CN112274480A - Preparation method of female contraceptive antibacterial gel lubricant - Google Patents

Preparation method of female contraceptive antibacterial gel lubricant Download PDF

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Publication number
CN112274480A
CN112274480A CN202011235443.0A CN202011235443A CN112274480A CN 112274480 A CN112274480 A CN 112274480A CN 202011235443 A CN202011235443 A CN 202011235443A CN 112274480 A CN112274480 A CN 112274480A
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component
preparing
antibacterial gel
female contraceptive
water
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耿忠民
亓会平
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Shandong Laishang Trading Co ltd
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Shandong Laishang Trading Co ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/194Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/716Glucans
    • A61K31/722Chitin, chitosan
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0034Urogenital system, e.g. vagina, uterus, cervix, penis, scrotum, urethra, bladder; Personal lubricants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Gynecology & Obstetrics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Reproductive Health (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

The invention relates to a preparation method of a female contraceptive antibacterial gel lubricant, which is characterized in that L-lactic acid, citric acid and potassium hydrogen tartrate are prepared into mixed solution according to a proportion; preparing a water-soluble chitin derivative into a solution; preparing a thickening agent and glycerol into gel; mixing and stirring a solution prepared by preparing L-lactic acid, citric acid, potassium hydrogen tartrate, a thickening agent and glycerol into gel to obtain a component A; mixing water soluble chitin derivative solution with thickener and glycerin solution prepared into gel, and stirring to obtain component B; filling the component A and the component B in a two-component injector respectively, and sterilizing; the pH value of the vagina is adjusted to be within the normal range of 3.5-4.5 by a buffer system consisting of L-lactic acid, citric acid and potassium hydrogen tartrate, and the acidic environment is not suitable for the existence of sperms but is essential for the existence of healthy bacteria in the vagina. Meanwhile, under the acidic environment, the water-soluble chitin derivative with higher molecular weight is subjected to acidolysis, and the bacteriostatic performance is exerted.

