.224.中国抗生素杂志2014年3月第39卷第3期文章编号：1001-8689(2014)03-0224-05替尼泊苷冻干粉针剂的处方及冻干工艺研究杨柳1姚瑰玮1王秀玲2余邦良1,*(1海南医学院药学院，海口571101；2海南紫杉园药业有限公司，海口570216)摘要：目的优化替尼泊苷冻干粉针剂的处方及冻干工艺。方法采用4正交试验优选处方，以原料药的浓度、L9(3)(A)聚氧乙烯氢化蓖麻油的用量(B)、甘露醇的用量(C)、药液pH值(D)为考察因素，以制剂溶解性和含量为质量评价指标，确定最优处方组合；采用4正交试验确定冻干工艺，以预冻温度和时间、升华干燥温度变化、升华干燥时间和真空压A1B3C3D3L9(3)(E)(F)力、解析干燥温度和真空压力为考察因素，以成品收率和残余水分为质量评价指标，确定最优冻干工艺组合。(G)(H)E2F3G1H2结果通过处方及冻干工艺制备批替尼泊苷冻干粉针样品，批样品的外观均为白色疏松块状，复溶性好，A1B3C3D3E2F3G1H233含量均在99.3%左右。结论该替尼泊苷冻干粉针处方及冻干工艺可行性好、重现性好。关键词：替尼泊苷；冻干粉针剂；正交试验；处方优选；冻干工艺研究中图分类号：R979.1文献标志码：ADOI:10.13461/j.cnki.cja.005296StudyontheprescriptionandpreparationtechniqueofteniposidefreezedriedpowderinjectionYangLiu1,YaoGui-wei1,WangXiu-ling2andYuBang-liang1(1TheDepartmentofPharmacy,HainanMedicalCollege,Haikou571101;2HainanYewPharmaceuticalCo.,Ltd.,Haikou570216)AbstractObjectiveTooptimizetheprescriptionandfreeze-drytechniqueofteniposidefreezedriedpowderinjection.MethodsTheoptimalprescriptioncombinationA1B3C3D3wasdeterminedbyorthogonalexperimental4designL9(3)withtheconcentrationofpharmaceuticalproduct(A),thedosageofpoly-oxyethylenehydrogenatedcastoroil(B),thedosageofmannitol(C)andphysicliquorpH(D)asconsiderationfactors.Andthesolubilityandcontentofpreparationweretakenasqualityevaluationindex;Thefreeze-driedtechniquecombinationE2F3G1H2was4determinedbyorthogonalexperimentaldesignL9(3)withtheforefrozentemperatureandtime(E),thesublimationdryingtemperaturechange(F),theresolutiondryingtimeandvacuumpressure(G)andresolvedryingtemperatureanddryingtemperature(H)asconsiderationfactors.Andtheproductyieldandremnantwatercontentweretakenasqualityevaluationindex.ResultsThreebatchsofteniposideforfreezedriedpowderinjectionwerepreparedwithA1B3C3D3prescriptionandE2F3G1H2freeze-driedtechniqueandtheappearanceofthethreebatchsofsampleswereallwhiteporosityblock.There-dissolvabilitywasgood.Thecontentwasabout99.3%.ConclusionTheprescriptionandpreparationtechniqueofteniposideforfreezedriedpowderinjectionisbetterfeasibility