联糖米托蒽醌白蛋白微球的制备及其性质研究
PREPARATION AND CHARACTERIZATION OF MITOXANTRONEBOVIN SERUM ALBUMIN MICROSPHERES MODIFIED WITH A GALACTOSYLATED DERIVATIVE
作者:张志荣,张奇志
Author:
收稿日期: 年卷(期)页码:1998,(04):-217-222
期刊名称:华西药学杂志
Journal Name:WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字:联糖米托蒽醌白蛋白微球;体外药物释放;肝靶向给药系统
Key words:
基金项目:国家自然科学基金!39670862
中文摘要
以米托蒽醌为模型药物,用乳化热固化法制备了米托蒽醌白蛋白微球。以D-半乳糖为原料,经溴代、缩合、置换、加成等反应合成了2-亚氨基-2-甲氧基乙基-1-硫化-β-D-半乳吡喃糖苷(IME-thiogalactose)。以此为中间体与米托蒽醌白蛋白微球在室温下反应制备了联糖米托蒽醌白蛋白微球及其冻干剂。并对冻干剂的形态、球径及其分布、再分散性、糖密度、载药量、体外释药特性进行了研究,为白蛋白微球与联糖白蛋白微球在体内的肝靶向性探讨奠定了基础。
英文摘要
1 Morell AG,Van Den Hamer CTA Scheinberg IH.Phsical and chemical studies on ceruloplasmin.IV.preparation of radioactive,sialic acid-free ceruloplasmin labeled with tritium on terminal D-galactose residues.J Biol Chem,1966,241(16): 3745
2 Morell AG,Irvine RA,Sternlibe Ⅰ,et al.Phsical and chemical studies on ceruloplasmin.V.metabolic studies on sialic acid-free ceruloplasmin in vivo.J Biol Chem,1968,243(18):155
3范举正.李银铃,庞其捷等.肝靶向抗病毒药NGA-ACV的制备及其趋肝性、药学学报,1996,31(8):585
4庞其捷,杨麟,钟裕国.等半乳精基新糖白蛋白的制备及 其对肝特异性受体结合试验的研究.华西医科大学学报,1991,22(4):368
5张志荣,钱文.肝靶向米托蒽醌白蛋白微球的研究.药学学报,1997,32(1):72
6 Vogel’s.Textbook of practicle of practicle organic chemistry.4th 1978.457
7 Lee YC,Stowell CP,Krantz MJ.2-Imino-2- methoxyethl-1-thioglycosides:New reagents for attaching sugars to proteins.Biochemistry,1976,15(1):3956
8 Dubois M,Gilles KA,Hamilton JK,et al.Colorimetric method for determination of sugars and related substances.Anal Chem,1956,28(3):350
9 Vera DR.Krohn KA,Stadalnik RC,et al.Tc-99m galactosyl-neoglycoalbumin:In vitro Characterization of receptormediated binding.J Nucl Med,1984,25:779
10 Schwartz BA,Gray GR.Proteins containing reductively amiated disaccharides;synthesis and chemical characterization.Archives of Biochemistry and Biophysics,1977,181:542
【关闭】