Forms of cidofovir
AssigneeJohnson Matthey Public Limited Company
InventorsGeorge Scott Wilson, Angela Barkley, Jurjus Jurayj
Life of this patent
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Abstract
Cidofovir is obtained in different forms, including amorphous cidofovir, crystalline anhydrous cidofovir, crystalline cidofovir monohydrate, and crystalline cidofovir dihydrate, including various polymorphs.
Claims15
1-17. (canceled)
A method of preparing anhydrous cidofovir, comprising combining cidofovir monohydrate with water to form a mixture, heating the mixture at a temperature of from about 50° C. to about 80° C., cooling the mixture below about 50° C., and combining the mixture with ethanol.
19-20. (canceled)
A method of treating a disease, comprising administering to a patient in need of treatment a therapeutically effective amount of a pharmaceutical formulation comprising at least one form of cidofovir, wherein the form of cidofovir is selected from the group consisting of:
- a) cidofovir Form I, characterized by an XRPD pattern having main peaks expressed as 2-theta at about 15.8, 13.5, 24.9, 21.3, 27.0, 18.6, 25.2 and 23.8 degrees;
- b) cidofovir Form II, characterized by an XRPD pattern having main peaks expressed as 2-theta at about 11.5, 19.0, 18.4, 29.7, 26.2, 17.6, 17.4, 26.6, 23.1 and 21.3 degrees;
- c) cidofovir Form III, characterized by an XRPD pattern having main peaks expressed as 2-theta at about 5.5, 18.3, 14.2, 26.9, 21.1, 15.2, 19.9, 27.5, 21.3, 22.0, 7.6 and 22.3 degrees;
- d) cidofovir Form IV, characterized by an XRPD pattern having main peaks expressed as 2-theta at about 11.5, 18.4, 19.0, 29.7, 17.6, 26.6, 26.2 and 17.4 degrees;
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- e) cidofovir Form V, characterized by an XRPD pattern having main peaks expressed as 2-theta at about 17.6, 29.7, 19.0, 21.3, 18.4, 26.5, 26.2 and 11.5 degrees.
A method of making amorphous cidofovir, comprising freeze-drying a solution of cidofovir.
A method of making cidofovir dihydrate, comprising combining cidofovir monohydrate with water and adding ethanol.
A method of making cidofovir dihydrate, comprising combining cidofovir monohydrate with water to form a mixture, acidifying the mixture, and combining the mixture with ethanol.
A method of making cidofovir dihydrate, comprising combining cidofovir monohydrate with ethanol.
(canceled)
Dependencies are inferred from the claim text.