布洛芬钾 | 79261-49-7

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 苯丙酸
• 中文名称: 布洛芬钾
• 中文别名: IBUPROFEN钾
• CAS: 79261-49-7
• 化学式: C13H18KO2
• 分子量: 245.38
• InChiKey: LHRBNROBNBJSAF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.69
• 重原子数：
  16
• 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：
  37.3
• 氢给体数：
  1
• 氢受体数：
  2

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。
• Highly concentrated pourable aqueous solutions of potassium ibuprofen, their preparation and their uses
  申请人：Hu C. Patrick

  公开号：US20050137262A1

  公开（公告）日：2005-06-23

  Concentrated pourable potassium ibuprofen liquid compositions and their preparation are described. They are comprised of (i) potassium ibuprofen, (ii) water; and (iii) methanol, ethanol, 1-propanol, 2-propanol, 1,1-dimethylethanol, or a mixture of any two or more of them. The amount of dissolved potassium ibuprofen in the composition is in the range of about 60 to about 90 wt %. These compositions are suitable for use in the preparation of pharmaceutical dosage forms such as liquid-filled soft gelatin capsules, syrups, elixirs, suspensions; solid dosage forms such as tablets or caplets; and topically-applied products such as lotions, creams or ointments.

  本文介绍了浓缩可倾注式布洛芬钾液体组合物及其制备方法。它们由(i)布洛芬钾，(ii)水，和(iii)甲醇、乙醇、1-丙醇、2-丙醇、1,1-二甲基乙醇或任意两种或两种以上的混合物组成。组合物中溶解的布洛芬钾的含量在约60到约90重量%之间。这些组合物适用于制备药物剂型，如液体软胶囊、糖浆、口服溶液、悬浮液；固体剂型，如片剂或胶囊；以及局部应用产品，如乳液、霜或药膏。
• Forms of pharmaceutically active agents and method for manufacture thereof
  申请人：——

  公开号：US20030055107A1

  公开（公告）日：2003-03-20

  A pharmaceutical composition comprising a pharmaceutically active agent and a salt of said pharmaceutically active agent with the proviso that said composition does not contain hydrolyzed cellulose, wherein said pharmaceutical active agent is a weak acid or weak base. The present invention is also directed to a new ibuprofen form having, when potassium is present in said form as a counter ion, an IR peak at 1706 cm −1 shifted and broadened in absorbance relative to racemic ibuprofen free acid, the form's characteristic absorbance profile from 1000 to 650 cm −1 and broadened in absorbance relative to racemic ibuprofen free acid, the form's characteristic absorbance profile from 1000 to 650 cm −1 and D-spacings of 21.1, 7.1, and 3.4 Å by X-ray diffraction.

  一种制药组合物，包括一种药物活性剂和该药物活性剂的盐，但该组合物不含水解纤维素，其中所述药物活性剂是弱酸或弱碱。本发明还涉及一种新的布洛芬形式，当钾存在于该形式中作为对离子时，其在1706 cm-1处的IR峰相对于外消旋布洛芬自由酸发生了位移和增宽，该形式的特征吸收谱从1000到650 cm-1处发生了增宽，并且其D间距分别为21.1、7.1和3.4Å，通过X射线衍射确定。
• [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。