普萘洛尔经皮吸收膜剂的研制 Ⅰ.促吸剂对普萘洛尔透皮速率的影响

Study-on Propranolol Transdermal Therapeutic System Ⅰ. Effect of Penetration Enhancers on the in vitro Permeability of Propranolol Through Excised Rabbit Skin

利用离体家兔皮肤为渗透屏障,研究了普萘洛尔在二甲基亚砜等5种促吸剂作用下的透皮效果。在1%普萘洛尔水溶液中各加入5%促吸剂,促进效果依次为二甲基亚砜>聚乙二醇400,油酸>丙三醇>吐温80。在羟丙基甲基纤维素为主要组分,油酸为促吸剂的膜剂中,普萘洛尔透皮速率比在水溶液中的速率低,但这两种情况下,普萘洛尔的渗透均符合零级动力学过程。

The effect of penetration enhancers on the in vitro permeability of propranolol from the aqueous solution through excised rabbit skin was examined using the standing type diffusion cells and the normal saline as receptor medium. The results showed that the penetration rate of propranolol from 1% (W/V) solution containing 5% (W/V) one of enhancers decreased in following order:, dimethyl sulfoxide (DMSO)>polyethylene glycol 400 (PEG 400) and oleic acid (OA)>glycerol (PG)>polysorbate 80 (Tween 80). A matrix-type transdermal therapeutic system of propranolol with olcic acid as enhancer was prepared, in which the concentration of both compounds was same as the solution, and the permeability of propranolol was determined under same condition. Comparing with the aqueous solution, the penetration rate decreased significantly. The fact implied that the release of drug was controlled by the system. For all the cases the penetration process could be described by zero-order kinetic mechanism.