Cochet P, Birckel P, Bromet-Petit M, Bromet N, Weil A
Biotec Centre, Orleans, France.
Eur J Drug Metab Pharmacokinet. 1997 Jul-Sep;22(3):211-6. doi: 10.1007/BF03189809.
To investigate the localisation of fipronil in dog skin, [14C]-fipronil was topically applied to a male beagle dog (spot-on administration) at the therapeutic dose of 10 mg/kg. By means of autohistoradiography, the radioactivity was precisely detected in the skin and appendages at various intervals after application. Radioactivity was predominantly observed within the stratum corneum, the viable epidermis, and in the pilo-sebaceous units (mainly in the sebaceous glands and epithelial layers). [14C]-fipronil was significantly detected in these structures up to 56 days post-treatment, in the application zone (neck) but also in the lumbar zone, thus indicating the mechanical displacement of fipronil. No radioactivity was detected in either the dermal or the hypodermal layers, confirming the low percutaneous passage of fipronil.
为研究氟虫腈在犬皮肤中的定位,以10 mg/kg的治疗剂量将[14C] - 氟虫腈局部应用于一只雄性比格犬(滴剂给药)。通过自动放射自显影术,在给药后的不同时间间隔精确检测到皮肤和附属器中的放射性。放射性主要在角质层、活表皮以及毛囊皮脂腺单位(主要在皮脂腺和上皮层)中观察到。在治疗后长达56天,在涂抹区域(颈部)以及腰部区域的这些结构中均显著检测到[14C] - 氟虫腈,这表明氟虫腈发生了机械性移位。在真皮层或皮下层均未检测到放射性,证实氟虫腈的经皮渗透率较低。