布比卡因聚乳酸缓释微球在家兔体内药动学研究

Study on pharmacokinetics of bupivacaine polylactic acid microspheres in rabbits

目的 考察布比卡因聚乳酸微球在家兔体内的药动学过程。方法 家兔单次皮下植入布比卡因聚乳酸微球和皮下注射盐酸布比卡因注射液后 ,用HPLC测定血中布比卡因浓度。结果 布比卡因聚乳酸微球和盐酸布比卡因注射液的cmax分别为 0 .78和 2 .4 7μg·mL-1,tmax分别为 12 .99和 0 .34h ,MRT分别为 39.37和 5 .5 6h。结论 微球在家兔体内具有明显的缓释作用 ,可在较长时间内维持较低血药浓度 。

OBJECTIVE: To study the pharmacokinetics of bupivacaine polylactic acid microspheres in rabbits. METHODS: Bupivacaine polylactic acid microspheres was implanted and bupivacaine hydrochloride injection was administered i.h. to rabbits respectively. The bupivacaine concentrations in plasma were measured by HPLC method. RESULTS: cmax, tmax and MRT were 0.78 μg&middot mL-1 12.99, 39.37 h for microspheres and 2.47 μg&middotmL-1, 0.34, 5.56 h for injection, respectively. CONCLUSION: The absorption of the microspheres in rabbits was slower and kept a lower concentration in plasma for a long time compared with injection. This showed that microspheres was obvious safety.