公开(公告)号：US20070059247A1

公开(公告)日：2007-03-15

申请号：US11511721

申请日：2006-08-29

Applicant: Jonathan Lindner ,  Beat Kaufmann ,  Alexander Klibanov

Inventor： Jonathan Lindner ,  Beat Kaufmann ,  Alexander Klibanov

IPC: A61K49/22

CPC classification number: A61K49/223

Abstract: A method for generating an enhanced ultrasound image comprises intravenously administering to a subject a plurality of microbubbles of sufficient diameter to lodge in the microvasculature of a subject. An ultrasound image of a portion of the subject is generated wherein the image is enhanced by one or more of the administered microbubbles that has lodged in the microvasculature of the imaged portion. An ultrasound contrast media composition comprises a plurality of gas filled microbubbles. At least about 5% of the microbubbles have a diameter of at least about 4 microns (μm), and wherein the composition is suitable for intravenous administration. The administered microbubbles are of sufficient diameter to lodge in the microvasculature of a subject and can be used enhance ultrasound images small animal subjects including mice, rats and rabbits. The described methods and compositions can be used to enhance ultrasound images produced using high frequency ultrasound.

Abstract translation: 用于产生增强的超声图像的方法包括向受试者静脉内施用足够直径的多个微泡以放置在受试者的微血管中。 产生受试者的一部分的超声图像，其中通过被放置在成像部分的微血管中的一个或多个所施用的微泡来增强图像。 超声造影剂组合物包括多个气体填充的微泡。 至少约5％的微泡具有至少约4微米（mum）的直径，并且其中该组合物适用于静脉内施用。 施用的微泡具有足够的直径以置于受试者的微血管中，并且可以使用增强超声图像的小动物对象，包括小鼠，大鼠和兔。 所描述的方法和组合物可用于增强使用高频超声波产生的超声图像。

公开(公告)号：US20050281748A1

公开(公告)日：2005-12-22

申请号：US11149867

申请日：2005-06-10

Applicant: Jane Hirsh ,  Alison Fleming ,  Roman Rariy ,  Alexander Klibanov

Inventor： Jane Hirsh ,  Alison Fleming ,  Roman Rariy ,  Alexander Klibanov

IPC: A61K9/14 ,  A61K9/20 ,  A61K9/48 ,  A61K9/50 ,  A61K49/00

CPC classification number: A61K31/485 ,  A61K9/0053 ,  A61K9/145 ,  A61K9/148 ,  A61K9/1617 ,  A61K9/1664 ,  A61K9/2013 ,  A61K9/4808 ,  A61K9/4858 ,  A61K9/5015 ,  A61K9/5042 ,  A61K31/13 ,  A61K31/20 ,  A61K45/06 ,  A61K47/12 ,  A61K2300/00

Abstract: An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble. The abuse-deterrent composition prevents the immediate release of a substantial portion of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

Abstract translation: 已经开发了一种滥用威慑药物组合物，以减少药物不当管理的可能性，特别是诸如阿片类药物。 在优选的实施方案中，通过在药物和一种或多种脂肪酸之间形成盐，来修饰药物以增加其亲油性，其中一种或多种脂肪酸的浓度是活性剂的摩尔量的1至15倍 活性剂摩尔量的2〜10倍。 在一个实施方案中，改性药物均匀地分散在由缓慢溶解或不溶于水的材料组成的微粒内。 在一些实施方案中，含有微粒或药物颗粒的药物涂覆有一个或多个涂层，其中至少一个涂层是水不溶性的，优选有机溶剂不溶。 即使制剂的物理完整性受损（例如通过用刀片切碎或破碎），所述滥用威慑物组合物可以立即释放大部分药物，并将所得材料置于水中，嗅到或 吞下去 然而，当按照指导施用时，通过酶降解，胆汁酸的表面活性作用和机械侵蚀的组合，组合物被分解或逐渐溶解在胃肠道内，药物从组合物中缓慢释放。

