聚(油酸/亚油酸-癸二酸)-庆大霉素在家兔体内的释药实验及相容性研究  

Investigation of the poly(oleic/linoleic acid dimer-sebacic acid)-gentamicin:in vivo release and its biocompatibility in rabbits

作　　者：杨秀芬[1] 曾繁典[2] 周志彬[3] 黄开勋[3] 徐辉碧[3] 

机构地区：[1]广西中医学院药学院药理教研室,南宁530001 [2]华中科技大学同济医学院药理学系,武汉430030 [3]华中科技大学生命科学院化学系,武汉430074

出　　处：《中国新药杂志》2007年第16期1265-1268,共4页Chinese Journal of New Drugs

基　　金：武汉市科委攻关项目(996005122G)

摘　　要：目的:观察聚(油酸/亚油酸-癸二酸)-庆大霉素在家兔体内释药情况及相容性。方法:将聚(油酸/亚油酸-癸二酸)-庆大霉素药丸植入家兔骨髓腔,数周后观察家兔骨、肌肉、肝、肾及血清中的庆大霉素浓度,并检测局部骨组织上清液的抑菌能力。在家兔背部脊柱旁肌肉组织和皮下植入不含庆大霉素的聚(油酸/亚油酸-癸二酸)-庆大霉素空药丸,以观察其与家兔组织的生物相容性。结果:药丸在家兔骨髓腔中释药良好,药丸释出的庆大霉素浓集在植入部位的骨组织中超过4周,在血清、肝、肾及局部肌肉中的庆大霉素含量甚微,骨组织上清液对常见的骨髓炎感染菌金葡球菌和大肠杆菌均有强大的抑菌活性。此外,聚(油酸/亚油酸-癸二酸)-庆大霉素还可在家兔体内自动降解。在观察期间没有发现明显的生物不相容性。结论:聚(油酸/亚油酸-癸二酸)-庆大霉素有望用于治疗慢性骨髓炎。Objective： To investigate the in vivo release of poly（ oleic/linoleic acid dimer-sebacic acid）-gentamicin[Poly（ OAD/LOAD-SA）-gentamicin] and its biocompatibility in rabbits. Methods： Poly（OAD/LOAD-SA）-gentamicin was implanted into the bone marrow cavity of the rabbits, the gentamicin concentration in bone, muscles, liver, kidney, and serum were observed in the following weeks. The bactericidal activity of the supernatants of the local bone tissues was also determined. Poly （OAD/LOAD- SA）-gentamicin free pills（blanks） were implanted into the paravertebral muscle and subcutaneous tissue on the side of the rabbits for investigation of the biocompatibility. Results： The pills could release genta- micin freely in the bone-marrow cavity and concentrated in the local bone over 4 weeks. Only a small quantity of gentamicin was determined in serum, liver, kidney, and local muscles. The supernatants of the local bone tissues strongly inhibited the common causative bacteria of the chronic osteomyelitis： Staphylococcus aureaus and Escyherichia coli. Moreover, Poly（OAD/LOAD-SA）-gentamicin could be degraded in vivo in rabbits. It was not found manifest non-biocompatibility in the rabbits during the experimental period. Conclusion： These findings indicated that Poly（OAD/LOAD-SA）-gentamicin was helpful for the treatment of chronic osteomyelitis.

关 键 词：聚(油酸/亚油酸-癸二酸)-庆大霉素 体内释药 抑菌活性 生物相容性 

分 类 号：R965.1[医药卫生—药理学] R978.12[医药卫生—药学]