Optimized Benzalkonium Chloride Gel: A Potential Vaginal Microbicides  

作　　者：Xun-cheng DING Wei-hua LI Jie-fei LI Qiang-yi WANG 

机构地区：[1]Shanghai Institute of Planned Parenthood Research, Shanghai 200032, China

出　　处：《Journal of Reproduction and Contraception》2007年第2期89-92,共4页生殖与避孕（英文版）

摘　　要：Objective To develop an optimized BZK gel with good pharmaceutical effect and less toxicity to vaginal mucosa. Methods Four methods as below were used to research the spermicidal activity of BZK gel： 1） in vitro spermicidal test; 2） in vivo spermicidal test in rabbits; 3） anti-fertility test in rabbits; 4） contraceptive test in rabbits. Mucosal irritation test was used in rats to evaluate the safety of optimized BZK gel. Microbiological assessments were used to research anti-STI pathogens （including treponema pallidum, neisseria gonorrhoeae, trichomona vaginalis, candida albicans, ureaplama urealyticum, herpes simplex virus type-2, chlamydiae trachomatis） effect of optimized BZK gel. Results In vitro spermicidal test, EC50 of BZK gel was 0.029mg/ml, a little higher than that of N-9 （0.019mg/ml）. The MIC of BZK gel was 0.25mg/ml, similar to that of N-9 （0.20mg/ml）. The vaginal mucosal irritation test in rats showed that 0.429% BZK gel showed only minimal vaginal irritation, and did not damage the vaginal epithelium or cause local inflammation in rats. Microbiological assessments showed that optimized BZK gel could inhibit or inactivate common ST1 pathogens even after 3-fold or 5-fold dilution. Conclusion Optimized BZK gel was an effective microbicides.Objective To develop an optimized BZK gel with good pharmaceutical effect and less toxicity to vaginal mucosa. Methods Four methods as below were used to research the spermicidal activity of BZK gel： 1） in vitro spermicidal test; 2） in vivo spermicidal test in rabbits; 3） anti-fertility test in rabbits; 4） contraceptive test in rabbits. Mucosal irritation test was used in rats to evaluate the safety of optimized BZK gel. Microbiological assessments were used to research anti-STI pathogens （including treponema pallidum, neisseria gonorrhoeae, trichomona vaginalis, candida albicans, ureaplama urealyticum, herpes simplex virus type-2, chlamydiae trachomatis） effect of optimized BZK gel. Results In vitro spermicidal test, EC50 of BZK gel was 0.029mg/ml, a little higher than that of N-9 （0.019mg/ml）. The MIC of BZK gel was 0.25mg/ml, similar to that of N-9 （0.20mg/ml）. The vaginal mucosal irritation test in rats showed that 0.429% BZK gel showed only minimal vaginal irritation, and did not damage the vaginal epithelium or cause local inflammation in rats. Microbiological assessments showed that optimized BZK gel could inhibit or inactivate common ST1 pathogens even after 3-fold or 5-fold dilution. Conclusion Optimized BZK gel was an effective microbicides.

关 键 词：Benzalkonium Chloride MICROBICIDES CONTRACEPTION HIV/AIDS 

分 类 号：R169.41[医药卫生—公共卫生与预防医学] R984