Anti-HIV (human immunodeficiency virus) composite protection human body lubricating liquid as well as preparation method and application thereof

Abstract

The invention relates to an anti-HIV composite protective human body lubricating liquid. The anti-HIV composite protective human body lubricating liquid comprises the following components in percentage by weight: 0.5-1.2% of composite quaternary ammonium salt, which is composed of dodecyl dimethyl benzyl ammonium chloride and didecyl dimethyl ammonium chloride according to a mass ratio of 3: 1; 0.8 to 1.5 percent of polyquaternium-10; 0.5 to 1.0 percent of chitosan quaternary ammonium salt; 0.2 to 0.5 percent of Lipidium-PMB (Polymethyl Benzene); 0.3 to 0.8 percent of polyvinyl alcohol; 5-10% of a humectant; the pH regulator is used for regulating the pH of the system to 4.5-5.5; and the balance of deionized water. Wherein the inactivation rate of the lubricating liquid to HIV-1 virus is greater than or equal to 99.99%. The preparation method has the advantages that the composite quaternary ammonium salt is combined with the film-forming material, so that the lubricating liquid is endowed with the capability of actively inactivating the HIV virus; the physical barrier effect is enhanced through the biomimetic membrane technology, and viruses are prevented from invading minimal mucous membrane wounds; the formula is optimized, the biological adhesiveness is improved, and long-acting protection is ensured.

Description

Technical Field

[0001] This invention relates to an anti-HIV composite protective human lubricant, belonging to the field of lubricants. Background Technology

[0002] Personal lubricants, as a common product used during intimate sexual activity, are currently mainly based on water, silicone, or oil, with their core functions being lubrication and moisturizing (such as glycerin and propylene glycol). Although some products add antibacterial agents (such as benzalkonium chloride), their blocking effect on HIV is not specific and they do not possess anti-HIV functions. HIV sexual transmission primarily occurs through mucosal contact. Globally, approximately 30% of new HIV infections each year are related to unprotected sex, and traditional lubricants cannot reduce the risk of viral entry through mucosal wounds.

[0003] Defects and shortcomings of existing technology: (1) No specific anti-HIV mechanism: Conventional antibacterial agents are only effective against bacteria and cannot destroy the HIV viral envelope or inhibit reverse transcriptase activity; (2) Lack of physical barrier: lack of film-forming materials, unable to form an effective physical barrier on the mucosal surface; (3) Short duration of action: Poor biological adhesion, easily washed away and ineffective during sexual activity. Summary of the Invention

[0004] To overcome the shortcomings of existing technologies, this invention provides an anti-HIV composite protective human lubricant, its preparation method, and its application. The technical solution of this invention is as follows: An anti-HIV compound protective human lubricant, comprising the following components by weight percentage: compound quaternary ammonium salt: 0.5%–1.2%; polyquaternary ammonium salt-10: 0.8%–1.5%; chitosan quaternary ammonium salt: 0.5%–1.0%; Lipidure-PMB: 0.2%–0.5%; polyvinyl alcohol: 0.3%–0.8%; humectant: 5%–10%; pH adjuster: used to adjust the pH of the system to 4.5–5.5; the balance being deionized water; wherein, the lubricant has an inactivation rate of ≥99.99% against HIV-1 virus; The composition is as follows: 0.8% composite quaternary ammonium salt, 1.2% polyquaternary ammonium salt-10, 0.8% chitosan quaternary ammonium salt, 0.3% Lipidure-PMB, 0.5% polyvinyl alcohol, 8% humectant, and the remainder is deionized water.

[0005] The composite quaternary ammonium salt is composed of dodecyl dimethyl benzyl ammonium chloride and decyl dimethyl ammonium chloride in a mass ratio of 3:1; the humectant is a mixture of glycerin and propylene glycol in a ratio of 5:3.

[0006] The physical barrier component forms a dense film with a pore size of 50–80 nm to intercept HIV virus particles with a diameter ≥100 nm; the Lipidure-PMB reduces the affinity between the virus and mucosal cells through a biomimetic membrane structure.

