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    • 5. 发明授权
    • Radioiodinated arylaliphatic ether analogues of cholesterol
    • 胆固醇的放射碘化芳基脂肪醚类似物
    • US4933157A
    • 1990-06-12
    • US212196
    • 1988-06-27
    • Raymond E. CounsellMohamed K. RuyanSusan W. SchwendnerLaura E. Deforge
    • Raymond E. CounsellMohamed K. RuyanSusan W. SchwendnerLaura E. Deforge
    • C07J9/00
    • C07J9/00
    • Novel radioiodinated analogues of naturally-occurring cholestrol esters, arylaliphatic cholesteryl ethers, are selective for low density lipoproteins and have been shown to be successful imaging agents for adrenal glands. The arylaliphatic cholesteryl ethers have the general formula: ##STR1## where X is a radioactive isotope of iodine and n is an integer between 1 and 20. Two illustrative examples, m-iodobenzyl cholesteryl ether and 12-(m-iodophenyl) dodecyl cholesteryl ether, were radiolabeled with .sup.125 I by an isotope exchange reaction. Tissue distribution studies indicate significant accumulation of the cholesteryl ethers in the adrenal glands, and to a lesser extent in the liver. The cholesteryl ethers selectively incorporate into plasma lipoproteins as determined by polyacrylamide gel electrophoresis.
    • 天然存在的胆甾醇酯,芳基脂族胆固醇醚的新型放射性碘化物类似物对于低密度脂蛋白是选择性的,并且已被证明是用于肾上腺的成功的成像剂。 芳基脂族胆甾醇醚具有以下通式:其中X是碘的放射性同位素,n是1至20之间的整数。两个说明性实例,间 - 碘苄基胆固醇醚和12-(间碘苯基)十二烷基胆固醇醚 用125I通过同位素交换反应进行放射性标记。 组织分布研究表明胆固醇醚在肾上腺中的显着积累,在肝脏中的程度较小。 通过聚丙烯酰胺凝胶电泳测定,胆固醇醚选择性地掺入到血浆脂蛋白中。
    • 9. 发明授权
    • Blood-pool carrier for lipophilic imaging agents
    • 用于亲脂显像剂的血液池载体
    • US07582279B2
    • 2009-09-01
    • US10692311
    • 2003-10-23
    • Raymond E. CounsellMarc A. LonginoJamey P. Weichert
    • Raymond E. CounsellMarc A. LonginoJamey P. Weichert
    • A61K51/00A61M36/14
    • A61K49/0461A61K9/1075A61K9/1275A61K49/0433A61K49/1806A61K51/0406A61K51/0478A61K51/1217B82Y5/00Y10S514/938Y10S977/829Y10S977/905Y10S977/927Y10S977/93
    • A surface-modified lipoprotein-like oil-in-water emulsion useful as a blood-pool selective delivery vehicle for lipophilic imaging agents or lipophilic derivatives of water-soluble imaging agents. The blood-pool selective delivery vehicle remains in the blood for several hours, shows very little early hepatic sequestration, and is cleared from the blood within 24 hours. The mean diameter of the oil phase is less than 150 nm which minimizes sequestration by the reticuloendothelial system. The surface of the oil phase is modified with a polyethyl glycol-modified phospholipid to prevent normal interactions with the receptor sites of the hepatocytes. In radiographic imaging, radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate], or lipid soluble derivatives of traditional water-soluble contrast agents, such as aliphatic esters of iopanoic, diatrizoic, and acetrizoic acid, may be incorporated into the lipophilic core of a lipoprotein-like emulsion particle.
    • 用作脂溶性成像剂或水溶性成像剂的亲脂性衍生物的血液池选择性递送载体的表面改性脂蛋白样水包油乳液。 血液池选择性输送载体在血液中保持数小时,显示出非常少的早期肝脏螯合,并在24小时内从血液中清除。 油相的平均直径小于150nm,其最小化网状内皮系统的螯合。 用聚乙二醇修饰的磷脂修饰油相的表面以防止与肝细胞的受体位点的正常相互作用。 放射摄影成像中,放射性或稳定的合成或半合成多卤甘油三酸酯如2-油酰甘油-1,3-双[7-(3-氨基-2,4,6-三碘苯基)庚酸酯]或脂溶性衍生物 的传统的水溶性造影剂,如碘,脂肪族和代谢酸的脂肪族酯可以并入脂蛋白样乳液颗粒的亲脂性核心中。
    • 10. 发明授权
    • Hepatocyte-selective oil-in-water emulsion
    • 肝细胞选择性水包油乳剂
    • US6103216A
    • 2000-08-15
    • US737429
    • 1996-11-15
    • Raymond E. CounsellMarc A. LonginoJamey P. WeichertDouglas A. Bakan
    • Raymond E. CounsellMarc A. LonginoJamey P. WeichertDouglas A. Bakan
    • A61K9/107A61K9/127A61K47/14A61K49/00A61K49/04A61K49/18A61K51/12B01F3/00
    • A61K9/1075A61K49/0433A61K49/1806A61K51/1217A61K9/1275Y10S514/893Y10S514/894Y10S514/938Y10S514/941Y10S516/923Y10S516/93
    • A heat and shelf-stable oil-in-water emulsion useful as a tissue or cell-selective delivery vehicle. Radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate] or 2-oleoylglycerol-1,3-bis[.omega.-(3,5-bis-trifluoromethyl)-heptanoate] or phenyl acetate, can be incorporated into the lipophilic core of a lipoprotein-like emulsion particle. The lipophilic core is surrounded by a phospholipid membrane comprising cholesterol and apolipoproteins. For hepatocyte-selective delivery, the emulsion is chylomicron remnant-like by being in a size range of 50 to 200 nm as measured by number weighting analysis with a narrow size distribution (
    • PCT No.PCT / US95 / 05974 371日期1996年11月15日 102(e)日期1996年11月15日PCT提交1995年5月16日PCT公布。 公开号WO95 / 31181 日期1995年11月23日用作组织或细胞选择性递送载体的热稳定的水包油乳液。 放射性或稳定的合成或半合成多卤甘油三酸酯,如2-油酰甘油-1,3-双[7-(3-氨基-2,4,6-三碘苯基)庚酸酯]或2-油酰甘油-1,3-二 双(ω-(3,5-双 - 三氟甲基) - 庚酸酯]或乙酸苯酯可加入脂蛋白样乳液颗粒的亲脂性核心中。 亲脂性核被包含胆固醇和载脂蛋白的磷脂膜包围。 对于肝细胞选择性递送,通过具有窄尺寸分布的数量加权分析(<3%大于300nm)测量并具有自然模拟的组成,通过在50至200nm的尺寸范围内,乳液是乳糜微粒残留的 发生乳糜微粒残留物。 在乳液配方中使用胆固醇促进载脂蛋白,特别是由肝细胞识别并且是结合和摄取所必需的Apo E的缔合。 稳定性和尺寸限制可以通过超高能量混合设备(例如MicroFluidizer(Microfluidics Corp.,Newton,Mass。))来实现,以形成乳液。 在优选的实施方案中,乳液的重量摩尔渗透压浓度由甘油而不是生理盐水控制。