促透皮吸收剂对菌克软膏中盐酸林可霉素和醋酸地塞米松透皮吸收研究  

Effects of Penetration Enhancers on Percutaneous Permeability of Lincomycin Hydrochlorideand and Dexamethasone Acetate in Junke Cream

作　　者：董文燊[1] 林芝[1] 邵留英 李清[1] 张强强[2] 瞿发林[1] 

机构地区：[1]解放军102医院,江苏常州213003 [2]蚌埠医学院,安徽蚌埠233030

出　　处：《解放军药学学报》2017年第1期68-71,85,共5页Pharmaceutical Journal of Chinese People's Liberation Army

摘　　要：目的考察促透皮吸收剂对菌克软膏中盐酸林可霉素、醋酸地塞米松透皮吸收的影响,并筛选最佳透皮吸收剂及用量。方法采用Franz扩散池法,以离体裸鼠皮肤为透皮屏障,HPLC法测定盐酸林可霉素、醋酸地塞米松含量,计算累积透皮量。结果累积透皮量表明,促透皮吸收剂对盐酸林可霉素的促透皮吸收强弱顺序依次为3%氮酮>5%丙二醇>1%氮酮>5%油酸>5%氮酮>3%薄荷脑>0.6%氮酮>不加促透剂;对醋酸地塞米松的促透皮吸收强弱顺序依次为1%氮酮>5%油酸>5%丙二醇>3%氮酮>0.6%氮酮>3%薄荷脑>不加促透剂,而高剂量5%氮酮则有抑制作用。结论本试验中3%氮酮对盐酸林可霉素具有显著的促透皮吸收作用,对醋酸地塞米松的促透皮吸收作用也强于原处方中0.6%氮酮,结合前期试验结果3%氮酮对硝酸咪康唑有较显著的促透皮吸收作用,综合评价建议将原处方中氮酮的浓度提高为3%,以发挥菌克软膏的最大药效。Objective To study the effect of penetration enhancers on the percutaneous permeability of lincomycin hydrochloride and dexamethasone acetate in Junke cream in order to screen the most appropriate transdermal absorption and dosage.Methods Using Franz diffusion cell method and with the excised nude mouse skin as an apercutaneous barrier, the content of lincomycin hydrochloride and dexamethasone acetate was measured with an HPLC method and the amount of cumulative permeation was calculated. Results The amount of cumulative permeation quantity that the absorbefacient effect in different penetration enhancers was found in 3% azone, followed by 5 % oleic acid, 5% propylene glycol, 3% menthol, or in the absence of any penetration enhancer. The best absorbefacient effect in different dosage of azone was exerted by 1% azone, followed by 3 0% azone, 5% azone, and 0.6% azone. High-dose 5% azone showed inhibitory effect on dexasmethasone acetate.Conclusion A prominent absorbefacient effect on lincomycin hydrochloride by 3% azone has been discovered in this test.3% azone also has a better absorbefacient effect on dexamethasone acetate than the original prescription （0.6% azone）.It is suggested that the concentration of azone be increased to 3% in the prescription to allow Junke cream to perform a maximum pharmacological function.

关 键 词：菌克软膏 盐酸林可霉素 醋酸地塞米松 促透皮吸收剂 透皮吸收 HPLC 

分 类 号：R94[医药卫生—药剂学]