Peters H, Moll F
Institute of Pharmacy, University of Mainz, Germany.
Arzneimittelforschung. 1995 Dec;45(12):1253-6.
A phospholipid containing formulation with tetracaine (CAS 94-24-6) for topical anaesthesia was developed. In vitro drug liberation as well as in vivo efficacy and duration of the anaesthetic effect were investigated. The in vitro liberation constant was 0-.626 +/- 0.005 mg/(cm2.square root of h for a liposomal gel formulation containing 2% (m/l) tetracaine. The gel showed high efficacy in anaesthetizing the skin after topical application. After 60 min of application complete anaesthesia of the skin was observed with all volunteers. The duration of anaesthesia after removing the application system was 150 min on average. The determination of the in vivo penetration rate resulted in values between 0.010 and 0.015 mumol/min.cm2 tetracaine.
开发了一种含丁卡因（CAS 94-24-6）的用于局部麻醉的磷脂制剂。研究了体外药物释放以及体内麻醉效果的功效和持续时间。对于含有2%（m/l）丁卡因的脂质体凝胶制剂，体外释放常数为0.626±0.005毫克/（平方厘米·h的平方根）。该凝胶局部应用后对皮肤具有高效麻醉作用。应用60分钟后，所有志愿者的皮肤均出现完全麻醉。去除应用系统后的麻醉持续时间平均为150分钟。体内渗透速率的测定结果为丁卡因的值在0.010至0.015微摩尔/分钟·平方厘米之间。
