盐酸托烷司琼醇质体凝胶贴膏的制备与体外评价  

Preparation and in vitro Evaluation of Tropisetron Hydrochloride Ethosomal Cataplasm

作　　者：张倩 闫娜娜 高欣怡 贺萍[3] 刘万卉[1,2] ZHANG Qian;YAN Nana;GAO Xinyi;HE Ping;LIU Wanhui(Key Lab.of Molecular Pharmacology and Drug Evaluation,Ministry of Education,Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong,School of Pharmacy,Yantai University,Yantai 264005;State Key Lab.of Long-acting and Targeting Drug Delivery System,Shandong Luye Pharmaceutical Co.,Ltd.,Yantai 264003;School of Chemistry and Chemical Engineering,Yantai University,Yantai 264005)

机构地区：[1]烟台大学药学院,新型制剂与生物技术药物研究山东省高校协同创新中心,分子药理和药物评价教育部重点实验室,山东烟台264005 [2]山东绿叶制药有限公司,长效和靶向制剂国家重点实验室,山东烟台264003 [3]烟台大学化学化工学院,山东烟台264005

出　　处：《中国医药工业杂志》2022年第4期530-538,共9页Chinese Journal of Pharmaceuticals

基　　金：“国家重大新药创制”科技重大专项(2017ZX09101001)。

摘　　要：采用乙醇注入法制备不同载药量的盐酸托烷司琼(TRO)醇质体,并表征所得制品的粒径、ζ电位、形态、包封率和体外经皮渗透性等性质。采用正交试验进行凝胶贴膏中关键辅料的筛选,同时将不同载药量的TRO醇质体制备成凝胶贴膏,解决了醇质体用药不便且难以持续递送药物的问题。体外经皮渗透试验结果表明,载药量0.36%的TRO醇质体凝胶贴膏的经皮渗透率可达到21.66%,24 h累积透皮量为(92.45±6.85)μg·cm^(-2)。进一步比较了该醇质体凝胶贴膏与同浓度水溶液凝胶贴膏的体外释放速率和体外经皮渗透量,结果显示醇质体凝胶贴膏中TRO的释放速度慢于水溶液凝胶贴膏,但其经皮渗透量却显著高于水溶液凝胶贴膏(P<0.05),能够起到缓释且促进渗透的作用。通过黏附性试验证明本研究所制备TRO醇质体凝胶贴膏的黏附性良好,满足贴附需求。The tropisetron hydrochloride(TRO)ethosomes with different drug loadings were prepared by ethanol injection method.The particle size,ζpotential,morphology,entrapment efficiency and skin permeability in vitro of the products were characterized.Orthogonal design was adopted to screen the critical excipients in cataplasm.Meanwhile,the TRO ethosomes with different drug loadings were incorporated into cataplasms to solve the problems of inconvenient administration and difficult to continuous delivery.The results of in vitro transdermal permeation study showed that the percutaneous penetration rate and cumulative permeability within 24 h of the cataplasm containing ethosomes with drug loading of 0.36%were 21.66%and(92.45±6.85)μg·cm^(-2),respectively.Moreover,the in vitro release and in vitro skin permeation of the TRO ethosomal cataplasm and common TRO cataplasm with the same concentration were investigated and compared.It was found that the release of TRO from the ethosomal cataplasm was slower than the common cataplasm,while the transdermal permeation of the ethosomal cataplasm was significantly higher than that of the common cataplasm(P<0.05).The tack and peel adhesion of TRO ethosomal cataplasm was investigated,and the results showed good adhesive properties.

关 键 词：盐酸托烷司琼 醇质体 凝胶贴膏 体外释放 体外经皮渗透 黏附性 

分 类 号：R944.9[医药卫生—药剂学]