摘要
目的制备蒙花苷磷脂复合物固体脂质纳米粒,并研究其体内药动学。方法乳化-超声分散法制备固体脂质纳米粒,考察其粒径、Zeta电位、包封率、载药量。SD大鼠灌胃给予蒙花苷、蒙花苷磷脂复合物、蒙花苷磷脂复合物固体脂质纳米粒的0.5%CMC-Na混悬液(含40 mg/kg蒙花苷)后,HPLC法测定蒙花苷血药浓度,计算主要药动学参数。结果蒙花苷磷脂复合物固体脂质纳米粒的粒径为(216.72±3.57)nm,Zeta电位为(-8.7±0.7)mV,包封率为82.06%,载药量为4.72%。与原料药比较,磷脂复合物、固体脂质纳米粒tmax延长(P<0.05),Cmax、AUC0~t、AUC0~∞升高(P<0.05,P<0.01),以后者更明显(P<0.05,P<0.01),相对生物利用度分别增加至1.39、2.89倍。结论固体脂质纳米粒可进一步促进蒙花苷磷脂复合物体内吸收,提高其生物利用度。
AIM To prepare the solid lipid nanoparticles of buddleoside phospholipid complex and to study the in vivo pharmacokinetics.METHODS For the solid lipid nanoparticles prepared by emulsion-ultrasonic dispersion method, the particle size, Zeta potential, encapsulation efficiency and drug loading were investigated. SD rats were given intragastrical administration of the 0.5%CMC-Na suspensions of buddleoside, buddleoside phospholipid complex and solid lipid nanoparticles of buddleoside phospholipid complex(containing 40 mg/kg buddleoside), after which HPLC was adopted in the plasma concentration determination of buddleoside, and main pharmacokinetic parameters were calculated.RESULTS The solid lipid nanoparticles of buddleoside phospholipid complex demonstrated the particle size, Zeta potential, encapsulation efficiency and drug loading of(216.72±3.57) nm,(-8.7±0.7) mV, 82.06% and 4.72%, respectively. Compared with raw medicine, phospholipid complex and solid lipid nanoparticles displayed prolonged tmax(P<0.05) and increased Cmax, AUC0-t, AUC0-∞(P<0.05, P<0.01), especially for the latter(P<0.05, P<0.01), and their relative bioavailabilities were increased to 1.39 times and 2.89 times, respectively.CONCLUSION Solid lipid nanoparticles can further promote buddleoside phospholipid complex’s in vivo absorption and enhance its bioavailability.
作者
周开
张佩琛
郝海军
付金芳
范明松
ZHOU Kai;ZHANG Pei-chen;HAO Hai-jun;FU Jin-fang;FAN Ming-song(Zhengzhou Shuqing Medical College,Zhengzhou 450064,China;Technical Center,Shanghai Leiyunshang Pharmaceutical Co.,Ltd.,Shanghai 201401,China)
出处
《中成药》
CAS
CSCD
北大核心
2020年第6期1401-1405,共5页
Chinese Traditional Patent Medicine
基金
上海市科委专项计划(17DZ1900107)。
关键词
蒙花苷
磷脂复合物
固体脂质纳米粒
制备
体内药动学
乳化-超声分散法
HPLC
buddleoside
phospholipids complex
solid lipid nanoparticles
preparation
in vivo pharmacoki-netics
emulsion-ultrasonic dispersion method
HPLC
