alpha-[1-[甲基(3-苯基-2-丙烯-1-基)氨基]乙基]-苯甲醇盐酸盐(1:1) | 25441-16-1

• 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: alpha-[1-[甲基(3-苯基-2-丙烯-1-基)氨基]乙基]-苯甲醇盐酸盐(1:1)
• 英文名称: 2-[Methyl(3-phenylprop-2-enyl)amino]-1-phenylpropan-1-ol;hydrochloride
• CAS: 25441-16-1
• 化学式: C19H24ClNO
• 分子量: 317.9
• InChiKey: RSBLYYMNHJDITE-UHFFFAOYSA-N

物化性质

• 熔点：
  175 °C

计算性质

• 辛醇/水分配系数(LogP)：
  4.18
• 重原子数：
  22
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  23.5
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• Dendrimers as molecular translocators
  申请人：Goodman Murray

  公开号：US20060216265A1

  公开（公告）日：2006-09-28

  Transport molecules include a dendrimer and a biologically active molecule. The dendrimer of such transport molecules includes at least one guanidine group, at least one protonated guanidine group, at least one protected guanidine group, at least one amidine group, at least one protonated amidine group, at least one protected amidine group, at least one ureido group, at least one protonated ureido group, at least one protected ureido group, at least one thioureido group, at least one protonated thioureido group, or at least one protected thioureido group. The biologically active molecule is bonded to the dendrimer. A method of increasing the bioavailability of a drug includes bonding the drug to a dendrimer of the invention.

  转运分子包括一种树枝状聚合物和一种生物活性分子。这些转运分子的树枝状聚合物包括至少一个胍基团、至少一个质子化的胍基团、至少一个保护的胍基团、至少一个酰胺基团、至少一个质子化的酰胺基团、至少一个保护的酰胺基团、至少一个脲基团、至少一个质子化的脲基团、至少一个保护的脲基团、至少一个硫脲基团、至少一个质子化的硫脲基团，或至少一个保护的硫脲基团。生物活性分子与树枝状聚合物结合。一种增加药物生物利用度的方法包括将药物与本发明的树枝状聚合物结合。
• [EN] NANOPARTICLE FORMULATIONS AND USES THEROF<br/>[FR] FORMULATIONS DE NANOPARTICULES ET LEURS UTILISATIONS
  申请人：ABRAXIS BIOSCIENCE LLC

  公开号：WO2010118365A1

  公开（公告）日：2010-10-14

  The present invention provides compositions comprising nanoparticles comprising: 1) a drug, such as a hydrophobic drug derivative; and 2) a carrier protein. Also provided are methods of treating diseases (such as cancer) using the compositions, as well as kits and unit dosages.

  本发明提供了包含纳米粒子的组合物，其中包括：1）药物，如疏水性药物衍生物；和2）载体蛋白。还提供了使用这些组合物治疗疾病（如癌症）的方法，以及套件和单元剂量。
• Porous drug matrices and methods of manufacture thereof
  申请人：Acusphere Inc.

  公开号：US20020142050A1

  公开（公告）日：2002-10-03

  Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. The pore forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.

  药物，特别是低水溶性药物，以多孔性矩阵形式提供，最好是微粒，这可以增强药物在水性介质中的溶解。药物矩阵最好是使用包括以下步骤的过程制备的：(i)将药物，最好是低水溶性药物，溶解在挥发性溶剂中形成药物溶液，(ii)将至少一种孔形成剂与药物溶液结合形成乳液、悬浮液或第二溶液和亲水或疏水的赋形剂，以稳定药物并抑制结晶，(iii)从乳液、悬浮液或第二溶液中除去挥发性溶剂和孔形成剂，以得到多孔性的药物矩阵。亲水或疏水的赋形剂可以被选择用于通过抑制晶体生长来稳定药物的晶体形式，或者用于通过防止结晶来稳定药物的非晶形式。孔形成剂可以是与药物溶剂不相溶的挥发性液体或挥发性固体化合物，最好是挥发性盐。在一个优选实施例中，喷雾干燥用于除去溶剂和孔形成剂。所得到的多孔性矩阵在给患者治疗后具有更快的溶解速率，与非多孔性药物矩阵形式相比。在一个优选实施例中，多孔性药物矩阵的微粒被重组与水性介质，并通过标准技术处理成口服片剂或胶囊剂进行口服给药。
• [EN] TOPICAL FORMULATIONS BASED ON IONIC SPECIES FOR SKIN TREATMENT<br/>[FR] FORMULATIONS TOPIQUES A BASE D'ESPÈCES IONIQUES POUR LE TRAITEMENT DE LA PEAU
  申请人：UNIV CALIFORNIA

  公开号：WO2018044920A1

  公开（公告）日：2018-03-08

  Compositions containing a complex that contains a cation with alkyl chains and a macromolecule anion, and methods of making and using are disclosed. The compositions are typically charge neutral and a liquid at room temperature and standard pressure. The macromolecule anions may be nucleic acids, peptides, proteins, and/or carbohydrates. The compositions have enhanced penetration across the skin barrier (stratum corneum) and into the skin cells, delivering the macromolecules to the skin cells. The compositions are topically applied to the skin and are particularly useful for treatment of skin conditions.

  本发明揭示了含有含有烷基链阳离子和大分子阴离子的复合物的组合物及其制备和使用方法。这些组合物通常是电中性的，且在常温和标准压力下呈液态。大分子阴离子可以是核酸、肽、蛋白质和/或碳水化合物。这些组合物可以增强穿透皮肤屏障（角质层）并进入皮肤细胞，将大分子输送到皮肤细胞中。这些组合物可局部应用于皮肤，尤其适用于治疗皮肤状况。
• Sustained release pharmaceutical formulation for inhalation
  申请人：——

  公开号：US20040105821A1

  公开（公告）日：2004-06-03

  Pharmaceutical formulations and methods are provided for the sustained delivery of a pharmaceutical agent to the lungs of a patient by inhalation. The formulation includes porous microparticles which comprise a pharmaceutical agent and a matrix material, wherein upon inhalation of the formulation a therapeutically or prophylactically effective amount of the pharmaceutical agent is released from the microparticles in the lungs for at least 2 hours. Preferably, a majority of the pharmaceutical agent is released from the microparticles by 24 hours following inhalation, for example where a majority of the pharmaceutical agent is released no earlier than about 2 hours and no later than about 24 hours following inhalation. Methods for delivering a pharmaceutical agent, such as a corticosteroid, to the lungs of a patient are also provided. For example, the method includes having the patient inhale a dry powder blend comprising the present microparticles and a pharmaceutically acceptable bulking agent.

  提供了一种药物制剂和方法，通过吸入将药物剂量持续释放到患者的肺部。该制剂包括多孔微粒，其中包括药物剂量和基质材料，吸入该制剂后，肺部至少释放出治疗或预防有效剂量的药物剂量，持续时间至少为2小时。最好，药物剂量的大部分在吸入后的24小时内从微粒中释放出来，例如，药物剂量的大部分在吸入后不早于约2小时，不晚于约24小时内释放。还提供了将药物剂量（例如皮质类固醇）传递到患者肺部的方法。例如，该方法包括让患者吸入包括当前微粒和药用可接受的增容剂的干粉混合物。