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迷迭香叶精油对双氯芬酸钠透皮凝胶经皮吸收的促渗作用

Transdermal absorption enhancing effect of the essential oil of Rosmarinus officinalis on percutaneous absorption of Na diclofenac from topical gel.

作者信息

Akbari Jafar, Saeedi Majid, Farzin Davood, Morteza-Semnani Katayoun, Esmaili Zahra

机构信息

Department of Pharmaceutics, Faculty of Pharmacy, Mazandaran University of Medical Sciences , Sari , Iran .

出版信息

Pharm Biol. 2015;53(10):1442-7. doi: 10.3109/13880209.2014.984855. Epub 2015 Apr 8.

DOI:10.3109/13880209.2014.984855
PMID:25853969
Abstract

CONTEXT

Rosemary essential oil has been used topically for several purposes (analgesic, anti acne, and anti-inflammatory) in Iranian traditional medicine.

OBJECTIVES

This investigation aimed to study the effect of essential oil of Rosmarinus officinalis L. (Lamiaceae) on the transdermal absorption of Na diclofenac from topical gel.

MATERIAL AND METHODS

Diclofenac sodium topical gel was prepared with HPMC K4M and Carbopol 934P as a gelling agent, and several vehicles. The most stable gel was chosen and enhancing effects of the essential oil with different concentrations (0.1, 0.5, and 1.0% w/w) on the permeation of diclofenac were evaluated. The anti-nociceptive effect of preparations was evaluated based on the formalin and tail flick tests in mice.

RESULTS

The major constituents of the essential oil were 1,8-cineol (15.96%), α-pinene (13.38%), camphor (7.87%), bornyl acetate (6.54%), verbenone (5.82%), borneol (5.23%), camphene (4.96%), and (E)-caryophyllene (3.8%). Topical diclofenac containing 0.5% essential oil showed more analgesic effect after 25, 30, and 35 min (p < 0.001) than the reference drug in the tail flick test. The analgesic effect of preparation containing 1% essential oil was more than reference gel after 15 min (p < 0.05). This difference was observed after 20, 25, 30, 35, and 40 min (p < 0.001) too. Rosemary essential oil 1% promoted analgesic effect of drug in comparison with diclofenac gel in the formalin early phase (p < 0.05). The enhancing effect of rosemary was observed in 0.5 and 1% concentration (p < 0.05 and p < 0.001, respectively) in the late phase.

CONCLUSION

This study proved the enhancing effect of 0.5 and 1% of rosemary essential oil on diclofenac percutaneous absorption.

摘要

背景

迷迭香精油在伊朗传统医学中已被用于多种局部用途(止痛、抗痤疮和抗炎)。

目的

本研究旨在探讨迷迭香叶(唇形科)精油对双氯芬酸钠从局部凝胶透皮吸收的影响。

材料与方法

以羟丙基甲基纤维素K4M和卡波姆934P为凝胶剂,制备了几种不同基质的双氯芬酸钠局部凝胶。选择最稳定的凝胶,评估不同浓度(0.1%、0.5%和1.0%w/w)的精油对双氯芬酸渗透的增强作用。基于小鼠福尔马林试验和甩尾试验评估制剂的抗伤害感受作用。

结果

精油的主要成分是1,8-桉叶素(15.96%)、α-蒎烯(13.38%)、樟脑(7.87%)、乙酸龙脑酯(6.54%)、马鞭草烯酮(5.82%)、冰片(5.23%)、莰烯(4.96%)和(E)-石竹烯(3.8%)。在甩尾试验中,含0.5%精油的局部双氯芬酸在25、30和35分钟后显示出比参比药物更强的镇痛效果(p<0.001)。含1%精油的制剂在15分钟后镇痛效果比参比凝胶更强(p<0.05)。在20、25、30、35和40分钟后也观察到这种差异(p<0.001)。与双氯芬酸凝胶相比,1%迷迭香精油在福尔马林早期促进了药物的镇痛作用(p<0.05)。在后期,0.5%和1%浓度的迷迭香均观察到增强作用(分别为p<0.05和p<0.001)。

结论

本研究证明了0.5%和1%迷迭香精油对双氯芬酸经皮吸收的增强作用。

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