Benzeneacetic acid, alpha-methyl-4-(2-methylpropyl)-, sodium salt, hydrate (1:1:2) | 527688-20-6

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 苯丙酸
• 英文名称: Benzeneacetic acid, alpha-methyl-4-(2-methylpropyl)-, sodium salt, hydrate (1:1:2)
• CAS: 527688-20-6
• 化学式: C13H20NaO3
• 分子量: 247.29
• InChiKey: SAEVWWQLQNPPIO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.87
• 重原子数：
  17
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  38.3
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• Rapidly solubilizing ibuprofen granulate
  申请人：Losan Pharma GmbH

  公开号：EP1800667A1

  公开（公告）日：2007-06-27

  A process for producing a rapidly solubilizing ibuprofen granulate, the process comprising providing a mixture comprising solid ibuprofen and at least 0.8 mole per mole ibuprofen of one or more basic compounds, which basic compounds comprise from 0.5 to 1.2 mole per mole ibuprofen, but not more, of a base selected from the group consisting of sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium glycinate, potassium glycinate, tribasic sodium and potassium phosphates and mixtures of said bases, and reacting the ibuprofen and said one or more basic compounds in the presence of not more free water than the quantity exceeding the amount of water required for forming solid hydrates in said granulate by more than 1 mole per mole of ibuprofen. The obtainable granulate and the pharmaceutical compositions and dosage forms that may be produced therefrom are distinguished by their high solubility and rapid disintegration and dissolution in aqueous media, by their good flow properties and compressibility, by rapidly achieving onset of analgesic effect, etc.

  一种制备快速溶解布洛芬颗粒的方法，该方法包括提供一种混合物，该混合物包括固态布洛芬和至少0.8摩尔/摩尔布洛芬的一种或多种碱性化合物，其中所述碱性化合物包括每摩尔布洛芬0.5至1.2摩尔，但不超过该数量的一种选自羟氧化钠、羟氧化钾、碳酸钠、碳酸钾、甘氨酸钠、甘氨酸钾、三碱性磷酸钠和钾及其混合物的碱。在不超过所述颗粒中所需水分数量超过每摩尔布洛芬1摩尔的自由水存在下，将布洛芬和所述一种或多种碱性化合物在反应中。可获得的颗粒以及可以从中制备的药物组成物和剂型具有高溶解度和快速在水性介质中分解和溶解，具有良好的流动性和可压缩性，快速达到镇痛效果等特点。
• [EN] ARYL ALKYL CARBOXYLIC ACID SALTS, PROCESS FOR PREPARATION AND DOSAGE FORMS<br/>[FR] SELS D’ACIDE ARYLALKYLCARBOXYLIQUE, PROCÉDÉ POUR LEUR PRÉPARATION ET FORMES GALÉNIQUES
  申请人：SHASUN CHEMICALS AND DRUGS LTD

  公开号：WO2011001228A1

  公开（公告）日：2011-01-06

  The invention particularly discloses a process for preparing aryl alkyl carboxylic acid salts by preparing aqueous alkali solution, adding aryl alkyl carboxylic acid to said alkali solution at a temperature ranging from 4° to 121° C for obtaining a clear solution, preferably by heating and/or stirring and concentrating and cooling to obtain aryl alkyl carboxylic acid salt The invention therefore discloses solid oral dosage forms and compositions of aryl alkyl carboxylic acid salts which are free of organic solvent/so. The solid oral dose compositions of aryl alkyl carboxylic acid salts of the invention arc prepared in situ from aryl alkyl carboxylic acids and bases to obtain aryl acid alkyl carboxylic acid sails in crystalline/powder form with or without the use of pharmaceutical excipients.

  该发明特别公开了一种制备芳基烷基羧酸盐的过程，包括制备水溶性碱溶液，在4℃至121℃的温度范围内将芳基烷基羧酸添加到碱溶液中，通过加热和/或搅拌使其变为清澈的溶液，然后浓缩和冷却以获得芳基烷基羧酸盐。因此，该发明公开了不含有机溶剂/酸的芳基烷基羧酸盐的固体口服剂型和组合物。该发明的芳基烷基羧酸盐的固体口服剂型是通过原位制备芳基烷基羧酸和碱来获得晶体/粉末形式的芳酸烷基羧酸盐，可以使用药用辅料来制备。
• ARYL ALKYL CARBOXYLIC ACID SALTS, PROCESS FOR PREPARATION AND DOSAGE FORMS
  申请人：Chodankar Nandkumar

  公开号：US20110144207A1

  公开（公告）日：2011-06-16

  The invention particularly discloses a process for preparing aryl alkyl carboxylic acid salts by preparing aqueous alkali solution, adding aryl alkyl carboxylic acid to said alkali solution at a temperature ranging from 4° to 121° C. for obtaining a clear solution, preferably by heating and/or stirring and concentrating and cooling to obtain aryl alkyl carboxylic acid salt The invention therefore discloses solid oral dosage forms and compositions of aryl alkyl carboxylic acid salts which are free of organic solvent/so. The solid oral dose compositions of aryl alkyl carboxylic acid salts of the invention are prepared in situ from aryl alkyl carboxylic acids and bases to obtain aryl acid alkyl carboxylic acid sails in crystalline/powder form with or without the use of pharmaceutical excipients.

