Pharmaceutical formulations comprising high purity cangrelor and methods for preparing and using the same
AssigneeChiesi Farmaceutici S.p.A.
InventorsPanna DUTTA, Adel RAFAI FAR, Min DING, Rajeshwar MOTHERAM
Life of this patent
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Abstract
The present invention relates to high purity cangrelor, pharmaceutical formulations comprising high purity cangrelor as an active ingredient, methods for preparing such compounds and formulations, and methods for using the pharmaceutical formulations in the inhibition of platelet activation and aggregation.
Claims30
A pharmaceutical formulation comprising high purity cangrelor, or a salt thereof, as an active ingredient and one or more pharmaceutically acceptable excipients prepared by a method comprising:
- (a) dissolving cangrelor or a salt thereof in a solvent to form a first solution;
- (b) mixing a pH-adjusting agent with the first solution to form a second solution, wherein the pH of the second solution is between about 7.0 and 9.5;
- and
- (c) removing the solvent from the second solution to produce high purity cangrelor or a salt thereof under conditions wherein a level of moisture of less than about 2.0% by weight is achieved,
- wherein one or more pharmaceutically acceptable excipients is added to the first solution, or to the second solution, or to both,
- wherein the high purity cangrelor or salt thereof has a combined total of selected hydrolysis and oxidation degradants of cangrelor not exceeding about 1.5% by weight of the high purity cangrelor, and
- wherein the selected hydrolysis and oxidation degradants are one or more members selected from the group consisting of impurity A, impurity B, impurity C, impurity D and impurity E.
A pharmaceutical formulation consisting of high purity cangrelor, or a salt thereof, as an active ingredient and mannitol and/or sorbitol as a pharmaceutically acceptable excipient, prepared by a method comprising:
- (a) dissolving cangrelor or a salt thereof in a solvent to form a first solution;
- (b) mixing a pH-adjusting agent with the first solution to form a second solution, wherein the pH of the second solution is between about 7.0 and 9.5;
- and
- (c) removing the solvent from the second solution to produce high purity cangrelor or a salt thereof under conditions wherein a level of moisture of less than about 2.0% by weight is achieved,
- wherein the pharmaceutically acceptable excipient is added to the first solution, or to the second solution, or to both,
- wherein the high purity cangrelor or salt thereof has a combined total of selected hydrolysis and oxidation degradants of cangrelor not exceeding about 1.5% by weight of the high purity cangrelor, and
- wherein the selected hydrolysis and oxidation degradants are one or more members selected from the group consisting of impurity A, impurity B, impurity C, impurity D and impurity E.
A pharmaceutical formulation consisting of high purity cangrelor, or a salt thereof, as an active ingredient and mannitol and/or sorbitol as a pharmaceutically acceptable excipient, prepared by a method consisting of:
- (a) dissolving cangrelor or a salt thereof in methanol to form a first solution;
- (b) mixing a pH-adjusting agent with the first solution to form a second solution, wherein the pH of the second solution is between about 7.0 and 9.5;
- and
- (c) removing the methanol from the second solution to produce high purity cangrelor or a salt thereof under conditions wherein a level of moisture of less than about 2.0% by weight is achieved,
- wherein the pharmaceutically acceptable excipient is added to the first solution, or to the second solution, or to both,
- wherein the high purity cangrelor or salt thereof has a combined total of selected hydrolysis and oxidation degradants of cangrelor not exceeding about 1.5% by weight of the high purity cangrelor, and
- wherein the selected hydrolysis and oxidation degradants are one or more members selected from the group consisting of impurity A, impurity B, impurity C, impurity D and impurity E.
Dependencies are inferred from the claim text.