Ibuprofen-arginine and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical chemistry and discloses a preparation method of ibuprofen-arginine. The preparation method is characterized by comprising the following steps of: under the conditions of room temperature and stirring, simultaneously dissolving ibuprofen and arginine in an alcohol-water solution by using the difference between solubility of the components, then adding a right amount of alcohol to clear reaction liquid, salifying and crystallizing. The preparation method has the advantages of simple preparation technology, mild reaction conditions, low cost, high yield, controlled quality and suitability for industrial production.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to an ibuprofen arginine salt and a preparation method thereof. Background technique [0002] Ibuprofen is a phenylpropionic acid non-steroidal anti-inflammatory drug. It is clinically used to treat mild to moderate pain and inflammatory reactions, such as rheumatic and rheumatoid arthritis, acute gout, headache, soft tissue injury, etc. Its mechanism of action is: ①Inhibit cyclooxygenase, reduce the synthesis of prostaglandins, produce analgesic and anti-inflammatory effects; ②Produce antipyretic effect through the hypothalamic thermoregulation center. [0003] Ibuprofen is widely used clinically as an antipyretic and analgesic drug with definite curative effect, small adverse reactions and high safety. However, because ibuprofen is almost insoluble in water, the oral absorption is slow, which limits the development and clinical application of quick-acting preparatio...

AI Technical Summary

Problems solved by technology

Its disadvantages are: ①The solvent is high-concentration ethanol, so a large amount of ethanol needs to be used in production, and ethanol has the danger of inflammability and explosion under heating conditions, low safety in production, and increased production costs

② Two-phase dissolving and dropping process steps are cumbersome

However, the preparation method announced by the CN102617329A patent is to carry out a salt-forming reaction in water, and after the reaction is finished, it is dried by spraying, freezing or decompression drying, and the process is cumbersome, time-consuming, and costly.

In addition, the CN102180786A patent uses a classic salt-forming reaction preparation method to dissolve the two phases in ethanol and water respectively, add dropwise and mix the two phases under stirring to form ibuprofen arginine salt, and then use distillation to remove the solvent. When the solvent is recovered, it needs to be heated for a long time, which will affect the product quality