布南色林片的制备及体内外评价  

Preparation and in vitro/in vivo evaluation of blonanserin tablets

作　　者：刘东娜 徐晖[1] LIU Dongna;XU Hui(School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China;Hebei Hejia Pharmatech Group Co.,Ltd.,Shijiazhuang 050000,China)

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016 [2]河北合佳医药科技集团股份有限公司,河北石家庄050000

出　　处：《沈阳药科大学学报》2020年第11期961-967,997,共8页Journal of Shenyang Pharmaceutical University

摘　　要：目的制备布南色林片,考察其溶出特征,评价其与参比制剂(洛珊?)的生物等效性。方法以溶出度作为主要评价指标,考察原料药粒径、辅料用量等对药物溶出的影响,确定布南色林片的处方工艺。采用相似因子(f2)法评价不同溶出介质中自制制剂与参比制剂溶出曲线的一致性。考察自制与参比制剂在比格犬体内的药物动力学。结果自制与参比制剂在不同溶出介质中溶出的f2均大于60,溶出曲线一致。自制与参比制剂在比格犬体内的药代动力学参数AUC0-24 h分别为(353.35±15.83)和(356.93±23.21)μg·h·L-1,ρmax分别为(90.30±6.95)和(96.70±5.46)μg·L-1,tmax均为1 h,药动学参数均无显著性差异(P>0.05)。结论自制布南色林片与参比制剂体外溶出和药物动力学行为一致,具有生物等效性。Objective To evaluate the quality consistency in vitro and bioequivalence in beagle dogs between self-made and original preparation(Lonasen?),Blonanserin tablets were prepared,and their dissolution characteristics were further examined.Methods By using the dissolution curve as the main evaluation index,the effects of API particle size and excipients on drug dissolution were studied.And the prescription and processing parameters were determined.The similarity factor(f2)was used to evaluate the dissolution behavior of the self-made and original preparations in different pH buffer media.Pharmacokinetics of self-made and original preparations were evaluated in beagle dogs.Results In different pH buffer solutions,the f2 values of the self-made and original preparations were both above 60,then the dissolution behaviors of both drugs were consistent.In beagle dogs,the AUC0-24 h values were(353.35±15.83)and(356.93±23.21)μg·h·L^-1,theρmax values were(90.30±6.95)and(96.70±5.46)μg·L^-1,and the tmax values were both 1 h of the self-made and original preparations,respectively.There was no significant difference in the pharmacokinetics between the two preparations(P>0.05).Conclusion The dissolution in vitro and pharmacokinetic behavior in vivo of self-made preparation are consistent and bioequivalent compared with the original preparation.

关 键 词：布南色林 溶出曲线 液相色谱-质谱联用 药物动力学 

分 类 号：R94[医药卫生—药剂学]