Aqueous oral pharmaceutical suspension compositions
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Assignees
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Publication Number
US-11471471-B2
Publication Date
2022-10-18
Expiration Date
Abstract
Provided is an aqueous oral pharmaceutical suspension composition comprising vamorolone Form I. Also provided are methods for its preparation and its use.
Core Innovation
The invention concerns aqueous oral pharmaceutical suspension compositions comprising vamorolone Form I. The compositions include a therapeutically effective amount of vamorolone Form I together with at least one suspending agent and at least one suspension vehicle, for oral administration. The suspension compositions are further characterized by solid-form characterization criteria including X-ray powder diffractometry, thermogravimetric analysis, and differential scanning calorimetry.
For the crystalline form, the invention specifies X-ray powder diffraction patterns comprising peaks in terms of ±2θ at about 11.9, about 13.7, about 16.1, and about 18.3 with radiation Cu Kα, and/or patterns substantially as shown in FIG. 1. It further specifies a thermogravimetric analysis profile showing less than about 0.5% weight loss below about 175° C and/or substantially as shown in FIG. 2.
The invention also specifies an exothermic event onset at 180.7° C and a melting event with an onset temperature of 231.0° C and a peak temperature of 234.7° C as measured by differential scanning calorimetry, and/or a DSC trace substantially as shown in FIG. 3. The invention additionally relates to treating or reducing symptoms of diseases by administering the suspension composition comprising vamorolone Form I with the selected suspending agent and suspension vehicle.
Claims Coverage
The independent claims cover four main inventive features: treating muscular dystrophy using an aqueous oral pharmaceutical suspension comprising vamorolone Form I with specified suspension components, treating muscular dystrophy using a crystalline form of vamorolone defined by pXRD/TGA/DSC characterization criteria and administered in an aqueous oral suspension, treating a selected list of diseases using the aqueous oral pharmaceutical suspension comprising vamorolone Form I with specified suspension components, and treating the same selected disease list using the crystalline form characterized by pXRD/TGA/DSC properties.
Treating muscular dystrophy with an aqueous oral suspension of vamorolone Form I
A method of treating or reducing the symptoms of muscular dystrophy by administering to a patient in need thereof a therapeutically effective amount of an aqueous oral pharmaceutical suspension composition comprising vamorolone Form I, at least one suspending agent, and at least one suspension vehicle.
Treating muscular dystrophy with a crystalline form of vamorolone characterized by pXRD, TGA, and DSC properties
A method of treating or reducing the symptoms of muscular dystrophy by administering to a patient in need thereof a therapeutically effective amount of a crystalline form of vamorolone characterized by one or more of: an X-ray powder diffraction pattern with peaks at about 11.9, about 13.7, about 16.1, and about 18.3 with radiation Cu Kα; an X-ray powder diffraction pattern substantially as shown in FIG. 1; a thermogravimetric analysis profile showing less than about 0.5% weight loss below about 175° C; a thermogravimetric analysis profile substantially as shown in FIG. 2; an exothermic event onset at 180.7° C and a melting event with onset and peak temperatures of 231.0° C and 234.7° C, respectively, as measured by differential scanning calorimetry; and a differential scanning calorimetry trace substantially as shown in FIG. 3.
Treating a selected disease list with an aqueous oral suspension of vamorolone Form I
A method of treating or reducing the symptoms of a disease chosen from chronic obstructive pulmonary disease, asthma, arthritis, Crohn's disease, inflammatory bowel disease, heart disease, multiple sclerosis, glioma, Behçet's disease, Henoch-Schönlein purpura, polyarteritis nodosa, polymyositis, dermatomyositis, Wegener's granulomatosis, and graft-versus-host disease by administering to a patient in need thereof a therapeutically effective amount of an aqueous oral pharmaceutical suspension composition comprising vamorolone Form I, at least one suspending agent, and at least one suspension vehicle.
Treating a selected disease list with a crystalline form of vamorolone characterized by pXRD, TGA, and DSC properties
A method of treating or reducing the symptoms of a disease chosen from chronic obstructive pulmonary disease, asthma, arthritis, Crohn's disease, inflammatory bowel disease, heart disease, multiple sclerosis, glioma, Behçet's disease, Henoch-Schönlein purpura, polyarteritis nodosa, polymyositis, dermatomyositis, Wegener's granulomatosis, and graft-versus-host disease by administering to a patient in need thereof a therapeutically effective amount of a crystalline form of vamorolone characterized by one or more of: an X-ray powder diffraction pattern with peaks at about 11.9, about 13.7, about 16.1, and about 18.3 with radiation Cu Kα; an X-ray powder diffraction pattern substantially as shown in FIG. 1; a thermogravimetric analysis profile showing less than about 0.5% weight loss below about 175° C; a thermogravimetric analysis profile substantially as shown in FIG. 2; an exothermic event onset at 180.7° C and a melting event with onset and peak temperatures of 231.0° C and 234.7° C, respectively, as measured by differential scanning calorimetry; and a differential scanning calorimetry trace substantially as shown in FIG. 3.
Across the independent claims, the claim coverage centers on administering therapeutically effective amounts of vamorolone Form I in an aqueous oral suspension comprising at least one suspending agent and at least one suspension vehicle, and separately on crystalline forms of vamorolone defined by pXRD, TGA, and DSC characterization criteria, with treatment indications including muscular dystrophy and additional specified diseases from defined lists.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Treating or reducing the symptoms of muscular dystrophy.
Treating or reducing the symptoms of chronic obstructive pulmonary disease.
Treating or reducing the symptoms of asthma.
Treating or reducing the symptoms of arthritis.
Treating or reducing the symptoms of Crohn's disease.
Treating or reducing the symptoms of inflammatory bowel disease.
Treating or reducing the symptoms of heart disease.
Treating or reducing the symptoms of multiple sclerosis.
Treating or reducing the symptoms of glioma.
Treating or reducing the symptoms of Behçet's disease.
Treating or reducing the symptoms of Henoch-Schönlein purpura.
Treating or reducing the symptoms of polyarteritis nodosa.
Treating or reducing the symptoms of polymyositis.
Treating or reducing the symptoms of dermatomyositis.
Treating or reducing the symptoms of Wegener's granulomatosis.
Treating or reducing the symptoms of graft-versus-host disease.
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