Method for preparing ibuprofen arginine

Abstract

The invention discloses a preparation method of an arginine ibuprofen salt. The method is that ibuprofen is adopted to dissolve into ethanol with 95 percent concentration and added with solid arginine while stirring, and then heated to 40 to 80 DEG C, stirred for 15 to 60 minutes, after reaction, cooled to room temperature and crystallized. The preparation method of the invention adopts that the solid arginine is directly added to the ibuprofen solution and no solvent is added before the solid arginine addition, thus shortening production technique steps and reducing reaction equipment. The process that directly crystallization from mother liquid in room temperature, need not be added with other solvent to dilute, thus reducing consumption of solvent and kinds, shortening production technique flow; as the solvent can be recycled and reused, thus reducing production cost and saving energy.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical synthesis chemistry, and relates to a preparation method for increasing water-soluble derivatives of an antipyretic and analgesic drug ibuprofen, more specifically a new preparation method for an antipyretic and analgesic drug arginine ibuprofen salt. Background technique [0002] Ibuprofen is a commonly used non-steroidal anti-inflammatory and analgesic drug in clinical practice. Its analgesic effect is significant, and its tolerance is stronger than that of aspirin. It has become the mainstay product of antipyretic and analgesic drugs in many countries. But because of its low water solubility, the development and application of its quick-acting water-soluble preparations have been limited. Therefore, a large amount of alcohol or a reducing substance that is several times that of ibuprofen are all added to the syrup formulations reported in the existing literature. to increase its water ...

AI Technical Summary

Problems solved by technology

Its disadvantages are: (1) two reaction tanks are required to dissolve ibuprofen and arginine respectively and because arginine is insoluble in 95% ethanol, it is not easy to make a uniform suspension, and strong stirring equipment is required, otherwise solid precipitation will occur phenomenon at the bottom of the tank, which greatly increases the requirements and costs of reaction equipment

(2) If arginine is dissolved with water-containing alcohol, it will be difficult to crystallize or incomplete crystallization at room temperature

(3) In the disclosed embodiment of CN1246306C, because of the use of hydrous ethanol to dissolve, it is difficult to precipitate crystals when placed at room temperature, and it must be placed overnight in a refrigerator at -4 ° C, which is time-consuming, laborious, and energy-consuming

Its disadvantage is that it increases the amount and types of solvents. Since the final crystallization is from the mixed solvent, it is difficult to recycle the solvent, thus increasing the industrial cost.

In addition, this method also requires 12 hours of crystallization in the refrigerator, which also has the problems of time-consuming and energy-consuming. In quality control, the residues of two solvents need to be determined, which increases the difficulty of quality control.

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