abstract |
The invention relates to a method of improving the stability of clopidogrel in a composition comprising clopidogrel, the method comprising adding a sulfoalkyl ether cyclodextrin (SAE-CD) of Formula 1:wherein: n is 4, 5, or 6; R<sub>1</sub>, R<sub>2</sub>, R<sub>3</sub>, R<sub>4</sub>, R<sub>5</sub>, R<sub>6</sub>, R<sub>7</sub>, R<sub>8</sub>, and R<sub>9</sub> are each, independently, -O- or a -O-(C<sub>2</sub>-C<sub>6</sub> alkylene)-SO<sub>3</sub><sup>-</sup> group, wherein at least one of R<sub>1</sub> to R<sub>9</sub> is independently a -O-(C<sub>2</sub>-C<sub>6</sub> alkylene)-SO<sub>3</sub><sup>-</sup> group; and S<sub>1</sub>, S<sub>2</sub>, S<sub>3</sub>, S<sub>4</sub>, S<sub>5</sub>, S<sub>6</sub>, S<sub>7</sub>, S<sub>8</sub>, and S<sub>9</sub> are each, independently, a pharmaceutically acceptable cation, to the composition,wherein the molar ratio of the SAE-CD to the clopidogrel is at least 6:1, when the pH of the formulation is 3.5 or greater. |