Takayama Kozo, Hirose Akihiko, Suda Ikuko, Miyazaki Atsushi, Oguchi Masao, Onotogi Masako, Fotopoulos Grigorios
Hoshi University, Japan;
Int J Biomed Sci. 2011 Sep;7(3):222-9.
Topically applied nonsteroidal anti-inflammatory drugs (NSAIDs) are used widely for the treatment of pain and inflammation in musculoskeletal disorders. This study compared the analgesic and anti-inflammatory effects of patches of 1% diclofenac-sodium, 3.5% and 0.5% felbinac and 3.75% indomethacin in rats using the carrageenan-induced paw pad edema model and the brewer's yeast-induced hyper algesia model. Two studies were conducted: in the preliminary study, the patch was removed at 2 or 24 hrs after application, and in the main study the patch was removed at 2 hrs. The volume of the right hind paw and the pain threshold were assessed at 1, 3, 5, and 7 hrs after induction of inflammation in both studies.
In the main study, the edema ratio in the 1% diclofenac group at 5 hrs after induction of inflammation and the AUEC (Area Under the Effect Curve) were significantly lower than in the control animals (p=0.009). The edema suppression rate in the 1% diclofenac group (12.1-33.2%) was higher than in the 3.5% and 0.5% felbinac and 3.75% indomethacin groups. The pain threshold ratio did not decrease in the 1% diclofenac group and it was significantly higher than in the control group at 3 (p=0.0004) and 5 hrs (p=0.029). The 1/AUEC was significantly lower than that in the control group (p=0.004) and the lowest among all the NSAID groups.
This study demonstrated that the analgesic and anti-inflammatory effects of the 1% diclofenac sodium patch in a rat model may be exerted more promptly and persistently than with the 3.5% and 0.5% felbinac and 3.75% indomethacin patches.
局部应用的非甾体抗炎药(NSAIDs)被广泛用于治疗肌肉骨骼疾病中的疼痛和炎症。本研究使用角叉菜胶诱导的爪垫水肿模型和啤酒酵母诱导的痛觉过敏模型,比较了1%双氯芬酸钠、3.5%和0.5%氟比洛芬以及3.75%吲哚美辛贴片在大鼠中的镇痛和抗炎作用。进行了两项研究:在初步研究中,贴片在应用后2或24小时去除,在主要研究中,贴片在2小时去除。在两项研究中,均在炎症诱导后1、3、5和7小时评估右后爪的体积和疼痛阈值。
在主要研究中,炎症诱导后5小时,1%双氯芬酸组的水肿率和效应曲线下面积(AUEC)显著低于对照动物(p = 0.009)。1%双氯芬酸组的水肿抑制率(12.1 - 33.2%)高于3.5%和0.5%氟比洛芬以及3.75%吲哚美辛组。1%双氯芬酸组的疼痛阈值比率没有降低,在3小时(p = 0.0004)和5小时(p = 0.029)时显著高于对照组。1/AUEC显著低于对照组(p = 0.004),且在所有NSAID组中最低。
本研究表明,在大鼠模型中,1%双氯芬酸钠贴片的镇痛和抗炎作用可能比3.5%和0.5%氟比洛芬以及3.75%吲哚美辛贴片更迅速和持久。