白藜芦醇三甲醚乳胶局部外用于兔踝关节后的体内药物浓度研究  

Study on Drug Concentration in Vivo of Local Application of Trimethylether Resveratrol Emulsion Gel on Rabbit Ankles

作　　者：何青 易鸿[2,3] 林鹏程[3] 周彦彬[3] 向大雄[3] 丁劲松[3] 

机构地区：[1]湖南省结核病防治所,长沙410013 [2]深圳致君制药有限公司,广东深圳518000 [3]中南大学药学院,长沙410013

出　　处：《中国药房》2012年第17期1546-1548,共3页China Pharmacy

基　　金：国家"十一五"重大专项基金资助项目(2009ZX09103)

摘　　要：目的:比较家兔灌胃给药与踝骨关节局部给药后的血药浓度和关节组织中药物浓度,评价白藜芦醇三甲醚(BTM)乳胶局部用药的可行性。方法:36只家兔随机分成2组即灌胃给药(对照)组与局部给药组,每组18只家兔又随机分成6个时间组,分别于给药后0.5、1、3、6、9、12 h取血样和关节组织样品;采用高效液相色谱-紫外法测定各时间点血浆和关节样品中的药物浓度。结果:家兔局部给药组的血药浓度均低于检测限(9.2 ng.mL-1),对照组0.5 h血药浓度最高((334.6±42.8)ng.mL-1),9 h下降为(17.9±17.0)ng.mL-1;对照组关节组织中药物浓度在0.5 h时大于局部给药组(P<0.05),在1、3 h 2组比较无显著性差异(P>0.05),在6、9、12 h低于局部给药组(P<0.05)。结论:外用BTM乳胶能透过皮肤进入家兔关节局部,与口服灌胃给药后比较,血药浓度更低而关节组织处药物浓度更高,并具有一定缓释作用,且可提高药物治疗的安全性,具有局部用药的可行性。OBJECTIVE： To compare the concentration of drug in plasma and joints of rabbits after intragastrical administration and local drug use of ankle joints,and to evaluate the feasibility of local application of trimethylether resveratrol（BTM）.METHODS： Firstly,36 rabbits were randomly divided into 2 groups,i.e.intragastrical administration（control） group and local administration group,and then 18 rabbits of each group were further divided into 6 time-groups.Blood sample and ankle joint tissue sample were collected at 0.5,1,3,6,9,12 h after administration.HPLC-UV method was applied to determine the concentration of drug in plasma and joint sample.RESULTS： All the concentration of drug in plasma of local administration group were below the detection limit（9.2 ng·mL-1） while plasma concentration of control group reached the peak（（334.6±42.8） ng·mL-1） at 0.5 h and decreased to（17.9±17.0） ng·mL-1 at 9 h.The concentration of BTM in joint tissue of control group was higher than local administration group at 0.5 h（P0.05）,and no significant differences were found at 1,3 h between 2 groups（P0.05）,but that of control group was lower than local administration group at 6,9,12 h（P0.05）.CONCLUSION： External use of BTM emulsion gel can penetrate into the skin and reach the joint tissue.Compared with oral intragastrical administration,external use of BTM obtains lower plasma concentration and higher drug concentration of joint tissue and shows sustained-release effect.It is feasible and can improve the safety of drug therapy.

关 键 词：白藜芦醇三甲醚 乳胶 家兔 血药浓度 关节组织 高效液相色谱法 

分 类 号：R965[医药卫生—药理学]