Description

Preparation method of female contraceptive antibacterial gel lubricant
Technical Field
The invention relates to the technical field of medical materials, in particular to a preparation method of a female contraceptive antibacterial gel lubricant.
Background
The current oral contraceptive is a commonly used contraceptive method for women, the main component of the oral contraceptive is estrogen-progestogen, wherein the success rate of the short-acting oral contraceptive can reach as high as 99 percent, however, people with the disease history of liver and kidney metabolic abnormality, embolic diseases, cardiac dysfunction, hypertension, diabetes and the like are not suitable to use the oral contraceptive. The long-term use of normal people can also cause disorder of the reproductive and endocrine system, and cause diseases such as breakthrough bleeding, venous embolism, myocardial infarction and the like. Meanwhile, gynecological diseases are common diseases of women, such as vaginitis, cervicitis and the like, and are mostly caused by insanitary sexual life. Thus, there is a real need for a non-hormonal contraceptive method and an antimicrobial gel emollient for women.
Disclosure of Invention
The invention aims to provide a preparation method of a gel lubricant for female contraception and antibiosis, which achieves the purpose of contraception by adjusting the pH value of a vagina and is a non-hormonal contraception method; meanwhile, the water-soluble chitin derivative achieves the aim of antibiosis in an acid environment.
In order to achieve the purpose, the technical scheme adopted by the invention is as follows: a preparation method of a female contraceptive antibacterial gel lubricant comprises the following steps:
(1) preparing mixed solution of L-lactic acid, citric acid and potassium hydrogen tartrate according to a proportion;
(2) preparing a water-soluble chitin derivative into a solution;
(3) preparing a thickening agent and glycerol into gel;
(4) mixing and stirring the solutions prepared in the steps (1) and (3) to obtain a component A;
(5) mixing and stirring the solutions prepared in the steps (2) and (3) to obtain a component B;
(6) and respectively filling the component A and the component B into a two-component injector, and sterilizing.
At present, the main component of the oral contraceptive is mainly female progestogen, however, people with the disease history of abnormal metabolism of liver and kidney, embolic diseases, cardiac dysfunction, hypertension, diabetes and the like are not suitable to use the oral contraceptive. The long-term use of normal people can also cause disorder of the reproductive and endocrine system, and cause diseases such as breakthrough bleeding, venous embolism, myocardial infarction and the like. The pH value of the vagina is controlled to be within a normal range of 3.5-4.5 by a buffer system consisting of L-lactic acid, citric acid and potassium hydrogen tartrate, and the acidic environment is not suitable for the existence of sperms.
Preferably, the mass ratio of the component A to the component B is 1: 1.
Preferably, the proportion of the L-lactic acid, the citric acid, the potassium hydrogen tartrate, the glycerol and the thickening agent in the component A is (0.5-3%), (0.4-2%), (0.1-1%) (0.6-12%), (0.5-15%) and the balance of deionized water.
Preferably, the ratio of the water-soluble chitin derivative to the glycerin to the thickener in the component B is (0.6-12%) to (0.5-12%), and the balance is deionized water.
Preferably, the water-soluble chitin derivative is one or more of chitosan lactate, chitosan hydrochloride, carboxymethyl chitosan potassium salt or sodium salt, chitosan acetate and chitosan quaternary ammonium salt.
Preferably, the thickening agent comprises cellulose and polypropylene substances, wherein the cellulose comprises hydroxymethyl cellulose and hydroxyethyl cellulose; the polypropylene includes carbomer and polycarbophil; hyaluronic acid, gelatin.
Compared with the prior art, the invention has the beneficial effects that:
(1) contains no hormone; the pH value of the vagina is usually increased to 7.0-8.0 by semen, and the pH value of the vagina is adjusted to be within a normal range of 3.5-4.5 (the normal pH value of the vagina of a female is within the range) by a buffer system consisting of L-lactic acid, citric acid and potassium hydrogen tartrate, so that the acidic environment of the vagina of the female is maintained, and the acidic environment is not suitable for the survival of sperms but is essential for the survival of healthy bacteria in the vagina. Meanwhile, under the acidic environment, the water-soluble chitin derivative with higher molecular weight is subjected to acidolysis, and the bacteriostatic performance is exerted.
Drawings
FIG. 1 is a schematic diagram of A, B components in example 1 of the preparation method of the female contraceptive antibacterial gel lubricant.
Detailed Description
The technical solutions in the embodiments of the present invention will be clearly and completely described below with reference to the drawings in the embodiments of the present invention, and it is obvious that the described embodiments are only a part of the embodiments of the present invention, and not all of the embodiments. All other embodiments, which can be derived by a person skilled in the art from the embodiments given herein without making any creative effort, shall fall within the protection scope of the present invention.
The invention relates to a preparation method of a female contraceptive antibacterial gel lubricant, which consists of a component A and a component B according to the mass ratio of 1: 1, wherein the component A consists of the following raw materials in percentage by mass: 0.5-3% of L-lactic acid, 0.4-2% of citric acid, 0.1-1% of potassium hydrogen tartrate, 0.6-12% of glycerol, 0.5-15% of thickening agent and the balance of deionized water; the component B consists of the following raw materials in percentage by mass: 0.6-12% of water-soluble chitin derivative, 0.6-12% of glycerol, 0.5-12% of thickening agent and the balance of deionized water. The invention specifically comprises the following steps:
(1) preparing mixed solution of L-lactic acid, citric acid and potassium hydrogen tartrate according to a proportion;
(2) preparing a water-soluble chitin derivative into a solution according to a proportion;
(3) preparing gel with thickener and glycerol;
(4) mixing and stirring the solutions prepared in the steps (1) and (3) to obtain a component A;
(5) mixing and stirring the solutions prepared in the steps (2) and (3) to obtain a component B;
(6) filling component A and component B into two-component injector, and sterilizing
The component A of the invention comprises the following raw materials in a proper mass ratio: 1-2.5% of L-lactic acid, 0.5-1% of citric acid, 0.2-8% of potassium hydrogen tartrate, 1-8% of glycerol, 1-10% of thickening agent and the balance of deionized water; the component A comprises the following raw materials in a proper mass ratio: 0.6-12% of water-soluble chitin derivative, 0.6-12% of glycerol, 1-8% of thickening agent and the balance of deionized water.
The water-soluble chitin derivative is one or more of chitosan lactate, chitosan hydrochloride, carboxymethyl chitosan potassium salt or sodium salt, carboxymethyl chitin potassium salt or sodium salt, chitosan acetate and chitosan quaternary ammonium salt; cellulose as the thickener such as hydroxymethyl cellulose and hydroxyethyl cellulose; polypropylenes such as: carbomer, polycarbophil; hyaluronic acid, gelatin.
Example 1:
as shown in figure 1, the preparation method of the female contraceptive antibacterial gel lubricant comprises a component A and a component B according to the mass ratio of 1: 1, wherein the component A comprises the following raw materials in percentage by mass: l-lactic acid, citric acid, potassium hydrogen tartrate, glycerol, a thickening agent and the balance of deionized water; the component B consists of the following raw materials in percentage by mass: water-soluble chitin derivative, glycerin, thickening agent and the balance of deionized water. The invention specifically comprises the following steps:
(1) preparing mixed solution of L-lactic acid, citric acid and potassium hydrogen tartrate according to a proportion;
(2) preparing a water-soluble chitin derivative into a solution according to a proportion;
(3) preparing gel with thickener and glycerol;
(4) mixing and stirring the solutions prepared in the steps (1) and (3) to obtain a component A;
(5) mixing and stirring the solutions prepared in the steps (2) and (3) to obtain a component B;
(6) filling component A and component B into two-component injector, and sterilizing
The component A of the invention comprises the following raw materials in a proper mass ratio: 1% of L-lactic acid, 0.5% of citric acid, 0.2% of potassium hydrogen tartrate, 1% of glycerol, 1% of thickening agent and the balance of deionized water; the component A comprises the following raw materials in a proper mass ratio: 0.6 percent of water-soluble chitin derivative, 0.6 percent of glycerin, 1 percent of thickening agent and the balance of deionized water.
The water-soluble chitin derivative is one or more of chitosan lactate, chitosan hydrochloride, carboxymethyl chitosan potassium salt or sodium salt, carboxymethyl chitin potassium salt or sodium salt, chitosan acetate and chitosan quaternary ammonium salt; cellulose as the thickener such as hydroxymethyl cellulose and hydroxyethyl cellulose; polypropylenes such as: carbomer, polycarbophil; hyaluronic acid, gelatin.
Example 2:
a preparation method of a female contraceptive antibacterial gel lubricant comprises a component A and a component B according to the mass ratio of 1: 1, wherein the component A comprises the following raw materials in parts by mass: l-lactic acid, citric acid, potassium hydrogen tartrate, glycerol, a thickening agent and the balance of deionized water; the component B consists of the following raw materials in percentage by mass: water-soluble chitin derivative, glycerin, thickening agent and the balance of deionized water. The invention specifically comprises the following steps:
(1) preparing mixed solution of L-lactic acid, citric acid and potassium hydrogen tartrate according to a proportion;
(2) preparing a water-soluble chitin derivative into a solution according to a proportion;
(3) preparing gel with thickener and glycerol;
(4) mixing and stirring the solutions prepared in the steps (1) and (3) to obtain a component A;
(5) mixing and stirring the solutions prepared in the steps (2) and (3) to obtain a component B;
(6) filling component A and component B into two-component injector, and sterilizing
The component A of the invention comprises the following raw materials in a proper mass ratio: 2.5% of L-lactic acid, 1% of citric acid, 8% of potassium hydrogen tartrate, 8% of glycerol, 10% of thickening agent and the balance of deionized water; the component A comprises the following raw materials in a proper mass ratio: 12% of water-soluble chitin derivative, 12% of glycerol, 8% of thickening agent and the balance of deionized water.
The water-soluble chitin derivative is one or more of chitosan lactate, chitosan hydrochloride, carboxymethyl chitosan potassium salt or sodium salt, carboxymethyl chitin potassium salt or sodium salt, chitosan acetate and chitosan quaternary ammonium salt; cellulose as the thickener such as hydroxymethyl cellulose and hydroxyethyl cellulose; polypropylenes such as: carbomer, polycarbophil; hyaluronic acid, gelatin.
The preparation method of the female contraceptive antibacterial gel lubricant selects the raw materials, is safe to use, is simple and convenient to operate, and has no toxic or side effect; meanwhile, the preparation method of the female contraceptive antibacterial gel lubricant provided by the invention is low in cost, low in requirements on medical technical environment and simple to use.
The above description is only for the preferred embodiment of the present invention, but the scope of the present invention is not limited thereto, and any person skilled in the art should be considered to be within the technical scope of the present invention, and the technical solutions and the inventive concepts thereof according to the present invention should be equivalent or changed within the scope of the present invention.