[0007] A method for preparing the aforementioned anti-HIV composite protective human lubricant includes the following steps: (1) Dissolution of film-forming materials: Add polyquaternium-10 and chitosan quaternium salt to deionized water at 48-52℃ and stir for 30-60 minutes until transparent; (2) Dispersion of composite quaternary ammonium salt: Add composite quaternary ammonium salt and stir for 30-60 minutes at a speed of 200-400 rpm; (3) Addition of functional components: Add polyvinyl alcohol solution and Lipidure-PMB in sequence, and stir for 30-60 min; (4) Adding moisturizer: Add the pre-mixed glycerin and propylene glycol, and continue stirring for 30–60 minutes; (5) pH adjustment and homogenization: Adjust the pH to 4.5–5.5 with citric acid solution, and homogenize under high pressure at 20–30 MPa 2–3 times; (6) Degassing: Degas for 10–20 minutes under vacuum conditions of -0.08 to -0.09 MPa.

[0008] In step (3), the concentration of the polyvinyl alcohol solution is 5%; in step (4), the mass ratio of glycerol to propylene glycol is 5:3; in step (5), the concentration of citric acid is 10%.

[0009] The application of the aforementioned anti-HIV composite protective lubricant in the preparation of protective products for preventing HIV sexual transmission.

[0010] The protective products include, but are not limited to, lubricants, condom coatings, vaginal films, or rectal gels.

[0011] The advantages of this invention are: (1) Combining composite quaternary ammonium salts with film-forming materials to endow lubricants with the ability to actively inactivate HIV virus; (2) Enhance the physical barrier effect through biomimetic membrane technology to block the virus from invading the mucosal micro-wounds; (3) Optimize the formula to improve bioadhesion and ensure long-lasting protection.

[0012] (4) Triple protection mechanism: Active inactivation: The compound quaternary ammonium salt achieved an inactivation rate of 99.9% against HIV-1 virus; Physical barrier: The film-forming material has a pore size of 50-80nm, which can intercept HIV virus particles with a diameter of about 100nm; Bionic protection: Lipidure-PMB mimics the cell membrane structure, reducing the affinity between the virus and mucosal cells; (5) Biosafety: It is non-irritating after mucosal irritation test. Detailed Implementation

[0013] The present invention will be further described below with reference to specific embodiments, and the advantages and features of the present invention will become clearer as a result. However, these embodiments are merely exemplary and do not constitute any limitation on the scope of the present invention. Those skilled in the art should understand that modifications or substitutions can be made to the details and form of the technical solutions of the present invention without departing from the spirit and scope of the present invention, but all such modifications and substitutions fall within the protection scope of the present invention.

[0014] Example 1: An anti-HIV compound protective human lubricant, comprising the following components by weight percentage: 0.5% compound quaternary ammonium salt: composed of dodecyl dimethyl benzyl ammonium chloride and disacyl dimethyl ammonium chloride in a mass ratio of 3:1; 0.8% polyquaternary ammonium salt-10; 0.5% chitosan quaternary ammonium salt; 0.2% Lipidure-PMB; 0.3% polyvinyl alcohol; 5% humectant; pH adjuster: adjusts the system pH to 4.5; the balance is deionized water; wherein the humectant is a mixture of glycerol and propylene glycol in a 5:3 ratio; the lubricant has an inactivation rate of ≥99.99% against HIV-1 virus.

[0015] The physical barrier component forms a dense film with a pore size of 50 nm, which is used to intercept HIV virus particles with a diameter of ≥100 nm; the Lipidure-PMB reduces the affinity between the virus and mucosal cells through a biomimetic membrane structure.

[0016] A method for preparing the aforementioned anti-HIV composite protective human lubricant includes the following steps: (1) Dissolution of film-forming materials: Add polyquaternium-10 and chitosan quaternium to deionized water at 48°C and stir for 30 minutes until transparent; (2) Dispersion of composite quaternary ammonium salt: Add composite quaternary ammonium salt and stir for 30 min at a speed of 200 rpm; (3) Addition of functional components: Add polyvinyl alcohol solution and Lipidure-PMB in sequence and stir for 30 min; (4) Adding moisturizer: Mix glycerin and propylene glycol in a ratio of 5:3 and add to the mixture, stirring for 30 minutes; (5) pH adjustment and homogenization: Adjust the pH to 4.5 with citric acid, and homogenize twice under high pressure at 20 MPa; (6) Degassing: Degas for 10 min under a vacuum of -0.08 MPa.

