vaginal health score is not less than 1, and the vaginal atrophy index after administration-before administration vaginal atrophy index is not less than 1; 3) and (4) invalidation: the main symptoms such as vaginal dryness and dyspareunia are not reduced, the vagina health score after the medicine is taken-before-the-vagina health score is less than 1, and the vagina atrophy index after the medicine is taken-before-the-vagina atrophy index is less than 1. The effective and effective cases are counted into clinical effective cases, and the clinical effective rate is calculated.
Table 1: vaginal health score
Item 1 minute (1) 2 is divided into 3 points of 4 is divided into
Elasticity of Is free of Lack of Medium and high grade Women in the same sexual maturity stage
Degree of wetness Non-wetting Chinese character shao (a Chinese character of 'shao') Medium and high grade Women in the same sexual maturity stage
pH 7 6 5 4
Mucous membrane Punctate hemorrhage Palpation with blood Thin sheet Women in the same sexual maturity stage
Secretion material Is free of Lack of Chinese character shao (a Chinese character of 'shao') Normal amount
Table 2: index of vaginal atrophy
Figure BDA0002325539160000061
The results of the test group and the control group on the treatment of vaginal dryness are shown in table 3:
table 3: treatment effect of vaginal dryness disease of patients in test group and control group
Figure BDA0002325539160000071
The results in table 3 show that the test group squamous water aqua has the significant efficiency of 43.3 percent on the vaginal dryness, the effective rate of 56.7 percent and the total effective rate of 100 percent; the obvious effective rate of the estrogen of the control group on the vaginal dryness is 50%, the effective rate is 43.3%, and the total effective rate is 93.3%. Therefore, the effect of the squamous water agent for treating vaginal dryness is not better than that of estrogen.
Secondly, the clinical symptoms of atrophic vaginitis are shown as follows: pruritus vulvae, burning pain of vulva and vagina, red swelling and congestion of vaginal wall, and leukorrhagia. The patients in the test group applied the scaly aqua after cleaning private parts every night, the dosage of the scaly aqua is about 3ml each time, the treatment effect is evaluated according to clinical grading standard after the scaly aqua is continuously used for 14 days. The control group patients applied estrogen after cleaning private parts every night, the dosage of the estrogen is about 0.5g each time, the estrogen is used once a day, and the treatment effect is evaluated according to clinical grading standards after the estrogen is continuously used for 14 days. The scoring criteria of clinical symptoms of atrophic vaginitis are shown in table 4, and the treatment effect is evaluated according to the score change percentage before and after the product is used: 1) the effect is shown: clinical symptoms disappear or are obviously improved, and the score change is more than or equal to 65 percent; 2) the method has the following advantages: the clinical symptoms are improved, and the score changes by 30-65%; 3) and (4) invalidation: no significant improvement in clinical symptoms occurred, with a score change of < 30%. The effective and effective cases are counted into clinical effective cases, and the clinical effective rate is calculated. The score change percentage calculation formula is as follows:
percent change score ═ 100% (pre-dose clinical score-post-dose clinical score)/pre-dose clinical score%
TABLE 4 atrophic vaginitis clinical symptom score criteria
Figure BDA0002325539160000081
The results of the treatment of atrophic vaginitis in the test and control groups are shown in table 5:
table 5: therapeutic effect of atrophic vaginitis of test group and control group
Figure BDA0002325539160000082
The results in table 5 show that the test group squamous water aqua has the significant efficiency of 40 percent, the effective rate of 53.3 percent and the total effective rate of 93.3 percent on atrophic vaginitis; the obvious effective rate of the estrogen of the control group on atrophic vaginitis is 50%, the effective rate is 40%, and the total effective rate is 90%. The squamous water aqua can achieve the treatment effect equivalent to that of estrogen on atrophic vaginitis.
The above description is only an embodiment of the present invention, and not intended to limit the scope of the present invention, and all modifications of equivalent structures and equivalent processes performed by the present invention in the specification and the content of the embodiment, or directly or indirectly applied to other related technical fields, are included in the scope of the present invention.

Claims (4)

1. The vaginal squamous epithelium repairing water aqua is characterized by comprising the following components in percentage by mass:
l-glutamine: 0.005% -1%;
0.001% -0.5% of epidermal cell growth factor;
transferrin: 0.001% -0.5%;
0.005% -1% of vitamin C;
hydrolyzing collagen: 0.1% -10%;
sodium hyaluronate: 0.1% -1.0%;
glycerol: 5% -10%;
lactic acid: 0.1% -1.0%;
sodium lactate: 0.2% -2.0%;
the balance being purified water.
2. The aqueous solution for repairing the vaginal squamous epithelium as claimed in claim 1, wherein the mass percentages of the components and the formula thereof are as follows:
l-glutamine 0.01%;
epidermal growth factor 0.02%;
transferrin is 0.02%;
vitamin C is 0.05%;
the hydrolyzed collagen is 2%;
0.2% of sodium hyaluronate;
5% of glycerin;
0.5 percent of lactic acid;
sodium lactate is 1 percent;
the purified water was 91.2%.
3. The method for preparing the aqueous agent for repairing the vaginal squamous epithelium, according to claim 1, is characterized in that: dissolving hydrolyzed collagen, sodium hyaluronate, glycerol, lactic acid and sodium lactate in purified water, heating to 80 deg.C, maintaining the temperature at 80 deg.C for 20 min, cooling, adding L-glutamine, epidermal growth factor, transferrin and vitamin C when the temperature of the system is reduced to below 40 deg.C, and stirring.
4. The preparation method of the aqueous agent for repairing vaginal squamous epithelium, according to claim 3, is characterized in that: the prepared aqueous solution is subpackaged in a trunk tube spray bottle, the front half section of the trunk tube wall of the spray bottle is provided with a plurality of uniformly arranged small holes, and when the spray bottle is used, the trunk tube of the spray bottle is deeply inserted into a vagina and is pressed to spray liquid to the vaginal wall.
CN201911314731.2A 2019-12-19 2019-12-19 Vaginal squamous epithelium repair aqua and preparation method thereof Pending CN110917132A (en)

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