摘要
本试验比较了地佐辛贴片、凝胶和溶液剂对离体大鼠皮肤和乳猪皮肤的体外经皮渗透性能,并对其不同剂型做出评价。采用Franz扩散池进行体外透皮试验,以HPLC法测定接收液中的地佐辛浓度。结果显示:以大鼠皮肤为屏障时,贴片、凝胶和溶液剂3种剂型的24 h累积渗透量分别为(227.52±26.55)、(357.87±26.34)和(597.69±102.63)μg/cm^2;以猪皮为屏障时,24 h累积渗透量分别为(68.09±19.06)、(39.84±10.44)和(54.99±50.48)μg/cm^2。说明大鼠皮肤比猪皮更易透过,因此更适用于前期处方的区分及筛选。而贴片在与人皮肤更相似的猪皮上累积透过量更高,且释放行为符合零级模型,更适合开发为地佐辛外用制剂。
This paper aimed to compare and evaluate the in vitro percutaneous permeability of dezocine patch, gel and solution preparations through different kinds of skin. In vitro transdermal experiments were performed in Franz diffusion cells. The concentration of dezocine in the receiving solution was measured by HPLC. The results showed that when using rat skin as the barrier, the cumulative permeation amounts at 24 h of above three formulations were(227.52±26.55),(357.87±26.34) and(597.69±102.63)μg/cm2;when the Bama miniature pig skin was used as the barrier, the cumulative permeation amounts were(68.09±19.06),(39.84±10.44) and(54.99±50.48)μg/cm2, respectively. In conclusion, rat skin was more permeable than Bama miniature pig skin because of the difference of the thickness of stratum corneum, so that it is more suitable for the differentiation and screening in early formulation development. However, the patches exhibited relatively better permeability through Bama miniature pig skin which was similar to human skin due to its greater lipophilic ability to penetrate through the stratum corneum. The transdermal behavior of dezocine from the patches was fitted to zero-order model. Therefore, patches were more suitable for the development of the external preparation of dezocine.
作者
杨雅丽
童想柳
林国钡
罗华菲
YANG Yali;TONG Xiangliu;LIN Guobei;LUO Huafei(National Pharmaceutical Engineering Research Center,China State Institute of Pharmaceutical Industry,Shanghai 201203)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2019年第12期1463-1467,共5页
Chinese Journal of Pharmaceuticals
基金
上海市科委研发平台专项(18DZ2290500)
关键词
地佐辛
贴片
凝胶
溶液
体外透皮
dezocine
patch
gel
solution
transdermal in vitro
