Shokri J, Azarmi Sh, Fasihi Z, Hallaj-Nezhadi S, Nokhodchi A, Javadzadeh Y
Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, I.R. Iran . ; Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, I.R. Iran .
Res Pharm Sci. 2012 Oct;7(4):225-34.
A suitable emulgel formulation of piroxicam was prepared and its percutaneous permeation was investigated using Wistar rat skin and diffusion cell technique. The concentrations of the drug in receptor phase of diffusion cells were measured using HPLC method. The effect of three types of penetration enhancers (Myrj 52, cineol and Transcutol P) with different concentrations on transdermal permeation of the drug was also evaluated. Flux, Kp and enhancement ratios (ERs) of piroxicam in the presence of enhancers was measured and compared with emulgel base alone and simple commercial gel. The results showed a significant enhancement in the flux from emulgel base compared to hydroalcoholic gel formulation (9.91 folds over simple gel). The highest enhancement ratio (ER=3.11) was observed for Myrj 52 at the concentration of 0.25%. Higher concentrations of Myrj 52did not show any enhancement in the drug flux due to micelle formation and solubilization of the drug by micelles. The increase in solubility, in turn, increases the saturated concentration and reduces the thermodynamic activity of the drug. Transcutol(®) P with concentrations higher than 0.25% w/w showed burst transportation of the drug through the skin. All concentrations of cineol and Transcutol did not show any enhancing effects over emulgel base alone (ER <1).
制备了一种合适的吡罗昔康乳胶凝胶制剂,并使用Wistar大鼠皮肤和扩散池技术研究了其经皮渗透情况。采用高效液相色谱法测定扩散池中受体相的药物浓度。还评估了三种不同浓度的渗透促进剂(聚山梨酯52、桉叶油素和肉豆蔻酸异丙酯)对药物透皮渗透的影响。测定了存在促进剂时吡罗昔康的通量、渗透系数(Kp)和增强比(ER),并与单纯的乳胶凝胶基质和市售凝胶进行比较。结果表明,与水醇凝胶制剂相比,乳胶凝胶基质的通量有显著提高(比单纯凝胶高9.91倍)。在浓度为0.25%时,聚山梨酯52的增强比最高(ER = 3.11)。较高浓度的聚山梨酯52由于胶束形成和药物被胶束增溶,未显示出药物通量的任何增强。溶解度的增加反过来又提高了饱和浓度并降低了药物的热力学活性。浓度高于0.25% w/w的肉豆蔻酸异丙酯显示药物通过皮肤的爆发性转运。所有浓度的桉叶油素和肉豆蔻酸异丙酯与单纯乳胶凝胶基质相比均未显示出任何增强作用(ER <1)。