摘要
本文研制的酮康唑阴道粘附缓释片具有粘膜粘附、缓慢释药特点,其体外释药行为呈现一级动力学(K_r=0.4516h^(-1),r=0.9912) ,Pco_2为38mmHg,粘附强度为12976.86dyn/cm。9例霉菌性阴道炎患者单剂量给药24h后体内局部残留量至少为13%(标示量 ),另7例给药48h后大于5%,10例患者应用该制剂结果表明:无刺激性、不改变环境pH,症状可明显改善。
A ketoconazole vaginal adhesive tablet (KVAT) was developed. KVAT could stick to the vaginal vault surface and release the drug steadily. It was found that dissolution of KVAT in vitro presented first order kinetics (0~6) with a dissolution rate constants of 0.4516 h^(-1). The Pco_2 was 38 mm Hg and the surface tension was 12976.86 dyn/cm for KVAT. At least 13% of the ketoconazole in KVAT remained in vagina in nine patients suffered from mycotic vaginitis after 24 h and exceeded 5 % in the other seven patients after 48 h. Moreover, the preparation was not irritatative and did not alter vaginal pH. Symptoms improved significantly in ten patients.
关键词
酮康唑
阴道炎
阴道粘附片
研制
ketoconazole
ketoconazole vaginal adhesive tablet
mycotic
vaginitis