Wu P C, Fang J Y, Huang Y B, Tsai Y H
School of Pharmacy, Kaohsiung Medical College, Taiwan, ROC.
Pharmazie. 1997 Feb;52(2):135-8.
Transdermal patches were developed and evaluated for two synthetic derivatives of capsaicin, nonivamide (NVA) and sodium nonivamide acetate (SNA), by in vitro and in vivo skin permeation. The designed system was essentially based on natural rubber or polymeric Gelva dispersion. The characterization of physicochemical properties of the patches showed adequate adhesive force and low thickness which suggested these patch formulations possessed good quality. In the study of in vitro percutaneous experiment, the predicted therapeutic activities of patches were all higher than that of a commercially available plaster after the calculation of antinociceptive index. The highest in vitro penetration flux was found in the Gelva patch for NVA. The result of in vivo experiments revealed a high obverse correlation with that of in vitro experiments. The information of this present study is helpful for the further development of NVA and SNA transdermal drug delivery system.
通过体外和体内皮肤渗透实验，对辣椒素的两种合成衍生物——壬酸香草酰胺（NVA）和壬酸香草酰胺醋酸钠（SNA）的透皮贴剂进行了研发和评估。所设计的系统主要基于天然橡胶或聚合物Gelva分散体。贴剂的物理化学性质表征显示出足够的粘附力和低厚度，这表明这些贴剂配方质量良好。在体外经皮实验研究中，计算抗伤害感受指数后发现，贴剂的预测治疗活性均高于市售膏药。在Gelva贴剂中，NVA的体外渗透通量最高。体内实验结果与体外实验结果显示出高度正相关。本研究的信息有助于NVA和SNA透皮给药系统的进一步开发。
