黄芩素磷脂复合物白蛋白纳米粒的制备及其体内药动学研究  

Preparation and in vivo pharmacokinetics of albumin nanoparticles of baicalein phospholipid complex

作　　者：王风云 李伟宏 WANG Feng-yun;LI Wei-hong(Henan Vocational College of Applied Technology,Zhengzhou 450042,China)

机构地区：[1]河南应用技术职业学院,河南郑州450042

出　　处：《中成药》2021年第11期2939-2944,共6页Chinese Traditional Patent Medicine

基　　金：河南省高等学校重点科研计划项目(18A320081)。

摘　　要：目的制备黄芩素磷脂复合物白蛋白纳米粒,并考察其体内药动学。方法高压均质法制备白蛋白纳米粒,单因素试验筛选白蛋白与磷脂复合物比例、均质压力、均质次数,测定包封率、载药量、粒径、Zeta电位、体外释药。18只大鼠分别灌胃给予黄芩素、磷脂复合物、白蛋白纳米粒的0.5%CMC-Na溶液(100 mg/kg),于0、0.25、0.5、1、2、4、6、8、12、18、24、36 h采血,HPLC法测定黄芩素血药浓度,计算主要药动学参数。结果最佳条件为白蛋白与磷脂复合物比例12.5∶1,均质压力90 MPa,均质次数10次,平均包封率为83.19%,载药量为1.53%,粒径为177.62 nm,Zeta电位为-33.79 mV,36 h内累积溶出度为72.43%。与原料药比较,磷脂复合物、白蛋白纳米粒C_(max)、AUC_(0~t)、AUC_(0~∞)升高(P<0.05,P<0.01),以后者更明显(P<0.01),相对生物利用度分别增加至1.67、2.58倍。结论白蛋白纳米粒可促进黄芩素磷脂复合物的体外溶出和体内吸收。AIM To prepare the albumin nanoparticles of baicalein phospholipid complex and to investigate their in vivo pharmacokinetics.METHODS After preparation of albumin nanoparticles by high pressure homogenization method,single factor test was used to screen albumin-phospholipid complex ratio,homogenization pressure and homogenization frequency,the encapsulation efficiency,drug loading,particle size,Zeta potential and in vitro drug release were determined.Eighteen rats were given intragastric administration of 0.5%CMC-Na solutions of baicalein,phospholipid complex and albumin nanoparticles(100 mg/kg),respectively,after which blood collection was made at 0,0.25,0.5,1,2,4,6,8,12,18,24,36 h,HPLC was adopted in the plasma concentration determination of baicalein,and main pharmacokinetic parameters were calculated.RESULTS The optimal conditions were determined to be 12.5∶1 for albumin-phospholipid complex ratio,90 MPa for homogenization pressure,and ten times for homogenization frequency,the average encapsulation efficiency,drug-loading,particle size,Zeta potential and accumulative dissolution rate within 36 min were 83.19%,1.53%,177.62 nm,-33.79 mV and 72.43%,respectively.Compared with raw medicine,the phospholipid complex and albumin nanoparticles demonstrated increased C_(max),AUC_(0-t)and AUC_(0-∞)(P<0.05,P<0.01),especially for the latter(P<0.01),and the relative bioavailabilities were enhanced to 1.67 times and 2.58 times,respectively.CONCLUSION Albumin nanoparticles can promote the in vitro dissolution and in vivo absorption of baicalein phospholipids complex.

关 键 词：黄芩素 磷脂复合物 白蛋白纳米粒 制备 体内药动学 高压均质法 HPLC 

分 类 号：R944[医药卫生—药剂学]