羟丁卡因 | 490-98-2

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 羟丁卡因
• 英文名称: Hydroxytetracain
• 英文别名: Hydroxytetracaine；2-(dimethylamino)ethyl 4-(butylamino)-2-hydroxybenzoate
• CAS: 490-98-2
• 化学式: C₁₅H₂₄N₂O₃
• 分子量: 280.367
• InChiKey: DHCUQNSUUYMFGX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.9
• 重原子数：
  20
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  61.8
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  羟丁卡因 、 溴丙烷 在 氢氧化钾 、 异丙醇 作用下， 生成 4-butylamino-2-propoxy-benzoic acid-(2-dimethylamino-ethyl ester)
  参考文献：
  名称：

  Grimme; Schmitz, Chemische Berichte, 1954, vol. 87, p. 179,181

  摘要：

  DOI：
• 作为产物：
  描述：

  4-硝基水杨酸 在 吡啶 、 盐酸 、 palladium on activated charcoal 、 氯化亚砜 、 乙醇 、 sodium carbonate 、 溶剂黄146 、 sodium iodide 、 锌 、 苯 作用下， 生成 羟丁卡因
  参考文献：
  名称：

  Derivatives of 4-Amino-2-hydroxybenzoic Acid. I

  摘要：

  DOI：

  10.1021/ja01152a032

文献信息

• Nitric Oxide Releasing Prodrugs of Therapeutic Agents
  申请人：SATYAM Apparao

  公开号：US20110263526A1

  公开（公告）日：2011-10-27

  The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

  本发明涉及已知药物或治疗剂的一氧化氮释放前药，其在此处表示为式(I)的化合物，其中药物或治疗剂包含一个或多个功能基团，独立地选自羧酸、氨基、羟基和巯基。该发明还涉及制备一氧化氮释放前药（式(I)的化合物）的方法，含有它们的药物组合物以及使用这些前药的方法。
• Crosslinked hyaluronic acid compositions for tissue augmentation
  申请人：Sadozai K. Khalid

  公开号：US20050136122A1

  公开（公告）日：2005-06-23

  A hyaluronic acid (HA) composition includes crosslinked, water-insoluble, hydrated HA gel particles. The HA includes crosslinks represented by the following structural formula: HA—U—R 2 —U—HA The variables are defined herein. A method of augmenting tissue in a subject includes inserting a needle into a subject at a location in the subject that is in need of tissue augmentation, wherein the needle is coupled to a syringe loaded with the HA composition, and applying force to the syringe, to deliver the HA composition into the subject. A method of preparing the HA composition, includes forming water-insoluble, dehydrated crosslinked HA particles, separating the water-insoluble, dehydrated particles by average diameter, selecting a subset of particles by average diameter, and hydrating the subset of dehydrated particles with a physiologically compatible aqueous solution. Another method of preparing the crosslinked HA composition includes crosslinking a precursor of the crosslinked HA with a biscarbodiimide in the presence of a pH buffer and dehydrating the crosslinked HA. Also included is a method of augmenting tissue in a subject that is in need of tissue augmentation. A method of stabilizing crosslinked HA includes hydrating water-insoluble, dehydrated crosslinked HA with a physiologically compatible aqueous solution that includes a local anesthetic, wherein the value of storage modulus G′ for the stabilized composition is at least about 110% of the value of G′ for a non-stabilized composition,. Also included is the stabilized HA composition.

  一种透明质酸（HA）组合物包括交联的、不溶于水的、水合的HA凝胶颗粒。HA包括由以下结构式表示的交联：HA—U—R2—U—HA。变量在此定义。一种在受试者中增强组织的方法包括将针插入受试者体内需要组织增强的位置，其中针连接到装有HA组合物的注射器，并施加力量到注射器，将HA组合物注入受试者体内。一种制备HA组合物的方法包括形成不溶于水的、脱水的交联HA颗粒，通过平均直径分离不溶于水的、脱水的颗粒，通过平均直径选择颗粒的子集，并用生理兼容的水溶液使脱水的颗粒子集水化。另一种制备交联HA组合物的方法包括在pH缓冲剂存在下用双异氰酸酯交联交联HA的前体，并脱水交联HA。还包括一种在需要组织增强的受试者中增强组织的方法。一种稳定交联HA的方法包括用含有局部麻醉剂的生理兼容水溶液水化不溶于水的、脱水的交联HA，其中稳定组合物的存储模量G′的值至少为非稳定组合物G′值的约110%。还包括稳定的HA组合物。
• High molecular wegiht polymers, devices and method for making and using same
  申请人：East Anthony

  公开号：US20050048121A1

  公开（公告）日：2005-03-03

  Anhydride polymers that release active or activatable agent(s) have pre-selected properties such as molecular weight, flexibility, hardness, adhesiveness, and other valuable properties. The polymers are suitable for use in compositions, formulations, coatings, devices, and the like that benefit from the controlled release of an agent(s) over a period of time. The polymers are prepared by a process involving various alternative and sequential steps that allow the design a priori of products with specific characteristics. The polymers are suitable as delivery systems, either by themselves, as compositions, formulations or devices.

  无水酐聚合物释放活性或可激活的药剂，具有预选特性，如分子量、柔韧性、硬度、粘附性等其他有价值的特性。这些聚合物适用于在一段时间内控制释放药剂的组合物、配方、涂层、设备等，这些产品受益于药剂的控制释放。这些聚合物是通过涉及各种替代和连续步骤的过程制备的，这些步骤允许事先设计具有特定特性的产品。这些聚合物适合作为传递系统，可以单独使用，也可以作为组合物、配方或设备。
• Technology for the Preparation of Microparticles
  申请人：Malakhov Michael

  公开号：US20090098207A1

  公开（公告）日：2009-04-16

  Microspheres are produced by contacting a solution of a macromolecule or small molecule in a solvent with an antisolvent and a counterion, and chilling the solution. The microspheres are useful for preparing pharmaceuticals, nutraceuticals, cosmetic products and the like of defined dimensions.

  微球是通过将溶液中的大分子或小分子与抗溶剂和对离子接触，并冷却溶液而制备的。这些微球可用于制备具有明确定义尺寸的药物、营养保健品、化妆品等产品。
• Pharmaceutical preparation comprising an active dispersed on a matrix
  申请人：——

  公开号：US20040058896A1

  公开（公告）日：2004-03-25

  The present invention relates to the field of pharmaceutical technology and describes a novel advantageous preparation for an active ingredient. The novel preparation is suitable for producing a large number of pharmaceutical dosage forms. In the new preparation an active ingredient is present essentially uniformly dispersed in an excipient matrix composed of one or more excipients selected from the group of fatty alcohol, triglyceride, partial glyceride and fatty acid ester.

  本发明涉及制药技术领域，描述了一种新的有利的活性成分制备方法。这种新的制备方法适用于生产大量的药物剂型。在这种新的制备方法中，活性成分基本上均匀地分散在由脂肪醇、甘油三酯、部分甘油酯和脂肪酸酯等多种赋形剂中选择的一种或多种赋形剂组成的赋形剂基质中。