中国医药工业杂志
中國醫藥工業雜誌
중국의약공업잡지
CHINESE JOURNAL OF PHARMACEUTICALS
2009年
11期
833-836
,共4页
王九成%刘继三%梁丹%梁国正
王九成%劉繼三%樑丹%樑國正
왕구성%류계삼%량단%량국정
氟维司群:嵌段共聚物%微球%皮下注射:释放性质%药代动力学
氟維司群:嵌段共聚物%微毬%皮下註射:釋放性質%藥代動力學
불유사군:감단공취물%미구%피하주사:석방성질%약대동역학
fulvestrant%block copolymer%microsphere%subcutaneous%releasing property%pharmacokinetics
分别以嵌段共聚物(聚乳酸-单甲氧基聚乙二醇,分子量比为40 000:2 000)和非嵌段共聚物(聚乳酸-聚羟乙酸,分子量均为40 000,摩尔比分别为75:25、50:50)作为载体材料,采用乳化-液中干燥法制备包载氟维司群的微球.大鼠单剂量(50 mg/kg)皮下注射3种氟维司群微球,采用LC-MS/MS法测定血药浓度,计算药动学参数.结果表明,使用嵌段共聚物制备的微球,药-时曲线较平稳,释放效果较好.
分彆以嵌段共聚物(聚乳痠-單甲氧基聚乙二醇,分子量比為40 000:2 000)和非嵌段共聚物(聚乳痠-聚羥乙痠,分子量均為40 000,摩爾比分彆為75:25、50:50)作為載體材料,採用乳化-液中榦燥法製備包載氟維司群的微毬.大鼠單劑量(50 mg/kg)皮下註射3種氟維司群微毬,採用LC-MS/MS法測定血藥濃度,計算藥動學參數.結果錶明,使用嵌段共聚物製備的微毬,藥-時麯線較平穩,釋放效果較好.
분별이감단공취물(취유산-단갑양기취을이순,분자량비위40 000:2 000)화비감단공취물(취유산-취간을산,분자량균위40 000,마이비분별위75:25、50:50)작위재체재료,채용유화-액중간조법제비포재불유사군적미구.대서단제량(50 mg/kg)피하주사3충불유사군미구,채용LC-MS/MS법측정혈약농도,계산약동학삼수.결과표명,사용감단공취물제비적미구,약-시곡선교평은,석방효과교호.
Fulvestrant microspheres entrapped by PLA-block-mPEG copolymer (molecular weight ratio 40 000 : 2 000) and two kind of PLGA (molecule weight 40 000, molar ratio 75 : 25 and 50 : 50) were prepared with emulsion in liquid drying method. Three kinds of fulvestrant microspheres were given subcutaneously to rats respectively, with single dosage of 50 mg/kg. The drug concentrations were determined by LC-MS/MS. The results showed that the fulvestrant microsphere prepared by PLA-block-mPEG copolymer had a smooth concentration-time chart. The releasing effect of the PLA-block-mPEG microsphere was better than that prepared by two kind of PLGA.