摘要
目的制备盐酸青藤碱固体脂质纳米粒,并观察经皮和静脉注射两种给药方式对其药动学和药效学的影响。方法用高温乳化-低温固化法制备盐酸青藤碱固体脂质纳米粒,考察其形态、粒径分布和体外释药;分别测定经皮和静脉注射给药方式下小鼠的血药浓度,以及对大鼠中枢镇痛作用和外周抗炎镇痛作用的影响。结果所制得的盐酸青藤碱固体脂质纳米粒形态为球形,粒径分布均匀,平均粒径为(145.3±7.2)nm,平均包封率为64.4%,载药量平均为4.2%,48 h累积释放达88%。静脉注射盐酸青藤碱固体脂质纳米粒增强了中枢镇痛作用。结论与盐酸青藤碱水溶液相比,盐酸青藤碱固体脂质纳米粒具有明显的缓释作用。
AIM To prepare sinomenine hydrochloride solid lipid nanoparticles,and to observe the pharmacokinetic and pharmacodynamic after transdermal and intravenous administration.METHODS Sinomenine hydrochloride solid lipid nanoparticles were prepared by high temperature emulsification-low temperature solidification method.The particle size distribution,morphology and in vitro release characteristics were measured.After respectively administrating solid lipid nanoparticles in intravenous injection and transdermal delivery,the blood concentration and the impacts of sinomenine hydrochloride solid lipid nanoparticles on central analgesia and peripheral inflammatory pain were monitored. RESULTS The morphology of sinomenine hydrochloride solid lipid nanoparticles obtained were approximately spherical with the average particles size of（145.3±7.2） nm,and the average encapsulation rate reached up to 64.4% with the average drug loading of 4.2%.Sinomenine hydrochloride solid lipid nanoparticles release rate reached 88% in 48 hours.The sinomenine hydrochloride solid lipid nanoparticles by intravenous injection could significantly increase the analgesic effect.CONCLUSION Compared with sinomenine hydrochloride solution,sinomenine hydrochloride solid lipid nanoparticles have remarkable sustained release property.
出处
《中成药》
CAS
CSCD
北大核心
2013年第9期1882-1887,共6页
Chinese Traditional Patent Medicine
基金
国家重大新药创制科技重大专项(2009ZX09502-019)
陕西省教育厅产业化中试项目(2010jc20)
关键词
盐酸青藤碱
固体脂质纳米粒
药动学
药效学
sinomenine hydrochloride
solid lipid nanoparticles
pharmacokinetics
pharmacodynamics
