Dosage forms comprising a plasma kallikrein inhibitor
AssigneeKalvista Pharmaceuticals Limited
InventorsJohn Herman COLLETT, Gary Paul COOK, Jamie Joseph FARRAR, Michael John FRODSHAM, Michael Bryan ROE, Richard Simon TODD, Robert Neil WARD
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Abstract
The present invention relates to oral solid dosage forms comprising a plasma kallikrein inhibitor, in particular a solid form (Form 1) of the compound of Formula A. Also provided are methods of preparing oral solid dosage forms comprising the compound of Formula A using Form 1 of the compound of Formula A.
Claims44
An oral solid dosage form comprising a solid form of the compound of Formula A
- wherein the solid form of the compound of Formula A exhibits at least the following characteristic X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at approximately 11.2, 12.5, 13.2, 14.5 and 16.3.
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A method of preparing an oral solid dosage form comprising a compound of Formula A
- wherein the method comprises method (i), method (ii), or method (iii), method (i) comprising the steps of:
- (a) mixing a solid form of the compound of Formula A which exhibits at least the following characteristic X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at approximately 11.2, 12.5, 13.2, 14.5 and 16.3 with a granulation fluid comprising a binder optionally further comprising water, and optionally a diluent, a disintegrant, and/or a surfactant;
- (b) granulating the dispersion of step (a) to form granules;
- (c) drying the granules;
- (d) optionally blending the granules of step (b) or (c) with a diluent, an acid, a surfactant, and/or a lubricant to form blended granules;
- and
- (e) compressing or filling the granules or blended granules into a solid oral dosage form;
- or
- method (ii) comprising the steps of:
- (a) dispersing a solid form of the compound of Formula A which exhibits at least the following characteristic X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at approximately 11.2, 12.5, 13.2, 14.5 and 16.3 in molten lipid excipient;
- (b) loading the molten dispersion into a capsule;
- or
- method (iii) comprising loading a capsule with a solid form of the compound of Formula A which exhibits at least the following characteristic X-ray powder diffraction peaks (Cu Kα radiation, expressed in degrees 2θ) at approximately 11.2, 12.5, 13.2, 14.5 and 16.3.
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The method of claim 36 that is method (ii) and wherein the lipid excipient is TPGS or Gelucire 44/14, preferably TPGS and/or the capsule shell is made from gelatin, hydroxypropyl methylcellulose or starch.
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Dependencies are inferred from the claim text.