甲磺酸罗哌卡因缓释微球的制备及加速释放度试验研究  

Preparation and accelerated release test of ropivacaine mesilate micropheres

作　　者：赵希青 李志平[2] 赵诗情[1,2] 刘燕[2] 肖若蕾[1] 梅兴国[2] 

机构地区：[1]湖北科技学院药学院,咸宁437000 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《中国新药杂志》2015年第10期1113-1118,共6页Chinese Journal of New Drugs

基　　金：国家"重大新药创制"科技重大专项(2012ZX09301003-001-009)

摘　　要：目的:制备甲磺酸罗哌卡因微球,建立甲磺酸罗哌卡因微球的加速释放度试验方法。方法:采用S/O/W法制备甲磺酸罗哌卡因微球,通过考察振摇频率、温度和释放介质p H对甲磺酸罗哌卡因微球释药速度的影响,确定体外加速释放的条件,通过评价加速与长期释放度的相关性,建立甲磺酸罗哌卡因微球的体外加速释放方法。结果:微球外观圆整,表面光滑,无黏连。F1批及F2批的平均粒径分别为(12.06±0.45)和(15.11±0.79)μm,载药量分别为(17.86±0.38)%和(23.62±0.15)%;包封率分别为(50.46±0.63)%和(66.74±0.31)%。振摇频率和释放介质的p H对微球的释药速率影响不大,温度的提高可显著加快药物的释放。结果表明,以p H 7.4磷酸盐缓冲液为释放介质,在100 r·min-1和程序升温条件下,加速释放度与长期释放度数据之间具有良好的非线性相关(r=0.988 0)。结论:加速释放度试验可用于快速评价甲磺酸罗哌卡因微球的释药特性。Objective： To prepare ropivacaine mesilate-loaded PLGA microspheres and develop an acceler- ated release method of these microspheres correlated with long-term release. Methods： Ropivacaine mesilate-load- ed PLGA mierospheres were produced by S/O/W emulsion solvent evaporation technique. The accelerated release condition of the microspheres was established by investigating the effect of vibration frequency, pH of release medi- um and temperature on ropivacaine mesilate release. The regression equation was built by correlative evaluation of accelerated release and long-term release. Results： It was shown from SEM that the microspheres was spherical and the surface of microspheres was smooth. The microsphere particle sizes of F1 and F2 were （ 12.06 ± 0.45） and （15.11 ±0.79） μm, the drug loadings were （17.86 ±0.38）% and （23.62 ±0.15）%, and the encapsulation efficiencies were （50.46 ± 0.63 ） % and （66.74 ± 0.31 ） % , respectively. The oscillation frequency and pH of re- lease medium had a little effect on ropivacaine mesilate released from the microspheres, but the temperature affect- ed release rate markedly. The accelerated release was conducted in release medium of pH 7.4 at 100 r·min-1 un-der a sion ： PLGA gradie Accel nt heating program. Accelerated release erated release metho microspheres in a shorter d can be applied to time. correlated well with long-term release （ r = 0. 988 0）. Conclu- evaluate the drug release profile of ropivacaine mesilate from

关 键 词：甲磺酸罗哌卡因 微球 长期释放 加速释放 相关性 

分 类 号：R943.41[医药卫生—药剂学]