氟比洛芬酯微乳注射液大鼠组织分布及靶向性研究

Study on distribution in rats and targeting property of flurbiprofen axetil microemulsion

目的:研究自制的氟比洛芬酯(FA)微乳注射液在大鼠体内的组织分布并评价其在手术切口创伤炎症部位靶向性。方法:建立大鼠手术切口创伤模型,随机分成2组,分别经尾静脉注射氟比洛芬酯微乳和氟比洛芬溶液注射液,在给药后15,30,60,120,240 min处死大鼠,取血清、心、肝、脾、肺、肾、创伤肌肉组织及正常肌肉组织,HPLC法测定样本氟比洛芬浓度。结果:微乳注射液组在体内血液及各组织脏器消除速度较溶液组慢,5个时间点氟比洛芬酯微乳注射液组手术侧创伤肌肉组织中药物浓度均高于非手术侧正常肌肉组织(P<0.05),而溶液注射液组差异无统计学意义(P>0.05)。微乳组药物创伤肌肉组织靶向效率Te=12.21%,而溶液组Te=3.97%,微乳注射液对普通溶液注射液创伤肌肉组织相对摄取率Re=4.15。结论:氟比洛芬酯微乳注射液静脉注射后在大鼠手术切口创伤炎症部位有靶向性,具有靶向消炎镇痛的作用。

Objective： To study the distribution of flurbiprofen axetil （FA） microomulsion in rats and evaluate the targeting property to traumatic inflammation tissue. Methods： Traumatic injury model rats were established by hip surgery on the rat right thigh muscle and randomly divided into 2 groups ： microemulsion group and solution group. Serums and tissues of rats were collected at 15, 30, 60, 120 and 240min after administration （iv. 5 mg· kg^-1）. A high performance liquid chromatography （HPLC） with UV detection was developed to study the concentration of flurbiprofen in biological samples. Results： The elimination of flurbiprofen axetil microemulsion from blood and tissues was slower than flurbiprofen solution. At each 5 time points, drug concentrations of microemulsion group in injury muscle were higher than in normal muscle （P 〈 0.05 ）, while solution group had no significant difference（ P 〉 0.05 ）. Microemulsion group injury muscle T~ （targeting efficiency） = 12.21%, and the solution group Te = 3.97%. The Re （relative uptake rate） of injury muscle was 4.15. Conclusion： The flurbiprofen axetil microemulsion has the targeting property to traumatic injury tissues.