WO2021036294A1 - Vaginal acid-base buffer gel and preparation method - Google Patents

Abstract

A vaginal acid-base buffer gel and a preparation method, the gel consisting of the following components by mass: 1%-39% of an oil phase base, 60%-99% of a water phase base, 0.001%-2% of a pH regulator and 0.05%-5% of a bacteriostat, wherein the oil phase base is white petrolatum or liquid paraffin or glyceryl behenate or Span or Tween or glycerol or propylene glycol; the water phase base is hydroxypropyl methylcellulose or carbomer or sodium carboxymethylcellulose or polycarbophil or polyethylene glycol or azone or gelatin or purified water; the pH regulator is citric acid or sodium citrate or sodium hydroxide or hydrochloric acid or triethanolamine or boric acid or borax or sodium dihydrogen phosphate or disodium hydrogen phosphate; and the bacteriostat is benzoic acid or sodium benzoate or benzyl alcohol or benzalkonium bromide or benzalkonium chloride or sorbic acid or potassium sorbate or nipalgin. The prepared product may effectively regulate the original vaginal environment of inflammation, remove vaginal odor and relieve symptoms such as increased vaginal secretions or itching.

Description

Vaginal acid-base buffer gel and preparation method Technical field

The invention belongs to the field of pharmacy, and specifically relates to a vaginal acid-base buffer gel and a preparation method.

Background technique

The vaginal pH of women of normal childbearing age is between 3.8 and 4.5. This acidic environment is formed because of the glycogen of the vaginal epithelial tissue and the presence of lactobacilli in the vaginal flora of women of childbearing age. Lactobacillus uses glycogen to produce lactic acid to maintain the acidic environment of the vagina while inhibiting the growth of pathogens, which is called vaginal self-purification. Lactobacillus is also called vagina guard.

The change in vaginal pH can be the cause of vaginal disease, or it can be the result of disease. Maintaining a normal vaginal pH is an important guarantee for vaginal health; there are many microorganisms in the normal vagina, but due to the formation of the ecological balance between these microorganisms in the vagina, it does not cause disease. Once the ecological balance is broken or foreign pathogens invade, That is, inflammation occurs. Lactobacillus, vaginal pH, and estrogen are the most important factors in maintaining the ecological balance of the vagina;

For the above-mentioned diseases or symptoms, buffer gels are currently used for treatment, but the existing buffer gels have the following shortcomings: 1. The appearance of the product gel is soft, not shaped, cannot stay in the body for a long time, and is easy to flow out and pollute. Underwear; 2. The product is not effective in use, and the auxiliary treatment effect of vaginitis is quite poor; 3. Patients with damaged vaginal mucosa have a temporary irritation and pain during use; 4. The price is too high; the performance of the product is relatively high Poor; the preparation process takes a long time, which easily causes the product to be easily oxidized and discolored;

In view of the above shortcomings, there is a need for a vaginal acid-base buffer gel and a preparation method. The product prepared by the present invention can effectively adjust the vaginal environment of original inflammation, remove vaginal odor, and improve symptoms such as increased vaginal discharge and itching.

Summary of the invention

The purpose of the present invention is to provide a vaginal acid-base buffer gel and a preparation method. The product prepared by the present invention can effectively adjust the vaginal environment of original inflammation, remove vaginal odor, and improve symptoms such as increased vaginal discharge and itching.

The present invention provides the following technical solutions:

A vaginal acid-base buffering gel, which is characterized in that it is composed of the following mass components: oil phase base 1% to 39%, water phase base 60% to 99%, acid base regulator 0.001% to 2% and Bacteriostatic agent 0.05% to 5%;

The oil phase-based component is a mixture of one or more of white petrolatum, liquid paraffin, glyceryl behenate, Span, Tween, glycerin or propylene glycol;

The water-based components are hydroxypropyl methyl cellulose, carbomer, sodium carboxymethyl cellulose, polycarbophil, polyethylene glycol, azone, gelatin or a mixture of one or more of purified water ；

The acid-base regulator is a mixture of one or more of citric acid, sodium citrate, sodium hydroxide, hydrochloric acid, triethanolamine, boric acid, borax, sodium dihydrogen phosphate or disodium hydrogen phosphate;

The bacteriostatic agent is a mixture of one or more of benzoic acid, sodium benzoate, benzyl alcohol, benzalkonium bromide, benzalkonium chloride, sorbic acid, potassium sorbate or parabens.

