论文部分内容阅读
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 tissue distribution of homemade micro-emulsion of flurbiprofen axetil (FA) in rats and to evaluate its targeting in the inflammation site of wounds in surgical incisions. Methods: A rat model of surgical incision trauma was established and randomly divided into 2 groups. Fluvastopyrate microemulsion and flurbiprofen solution injection were injected through caudal vein respectively. Rats were killed at 15, 30, 60, 120 and 240 min after administration. Serum, heart, liver, spleen, lung, kidney, traumatic muscle tissue and normal muscle tissue were collected. The concentrations of flurbiprofen in the samples were determined by HPLC. Results: In the microemulsion injection group, the elimination rate of blood and tissues in the tissues was slower than that of the solution group. The concentration of drug in traumatic muscle tissue of the flurbiprofen axetil microemulsion injection group was higher than that of the non-surgical group at 5 time points Normal muscle tissue (P <0.05), while there was no significant difference in solution injection group (P> 0.05). The target efficiency Te = 12.21% of the muscle tissue in the microemulsion group was Te = 3.97%, while Te = 3.97% in the solution group. The relative uptake rate of the microemulsion injection to the trauma muscle tissue in the ordinary solution injection was 4.15. Conclusion: The injection of flurbiprofen axetil microemulsion injection has the targeting effect on the inflammation site of wounds in rats after operation, and has the effect of anti-inflammation and analgesia.