2-(3-cyano-4-isobutyloxyphenyl)-4-methylthiazole-5-carboxylic acid Solid Dispersion
Publication Date: 2010-Nov-22
The IP.com Prior Art Database
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2-(3-cyano-4-isobutyloxyphenyl)-4-methylthiazole-5-carboxylic acid Solid
2-(3-cyano-4-isobutyloxyphenyl)-4-methylthiazole-5-carboxylic acid (referred as "FBX") of the following formula:
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is an orally administered xanthine oxidase (XO) inhibitor, indicated for the chronic management of hyperuricemia in patients with gout.
A sample of solid dispersion of FBX in a combination with a pharmaceutically suitable excipient was prepared according to the process described below. The sample is characterized by XRPD substantially as depicted in figure 1.
Figure 1: a characteristic XRPD of a solid dispersion of FBX in a combination with hydropropyl cellulose (HPC).
ARL X-ray powder diffractometer model X`TRA-019, Peltier detector, round standard sample holder with round zero background plate was used. The cathode
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is CuKa radiation, λ = 1.5418 Å. Scanning parameters: Range: 2-40 deg. 2, continuous Scan, Rate: 3 deg/min. The accuracy of peak positions is defined as +/- 0.2 degrees due to experimental differences like instrumentations, and sample preparations.
Example 1: Preparation of a solid dispersion of FBX in a combination with hydropropyl cellulose (HPC).
To 250 ml flask, Acetone was added (100mL) .Hydropropyl cellulose (2.5 g) and 10 ml of water was added gradually until fully dissol...