Preferably, the formula is 39% oil phase base, 60% water phase base, 0.6% acid-base regulator and 0.4% bacteriostatic agent;

The oil phase base component is composed of white petrolatum, Span 60 and Tween 80;

The water phase base component is composed of hydroxypropyl methyl cellulose and purified water;

Acid-base regulator is composed of sodium citrate;

The bacteriostatic agent is composed of methyl p-hydroxybenzoate and propyl p-hydroxybenzoate.

Preferably, 39% of the oil phase base is composed of 36% white petrolatum, 1% Span 60 and 2% Tween 80;

60% of the water phase base is composed of 1% hydroxypropyl methylcellulose, 1% polycarbophil and 58% purified water;

The acid-base regulator is composed of 0.6% sodium citrate;

The antibacterial agent 0.4% is composed of 0.3% methyl p-hydroxybenzoate and 0.1% propyl p-hydroxybenzoate.

A method for preparing vaginal acid-base buffer gel, the steps are as follows:

S1. Weigh an appropriate amount of sodium citrate, add an appropriate amount of purified water, stir and dissolve for later use;

S2. According to the ratio of raw materials, inject half of the purified water into the batching tank of the emulsification unit, then heat the purified water to 100°C for sterilization, and cool it to 80°C, and then add it to the batching tank of the emulsification unit according to the ratio. White Vaseline, Span 60, Tween 80, Polycarbophil, Hydroxypropyl Methyl Cellulose and White Vaseline, swell while stirring for 1 hour;

S3. According to the ratio, add the antibacterial agent to the batching tank of the emulsification unit, and stir for 30 minutes;

S4. Turn on the vacuum and turn on the cooling water to cool the batching tank of the emulsification unit. When the temperature drops to 45°C, turn off the cooling water;

S5. Add the prepared sodium citrate solution to the batching tank of the emulsification unit according to the ratio, add purified water to sufficient amount according to the ratio, and stir for 30 minutes to prepare this product.

Preferably, in step S2, the sterilization time is 30 to 60 minutes.

Preferably, in steps S3 and S5, a homogenizer is used for mixing and stirring.

The beneficial effects of the present invention:

(1) Vaginal acid-base buffer gel is a polymer gel product. In the process of preparation of this type of product, a process of polymer material swelling is required. The time of polymer swelling often determines the success or failure of the finished product; in the traditional process During the preparation process, it is necessary to swell the polymer materials and other raw materials with purified water one day in advance, and then mix and reprocess the materials the next day. This greatly increases the probability of contamination of the sample and also causes oxidation reaction between the gel and the stainless steel container. In this production process, by adding Span 60 and Tween 80, the original swelling time is shortened from about 8 hours to 1 hour, and the sample preparation time is shortened from the original two days to one day, which can effectively improve the problems of the existing process and can Greatly improve production efficiency.

(2) In this preparation process, polycarbophil is added to the traditional formula, and the molecular chain of polycarbophil has many hydroxyl groups, which endows the gel product with excellent acid-base buffering capacity and unique bioadhesiveness, which can promote activity The ingredients are transported to various mucosal surfaces and pressed onto the damaged mucosal surface with small wounds in the form of spherical molecules, which has the effect of relieving pain and hemostasis; and polycarbophil has significant water absorption and water retention, and can absorb its own weight of 600 It swells but does not dissolve, forming a hydrogel with high water content. This can solve the problem of the formation of the vaginal acid-base buffer gel. The gel can fit the vaginal mucosa 100% in an all-round way, is not easy to undercut, prolongs the time the product stays in the body, and enhances the product's auxiliary treatment effect.

detailed description

Example 1:

A vaginal acid-base buffer gel, comprising the following quality components: 19% oil phase base is composed of 16% white petrolatum, 1% Span 60 and 2% Tween 80;

80% of the aqueous phase is composed of 1% carbomer, 1% polycarbophil, and 78% purified water;

Acid-base regulator is composed of 0.6% sodium hydroxide;

The bacteriostatic agent consists of 0.4% benzalkonium bromide.