[0017] In step (3), the concentration of the polyvinyl alcohol solution is 5%; in step (5), the concentration of the citric acid is 10%.

[0018] The present invention also relates to the use of a lubricant in the preparation of protective products for preventing the sexual transmission of HIV.

[0019] Example 2: An anti-HIV compound protective human lubricant, comprising the following components by weight percentage: The composition of the lubricant is as follows: 0.8% composite quaternary ammonium salt, 1.2% polyquaternary ammonium salt-10, 0.8% chitosan quaternary ammonium salt, 0.3% Lipidure-PMB, and 0.5% polyvinyl alcohol; 8% humectant. pH adjuster: adjusts the pH of the system to 5.0; the balance is deionized water; wherein the humectant is a mixture of glycerol and propylene glycol in a 5:3 ratio; the lubricant has an inactivation rate of ≥99.99% against HIV-1 virus.

[0020] A method for preparing the aforementioned anti-HIV composite protective human lubricant includes the following steps: (1) Dissolution of film-forming materials: Add polyquaternium-10 and chitosan quaternium salt to deionized water at 50°C and stir for 45 minutes until transparent; (2) Dispersion of composite quaternary ammonium salt: Add composite quaternary ammonium salt and stir at 300 rpm for 45 min; (3) Addition of functional components: Add polyvinyl alcohol solution and Lipidure-PMB in sequence and stir for 45 min; (4) Addition of moisturizer: Mix glycerin and propylene glycol in a ratio of 5:3 and add the mixture, stirring for 45 minutes; (5) pH adjustment and homogenization: Adjust the pH to 5.0 with citric acid, and homogenize twice under high pressure at 25 MPa; (6) Degassing: Degas for 15 min under a vacuum of -0.085 MPa.

[0021] In step (3), the concentration of the polyvinyl alcohol solution is 5%; in step (5), the concentration of the citric acid is 10%.

[0022] The present invention also relates to the use of a lubricant in the preparation of protective products for preventing the sexual transmission of HIV.

[0023] Example 3: An anti-HIV compound protective human lubricant, comprising the following components by weight percentage: The lubricant comprises: 1.2% compound quaternary ammonium salt, composed of dodecyl dimethyl benzyl ammonium chloride and disacyl dimethyl ammonium chloride in a mass ratio of 3:1; 1.5% polyquaternary ammonium salt-10; 1.0% chitosan quaternary ammonium salt; 0.5% Lipidure-PMB; 0.8% polyvinyl alcohol; 10% humectant; pH adjuster: adjusting the system pH to 5.5; the remainder being deionized water; wherein the humectant is a mixture of glycerol and propylene glycol in a 5:3 ratio; the lubricant has an inactivation rate of ≥99.99% against HIV-1 virus.

[0024] The physical barrier component forms a dense film with a pore size of 80 nm, which is used to intercept HIV virus particles with a diameter ≥100 nm; the Lipidure-PMB reduces the affinity between the virus and mucosal cells through a biomimetic membrane structure.

[0025] A method for preparing the aforementioned anti-HIV composite protective human lubricant includes the following steps: (1) Dissolution of film-forming materials: Add polyquaternium-10 and chitosan quaternium salt to deionized water at 52°C and stir for 60 minutes until transparent; (2) Dispersion of composite quaternary ammonium salt: Add composite quaternary ammonium salt and stir at 400 rpm for 60 min; (3) Addition of functional components: Add polyvinyl alcohol solution and Lipidure-PMB in sequence and stir for 60 min; (4) Addition of moisturizer: Mix glycerin and propylene glycol in a ratio of 5:3 and add to the mixture and stir for 60 minutes; (5) pH adjustment and homogenization: Adjust the pH to 5.5 with citric acid, and homogenize at 30 MPa three times; (6) Degassing: Degas for 20 min under a vacuum of -0.09 MPa.

[0026] In step (3), the concentration of the polyvinyl alcohol solution is 5%; in step (5), the concentration of the citric acid is 10%.

[0027] The present invention also relates to the use of a lubricant in the preparation of protective products for preventing the sexual transmission of HIV.

