(2Z,4S,4aS,5aR,12aS)-2-[amino(hydroxy)methylidene]-4,7-bis(dimethylamino)-10,11,12a-trihydroxy-4a,5,5a,6-tetrahydro-4H-tetracene-1,3,12-trione;hydron;chloride

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 四环素类
• 英文名称: (2Z,4S,4aS,5aR,12aS)-2-[amino(hydroxy)methylidene]-4,7-bis(dimethylamino)-10,11,12a-trihydroxy-4a,5,5a,6-tetrahydro-4H-tetracene-1,3,12-trione;hydron;chloride
• 化学式: C23H28ClN3O7
• 分子量: 493.9
• InChiKey: KDLQIOPKJDNQIM-WUURTAMISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.45
• 重原子数：
  34
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  165
• 氢给体数：
  6
• 氢受体数：
  10

文献信息

• DOSAGE FORM COMPRISING AN ACTIVE INGREDIENT AND A PLURALITY OF SOLID POROUS MICROCARRIERS
  申请人：BioPharmX, Inc.

  公开号：US20150209296A1

  公开（公告）日：2015-07-30

  The present application provides a dosage form and related methods for making the dosage form. The dosage form generally comprises a hydrophilic active ingredient, a plurality of solid, porous microcarriers, each having a hydrophobic surface, an optional hydrophobic encapsulant, and a hydrophilic delivery agent, wherein (i) the hydrophilic active ingredient is associated with the plurality of solid, porous microcarriers, (ii) the plurality of solid, porous microcarriers is encapsulated by the hydrophobic encapsulant, and (iii) the hydrophilic delivery agent is physically separated from a majority of the hydrophilic active ingredient by a boundary between the hydrophilic delivery agent and the hydrophobic encapsulant. In some embodiments, the dosage form is for topical application. In some additional embodiments, the plurality of solid, porous microcarriers is formed by modifying the microcarriers to increase their hydrophobicity.

  本申请提供了一种剂型及相关制备方法。该剂型通常包括一种亲水性活性成分、多个固体、多孔微载体，每个载体具有疏水表面，可选的疏水封装剂以及一种亲水性传递剂。其中，(i) 亲水性活性成分与多个固体、多孔微载体相关联，(ii) 多个固体、多孔微载体被疏水封装剂封装，(iii) 亲水性传递剂与疏水封装剂之间通过边界物理隔离了大部分亲水性活性成分。在某些实施例中，该剂型用于局部应用。在某些额外实施例中，通过改变微载体以增加其疏水性，形成多个固体、多孔微载体。
• Topical minocycline compositions and methods of using the same
  申请人：Laboratory Skin Care, Inc.

  公开号：US10080764B2

  公开（公告）日：2018-09-25

  Topical minocycline compositions with reduced fluorescence are provided. In some instances, the compositions include an amount of a minocycline active agent associated with porous calcium particles. Also provided are methods of using the compositions, e.g., in the treatment of acne.

  提供了荧光减弱的局部米诺环素组合物。在某些情况下，组合物包括一定量的与多孔钙颗粒相关的米诺环素活性剂。还提供了使用这些组合物的方法，例如用于治疗痤疮。
• Dosage form comprising an active ingredient and a plurality of solid porous microcarriers
  申请人：BioPharmX, Inc.

  公开号：US10159686B2

  公开（公告）日：2018-12-25

  The present application provides a dosage form and related methods for making the dosage form. The dosage form generally comprises a hydrophilic active ingredient, a plurality of solid, porous microcarriers, each having a hydrophobic surface, an optional hydrophobic encapsulant, and a hydrophilic delivery agent, wherein (i) the hydrophilic active ingredient is associated with the plurality of solid, porous microcarriers, (ii) the plurality of solid, porous microcarriers is encapsulated by the hydrophobic encapsulant, and (iii) the hydrophilic delivery agent is physically separated from a majority of the hydrophilic active ingredient by a boundary between the hydrophilic delivery agent and the hydrophobic encapsulant. In some embodiments, the dosage form is for topical application. In some additional embodiments, the plurality of solid, porous microcarriers is formed by modifying the microcarriers to increase their hydrophobicity.

  本申请提供了一种剂型和制造该剂型的相关方法。该剂型一般包括亲水性活性成分、多个固体多孔微载体（每个都具有疏水表面）、任选的疏水性封装剂和亲水性递送剂，其中(i) 亲水性活性成分与多个固体多孔微载体相关联，(ii) 多个固体多孔微载体被疏水性封装剂封装、多孔固体微载体相关联，(ii) 多孔固体微载体被疏水性封装剂封装，(iii) 亲水递送剂通过亲水递送剂和疏水性封装剂之间的边界与大部分亲水活性成分物理隔离。在某些实施方案中，该剂型用于局部应用。在另外一些实施方案中，多个固态多孔微载体是通过改性微载体以增加其疏水性而形成的。
• Pharmaceutical tetracycline composition for dermatological use
  申请人：BioPharmX, Inc.

  公开号：US10391108B2

  公开（公告）日：2019-08-27

  Provided herein is a topical composition and related methods for making and using the composition. In a first aspect, the topical composition comprises minocycline, a magnesium salt, and a sulfite compound in a non-aqueous solvent. In yet another aspect, the topical composition comprises a tetracycline-class drug, a source of magnesium, a monohydric aliphatic alcohol, and a polyol, wherein (i) the ratio between the monohydric aliphatic alcohol and the propylene glycol is in the range of 1:1 to 99:1 by weight and (ii) the tetracycline-class drug is dissolved in the topical composition.

  本文提供了一种外用组合物以及制造和使用该组合物的相关方法。 在第一方面，外用组合物包括米诺环素、镁盐和非水溶剂中的亚硫酸盐化合物。 在另一个方面，外用组合物包括四环素类药物、镁源、一元脂肪醇和多元醇，其中(i)一元脂肪醇和丙二醇的重量比在 1:1 到 99:1 之间，(ii)四环素类药物溶解在外用组合物中。
• Antimicrobial compositions comprising minocycline and oxidized cellulose
  申请人：Omrix Biopharmaceuticals Ltd.

  公开号：US11000635B2

  公开（公告）日：2021-05-11

  Disclosed are compositions comprised of Oxidized Cellulose (OC), such as oxidized regenerated cellulose (ORC), and an antibiotic comprised of minocycline, methods of preparation thereof and uses thereof.

  公开了由氧化纤维素（OC）（如氧化再生纤维素（ORC））和米诺环素组成的抗生素组合物、其制备方法及其用途。