Coppi G, Silingardi S, Girardello R, De Aloysio D, Manzardo S
Pharmacological and Toxicological Department, Poli Industria Chimica, Rozzano, Milan, Italy.
J Chemother. 1993 Oct;5(5):302-6. doi: 10.1080/1120009x.1993.11755468.
The authors reported the plasma levels and pharmacokinetic parameters of ciclopirox olamine in rabbits after i.v. and intravaginal administrations and in female patients after vaginal administration. Plasma levels of total and free ciclopirox were determined by a HPLC method. In rabbit ciclopirox showed a half-life of 2.22 h and an intravaginal bioavailability of about 2%. In female patients ciclopirox showed low intravaginal absorption; this value might explain the good local and systemic tolerability and also the penetration of drug in deep tissue.
作者报告了静脉注射和阴道给药后兔体内环吡酮胺的血浆水平和药代动力学参数，以及阴道给药后女性患者体内的相关情况。采用高效液相色谱法测定总环吡酮和游离环吡酮的血浆水平。在兔体内，环吡酮的半衰期为2.22小时，阴道生物利用度约为2%。在女性患者中，环吡酮的阴道吸收较低；这一数值可能解释了其良好的局部和全身耐受性，以及药物在深部组织中的渗透情况。
