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Study of sustained release microspheres of human serum albumin containing bupivacaine hydrochloride
Author(s): 
Pages: 230-233
Year: Issue:  4
Journal: PHARMACEUTICAL CARE AND RESEARCH

Keyword:  布比卡因白蛋白微球迟效制剂高压电场法药动学药效学;
Abstract: 目的:制备缓释盐酸布比卡因人血清白蛋白微球(bupivacaine human serum albumin microspheres,Bupi-HSA-MS),并对其理化特性、体外释放、体内药动学、药效学进行评价.方法:采用高压电场法制备布比卡因人血清白蛋白微球,以高效毛细管电泳法测定微球的体外释放度.采用改良的RP-HPLC法测定体内布比卡因血药浓度,以家兔为实验对象,以针刺疼痛反应圈半径大小评价其麻醉效果.结果:微球的粒径分布集中,平均粒径为(108.9±2.6)μm,药物含量为31.56 %,包封率为91.62 %.体外释放结果表明,Bupi-HSA-MS具有明显缓释作用.药物动力学实验结果表明,注射剂组血药浓度达峰时间短,浓度高,药物驻留时间短.微球组峰浓度显著低于注射剂组并长时间维持低浓度.微球组的平均保留时间较对照组明显延长(P<0.01).微球组皮下给药最大麻醉圈直径显著小于注射剂对照组(P<0.01),而微球组局麻持续时间较对照组明显延长(P<0.01).结论:高压电场法是一种简单、易行的白蛋白微球制备新方法.Bupi-HSA-MS兔皮下给药,药物扩散少,局部麻醉作用持续时间长,是一种安全、长效的局部麻醉止痛新方法.
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