摘要
目的 :研究双氯芬酸钠和醋氯芬酸在溶液状态下透过离体小鼠皮肤的特性 ,为制剂的开发研究提供比较依据 ;方法 :利用Franz扩散池和用不同pH值的磷酸盐缓冲液所配制的一系列不同浓度药物扩散液 ,进行双氯芬酸钠、醋氯芬酸的体外经皮渗透实验 ,并用HPLC法测定接受液中双氯芬酸钠、醋氯芬酸浓度 ,求算它们在相应条件下的渗透速率 (Jss)和渗透系数 (P) ;结果 :醋氯芬酸在pH =6 .5 ,6 .8,7.0磷酸盐缓冲液中的渗透系数 (P)分别为 2 .5 4× 10 -4,1.2 9× 10 -4,0 .8× 10 -4cm/min ,而双氯芬酸钠在相同条件扩散液中的渗透系数 (P)分别为 4 .92× 10 -4,2 .6 3× 10 -4,1.6 4× 10 -4cm/min ;渗透系数随pH值的增加而减小 ;结论 :双氯芬酸钠和醋氯芬酸的累积渗透量和时间具有一级动力学特点 ;在溶液状态下 ,醋氯芬酸的渗透系数仅为双氯芬酸钠的一半左右。
AIM:To characterize the in vitro transdermal absorption of aceclofenac and diclofenac sodium through the isolated mice abdominal skins using the phosphate buffers;METHOD:Utilizing Franz diffusion cell,efforts were made to investigate the penetration of aceclofenac and diclofenac sodium,incorporated in the phosphate buffers of pH 6.5,6.8,and 7.0,through the mouse skins;RESULT:It was found that the accumulative amounts penetrated of both of drugs and the corresponding penetration rates were increased in direct proportion to the concentrations in the donor side of the cell. The estimated permeation coefficients of aceclofenac in the buffers of pH 6.5,6.8,7.0 were 2.54×10 -4,1.29×10 -4,and 0.8×10 -4 cm/min respectively,while the coefficients of diclofenac sodium in the same bases were 4.92×10 -4,2.63×10 -4,and 1.64×10 -4 cm/min respectively. The results indicated that,for both of drugs,the greatest permeability in the buffer of pH 6.5 was observed under the selected experimental conditions;CONCLUSION:There were linear relationships between the accumulative amounts of penetration of aceclofenac and diclofenac sodium across the mice skin and the time. The permeation coefficients for both of the species decreased when the pH of the matrix increased. In addition,the permeability coefficient of diclofenac sodium under the conditions studied was almost twice that of aceclofenac.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
2004年第4期311-314,共4页
Journal of China Pharmaceutical University
关键词
双氯芬酸钠
醋氯芬酸
透皮吸收
渗透速率
渗透系数
Aceclofenac
Diclofenac sodium
Transdermal absorption
Permeation coefficient
