Vaginal bacteriostatic agent containing lactic acid and / or lactate as well as preparation and application of vaginal bacteriostatic agent

Abstract

The invention discloses a vaginal preparation which comprises an inert drug-loaded matrix, lactic acid and / or lactate, and a medical device or a bacteriostatic agent for treating and / or preventing female urogenital system diseases. In addition, the invention also discloses the preparation of the vaginal preparation, the use of the vaginal preparation for treating and preventing female urogenital system diseases, and the treatment method thereof.

Description

Technical Field

[0001] The present invention relates to the field of vaginitis treatment, in particular to a vaginal topical preparation comprising lactic acid and / or lactate and an inert drug-carrying excipient for preventing and / or treating urogenital diseases. In addition, the present invention also relates to a production and use method of the topical preparation for preventing and / or treating urogenital diseases. Background Art

[0002] The ecological environment system in the vagina is a delicate microbial balance system, which is formed by the joint action of various bacteria including yeast.

[0003] Urogenital tract infections, including urethral infections, bacterial vaginosis and vaginal candidiasis, are common diseases among women worldwide. More than 75% of women have had at least one vaginal infection in their lifetime, and more than 50% of women have experienced multiple infections.

[0004] Bacterial vaginosis generally presents as mild infection or no infection of vaginal epithelial cells. It is more like a change in the vaginal environment caused by an imbalance of normal vaginal flora rather than an infection of tissues or epithelial cells. It is manifested by increased, thin vaginal discharge with a fishy odor, and often occurs in sexually active women. Currently, the main treatment method is anti-infective drugs, but anti-infective drugs can also kill beneficial bacteria in the vagina, such as lactic acid bacteria, which can further lead to an imbalance in the vaginal environment, increase the recurrence of bacterial vaginitis, or further develop into other vaginitis, such as vaginal candidiasis.

[0005] Candida is a harmless commensal microorganism in the human body, but can sometimes cause infection when the body's normal bacterial environment is out of balance. In patients with severe immunodeficiency, Candida can cause systemic infection that is life-threatening.

[0006] Lactobacillus is the dominant bacteria in the vagina of healthy women, and its main function is to maintain the acidic environment of the vagina. The acidic environment is an important mechanism for protecting the vagina. The acidic environment can reduce the number of bacteria such as chlamydia, mycoplasma, and trichomonas in the vagina, and can also reduce the amount of bacteria at the vaginal opening.

[0007] Vaginal acid-base balance refers to the fact that the pH of the vagina is acidic between 3.8 and 4.2 in a healthy state. In this acid-base environment, lactic acid bacteria are in a normal equilibrium state. This pH environment is most suitable for lactic acid bacteria and will also make the pH of mucosal secretions about 4. However, the pH environment in the vagina is affected by many factors, such as changes in estrogen concentration during menstruation or menopause, menstrual blood, etc., and local anti-infective drugs, IUDs, and detergents used to flush the vagina will also damage the vaginal microenvironment. When the pH in the vagina exceeds 4.5, anaerobic bacteria in the vagina will overgrow, causing vaginal bacterial infection.

[0008] Vaginal acid-base balance is a very important indicator of whether a woman is healthy. At present, the main clinical treatments for bacterial vaginosis in China are: (1) Systemic use of anti-infective drugs, such as metronidazole, tinidazole, clindamycin, etc. (2) Local use of anti-infective drugs, such as metronidazole vaginal suppositories, tinidazole suppositories, and clindamycin ointment (3) Topical use of beneficial bacteria preparations, such as lactobacillus suppositories.

[0009] The above treatment methods have the following shortcomings: (1) The use of anti-infective drugs will kill pathogenic bacteria as well as beneficial bacteria such as Lactobacillus, further unbalance the acid-base environment of the vagina and lead to recurrence of vaginitis.

[0010] (2) There are many types of bacteria in the vaginal flora, and the limited anti-infection drugs are not effective against all pathogens.

[0011] (3) Lactobacillus preparations. First, during the production and storage of lactobacillus preparations, beneficial bacteria will be lost, resulting in insufficient numbers. In addition, when lactobacillus is placed in the vagina where the acid-base environment is already unbalanced, the chance of survival of lactobacillus is not high, resulting in no effect.

[0012] Therefore, it is necessary to find an effective means and method for preventing and treating bacterial vaginitis, fungal vaginitis, especially candidal vaginitis, preferably a local treatment method that is easy for patients to accept and use.

[0013] Advantages of this technology: (1) This technical solution uses ingredients naturally present in the human body to regulate and maintain the acid-base balance of the female vagina, fully ensuring safety.

[0014] (2) The method of regulating and maintaining the acid-base balance of the female vagina to prevent and treat bacterial vaginitis, fungal vaginitis and candidal vaginitis is to provide targeted treatment based on the cause of vaginitis to reduce the chance of recurrence.

[0015] (3) In this technical solution, the preparation is developed into a concentrated small-dose dosage form that is convenient for administration, easy for patients to use and easy for them to accept. Summary of the invention

[0016] The object of the present invention is to provide a local vaginal therapy for treating urogenital diseases, which is effective for bacterial vaginosis and fungal infections, especially fungal infections caused by yeasts. The treatment should be simple, convenient, comfortable, and provide good patient acceptance. The present invention can achieve this goal through a vaginal topical preparation.

[0017] The suppository comprises an inert carrier and lactic acid or lactate, and is characterized in that the suppository comprises lactic acid and / or lactate in a concentration of 5.5-15% (w / w) by weight.