[0028] The following is a comparison table of key data on HIV virus inactivation rates for three examples, covering basic parameters, experimental conditions, and validation results: Conclusion 1. Inactivation rate stability: Even with the lowest amount of active ingredient (Example 1), the inactivation rate was still ≥99.99%, proving that the formulation is highly effective over a wide concentration range; 2. Tolerance to extreme environments: Example 2: After 2 hours of flushing with bodily fluids, the inactivation rate remained at 99.998% (existing products become ineffective after 15 minutes). Example 3: In simulated mucosal wounds (containing serum exudate), the virus invasion inhibition rate is >99.9%, solving a core pain point in the industry.

[0029] Conclusion: Through gradient concentration design, the three embodiments jointly demonstrate that the technical solution of the present invention can achieve an HIV inactivation rate of ≥99.99% in conventional environments, body fluid flushing, and mucosal wound scenarios.

[0030] The above description is only a preferred embodiment of the present invention, but the scope of protection of the present invention is not limited thereto. Any equivalent substitutions or modifications made by those skilled in the art within the scope of the technology disclosed in the present invention, based on the technical solution and inventive concept of the present invention, should be covered within the scope of protection of the present invention.

Claims

1. A composite protective lubricant against HIV, characterized in that, It contains the following components by weight percentage: Complex quaternary ammonium salts: 0.5%–1.2%; Polyquaternary ammonium salt-10: 0.8%–1.5%; Chitosan quaternary ammonium salts: 0.5%–1.0%; Lipidure-PMB: 0.2%–0.5%; Polyvinyl alcohol: 0.3%–0.8%; Humidifier: 5%–10%; pH adjuster: used to adjust the pH of the system to 4.5–5.5; the balance is deionized water; wherein, the lubricating fluid has an inactivation rate of ≥99.99% against HIV-1 virus.

2. The anti-HIV composite protective human lubricant according to claim 1, characterized in that, The composition is as follows: 0.8% composite quaternary ammonium salt, 1.2% polyquaternary ammonium salt-10, 0.8% chitosan quaternary ammonium salt, 0.3% Lipidure-PMB, 0.5% polyvinyl alcohol, 8% humectant, and the remainder is deionized water.

3. The anti-HIV composite protective human lubricant according to claim 2, characterized in that, The composite quaternary ammonium salt is composed of dodecyl dimethyl benzyl ammonium chloride and decyl dimethyl ammonium chloride in a mass ratio of 3:1; the humectant is a mixture of glycerin and propylene glycol in a ratio of 5:

3.

4. The anti-HIV composite protective human lubricant according to claim 3, characterized in that, The physical barrier component forms a dense film with a pore size of 50–80 nm to intercept HIV virus particles with a diameter ≥100 nm; the Lipidure-PMB reduces the affinity between the virus and mucosal cells through a biomimetic membrane structure.

5. A method for preparing the anti-HIV composite protective human lubricant according to any one of claims 1-4, comprising the following steps: (1) Dissolution of film-forming materials: Add polyquaternium-10 and chitosan quaternium salt to deionized water at 48-52℃ and stir for 30-60 minutes until transparent; (2) Dispersion of composite quaternary ammonium salt: Add composite quaternary ammonium salt and stir for 30-60 minutes at a speed of 200-400 rpm; (3) Addition of functional components: Add polyvinyl alcohol solution and Lipidure-PMB in sequence, and stir for 30-60 min; (4) Adding moisturizer: Add the pre-mixed glycerin and propylene glycol, and continue stirring for 30–60 minutes; (5) pH adjustment and homogenization: Adjust the pH to 4.5–5.5 with citric acid solution, and homogenize under high pressure at 20–30 MPa 2–3 times; (6) Degassing: Degas for 10–20 minutes under vacuum conditions of -0.08 to -0.09 MPa.

6. The preparation method of the anti-HIV composite protective human lubricant according to claim 5, characterized in that, In step (3), the concentration of the polyvinyl alcohol solution is 5%; in step (4), the mass ratio of glycerol to propylene glycol is 5:3; in step (5), the concentration of citric acid is 10%.

7. The use of the anti-HIV composite protective lubricant as described in any one of claims 1–6 in the preparation of protective products for preventing the sexual transmission of HIV.

8. The application according to claim 7, characterized in that, The protective products include, but are not limited to, lubricants, condom coatings, vaginal films, or rectal gels.

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