丙酸氟替卡松经鼻缓释膜的处方筛选和体外释放研究

Formulation screening and in vitro release study of Fluticasone propionate transnasal sustained-release films

目的优化丙酸氟替卡松经鼻缓释膜的处方,研究其释放度。方法通过单因素实验筛选聚乳酸-羟基乙酸共聚物(PLGA)的种类和用量、增塑剂的种类和用量、载药量和成膜溶剂;通过正交试验优化丙酸氟替卡松经鼻缓释膜的处方。结果丙酸氟替卡松经鼻缓释膜的最佳处方为:PLGA85/15(特性黏数0.65~0.75 dL·g^(-1))用量为17.62 mg·cm^(-2),丙酸氟替卡松的载药量4.75 mg·cm^(-2),增塑剂PEG400的用量0.78 mg·cm^(-2),溶剂为丙酮。结论丙酸氟替卡松经鼻缓释膜可缓慢释放丙酸氟替卡松12周,具备良好的长效缓释性能。

OBJECTIVE To optimize the formulation of Fluticasone propionate transnasal sustained-release films and to study its release.METHODSs Through single factor experiments,the types and dosage of poly(lactic-co-glycolic acid)(PLGA),the types and dosage of plasticizers,drug loading,and film forming solvents were selected.The optimal prescription of Fluticasone propionate transnasal sustained-release film was selected by Orthogonal experiments.RESULTS The optimal formulation for the transnasal sustained-release film of Fluticasone propionate is PLGA85/15(intrinsic viscosity was 0.65-0.75 dL·g^(-1))with a dosage of 17.62 mg·cm^(-2),fluticasone propionate loading at 4.75 mg·cm^(-2),PEC400 as a plasticizer at O.78 mg·cm^(-2),and the solvent was acetone solution.CONCLUSIONFluticasone propionate is slowly released through the transnasal sustained-release film for 12 weeks,exhibiting good long-term sustained-release performance.