非离子表面活性剂对布托啡诺通过马鼻粘膜通透性的影响

M. I. Velloso
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引用次数: 0

摘要

通过鼻内给药将作用部位进入中枢神经系统的药物,如布托啡诺,成为马药的一种潜在选择。本研究采用弗兰兹扩散细胞法对两种布托啡诺制剂在马鼻粘膜和呼吸粘膜的体外渗透率进行了估计和比较。两种配方具有相同的成分,但配方2除外,它含有2,5 x 10 -4 M的非离子表面活性剂(吐温80)。布托啡诺给药剂量为24.4 mg/cm2。构建了丁托啡酚累积量随时间变化的图,其中估计了稳态(Jss)下的最大通量值、表观渗透率系数(Kp)和滞后时间(lag)。Jss和Kp表明丁托啡诺通过嗅觉粘膜的渗透与呼吸粘膜的渗透不同。此外,制剂2在两个解剖区域的Jss均高于制剂1,可能是表面活性剂的作用所致。随着布托啡诺鼻内给药制剂的发展,本研究结果有望继续发展。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
EFECTO DE UN SURFACTANTE NO IONICO EN LA PERMEABILIDAD DE BUTORFANOL A TRAVES DE MUCOSA NASAL EQUINA
Implementation of intranasal administration for the delivery of drugs with site of action into the central nervous system, such as butorphanol, became a potential choice in equine medicine.  In this study, using Franz-diffusion cells the in vitro permeation rate through respiratory and olfactory equine nasal mucosa of two butorphanol formulations was estimated and compared.  Both formulations had the same composition, was the exception for formulation 2, that contained 2, 5 x 10 -4 M of a non-ionic surfactant (tween 80). Butorphanol administered dose was 24, 4 mg/cm2. Plots of the cumulative amounts of butorphanol against time were constructed, where maximum flux values at the steady state (Jss), apparent permeability coefficients (Kp) and lag-time (tlag) were estimated. The Jss and Kp show that permeation of butorphanol through olfactory mucosa is different than respiratory mucosa. Moreover, Jss for formulation 2 was higher than formulation 1 in both anatomical areas, probably for the effect of the surfactant. The present results are promising to carry on with the development of formulation of butorphanol for intranasal administration.
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