摘要
甲硝唑阴道粘膜粘附片是一类新型局部用缓释制剂,体外释药速率呈一级和零级混合型释放模式,用仿制张力仪测定其粘附强度为4768.9Pa。观察体内外滞留行为,呈良好的溶胀状态。HPLC 分析5例,正常受试者阴道给药60h 血浓度低于3μg/ml,6例滴虫性阴道炎患者给药36h后体内局部残留量最低限度为15%(标示量),甲硝唑血浓度为0.88～3.0μg/ml,另6例患者给药60h后分别为10%,0.25μg/ml 以下,且5例滴虫转阴。经临床试用50例,2～3d 给药1片,安全有效,不良反应发生少。
Metronidazole vaginal muco-adhesive tablet(MVMT)was a new topical sustained-release dosageform.The in vitro dissolution rate profile could bedescribed by the first order and zero order kinetics.Its adhesive strength was 4768.9Pa when a tensileapparatus was used with the rabbit sublingual mu- cus.The MVTM was vaginally administrated to fivehealthy voluntary women and its plasma level mea-sured by HPLC method.The absorption concentra-tion of the MVTM was below 3.0μg/ml from be-ginning to 60h after giving a single dose of theMVMT.This tablet swelled well in vitro and in vivo.It was found that the metronidazole(MTD)residentamount of the MVMT in the vagina existed at least15%,and the MTD plasma levels were 0.88～3.0μg/ml in 6 patients with trichomonas vaginitisafter 36h.For the other 6 patients the MTD resi-dent amount existed at least 10% and the MTDplasma levels were below 0.25μg/ml after 60h.The MVMT was used in 50 patients receiving 1tablet every two to three days,It was safe and ef-fective No ADR was found.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1992年第9期532-535,共4页
Chinese Pharmaceutical Journal
关键词
甲硝唑
粘膜粘附片
妇产科药物
metronidazole
vaginal muco-adhesive of metronidazole
adhesive strength
active system
HPLC
