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    • 8. 发明公开
    • 중성 지질중합체 및 그를 함유하는 리포솜 조성물
    • 中性脂质体和包含其的脂质组合物
    • KR1020070086708A
    • 2007-08-27
    • KR1020077014651
    • 2000-07-12
    • 알자 코포레이션
    • 자립스키사무엘
    • C08G65/329C08G65/00A61K9/127
    • A61K9/1272C08G65/329C08L2203/02Y10T428/2984
    • Liposomes containing PEG-substituted neutral lipopolymers provide similar circulation times to liposomes incorporating conventional, negatively charged PEG-substituted phospholipids. Use of the uncharged lipopolymers can also present advantages in terms of interactions with cell surfaces and reduced leakage of charged substances, particularly cationic drugs, from the liposomes. The lipopolymers are of formula (I) wherein each of R1 and R2is an alkyl or alkenyl chain having between about 8 to about 24 carbon atoms, n is about 10 to about 300, Z is selected from the group consisting of hydroxy, alkoxy, benzyloxy, carboxylic ester, sulfonic ester, alkyl or aryl carbonate, amino, and alkylamino, and the linkage L is selected from the group consisting of (i) -X-(C=O)-Y-CH 2-, (ii) -X-(C=O)-, and (iii) -X-CH2-, wherein X and Y are independently selected from oxygen, NH, and a direct linkage.
    • 含有PEG-取代的中性脂质聚合物的脂质体提供与掺入常规带负电荷的PEG-取代磷脂的脂质体相似的循环时间。 使用不带电荷的脂质聚合物也可以在与细胞表面的相互作用方面具有优势,并且从脂质体中减少带电物质,特别是阳离子药物的泄漏。 脂族聚合物具有式(I),其中R 1和R 2各自为具有约8至约24个碳原子的烷基或烯基链,n为约10至约300,Z选自羟基,烷氧基,苄氧基 羧酸酯,磺酸酯,碳酸烷基或芳基酯,氨基和烷基氨基,并且连接L选自(i)-X-(C = O)-Y-CH 2 - ,(ii) - X-(C = O) - 和(iii)-X-CH 2 - ,其中X和Y独立地选自氧,NH和直接键。
    • 10. 发明公开
    • 물리적 안정성이 증가된, 활성제, 현탁 비히클 및 밀도개질 고체를 포함하는 현탁액
    • 包含有效原理的悬架,悬挂式车辆,具有增加的物理稳定性的密度修正固体
    • KR1020070069151A
    • 2007-07-02
    • KR1020077006774
    • 2005-08-10
    • 알자 코포레이션
    • 로발렌티필립마이클
    • A61K9/10A61K47/22A61K47/02
    • A61K9/0004A61K9/0019A61K9/10A61K47/02
    • Density-matching is used to provide suspending vehicles, pharmaceutical suspensions, dosage forms, and kits as well as methods of making and using the vehicles, suspensions and dosage forms. Pharmaceutical suspensions comprising a pharmaceutically active agent having an active agent density, rhoA, and a suspending vehicle having a suspending vehicle density, rhosv; wherein the suspending vehicle density, rhosv is substantially equal to the active agent density, rhoA, are provided. Suspending vehicles comprise at least one suspending agent. The suspending vehicles can further comprise at least one density-modifying solid in such a combination with the suspending agent as to create a suspending vehicle that has a density that substantially matches the density of a desired drug particle or combination of drug particles. Pharmaceutical suspensions that remain homogenous during prolonged storage can be obtained.
    • 密度匹配用于提供悬浮剂,药物悬浮液,剂型和试剂盒,以及制备和使用载体,悬浮液和剂型的方法。 药物悬浮液,其包含具有活性剂密度的药物活性剂,rhoA和具有悬浮载体密度的悬浮剂, 其中悬浮车密度rhosv基本上等于活性剂密度rhoA。 悬挂车辆包括至少一种悬浮剂。 悬浮载体可以进一步包含至少一种与悬浮剂的组合的密度改变固体,以产生具有与所需药物颗粒或药物颗粒组合基本一致的密度的悬浮载体。 可以获得在延长储存期间保持均匀的药物悬浮液。