Kouchak Maryam, Handali Somayeh
Department of Pharmaceutics, Faculty of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, IR Iran ; Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, IR Iran.
Nanotechnology Research Center, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, IR Iran.
Jundishapur J Nat Pharm Prod. 2014 Feb;9(1):24-9. doi: 10.17795/jjnpp-12904. Epub 2014 Feb 20.
Cellulite is the accumulation of subcutaneous fat and connective tissue in tights and buttocks. Xanthines, such as aminophylline, are used as phosphodiesterase inhibitors, and are also adenosine receptor antagonists.
The aim of the present study was to characterize in vitro aminophylline transdermal absorption through shed snake skin, and to investigate the absorption enhancing effect of various enhancers.
Aminophylline gels were prepared using theophylline and ethylenediamine as raw materials of aminophylline, hydroxypropyl methyl cellulose (HPMC) F4M as gelling agent, and propylene glycol as a co-solvent. Sodium tauroglycocholate (STGC) (100, 200, and 500 μg/mL), lauric acid (1.7 and 15%), and ethanol (60%) were added as enhancers. In vitro percutaneous absorption experiments were performed on snake skin using Franz diffusion cells. Flux (J), permeability coefficient (P), and enhancement factor (EF) for each formulation were calculated.
The results indicated that all of enhancers significantly enhanced drug permeability. This effect was decreased by increasing the concentration of STGC; in contrast, by increasing the concentration of lauric acid from 1.7 to 15%, EF was enhanced Although ethanol (60%) and STGC (100 μg/mL) showed the highest EFs, the effect of ethanol on drug permeability appeared with a lag time.
According to the findings, type and concentration of penetration enhancers can effect on transdermal permeation of drug.
橘皮组织是大腿和臀部皮下脂肪和结缔组织的堆积。黄嘌呤类药物，如氨茶碱，用作磷酸二酯酶抑制剂，也是腺苷受体拮抗剂。
本研究旨在表征氨茶碱透过蛇蜕皮肤的体外透皮吸收情况，并研究各种促渗剂的促渗效果。
以茶碱和乙二胺为氨茶碱的原料，羟丙基甲基纤维素（HPMC）F4M为凝胶剂，丙二醇为助溶剂制备氨茶碱凝胶。添加牛磺胆酸钠（STGC）（100、200和500μg/mL）、月桂酸（1.7%和15%）和乙醇（60%）作为促渗剂。使用Franz扩散池在蛇皮上进行体外经皮吸收实验。计算每种制剂的通量（J）、渗透系数（P）和增强因子（EF）。
结果表明，所有促渗剂均显著提高了药物渗透性。随着STGC浓度的增加，这种作用减弱；相反，将月桂酸浓度从1.7%提高到15%，增强因子增加。尽管乙醇（60%）和STGC（100μg/mL）显示出最高的增强因子，但乙醇对药物渗透性的作用出现滞后。
根据研究结果，渗透促进剂的类型和浓度会影响药物的透皮渗透。
