Sodium salt compound of Iguratimod, preparation method thereof and pharmaceutical use thereof

Abstract

The invention relates to a sodium salt compound of Iguratimod and a hydrate or solvate thereof. The slat of the Iguratimod is far advantageous over the Iguratimod in water solubility, powder flowability and power stability. The compounds can be used in the preparation of medicaments for treating diseases such as rheumatoid arthritis, chronic infectious arthritis, osteoarthritis and ankylosing spondylitis and relieving pains caused by muscle or soft tissue damages and arthralgia. The invention also provides a preparation method of the sodium salt compound and the hydrate or solvate thereof, the use (medicinal compositions and medicinal composition preparation and use) of the compounds in medicaments, and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a derivative compound of iguratimod, a preparation method thereof and its application in medicine. Background technique [0002] Iguratimod (Iguratimod, T-614), the chemical name is N-[3-(formamido)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]- Methanesulfonamide, English name: N-[3-(formylamino)-4-oxo-6-phenoxy-4H-1-benzopyran-7-yl]-methanesulfonamide, the molecular structure is as follows: [0003] Molecular formula C 17 h 14 N 2 o 6 S, molecular weight 374.4. [0004] Iguratimod is a new non-steroidal anti-inflammatory drug that selectively inhibits cyclooxygenase-2. It has antipyretic, analgesic, anti-arthritis, and immunomodulatory effects. It is useful for the treatment of rheumatoid arthritis, rheumatoid Arthritis, osteoarthritis and ankylosing spondylitis have excellent curative effect, and can also relieve pain and joint pain caused by muscle and soft tissue damage. It c...

AI Technical Summary

Problems solved by technology

[0006] As a new type of high-efficiency non-steroidal anti-inflammatory drug, iguratimod also has deficiencies in drug preparation: one is that iguratimod is insoluble in water, and when administered orally, because of the poor insolubility of the drug in water, it contains In the common preparation composition of iguratimod, its active ingredient is not easy to wet and diffuse in water, and the oral dosage form prepared with conventional preparation auxiliary materials and dispersion system is easy to crystallize or precipitate out in gastrointestinal fluid and cannot be dissolved, which greatly Affecting the stripping and absorption utilization of medicines, there are unfavorable factors; the second is that the iguratimod compound is light in weight and prone to electrostatic interaction, which causes the iguratimod compound (crude drug) to gather into cotton wool, lacks brittleness, and is difficult to pulverize. The fluidity is very poor, and it is difficult to mix evenly with pharmaceutical excipients in the preparation of preparations, which brings great difficulties to the preparation of iguratimod preparations and the improvement of quality, and is not conducive to the needs of large-scale industrial production; the third is iguratimod Poor stability and degradation will occur, which will bring hidden dangers to the storage and quality safety of pharmaceutical preparations

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