资源描述:
《紫杉醇囊泡的研制及大鼠体内的药动学特征》由会员上传分享,免费在线阅读,更多相关内容在教育资源-天天文库。
1、[13]KATAOKAK,MATSUMOTOT,YOKOYAMAM,etal1Doxo-lactide)/poly(L-lactide)surfacegraftedhydroxyapatitecompos-rubicin-loadedpoly(ethyleneglycol)-poly(B-benzy-l-laspar-ite[J]1JJilinUniv(MedEd)(吉林大学学报:医学版),tate)copolymermicelles:theirpharmaceuticalcharacteristics2007,33
2、(1):57-601andbiologicalsignificance[J]1JControlledRelease,2000,64[17]FENGM,PANSR,WUWR1Haemolyticevaluationofampho-(1-3):143-1531tericinBloadedPEG-b-PBLAnanospheres[J]1JChinaPharm[14]NATALYAR1Physicalstimul-iresponsivepolymericmicellesforUniv(中国药科大学学报),2004,35(3
3、):263-2661ant-icancerdrugdelivery[J]1ProgPolymSci,2007,32(8-9):[18]CAOYB,JIANGYY,WANGN,etal1Invitroantifungal962-9901activitystudyofterbiaminazole,anewtriazoleantifungalagent,[15]KWONGS,KATAOKAK1Blockcopolymermicellesaslong-cir-bybrothmicrodilutiontesting[J]1Ch
4、inJAntibiotics(中国抗生culatingdrugvehicles[J]1AdvDrugDelivRev,1995,16(2-3):素杂志),2000,25(3):183-1871295-3091(收稿日期:2009-09-27)[16]SHAOY,LULJ,RONGL,etal1Biocompatibilityofpoly(L-紫杉醇囊泡的研制及大鼠体内的药动学特征朱铉,扶艳,苏美琴,阮航,张真,梁信芳(厦门大学医学院药学系,福建厦门361005)摘要:目的制备紫杉醇囊泡,对其进行表征,进一步研究其在大
5、鼠体内的药动学特征及组织分布情况。方法以司盘(Span)和胆固醇(CH)为主要膜材,用薄膜分散法制备紫杉醇囊泡,采用正交实验进行处方优化,用透射电镜考察其形态和构-1造,用激光粒度仪测定囊泡的粒径大小和F电位,按715,15,30mg#kg3个剂量大鼠颈静脉给药后检测一定时间点的血药-1浓度,对照为15mg#kg的紫杉醇注射液。结果紫杉醇囊泡的平均粒径为(157?16)nm,冻干后紫杉醇囊泡的平均粒径为(189?23)nm;冻干后的紫杉醇囊泡在贮存6个月的时间内包封率没有明显变化,粒径略有增大。紫杉醇囊泡相对于紫杉醇
6、注射液体内半衰期显著延长,生物利用度提高;组织分布结果显示明显的肝脾靶向性。结论成功研制了紫杉醇囊泡,囊泡有望成为紫杉醇新的剂型。关键词:囊泡;包封率;紫杉醇;药动学;组织分布中图分类号:R944文献标识码:A文章编号:1001-2494(2010)05-0365-07PreparationandPharmacokineticsofPaclitaxelNiosomesZHUXuan,FUYan,SUMe-iqin,RUANHang,ZHANGZhen,LIANGXin-fang(DepartmentofPharmac
7、y,MedicalCollegeofXiamenUniversity,Xiamen361005,China)ABSTRACT:OBJECTIVEToprepareandcharacterizethepaclitaxelniosomes,andtostudythepharmacokineticsandtissuedistr-ibutioninrats1METHODSThepaclitaxelniosomeswerepreparedwithSpanandcholesterolusingthin-filmhydration
8、method1ThevesicleswerevisualizedbytransmissionelectronmicroscopyandsizedbylaserparticleanalyzeronaMalvernMastersizer1Thepre-scriptionwasoptimizedbyusingorthogonaldesign1Thep