盐酸特比萘芬固体分散体微丸的制备及质量评价  

Preparation and quality evaluation of terbinifine hydrochloride solid dispersion pellets

作　　者：任丽莉[1] 裴希希 陈国广[1] REN Lili;PEI Xixi;CHEN Guoguang(School of Pharmaceutical Sciences,Nanjing Tech University,Nanjing 211800,China)

机构地区：[1]南京工业大学药学院,江苏南京211800

出　　处：《南京工业大学学报（自然科学版）》2018年第6期32-39,50,共9页Journal of Nanjing Tech University(Natural Science Edition)

摘　　要：为了提高盐酸特比萘芬的体外溶出度,制备盐酸特比萘芬的固体分散体微丸。采用流化床包衣技术中的喷雾干燥功能将盐酸特比萘芬和聚乙二醇6000(PEG6000)喷载于空白丸芯的表面,使固体分散体形成于微丸的表面。采用单因素法考察制备工艺。以上药效率、粘连率和体外溶出度作为效应值,采用星点设计-效应面法优化固体分散体微丸的制备处方。对盐酸特比萘芬固体分散体进行鉴别,并对固体分散体微丸进行溶出度考察和质量评价。结果表明:采用经优化后的制备工艺(雾化压力250 k Pa,进风量8 m3/min,泵液速率1. 0 mL/min,物料温度55℃)并按处方(盐酸特比萘芬与PEG6000质量比为1∶3. 96,丸芯增重72. 75%)制得的固体分散体微丸在30 min内体外溶出度达90%以上,上药效率为89. 9%,粘连率为0. 51%。傅里叶变换红外光谱仪(FT-IR)、X线粉末衍射仪(XRD)和差示扫描量热仪(DSC)表征了固体分散体的形成。盐酸特比萘芬的固体分散体微丸平均含药质量分数为6. 17%,粒径为0. 83～0. 88 mm,平均减重率仅0. 28%。以上结果表明制得的盐酸特比萘芬固体分散体微丸质量稳定,可显著改善盐酸特比萘芬的体外溶出度。To improve the in vitro dissolution of terbinafine hydrochloride,a fluid bed coating technique was used to prepare the solid dispersion pellets of terbinafine hydrochloride.Terbinafine hydrochloride and polyethyleneglycol(PEG)6000 were dissolved in 80%ethanol and then was sprayed onto the surface of blank pellets through fluid bed spray drying function,thus solid dispersion were formed on the surface of pellets.The preparation process was studied by single factor method.Drug loading efficiency,adhesion rate and in vitro dissolution were as the response values,the central composite design response surface method was adopted to optimize the prescription.The solid dispersion was characterized,and the dissolution and quality of solid dispersion pellets were evaluated.Results revealed that solid dispersion pellets reached a rapid dissolution which was over 90%within 30 min under optimized preparation conditions(atomizing pressure of 250 kPa,inlet air flow of 8 m 3/min,pump liquid rate of 1.0 mL/min,material temperature of 55℃and prescriptions(drug-carrier mass ratio of 1∶3.96,weight gain of 72.75%).The drug loading efficiency was 89.7%and the adhesion rate was only 0.55%.The solid dispersion was characterized by means of X-ray powder diffraction(XRD),differential scanning calorimetry(DSC)and Fourier transform infrared spectroscopy(FT-IR).The average drug content of terbinafine hydrochloride solid dispersion pellets was 6.17%,the particle size was 0.83 0.88 mm,and the average weight loss rate was only 0.28%.The above results showed that the quality of the prepared solid dispersible pellets of terbinafine hydrochloride was stable and its dissolution was significantly improved.

关 键 词：盐酸特比萘芬 固体分散体 微丸 流化床 响应面法 

分 类 号：R943[医药卫生—药剂学]