5H-二苯并[b,f]氮杂卓-5-甲酰胺,水合物(1:2) | 85756-57-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 中文名称: 5H-二苯并[b,f]氮杂卓-5-甲酰胺,水合物(1:2)
• 英文名称: Carbamazepine dihydrate
• 英文别名: benzo[b][1]benzazepine-11-carboxamide;dihydrate
• CAS: 85756-57-6
• 化学式: C15H16N2O3
• 分子量: 272.3
• InChiKey: UPTJXAHTRRBMJE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.74
• 重原子数：
  20
• 可旋转键数：
  0
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  48.3
• 氢给体数：
  3
• 氢受体数：
  3

文献信息

• Reaction co-crystallization of molecular complexes or co-crystals
  申请人：Rodriguez-Hornedo Nair

  公开号：US20070099237A1

  公开（公告）日：2007-05-03

  Multi-component crystals (co-crystals) are prepared by combining co-crystal components in non-stoichiometric concentrations in solution. The solubility of the molecular complex in the solvent is reduced, increasing the probability that the molecular complex is the least soluble form in the system, upon which it precipitates. A crystalline product is produced without the need for grinding, solvent evaporation, or temperature variation.

  多组分晶体（协晶体）是通过在溶液中以非化学计量浓度结合协晶组分来制备的。溶剂中分子复合物的溶解度降低，增加了分子复合物是系统中最不溶性形式的概率，从而沉淀出来。产生了结晶产品，无需研磨、溶剂蒸发或温度变化。
• CELLULOSE DERIVATIVES FOR INHIBITING CRYSTALLIZATION OF POORLY WATER-SOLUBLE DRUGS
  申请人：Virginia Tech Intellectual Properties, Inc.

  公开号：US20150004237A1

  公开（公告）日：2015-01-01

  Provided are cellulose esters useful for inhibiting solution crystallization of drugs. Specific polymers include cellulose esters of formula I: wherein n of the ω-carboxyalkanoyl group, is 3, 4, 6, or 8 to provide a ω-carboxyalkanoyl group chosen from succinoyl, glutaroyl, adipoyl, sebacyl, and suberyl groups; and wherein R is chosen from: a hydrogen atom; and an alkanoyl group chosen from acetyl, propionyl, butyryl, valeroyl, hexanoyl, nonanoyl, decanoyl, lauroyl, palmitoyl, and stearoyl groups; wherein there is a total degree of substitution of the alkanoyl group and the ω-carboxyalkanoyl group of at least 2.0; and wherein the polymer comprises m repeating units where n=1 to 1,000,000, or 10 to 100,000, or 100 to 1,000, such as 1 to 6,000. Embodiments further include compositions comprising cellulose esters and poorly water-soluble drugs, which compositions exhibit greater solubility and stability in solution as compared to the drugs alone.

  提供了对于抑制药物溶液结晶有用的纤维素酯。具体的聚合物包括式I的纤维素酯：其中ω-羧基烷酰基团的n为3、4、6或8，以提供从琥珀酰基、戊二酰基、己二酰基、癸二酰基和壬二酰基羧基烷酰基中选择的ω-羧基烷酰基；R从氢原子和从乙酰基、丙酰基、丁酰基、戊酰基、己酰基、壬酰基、癸酰基、月桂酰基、棕榈酰基和硬脂酰基羧酸基中选择的脂肪酰基中选择；其中脂肪酰基和ω-羧基烷酰基的总取代度至少为2.0；聚合物包括m个重复单元，其中n为1至1,000,000、10至100,000或100至1,000，例如1至6,000。实施例还包括包含纤维素酯和难溶于水的药物的组合物，该组合物在溶液中与药物单独相比表现出更高的溶解度和稳定性。
• Therapeutic approaches for treating CMT and related disorders
  申请人：PHARNEXT

  公开号：US10322101B2

  公开（公告）日：2019-06-18

  Compositions and methods for the treatment of Charcot-Marie-Tooth disease and related disorders. Also provided are combination therapies for treating this disease by decreasing PMP22 expression in a subject.

