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2-(3-cyano-4-isobutyloxyphenyl)-4-methylthiazole-5-carboxylic acid Solid Dispersion

IP.com Disclosure Number: IPCOM000201762D
Publication Date: 2010-Nov-22
Document File: 2 page(s) / 66K

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2-(3-cyano-4-isobutyloxyphenyl)-4-methylthiazole-5-carboxylic acid Solid
Dispersion

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).

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Examples:

PXRD

ARL X-ray powder diffractometer model X`TRA-019, Peltier detector, round standard sample holder with round zero background plate was used. The cathode

CPS

02.0 6.0 10.0 14.0 18.0 22.0 26.0 30.0 34.0 38.0

2

-

Theta

S

cale



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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...