公开(公告)号：US20050260189A1

公开(公告)日：2005-11-24

申请号：US10511383

申请日：2003-07-11

Applicant: Alexander Klibanov ,  Klaus Ley ,  Joshua Rychak

Inventor： Alexander Klibanov ,  Klaus Ley ,  Joshua Rychak

IPC: A61K9/127 ,  A61K39/395 ,  A61K47/48 ,  A61K49/22

CPC classification number: A61K9/127 ,  A61K47/6925 ,  A61K49/223

Abstract: Described are microbubble compositions including microbubbles having membranes that incorporate modified surface features that may be useful, for example, in facilitating binding to a target surface or substance. The surface features may include non-spherical attributes such as crenations, folds, projections, or wrinkles, which can increase the deformability of the microbubble membrane. Such microbubble compositions can be incorporated into targeted ultrasound contrast agents and methodologies. Methods for preparing modified microbubble compositions include providing microbubbles having spherical membranes, and converting the spherical membranes to non-spherical membranes having surface features as mentioned above. Targeting substances can be incorporated into the membranes before or after their conversion from spherical to non-spherical forms.

Abstract translation: 描述的是微泡组合物，其包括具有结合改性表面特征的膜的微泡，其可用于例如有助于结合靶表面或物质。 表面特征可以包括非球形属性，例如褶皱，褶皱，突起或皱纹，这可以增加微泡膜的变形性。 这种微泡组合物可以掺入靶向超声造影剂和方法中。 制备改性微泡组合物的方法包括提供具有球形膜的微泡，并将球形膜转化为具有上述表面特征的非球形膜。 靶向物质可以在从球形转换成非球形形式之前或之后并入膜中。

公开(公告)号：US20050249695A1

公开(公告)日：2005-11-10

申请号：US11107412

申请日：2005-04-14

Applicant: Joerg Tiller ,  Chun-Jen Liao ,  Kim Lewis ,  Alexander Klibanov

Inventor： Joerg Tiller ,  Chun-Jen Liao ,  Kim Lewis ,  Alexander Klibanov

IPC: A01N43/40 ,  A61L27/34 ,  A61L27/50 ,  A61K31/785

CPC classification number: A61L27/50 ,  A01N43/40 ,  A61L27/34 ,  A01N25/34 ,  A01N25/10 ,  A01N2300/00 ,  C08L33/14

Abstract: Bactericidal compositions are disclosed that comprise a polymeric compound immobilized on a material. Medical devices are also disclosed which comprise such a bactericidal composition. Methods are disclosed for covalently derivatizing the surfaces of common materials with an antibacterial polycation, e.g., poly(vinyl-N-pyridinium bromide); the first step of the methods involves coating the surface with a nanolayer of silica. Various commercial synthetic polymers derivatized in this manner are bactericidal, i.e., they kill on contact up to 99% of deposited Gram-positive and Gram-negative bacteria, whether deposited through air or water.

Abstract translation: 公开了包含固定在材料上的聚合物的杀菌组合物。 还公开了包含这种杀菌组合物的医疗装置。 公开了用抗菌聚阳离子共价衍生普通材料的表面的方法，例如聚（乙烯基-N-吡啶鎓溴化物）; 该方法的第一步包括用纳米二氧化硅涂覆表面。 以这种方式衍生的各种商业合成聚合物是杀菌剂的，即它们在接触高达99％的沉积的革兰氏阳性和革兰氏阴性细菌时杀死，无论是通过空气还是水沉积。

公开(公告)号：US5618539A

公开(公告)日：1997-04-08

申请号：US314571

申请日：1994-09-29

Applicant: Brent Dorval ,  Marie Chow ,  Alexander Klibanov

Inventor： Brent Dorval ,  Marie Chow ,  Alexander Klibanov

IPC: A61K31/195 ,  A61K9/08 ,  A61K31/785 ,  A61K39/00 ,  A61K39/12 ,  A61K39/13 ,  A61K47/16 ,  A61K47/18

CPC classification number: A61K39/13 ,  A61K39/12 ,  C12N2770/32634

Abstract: Non-lyophilized vaccine compositions which contain a poliovirus and, as stabilizer, a compound containing at least two amino or imine groups. The stabilizers include polyimines such as the amino acid lysine or ethylenediamine and polyimines such as poly(ethylenimine).

Abstract translation: 含有脊髓灰质炎病毒和作为稳定剂的含有至少两个氨基或亚胺基团的化合物的非冻干疫苗组合物。 稳定剂包括聚亚胺如氨基酸赖氨酸或乙二胺和聚亚胺如聚（亚乙基亚胺）。