Paclitaxel dihydrate | 197778-55-5

• 英文名称: Paclitaxel dihydrate
• 英文别名: [(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-diacetyloxy-15-[(2R,3S)-3-benzamido-2-hydroxy-3-phenylpropanoyl]oxy-1,9-dihydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate;dihydrate
• CAS: 197778-55-5
• 化学式: C47H55NO16
• 分子量: 889.9
• InChiKey: QCWYEQGCFLYALU-DEPJHIFXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.09
• 重原子数：
  64
• 可旋转键数：
  14
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  223
• 氢给体数：
  6
• 氢受体数：
  16

文献信息

• Taxane coatings for implantable medical devices
  申请人：Reyes Priscilla

  公开号：US20070212394A1

  公开（公告）日：2007-09-13

  This disclosure relates to implantable medical devices coated with a taxane therapeutic agent, such as paclitaxel, in one or more solid form(s) having varying dissolution rates. Particularly preferred coatings comprise amorphous and/or solvated solid forms of taxane therapeutic agents that provide durable coatings that release the taxane over a desired period of time, which can be varied in the absence of a polymer by selecting the type and amount of solid forms of the taxane therapeutic agent in the coating. Other preferred embodiments relate to methods of coating medical devices and methods of treatment. The coatings can provide a sustained release of the taxane therapeutic agent within a body vessel without containing a polymer to achieve the desired rate of paclitaxel elution.

  本公开涉及涂有紫杉醇治疗剂（如紫杉醇）的植入式医疗器械，其具有不同溶解速率的一个或多个固态形式的涂层。特别优选的涂层包括无定形和/或溶剂化的紫杉醇治疗剂的固态形式，其提供持久的涂层，可以在不含聚合物的情况下通过选择涂层中的治疗剂的固态形式的类型和数量来改变所需的释放时间。其他优选实施例涉及涂覆医疗器械的方法和治疗方法。这些涂层可以在不含聚合物的情况下提供紫杉醇治疗剂的持续释放，以达到所需的紫杉醇溶出速率。
• Stents with connectors and stabilizing biodegradable elements
  申请人：Med Institute, Inc.

  公开号：EP2374433A1

  公开（公告）日：2011-10-12

  Various stent structures are provided with improved axial and torsional flexibility. One type of stent structure includes multiple segmented stent structures connected to each other by biodegradable interconnectors. A delivery system adapted to delivery the multiple segmented stents is also described. Another type of stent structure includes biodegradable connectors that are incorporated into a framework of non-biodegradable interconnecting members that form the support structure of the stent. The biodegradable connectors in both stent structures degrade or are absorbed after the stent is deployed. Stabilizing elements may be provided to the stent structures to supplement the stiffness of the stent with stability during loading and deployment.

  各种支架结构具有更好的轴向和扭转柔韧性。其中一种支架结构包括通过生物可降解互连器相互连接的多个分段支架结构。此外，还介绍了一种适用于输送多个分段支架的输送系统。另一种支架结构包括可生物降解连接器，这些连接器与构成支架支撑结构的不可生物降解互连构件框架结合在一起。这两种支架结构中的可生物降解连接器在支架展开后都会降解或被吸收。支架结构中可加入稳定元件，以补充支架的刚度，并在加载和展开过程中保持稳定。
• Methods of manufacturing and modifying taxane coatings for implantable medical devices
  申请人：Cook Incorporated

  公开号：EP2380606A1

  公开（公告）日：2011-10-26

  This disclosure relates to endolumenal medical devices coated with a taxane therapeutic agent in one or more solid form(s) having varying dissolution rates. Particularly preferred coatings comprise amorphous paclitaxel, dihydrate paclitaxel, or combinations thereof that provide durable coatings that release paclitaxel over a desired period of time, which can be on the order of hours, days or weeks. Preferred embodiments relate to medical device coatings of paclitaxel, or paclitaxel analogs or derivatives, having one or more polymorph solid forms that provide a prolonged release of paclitaxel within a body vessel without requiring a polymer carrier or barrier layer to achieve the desired rate of paclitaxel elution.

  本公开涉及涂有具有不同溶解速率的一种或多种固体形式的紫杉类治疗剂的腔内医疗器械。特别优选的涂层包括无定形紫杉醇、二水合紫杉醇或其组合，可提供持久的涂层，在所需的时间内释放紫杉醇，释放时间可为数小时、数天或数周。优选的实施方案涉及紫杉醇或紫杉醇类似物或衍生物的医疗器械涂层，其具有一种或多种多晶体固态形式，可在体内容器中长时间释放紫杉醇，而无需聚合物载体或阻隔层来达到所需的紫杉醇洗脱率。
• ENCAPSULATED DRUG COMPOSITIONS AND METHODS OF USE THEREOF
  申请人：Cook Medical Technologies LLC

  公开号：EP2982389A1

  公开（公告）日：2016-02-10

  Various aspects of the present disclosure provide compositions, coatings and implantable devices including a drug and an excipient. In certain embodiments the excipient and the drug are present at a weight ratio of between 10 to 1 and 1 to 10 drug to excipient. In certain other embodiments, the excipient and the drug form particles in which the drug is encapsulated by the excipient. Other aspects of the disclosure provide methods of manufacturing and using such compositions, coatings and implantable devices.

  本公开的各个方面提供了包括药物和赋形剂的组合物、涂层和植入式装置。在某些实施方案中，赋形剂和药物的重量比介于 10 比 1 和 1 比 10 之间。在某些其他实施方案中，赋形剂和药物形成颗粒，其中药物被赋形剂包裹。本公开的其它方面提供了制造和使用此类组合物、包衣和植入装置的方法。
• OPTICAL TECHNIQUE FOR COATING CHARACTERIZATION
  申请人：Cook Medical Technologies LLC

  公开号：EP3272372A1

  公开（公告）日：2018-01-24

  The present invention generally relates to methods for determining the presence and distribution of a polarization active material present in a coating. In one embodiment, the coating is present on an implantable device, for example an implantable stent.

  本发明一般涉及确定涂层中存在的极化活性材料及其分布的方法。在一个实施方案中，涂层存在于植入式设备上，例如植入式支架。