Claims (8)

1. A preparation method of a female contraceptive antibacterial gel lubricant is characterized by comprising the following steps:
(1) preparing mixed solution of L-lactic acid, citric acid and potassium hydrogen tartrate according to a proportion;
(2) preparing a water-soluble chitin derivative into a solution;
(3) preparing a thickening agent and glycerol into gel;
(4) mixing and stirring the solutions prepared in the steps (1) and (3) to obtain a component A;
(5) mixing and stirring the solutions prepared in the steps (2) and (3) to obtain a component B;
(6) and respectively filling the component A and the component B into a two-component injector, and sterilizing.
2. A method of preparing a female contraceptive antibacterial gel lubricant as claimed in claim 1, wherein: the mass ratio of the component A to the component B is 1: 1.
3. A method of preparing a female contraceptive antibacterial gel lubricant as claimed in claim 2, wherein: the component A comprises L-lactic acid, citric acid, potassium hydrogen tartrate, glycerol and a thickening agent in a ratio of (0.5-3%), 0.4-2%, 0.1-1%, (0.6-12%), 0.5-15% and the balance of deionized water.
4. A method of preparing a female contraceptive antibacterial gel lubricant as claimed in claim 2, wherein: the proportion of the water-soluble chitin derivative, the glycerin and the thickening agent in the component B is 0.6-12 percent to 0.5-12 percent, and the balance is deionized water.
5. A method of preparing a female contraceptive antibacterial gel lubricant as claimed in claim 4, wherein: the water-soluble chitin derivative is one or more of chitosan lactate, chitosan hydrochloride, carboxymethyl chitosan potassium salt or sodium salt, carboxymethyl chitin potassium salt or sodium salt, chitosan acetate and chitosan quaternary ammonium salt.
6. A method of preparing a female contraceptive antibacterial gel lubricant as claimed in claim 4, wherein: the thickening agent comprises cellulose and polypropylene substances.
7. A method of preparing a female contraceptive antibacterial gel lubricant as claimed in claim 6, wherein: the cellulose comprises hydroxymethyl cellulose and hydroxyethyl cellulose.
8. A method of preparing a female contraceptive antibacterial gel lubricant as claimed in claim 6, wherein: the polypropylene includes carbomer and polycarbophil; hyaluronic acid, gelatin.
CN202011235443.0A 2020-11-06 2020-11-06 Preparation method of female contraceptive antibacterial gel lubricant Pending CN112274480A (en)

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112933109A (en) * 2021-02-03 2021-06-11 湖南奥朗特医疗器械有限公司 Vagina pH regulator and preparation method and application thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000015192A1 (en) * 1998-09-17 2000-03-23 Zonagen, Inc. Methods and materials related to bioadhesive contraceptive gels
CN101172159A (en) * 2006-10-30 2008-05-07 上海市计划生育科学研究所 Acidic biological adhesion heat-variable gelling agent, its preparing method and uses
CN101559036A (en) * 2008-04-18 2009-10-21 上海医药工业研究院 Conception control gel composition for vagina as well as preparation method and application thereof
CN101889974A (en) * 2010-07-12 2010-11-24 林一文 Chitosan contraceptive gel and preparation method thereof

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000015192A1 (en) * 1998-09-17 2000-03-23 Zonagen, Inc. Methods and materials related to bioadhesive contraceptive gels
CN101172159A (en) * 2006-10-30 2008-05-07 上海市计划生育科学研究所 Acidic biological adhesion heat-variable gelling agent, its preparing method and uses
CN101559036A (en) * 2008-04-18 2009-10-21 上海医药工业研究院 Conception control gel composition for vagina as well as preparation method and application thereof
CN101889974A (en) * 2010-07-12 2010-11-24 林一文 Chitosan contraceptive gel and preparation method thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112933109A (en) * 2021-02-03 2021-06-11 湖南奥朗特医疗器械有限公司 Vagina pH regulator and preparation method and application thereof

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