The preparation method of a vaginal acid-base buffer gel is as follows:

S1. Weigh an appropriate amount of sodium hydroxide to prepare a 0.5mol/L sodium hydroxide solution for later use;

S2. According to the ratio of raw materials, inject half of the purified water into the emulsification unit batching tank, then heat the purified water to 100°C for sterilization for 60 minutes, and cool it to 80°C, and send it to the emulsification unit batching tank according to the ratio Add Span 60, Tween 80, Polycarbophil, Carbomer and White Vaseline in sequence, and swell while stirring with a homogenizer for 1 hour;

S3. According to the ratio, add the antibacterial agent to the batching tank of the emulsification unit, and stir for 30 minutes;

S4. Turn on the vacuum and turn on the cooling water to cool the batching tank of the emulsification unit. When the temperature drops to 45°C, turn off the cooling water;

S5. According to the proportion, add the prepared 0.5mol/L sodium hydroxide solution to the emulsification unit batching tank, add purified water to sufficient amount according to the proportion, and stir for 30 minutes with a homogenizer to prepare this product.

Example 2:

A vaginal acid-base buffer gel, including the following quality components: 39% of the oil phase base is composed of 36% white petrolatum, 1% Span 60 and 2% Tween 80;

60% of the water phase base is composed of 1% hydroxypropyl methylcellulose, 1% polycarbophil, and 58% purified water;

Acid-base regulator is composed of 0.6% sodium citrate;

The antibacterial agent 0.4% is composed of 0.3% methyl p-hydroxybenzoate and 0.1% propyl p-hydroxybenzoate.

A preparation method of vaginal acid-base buffer gel is as follows:

S1. Weigh an appropriate amount of sodium citrate, add an appropriate amount of purified water, stir and dissolve for later use;

S2. According to the ratio of raw materials, inject half of the purified water into the emulsification unit batching tank, then heat the purified water to 100°C for sterilization for 30 minutes, and cool it to 80°C, and then send it to the emulsification unit batching tank according to the ratio Add Span 60, Tween 80, Polycarbophil, Hydroxypropyl Methyl Cellulose and White Vaseline in sequence, and swell while stirring with a homogenizer for 1 hour;

S3. According to the ratio, add the antibacterial agent to the batching tank of the emulsification unit and stir for 30 minutes;

S4. Turn on the vacuum and turn on the cooling water to cool the batching tank of the emulsification unit. When the temperature drops to 45°C, turn off the cooling water;

S5. According to the proportion, add the prepared 0.6% sodium citrate solution into the emulsification unit batching tank, add purified water according to the proportion to a sufficient amount, and stir with a homogenizer for 30 minutes to prepare this product.

Example 3:

On the basis of Example 2, a vaginal acid-base buffer gel, including the following mass components: oil phase base 29% composed of white petrolatum 26%, 1% Span 60 and 2% Tween 80 composition;

70% of the water phase base is composed of 1% carbomer, 1% polycarbophil, and 68% purified water;

The acid-base regulator 0.6% is composed of 0.3% sodium citrate and 0.3% sodium hydroxide;

The antibacterial agent 0.4% consists of benzalkonium chloride.

experiment analysis:

If the pH of the vagina is lost, bacteria can easily invade, leading to various vaginal inflammations. Vaginitis is most common with bacterial vaginitis. Women with bacterial vaginitis often have a vaginal pH greater than 6.0. In the setting of the pH value of the vaginal acid-base buffer gel, attention should be paid to establishing the micro-balance of the vaginal environment. The setting of pH value needs to break the conventional neutrality, and choose a pH value (4.0 to 5.5) that is neutral and acidic, so that the gel can effectively regulate the vaginal environment of the original inflammation, remove vaginal odor, and improve Symptoms such as increased vaginal discharge and itching;

From January 2018 to June 2018, a total of 198 women suffering from gynecological diseases (mainly vaginitis, pruritus, abnormal leucorrhea, etc.) from employees and their families were collected within the company as research subjects, and they were randomly divided into group A1 and group A1. Group B1, Group A2 and Group B2, Group A3 and Group B3, 33 people in each group;

Among them, the A1, A2, and A3 groups use the original prescription product vaginal pH buffer gel according to the instructions; the B1, B2 and B3 groups use the formulas of Example 1, Example 2, and Example 3 respectively according to the instructions. The vagina pH buffering gel, the corresponding drugs are used continuously, and once a day, 14 days after the drug, the statistics are as follows:

Table 1-Drugs prepared using Example 1

To	cure	Significant	effective	invalid	Efficient(%)
Group A1	0 people	8 people	17 people	8 people	75.7%
Group B1	1 person	9 people	17 people	6 people	81.8%

