薄荷醇和氮酮对甲硝唑在犬中体外透皮吸收的影响

研究不同的溶液载体（PBS，5％薄荷醇和5％氮酮）和不同部位的皮肤对甲硝唑在犬中体外透皮吸收和皮内摄取的影响。取下北京犬颈部、胸部以及腹部皮肤，-20℃保存。使用时，皮肤解冻固定在改良Franz透皮扩散仪上，保持恒速（200±1）r／min，恒温（35±0．5）℃。在扩散池中的皮肤角质层上加入2mL溶液载体（含甲硝唑58．4μmol），以20％乙醇为溶剂溶解薄荷醇和氮酮，在预定时间点取样1mL，采用HPLC方法测定各接受液中的药物量和皮肤中摄取的药物量。结果显示，与PBS相比，薄荷醇和氮酮能增加所有部位甲硝唑的透皮吸收量和皮内摄取量（P〈0．05）。同一溶液载体在不同部位的渗透性存在差异，腹部〉颈部〉胸部，不同部位的皮内摄取量也存在差异，颈部〉胸部〉腹部。说明甲硝唑在不同溶液载体和不同部位皮肤的渗透性存在差异。

Effect of menthol and Azone with on the transdermal delivery of metronidazole through the canine skin in vitro

This study investigated the effects of the vehicles（ PBS ,5% administration on the penetration and retention amount of metronidazole menthol and 5 % azone） and the region of through canine skin in vitro. Skin was harvested from the neck ,thorax and abdomen region of female Pekingese after euthanasia and stored at -20℃ until required. The skin was defrosted and placed in the Franz - type diffusion cells. The stirring rate was maintained at （200 ± 1 ）r/min and temperature was maintained at （35±0.5）℃. 2 mL of donor solutions that contained 58.4 μmol metronidazole in each formulation were applied to the stratum corneum （SC） surface of each skin sample with 20%EtOH to dissolve the menthol and azone. Samples （lmL） were collected at predetermined time inter- vals. The diffused metronidazole in the receptor solution and the retained amount of metronidazole in the skin were quantified by using high performance liquid chromatography （HPLC）. The results indicated that the penetration and the retention amount of metraoidazole were significantly higher for all sites when dissolved in a vehicle contaning menthol or azone, compared to PBS （ P 〈 0.05 ）. There was significantly difference in the penetration amount of metronidazole for all sites. The efficiency of the region of application to improve the penetration amount of metronidazole was sequenced in the order of： abdomen 〉 neck 〉 thorax. The retention amount for all sites was in the following order： neck 〉 thorax 〉 abdomen. This study showed that variablity in percutaneous penetrability of metronidazole could be expected with different vehicles and site application.