Benzalkonium chloride contraceptive gel capable of killing AIDS pathogens and preparation method of benzalkonium chloride contraceptive gel

By using modified cyclodextrin and amino acid grafting technology, combined with arginine and cysteine, and optimizing the grafting process, the problems of slow inactivation speed and short mucosal retention time of benzalkonium chloride contraceptive gel against HIV pathogens have been solved. This has achieved rapid and efficient virus inactivation and long-lasting mucosal adhesion, providing dual protection.

CN122376525APending Publication Date: 2026-07-14JIAN CHANGJIANG PHARM CO LTD
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Patent Information

Application Number
CN202610781115.1
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2026-06-02
Publication Date
2026-07-14

AI Technical Summary

Technical Problem

Existing benzalkonium chloride contraceptive gels have a slow inactivation rate against HIV pathogens, a short mucosal retention time, and low drug utilization, making them unable to quickly and efficiently kill HIV pathogens and provide a lasting protective barrier during sexual intercourse.

Method used

Modified cyclodextrin was used to generate aldehyde groups by oxidizing γ-cyclodextrin with sodium periodate, which then reacted with amino acids to form imine bonds. These imine bonds were then reduced to secondary amine bonds with sodium borohydride. The amino acids were grafted onto the cyclodextrin backbone. Combined with arginine and cysteine, the stepwise grafting process was optimized to improve mucosal adhesion and virus inactivation efficiency by utilizing the synergistic effect of electrostatic adsorption and thiol group disruption of the viral envelope.

Benefits of technology

It significantly improves the instantaneous inactivation rate and mucosal retention performance of benzalkonium chloride gel against HIV pathogens, achieving a dual protective effect of rapid and efficient virus clearance and long-lasting physical barrier.

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Abstract

The invention discloses benzalkonium chloride contraceptive gel for killing AIDS pathogens and a preparation method, and belongs to the technical field of biological medicine manufacturing, and the benzalkonium chloride contraceptive gel is prepared from water, hydroxypropyl methylcellulose, polyquaternium-10, modified cyclodextrin, edetate disodium, benzalkonium chloride and glycerin according to a specific ratio. The preparation method comprises the following steps: thermally dispersing hydroxypropyl methylcellulose and polyquaternium-10, cooling, sucking and mixing an aqueous solution of modified cyclodextrin, edetate disodium and benzalkonium chloride, adding glycerol, cooling, homogenizing, and carrying out vacuum degassing to obtain a finished product. Compared with the prior art, the amino acid grafted modified cyclodextrin is used for enhancing the inclusion and mucous membrane adhesion performance, and the obtained gel is high in AIDS pathogen inactivation rate and long in vagina residence time, has efficient antiviral and long-acting barrier effects, and is low in irritation, safe and reliable.
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