Table 2-Drugs prepared using Example 2

To	cure	Significant	effective	invalid	Efficient(%)
Group A2	0 people	10 people	16 people	7 people	78.8%
Group B2	2 people	11 people	18 people	2 people	94.0%

Table 3-Drugs prepared using Example 3

To	cure	Significant	effective	invalid	Efficient(%)
Group A3	0 people	9 people	17 people	7 people	78.8%
Group B3	0 people	11 people	17 people	5-people	84.8%

The data in the above table shows that the vaginal pH buffering gel prepared by this method has better effects than the original prescription vaginal pH buffering gel, and the drug product prepared in Example 2 can significantly improve the therapeutic effect;

The above are only the preferred embodiments of the present invention and are not intended to limit the present invention. Although the present invention has been described in detail with reference to the foregoing embodiments, for those skilled in the art, it is still possible to describe the foregoing various embodiments. Modify the technical solution or equivalently replace some of its technical features. Any modification, equivalent replacement, improvement, etc. made within the spirit and principle of the present invention should be included in the protection scope of the present invention.

Claims (6)

1. A vaginal acid-base buffer gel, which is characterized in that it is composed of the following mass components: oil phase base 1% to 39%, water phase base 60% to 99%, acid base regulator 0.001% to 2% and Bacteriostatic agent 0.05% to 5%;

   The oil phase base component is a mixture of one or more of white petrolatum, liquid paraffin, glyceryl behenate, Span, Tween, glycerin, and propylene glycol;

   The water-based components are one or more mixtures of hydroxypropyl methyl cellulose, carbomer, sodium carboxymethyl cellulose, polycarbophil, polyethylene glycol, azone, gelatin, and purified water ；

   The acid-base regulator is a mixture of one or more of citric acid, sodium citrate, sodium hydroxide, hydrochloric acid, triethanolamine, boric acid, borax, sodium dihydrogen phosphate, and disodium hydrogen phosphate;

   The bacteriostatic agent is one or more mixtures of benzoic acid, sodium benzoate, benzyl alcohol, benzalkonium bromide, benzalkonium chloride, sorbic acid, potassium sorbate, and parabens.
2. A vaginal acid-base buffer gel according to claim 1, characterized in that: oil phase base 39%, water phase base 60%, acid-base regulator 0.6% and bacteriostatic agent 0.4%;

   The oil phase base component is composed of white petrolatum, Span 60 and Tween 80;

   The water phase base component is composed of hydroxypropyl methyl cellulose and purified water;

   Acid-base regulator is composed of sodium citrate;

   The bacteriostatic agent is composed of methyl p-hydroxybenzoate and propyl p-hydroxybenzoate.
3. A vaginal acid-base buffer gel according to claim 2, wherein 39% of the oil phase base is composed of 36% white petrolatum, 1% Span 60 and 2% Tween 80;

   60% of the water phase base is composed of 1% hydroxypropyl methylcellulose, 1% polycarbophil and 58% purified water;

   The acid-base regulator 0.6% is composed of sodium citrate solution;

   The antibacterial agent 0.4% is composed of 0.3% methyl p-hydroxybenzoate and 0.1% propyl p-hydroxybenzoate.
4. A method for preparing vaginal acid-base buffer gel, which is characterized in that the steps are as follows:

   S1. Weigh an appropriate amount of sodium citrate, add an appropriate amount of purified water, stir and dissolve for later use;

   S2. According to the ratio of raw materials, inject half of the purified water into the batching tank of the emulsification unit, then heat the purified water to 100°C for sterilization, and cool it to 80°C, and then add it to the batching tank of the emulsification unit according to the ratio. White Vaseline, Span 60, Tween 80, Polycarbophil and Hydroxypropyl Methyl Cellulose, swell while stirring, for 1 hour;

   S3. According to the ratio, add the antibacterial agent to the batching tank of the emulsification unit, and stir for 30 minutes;

   S4. Turn on the vacuum and turn on the cooling water to cool the batching tank of the emulsification unit. When the temperature drops to 45°C, turn off the cooling water;

   S5. Add the prepared sodium citrate solution to the batching tank of the emulsification unit according to the ratio, add purified water to sufficient amount according to the ratio, and stir for 30 minutes to prepare this product.
5. The method for preparing vaginal acid-base buffer gel according to claim 4, characterized in that: in step S2, the sterilization time is 30 to 60 minutes.
6. The method for preparing vaginal acid-base buffer gel according to claim 4, characterized in that in steps S3 and S5, a homogenizer is used for mixing and stirring.