Sulfasalazine salt compositions and methods of using same

By preparing crystalline salt form of sulfasalazine and using ABCG2 inhibitors, the problems of degradation and insufficient solubility of sulfasalazine in pharmaceutical formulations were solved, resulting in higher bioavailability and stability, and reduced risk of side effects.

CN111971272AInactive Publication Date: 2020-11-20库布拉阿布伊扎 +3
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Patent Information

Application Number
CN201880076116.X
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2017-10-10
Filing Date
2018-10-09
Publication Date
2020-11-20
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Sulfasalazine is easily degraded in pharmaceutical formulations, leading to the formation of impurities. Furthermore, its conventional form has insufficient solubility and stability, affecting bioavailability and the risk of side effects.

Method used

To develop the crystalline salt form of sulfasalazine, thereby improving its water solubility and storage stability by reacting with organic acids or organic amines to form stable crystalline salts, and to enhance bioavailability by combining it with ABCG2 inhibitors.

Benefits of technology

It enhances the water solubility and stability of sulfasalazine, reduces the risk of side effects, and improves the bioavailability and therapeutic effect of the drug in vivo.

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Abstract

Sulfasalazine salt compositions are provided. In some cases, the sulfasalazine salts have a crystalline form. The subject crystalline sulfasalazine salts can provide a water soluble form of the activecompound that finds use in pharmaceutical compositions and therapeutic applications. The subject crystalline sulfasalazine salts can provide increased solubility as compared to the zwitterionic or free acid form of sulfasalazine. Also provided are pharmaceutical compositions including the subject sulfasalazine salt compositions. Methods of treating a neurological related disease such as refractory epilepsy using the subject crystalline sulfasalazine salts and pharmaceutical compositions are also provided.
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