Oral formulations of cladribine
AssigneeAres Trading S.A.
InventorsNicholas S. Bodor, Yogesh Dandiker
Life of this patent
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Abstract
Provided are compositions of cladribine and cyclodextrin which are especially suited for the oral administration of cladribine.
Claims55
A complex cladribine-cyclodextrin complex which is an intimate amorphous admixture consisting of (a) an amorphous inclusion complex of cladribine with the amorphous cyclodextrin hydroxypropyl-β-cyclodextrin and (b) amorphous free cladribine associated with said amorphous cyclodextrin as a non-inclusion complex, said complex cladribine-cyclodextrin complex having a weight ratio of cladribine to said amorphous cyclodextrin of from about 1:10 to about 1:16.
A pharmaceutical composition comprising a complex cladribine-cyclodextrin complex which is an intimate amorphous admixture consisting of (a) an amorphous inclusion complex of cladribine with the amorphous cyclodextrin hydroxypropyl-β-cyclodextrin and (b) amorphous free cladribine associated with said amorphous cyclodextrin as a non-inclusion complex, formulated into a solid oral dosage form, said composition comprising no significant amount of free crystalline cladribine therein, said composition having a weight ratio of cladribine to said amorphous cyclodextrin of from about 1:10 to about 1:16.
A method for enhancing the oral bioavailability of cladribine comprising orally administering to a subject in need thereof a pharmaceutical composition comprising a complex cladribine-cyclodextrin complex which is an intimate amorphous admixture consisting of (a) an amorphous inclusion complex of cladribine with the amorphous cyclodextrin hydroxypropyl-β-cyclodextrin and (b) amorphous free cladribine associated with said amorphous cyclodextrin as a non-inclusion complex, formulated into a solid oral dosage form, said composition comprising no significant amount of free crystalline cladribine therein, said composition having a weight ratio of cladribine to said amorphous cyclodextrin of from about 1:10 to about 1:16.
A method for the treatment of a condition selected from the group consisting of multiple sclerosis, rheumatoid arthritis and leukemia in a subject suffering from said condition comprising orally administering to said subject a pharmaceutical composition comprising a complex cladribine-cyclodextrin complex which is an intimate amorphous admixture consisting of (a) an amorphous inclusion complex of cladribine with the amorphous cyclodextrin hydroxypropyl-β-cyclodextrin and (b) amorphous free cladribine associated with said amorphous cyclodextrin as a non-inclusion complex, formulated into a solid oral dosage form, said composition comprising no significant amount of free crystalline cladribine therein, said composition having a weight ratio of cladribine to said amorphous cyclodextrin of from about 1:10 to about 1:16.
Dependencies are inferred from the claim text.