[0018] The present invention has found that vaginal topical preparations containing lactic acid and / or lactate in the range of 5.5-15% by weight (w / w) not only reduce vaginal malodor but also create a favorable acid environment that is beneficial to resist Gram-negative bacteria, Gram-positive bacteria and the yeast Candida albicans. These functions are not only due to the low pH value, but also related to the lactic acid molecule itself.

[0019] Typically, vaginal suppositories are composed of lactic acid and / or lactate salts at a concentration of 5.5 - 15% by weight (w / w), and optimally 13.5% by weight (w / w). These concentration intervals are particularly effective in killing harmful pathogens in the urogenital tract such as E. coli, GBS, and Candida albicans.

[0020] The suppository of the present invention is convenient for intravaginal administration and has high patient acceptability.

[0021] In an embodiment of the present invention, the inert carrier comprises polyethylene glycol (PEG).

[0022] Inert carriers enable the manufacture of suppositories that are relatively solid at room temperature and in a dry environment, but melt at body temperature and in contact with body fluids. During administration, the lactic acid and / or lactate salt comes into contact with the vaginal tissue. Polyethylene glycol (PEG) gradually melts in the vaginal environment.

[0023] In alternative embodiments, the vaginal suppository may further comprise a neutralizing substance designed to buffer the pH of the lactic acid.

[0024] The content of lactic acid and neutralizing substances is preferably between 3.5 and 4.5, and the optimal pH is 3.85. The pH value should not be too low, because high acidity may irritate vaginal tissue or damage the probiotics in the environment. For example, lactic acid bacteria require a moderately acidic environment.

[0025] Suitable neutralizing materials include sodium hydroxide.

[0026] In another aspect, the present invention relates to the use of a vaginal suppository for the production of a medicament for the prevention and / or treatment of urogenital tract diseases.

[0027] This drug has antibacterial activity.

[0028] Urogenital tract diseases usually include elevated pH and / or a disturbance in the microbiota. Typically, the disease is selected from bacterial vaginosis, intermediate vaginal microflora, and yeast infection.

[0029] In another aspect, the present invention relates to a vaginal suppository having the above characteristics for preventing and / or treating urogenital tract diseases.

[0030] The present invention also relates to a method for preventing and / or treating urogenital tract diseases, comprising administering a vaginal suppository having the above characteristics and a pharmaceutically effective amount to a patient in need thereof. Example

[0031] The production of this product is represented by the following specific production methods: In the clean production equipment, add a certain amount of lactic acid, sodium lactate, propylene glycol, polyethylene glycol 400 and polyethylene glycol 600 in turn. The lactic acid concentration is 5.5-15% by weight. Turn on the stirring, heat to ℃, and stir to mix the materials thoroughly. Dilute with deionized water, continue stirring, mix thoroughly, and then test the pH value. The pH value should be 3.5-4.5. If the pH value does not meet the requirements, you can choose 5%-10% lactic acid or sodium lactate according to the tested pH to adjust the pH to meet the requirements. The pH value test is carried out according to the above steps.

[0032] Qualified materials are degassed, packaged, packed and put into storage.

[0033] The instructions for use of the drug of the present invention and its treatment method are as follows: 1. Clean your hands and vulva.

[0034] 2. Lie flat on your back, raise your hips, take out the booster containing the product, remove the cover at the front end, insert the booster into the vagina 5cm~8cm, slowly push the solution in, take out the booster and discard it.

[0035] 3. Lie flat on your back for 5-10 minutes. Liquid will flow out during use, so you can use a sanitary pad.

[0036] The above examples are for illustrative purposes only, and the scope of the present invention is not limited thereto. Modifications are obvious to those skilled in the art, and the present invention is subject to the scope of protection of the appended claims.

Claims

1. The present invention provides a local vaginal therapy for treating urogenital diseases, which is effective for bacterial vaginosis and fungal infections, especially fungal infections caused by yeast. The treatment is simple, convenient, comfortable, and well accepted by patients.

2. The treatment is achieved by a vaginal topical suppository comprising an inert carrier and lactic acid and / or a lactate salt, characterized in that The suppository comprises lactic acid and / or a lactate salt in a concentration of 5.5-15% by weight (w / w).

3. Vaginal topical preparations containing lactic acid and / or lactate in a concentration range of 5.5 - 15% by weight (w / w) not only reduce vaginal malodor and create a favorable acid environment, but also help to resist Gram-negative bacteria, Gram-positive bacteria and the yeast Candida albicans. These functions are not only due to the low pH value, but also related to the lactic acid molecule itself.

4. Vaginal suppositories are composed of lactic acid and / or lactate salts at a concentration of 5.5 - 15% (w / w) by weight, preferably 13.5% (w / w) by weight. These concentration intervals are particularly effective in killing harmful pathogens in the urogenital tract such as E. coli, GBS and Candida albicans.

5. Inert carriers include polyethylene glycol (PEG), which gradually melts in the vaginal environment.

6. In an alternative embodiment, the vaginal suppository may further contain a neutralizing substance. This substance is used to buffer the pH value of lactic acid.

7. The content of lactic acid and neutralizing substances is preferably between pH 3.5 and 4.5, and the optimal pH is 3.

85.

8. Suitable neutralizing substances include sodium hydroxide.

9. The present invention relates to the use of vaginal suppositories for producing drugs for preventing and / or treating urogenital tract diseases.

10. The present invention also relates to a method for preventing and / or treating urogenital tract diseases, comprising administering a vaginal suppository having the above characteristics and a pharmaceutically effective amount to a patient in need thereof.