萜类促渗剂对盐酸普萘洛尔凝胶体外经皮渗透的影响

发布时间：2019-02-09 15:35

【摘要】：目的考察萜类促渗剂的种类、浓度及联用对盐酸普萘洛尔(PPL·HCl)经皮渗透的影响,为盐酸普萘洛尔经皮递药系统的处方筛选提供依据。方法采用改良Franz直立式扩散池,离体乳猪皮肤为渗透屏障,以体外经皮累积渗透量(Q)和促渗倍数(ER)为指标,比较萜类促渗剂对盐酸普萘洛尔经皮渗透的影响。结果 10种萜类促渗剂对凝胶中盐酸普萘洛尔体外经皮渗透促进作用顺序为:法尼醇L-薄荷脑橙花叔醇四氢香叶醇1,4-桉叶素≈香叶醇柠檬烯茴香脑冰片甘草酸二钾,均符合零级渗透规律,其中法尼醇、L-薄荷脑、橙花叔醇浓度为3%时具有最高的Q,最大的ER;浓度增至5%,其促渗作用反而降低;与单用3%促渗剂相比,与异丙醇联用具有协同促渗作用(P0.05),而与丙二醇联用则显示拮抗作用(P0.05)。结论新型萜类促渗剂(除甘草酸二钾)均能不同程度促进盐酸普萘洛尔经皮渗透,促渗剂为3%法尼醇+10%异丙醇时,盐酸普萘洛尔体外透皮可达最大吸收,该结果为盐酸普萘洛尔经皮给药研究提供了基础。
[Abstract]:Objective to investigate the effects of terpenoids on the transdermal permeation of propranolol hydrochloride (PPL HCl) in order to provide a basis for screening the prescription of propranolol hydrochloride. Methods the effects of terpenoids on the percutaneous permeation of propranolol hydrochloride were compared by using improved Franz vertical diffusion tank and in vitro porcine skin as the permeation barrier. The in vitro cumulative permeation capacity (Q) and multiple permeability enhancement (ER) were used to compare the effects of terpenoids on the transdermal permeability of propranolol hydrochloride. Results the effects of 10 terpenoids on the percolation of propranolol hydrochloride in the gel in vitro were as follows: Farnitol L- menthol tetrahydrogeraniol 1, 4-eucalyptin 鈮，

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