Novel pharmaceutical composition of 2-(2-fluoro-4-biphenyl)-propionic acid

Abstract

The invention provides a novel 2-(2-fluorine-4biphenyl)-propionic acid pharmaceutical composition. Flurbiprofen and basic amino acid arginine or lysine form a pharmaceutical composition solution. The composition can be administrated in an injection or oral administration manner and can also be further administrated in a freeze-drying manner. Compared with a flurbiprofen axetil injection, a flurbiprofen composition not only does not influence the antipyretic, anti-inflammation and analgestic effects of the flurbiprofen, but also has the advantages of simple technology, low cost, high quality, stable long shelf life and convenience in quality control, storage and transportation; moreover, compared with a conventional oral preparation, the flurbiprofen composition has the same low gastrointestinal tract adverse reaction as the flurbiprofen axetil injection.

Description

technical field [0001] The invention belongs to the field of medicine, and relates to lyophilized or solution form preparations of 2-(2-fluoro-4-biphenyl)-propionic acid, more specifically, the invention relates to basic amino acids arginine, lysine and 2 - Compositions of different ratios of (2-fluoro-4-biphenyl)-propionic acid, especially pharmaceutical compositions in the form of lyophilization or solution in which the molar ratio is less than or equal to 1, and a preparation method thereof. Background technique [0002] 2-(2-fluoro-4-biphenyl)-propionic acid is the chemical name of the famous non-steroidal anti-inflammatory analgesic flurbiprofen. NSAIDS), according to the latest statistics, the domestic consumption of flurbiprofen has ranked first among NSAIDS drugs. [0003] NSAIDS are a class of non-steroid hormone drugs that relieve pain, swelling, stiffness, and inflammation. NSAIDS are commonly used for painful conditions in a variety of conditions: including but...

AI Technical Summary

Problems solved by technology

[0014] However, flurbiprofen axetil also has obvious deficiencies. For example, the prodrug of flurbiprofen axetil has no activity and needs to be metabolized into active flurbiprofen to be effective. shortcoming; the synthesis difficulty of flurbiprofen axetil raw material is relatively large, especially flurbiprofen axetil is liquid, and production, quality control, storage and transportation are all inconvenient; Pushed up the cost of preparations, increased the burden on patients and society; in addition, the prescription and process of flurbiprofen axetil microsphere preparations are very complicated, which increases the difficulty of production and quality control; especially, although flurbiprofen axetil microspheres Because of the better targeting of spherical preparations, some adverse reactions will be reduced, but many special excipients need to be added in the process of preparing microspheres. For injections, it is very necessary to minimize the types and contents of excipients, because excipients also directly enter The human circulatory system can easily cause major adverse reactions throughout the body

Therefore, flurbiprofen axetil microsphere preparations still have a lot of room for improvement, at least it is necessary to provide more choices for many patients who cannot tolerate flurbiprofen axetil microsphere injections

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