摘要
目的制备左旋班布特罗(R-Bambuterol,R-BMB)吸入水雾剂,并对处方进行优化。方法以甘油和丙二醇为辅料,配比得到9个处方。测定9个处方的理化性质,包括pH值、渗透压、表面张力,并通过碰撞器法和激光衍射法测试其粒径、空气动力学中值粒径(mass median aerodynamic diameter,MMAD)、d0.5、细微粒子百分数及跨度参数。运用正交实验方差分析法探索甘油和丙二醇对左旋班布特罗吸入水雾剂粒径大小及分布的影响。结果随着甘油和丙二醇增加,左旋班布特罗吸入水雾剂的d0.5与MMAD均出现下降趋势。粒径测试及方差分析结果表明,含有1%甘油和15%丙二醇的处方具有最低的粒径(2.510μm)、较小的MMAD(4.577μm)及较高的肺部药物递送效率(54.314%)。结论由1%甘油和15%丙二醇及0.25%R-BMB构成的R-BMB吸入水雾剂具有较好的雾化粒径大小及肺部药物递送效率,有望用于支气管哮喘的治疗。
Objective To prepare and optimize the formulation of R-bambuterol(R-BMB)inhalation solution.Methods Nine prescriptions were obtained with glycerol and propylene glycol.Physico-chemical properties of nine prescriptions,including pH,osmotic pressure and surface tension were tested.Particle size was determined by method of cascade impactor and laser diffraction,and the parameters of Mass median aerodynamic diameter(MMAD),d0.5,Fine partical fraction(FPF)and Span were analyzed.The effects of glycerol and propylene glycol on particle size and distribution were investigated by Variance analysis.Results With the increase of glycerol and propylene glycol,the d0.5 and MMAD decreased.Particle size test and Variance analysis results showed that:1%glycerol 15%1,2-propanediol prescription had the lowest particle size of 2.510μm,the smaller MMAD of 4.577μm and the higher pulmonary drug delivery efficiency of 54.314%.Conclusion The R-BMB inhalation solution of 1%glycerol,15%propanediol and 0.25%R-BMB has good aerosol particle size and higher pulmonary drug delivery efficiency,which is expected to be used in the treatment of bronchial asthma.
作者
张睿
周浩銮
张雪娟
胡军华
王冠林
陈茜
谭文
ZHANG Rui;ZHOU Haoluan;ZHANG Xuejuan;HU Junhua;WANG Guanlin;CHEN Xi;TAN Wen(Institute of Biomedical and Pharmaceutical Science,Guangdong University of Technology,Guangzhou 510006,China;School of Pharmaceutical Sciences,Sun Yat-Sen University,Guangzhou 510006,China)
出处
《广东药科大学学报》
CAS
2020年第3期322-328,共7页
Journal of Guangdong Pharmaceutical University
基金
广东省科技厅省重大专项合作项目(2015B010109004)。
关键词
左旋班布特罗
丙二醇
甘油
粒径
PH值
渗透压
表面张力
R-bambuterol
propylene glycol
glycerol
particle size
pH
osmotic pressure
surface tension