  治疗夏科-玛丽-牙病及相关疾病的组合物和方法。此外，还提供了通过降低受试者体内 PMP22 表达来治疗该疾病的组合疗法。
• Oral osmotic controlled drug delivery system for a sparingly soluble drug
  申请人：——

  公开号：US20030008006A1

  公开（公告）日：2003-01-09

  The present invention is for an oral osmotic controlled drug delivery system for a sparingly soluble drug comprising: a. a core comprising (i) finely particulate anhydrous carbamazepine (ii) a polymeric swelling agent consisting of one or more swellable hydrophilic polymers selected such that the polymeric swelling agent exhibits controlled swelling and the wall does not rupture or burst, (iii) a crystal habit modifier in whose presence, upon contact with an aqueous medium, the anhydrous carbamazepine being transformed into cuboidal or rod-shaped crystals of the dihydrate of carbamazepine, or mixtures thereof, and (iv) water-soluble compounds for inducing osmosis, b. a wall made of acylated cellulose which is impermeable to the components of the core, but permeable to water, and c. a passageway through the wall for releasing the components present in the core to the surrounding environment.

  本发明用于稀溶性药物的口服渗透控制给药系统，包括 a.(i) 细颗粒的无水卡马西平 (ii) 聚合膨胀剂，由一种或多种可膨胀的亲水性聚合物组成，经选择， 聚合膨胀剂可控制膨胀，壁不会破裂或爆裂、(iii) 晶体习性改良剂，在它的存在下，无水卡马西平与水介质接触后会转变成卡马西平二 水合物的立方体或棒状晶体，或它们的混合物，以及 (iv) 用于诱导渗透的水溶性化合物、 b. 由酰化纤维素制成的壁，该壁不渗透核心成分，但可渗透水，以及 c. 穿过壁的通道，用于将芯中的成分释放到周围环境中。
• [DE] CARBAMAZEPIN-ARZNEIFORM MIT VERZÖGERTER WIRKSTOFFFREISETZUNG<br/>[EN] CARBAMAZEPINE MEDICAMENT WITH RETARDED ACTIVE SUBSTANCE RELEASE<br/>[FR] MEDICAMENT A LA CARBAMAZEPINE A LIBERATION RETARDEE DU PRINCIPE ACTIF
  申请人：ARZNEIMITTELWERK DRESDEN GMBH

  公开号：WO1996001112A1

  公开（公告）日：1996-01-18

  (DE) Die Erfindung betrifft eine oral applizierbare Carbamazepin-Arzneiform mit verzögerter Wirkstofffreisetzung. Hierbei wird eine weichmacherhaltige wäßrige Polymerdispersion auf die Carbamazepinkristalle aufgetragen ohne daß eine Dihydratbildung des Carbamazepins eintritt. Die wäßrig überzogenen Carbamazepinkristalle können mit geeigneten Hilfsstoffen gemischt, zu teilbaren Tabletten verarbeitet oder in Kapseln abgefüllt werden.(EN) An oral administration carbamazepine medicament with a retarded active substance release is disclosed. An aqueous plasticised polymer dispersion is applied on carbamazepine crystals without causing formation of carbamazepine dihydrate. The carbamazepine crystals with their aqueous coating may be mixed with appropriate auxiliary substances, shaped into divisible tablets or filled into capsules.(FR) L'invention concerne un médicament à la carbamazépine à administration orale et à libération retardée du principe actif. On applique une dispersion aqueuse de polymère plastifié sur les cristaux de carbamazépine sans qu'il y ait formation de dihydrate de carbamazépine. On peut mélanger les cristaux de carbamazépine enduits de dispersion aqueuse avec des substances auxiliaires appropriées, les transformer en comprimés sécables ou en remplir des capsules.

  这项发明涉及一种直接可应用的缓释Carcobamazepine医药制剂。其特点是通过直接将其(Integer)Die Erfindung betrifft eine oral applizierbare Carbamazepin-Arzneiform mit verzögerter Wirkstofffreisetzung. (((DE)))((EN))一种直接可应用的缓释Carcobamazepine医药制剂，其特点是：通过直接将其Carcobamazepine晶体表面."]Carcobamazepine晶体表面." 外部的“软化的水基聚合物分散系”进行覆盖，从而避免Carcobamazepine晶体在制备过程中形成结晶水。最终，“该水溶性覆盖层的Carcobamazepine晶体可以通过与适当辅助物质混合、制成易于溶解的片剂或填入胶囊。”