  本发明特别公开了一种制备芳基烷基羧酸盐的方法，包括制备水溶性碱性溶液，将芳基烷基羧酸加入该碱性溶液中，在4℃至121℃的温度范围内获得清晰的溶液，最好通过加热和/或搅拌、浓缩和冷却来获得芳基烷基羧酸盐。因此，本发明公开了不含有机溶剂/酮的芳基烷基羧酸盐的固体口服剂型和组合物。本发明的芳基烷基羧酸盐的固体口服剂型组合物通过从芳基烷基羧酸和碱基中原位制备获得，以获得晶体/粉末形式的芳酸烷基羧酸盐，可以使用药用辅料，也可以不使用。
• Solubilized ibuprofen
  申请人：Losan Pharma GmbH

  公开号：EP2559430A1

  公开（公告）日：2013-02-20

  A process for producing a solubilized ibuprofen, preferably in the form of a granulate, the process comprising the steps of: providing a mixture comprising solid ibuprofen and a first base selected from the group consisting of sodium carbonate and potassium carbonate and mixtures thereof, and reacting the ibuprofen and the first base in essentially dry state. The obtainable granulate and the pharmaceutical compositions and dosage forms that may be produced therefrom are distinguished by their high solubility and rapid disintegration and dissolution in aqueous media, by their good flow properties and compressibility, by rapidly achieving onset of analgesic effect.

  一种生产溶解布洛芬（最好是颗粒状）的工艺，该工艺包括以下步骤：提供由固体布洛芬和选自碳酸钠、碳酸钾及其混合物的第一碱组成的混合物，并使布洛芬和第一碱在基本干燥的状态下反应。由此获得的颗粒剂以及由此生产的药物组合物和剂型具有以下特点：在水介质中溶解度高、崩解和溶解速度快、流动性和可压缩性好、镇痛效果迅速显现。
• Method and apparatus for dry granulation
  申请人：ATACAMA LABS OY

  公开号：US10265272B2

  公开（公告）日：2019-04-23

  A dry-granulation method for producing a tablet comprising (a) pharmaceutical active ingredient in an amount 50-90% w/w and (b) one or more excipients in an amount 10-50% w/w including at least a binder which comprises (i) preparing granules from a powder comprising a binder, a pharmaceutically active ingredient and optionally one or more other excipients or pharmaceutical active ingredients by a process characterized in that a compaction force is applied to the powder to produce a compacted mass comprising a mixture of fine particles and granules and separating and removing fine particles and/or small granules from the granules by entraining the fine particles and/or small granules in a gas stream in which the compacted mass flows, wherein the direction of the flow of the gas stream has a component which is contrary to that of the direction of flow of the compacted mass, and collecting the accepted granules (ii) blending the accepted granules with other components of the tablet in granular or fine powder form wherein in step (ii) at least one other component of the tablet formulation is in granular form and is prepared from a powder comprising said other component by a process characterized in that a compaction force is applied to the powder to produce a compacted mass comprising a mixture of fine particles and granules and separating and removing fine particles and/or small granules from the granules by entraining the fine particles and/or small granules in a gas stream in which the compacted mass flows, wherein the direction of the flow of the gas stream has a component which is contrary to that of the direction of flow of the compacted mass; and (iii) compressing the resultant blend to form a tablet; with the proviso that the tablet does not comprise (a) paracetamol, maize starch and microcrystalline cellulose in a ratio of 60:20:20 w/w, (b) acebutolol HCl and starch in a ratio of 90:10 w/w, (c) sodium valproate, hypromellose and maize starch in a ratio of 90:5:5 w/w, (d) ketoprofen and maize starch in a ratio of 50:50 w/w or (e) metformin HCl, microcrystalline cellulose and maize starch in a ratio of 80:14:6 w/w.

  一种生产片剂的干制粒方法，该片剂包含(a)重量百分比为 50-90%的药物活性成分和(b)重量百分比为 10-50%的一种或多种赋形剂，其中至少包括一种粘合剂，该方法包括(i)用包含粘合剂的粉末制备颗粒、(i) 从粉末中制备颗粒，该粉末包括粘合剂、药用活性成分和一种或多种其它辅料或药用活性成分，制备工艺的特点是对粉末施加压实力以产生由细小颗粒和颗粒混合物组成的压实物，并通过将细小颗粒和/或小颗粒夹带在压实物流动的气流中，将细小颗粒和/或小颗粒从颗粒中分离和去除，其中气流的流动方向与压实物的流动方向相反、收集所接受的颗粒 (ii) 将所接受的颗粒与颗粒状或细粉末状的片剂的其他成分混合，其中在步骤(ii)中，片剂配方中的至少一种其他成分为颗粒状，由包含所述其他成分的粉末制备而成，其特征在于，对粉末施加压实力以产生包含细颗粒和颗粒混合物的压实物，并通过在压实物流动的气流中夹带细颗粒和/或小颗粒，从颗粒中分离和去除细颗粒和/或小颗粒、其中，气流的流动方向与压实物的流动方向相反；(iii) 压缩所得混合物以形成片剂；但片剂不包括 (a) 对乙酰氨基酚、玉米淀粉和微晶纤维素的重量比为 60：20:20 w/w，(b)盐酸醋丁洛尔和淀粉的比例为 90:10 w/w，(c)丙戊酸钠、 低聚异麦芽糖和玉米淀粉的比例为 90:5:5 w/w，(d)酮洛芬和玉米淀粉的比例为 50:50 w/w，或(e)盐酸二甲双胍、微晶纤维素和玉米淀粉的比例为 80:14:6 w/w。