CAJ | 학술논문

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。
목적：：연구자제적불비락분지( FA)미유주사액재대서체내적조직분포병평개기재수술절구창상염증부위파향성。방법：건립대서수술절구창상모형,수궤분성2조,분별경미정맥주사불비락분지미유화불비락분용액주사액,재급약후15,30,60,120,240 min처사대서,취혈청、심、간、비、폐、신、창상기육조직급정상기육조직,HPLC법측정양본불비락분농도。결과：미유주사액조재체내혈액급각조직장기소제속도교용액조만,5개시간점불비락분지미유주사액조수술측창상기육조직중약물농도균고우비수술측정상기육조직(P<0.05),이용액주사액조차이무통계학의의(P>0.05)。미유조약물창상기육조직파향효솔Te =12.21%,이용액조Te =3.97%,미유주사액대보통용액주사액창상기육조직상대섭취솔Re =4.15。결론：불비락분지미유주사액정맥주사후재대서수술절구창상염증부위유파향성,구유파향소염진통적작용。
Objective:To study the distribution of flurbiprofen axetil ( FA) microemulsion in rats and evaluate the targeting prop-erty to traumatic inflammation tissue. Methods:Traumatic injury model rats were established by hip surgery on the rat right thigh mus-cle 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 microe-mulsion 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). Micro-emulsion group injury muscle Te(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.