Crystalline form of triethylenetetramine tetrahydrochloride and its pharmaceutical use
AssigneeOrphalan S.A.
InventorsTimothy James Morley, Ronnie Maxwell Lawrence, Naseem Amin
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Abstract
The present invention describes a new crystalline form of triethylenetetramine tetrachloride which has improved room temperature stability over known forms and over the dichloride salt. The new crystalline form is characterised by having peaks in an XRPD spectrum at 22.9, 25.4, 25.8, 26.6, 34.6 and 35.3±0.1° 2θ and Raman shifts 943, 1173, 1527 and 1612±5 cm−1. The crystalline form of triethylenetetramine tetrachloride is useful in the treatment of Wilson's disease.
Claims24
A pharmaceutical composition for treating Wilson's disease in a subject in need thereof, wherein the composition comprises a therapeutically effective amount of crystalline triethylenetetramine tetrahydrochloride, wherein at least 50% by weight of the crystalline triethylenetetramine tetrahydrochloride is Form B and no more than 50% by weight of the crystalline triethylenetetramine tetrahydrochloride is Form A, wherein:
- Form B has at least one of the following characteristics:
- (i) an XRPD pattern having at least two peaks selected from the peaks at 22.9, 25.4, 25.8, 26.6, 34.6 and 35.3±0.1° 2θ;
- and/or
- (ii) a Raman spectrum having at least two peaks selected from the peaks at a Raman shift of 943, 1173, 1527 and 1612±5 cm−1;
- and
- Form A has an XRPD pattern having peaks at 25.2 and 35.7±0.1° 2θ, and wherein the therapeutically effective amount is from about 0.001 to 50 mg/kg per body weight of the subject.
A method of treating Wilson's disease in a subject in need thereof comprising administering to said subject a pharmaceutical composition which comprises a therapeutically effective amount of crystalline triethylenetetramine tetrahydrochloride, wherein at least 50% by weight of the crystalline triethylenetetramine tetrahydrochloride is Form B and no more than 50% by weight of the crystalline triethylenetetramine tetrahydrochloride is Form A, wherein:
- Form B has at least one of the following characteristics:
- (i) an XRPD pattern having at least two peaks selected from the peaks at 22.9, 25.4, 25.8, 26.6, 34.6 and 35.3±0.1° 2θ;
- and/or
- (ii) a Raman spectrum having at least two peaks selected from the peaks at a Raman shift of 943, 1173, 1527 and 1612±5 cm−1;
- and
- Form A has an XRPD pattern having peaks at 25.2 and 35.7±0.1° 2θ, and wherein the therapeutically effective amount is from about 0.001 to 50 mg/kg per body weight of the subject.
Dependencies are inferred from the claim text.