Formulations of pimavanserin
Inventors
Tejwani, Ravindra • Abele, Stephen Edward • Vizzotti, Emanuel Joseph
Assignees
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Publication Number
US-11452721-B2
Publication Date
2022-09-27
Expiration Date
Abstract
Provided herein are capsules containing pimavanserin, processes for manufacturing said capsule, and pharmaceutical compositions containing pimavanserin.
Core Innovation
The document describes pharmaceutically acceptable capsule formulations for orally delivering pimavanserin, including capsules having capsule shell size 3 or 4. The formulation includes granules containing 40 mg pimavanserin tartrate and optionally one or more pharmaceutically acceptable excipients, together with one or more blending excipients. A key formulation attribute is that the bulk density of the granules is greater than 0.4 g/ml as determined by USP<616>, method 1.
The document emphasizes manufacture of the capsule fill by high-shear granulation, using controlled low water content and monitoring during granulation, including impeller speed, amperage, and chopper speed. This high-shear granulation approach is described as increasing bulk density, flowability, and compressibility to enable reproducible high-speed capsule filling. The granulation can be achieved without binder and then optionally blended with diluents such as microcrystalline cellulose and optionally silicified microcrystalline cellulose, lubricants such as magnesium stearate, and optionally binders and disintegrants.
The document further specifies performance and quality measures used to confirm and characterize the granules and the final dosage form. These include Carr’s Index and FT4 Powder Rheometer metrics, conditioned bulk density, dissolution per USP<711>, content uniformity per USP<905>, and XRPD confirmation of crystalline form C/Form A. Particle size distribution is controlled using a D90 range, and example compositions and comparative rationale are provided versus conventional granulation and other processes.
Claims Coverage
The independent claims cover pharmaceutically acceptable size 3 or 4 capsules for orally delivering a defined pimavanserin dose with granules having a specific bulk density requirement by USP<616>, method 1. Across the independent claims, the main inventive features are capsule shell size 3 or 4 with encapsulated blended pimavanserin composition, granules comprising 40 mg pimavanserin tartrate with pharmaceutically acceptable excipients, and granules having bulk density greater than 0.4 g/ml as determined by USP<616>, method 1.
Size 3 or 4 pharmaceutically acceptable capsule delivering 34 mg pimavanserin
A pharmaceutically acceptable capsule for orally delivering 34 mg of pimavanserin to a patient, wherein the capsule has a size 3 or 4 capsule shell.
Granules with 40 mg pimavanserin tartrate in blended composition
The size 3 or 4 capsule shell contains a blended pimavanserin composition comprising granules comprising 40 mg pimavanserin tartrate and optionally one or more pharmaceutically acceptable excipients, and one or more blending excipients.
Bulk density greater than 0.4 g/ml by USP<616>, method 1
The bulk density of the granules is greater than 0.4 g/ml as determined by USP<616>, method 1.
Capsule shell encapsulating blended pimavanserin composition with granules
A pharmaceutically acceptable capsule for orally delivering 34 mg of pimavanserin to a patient, wherein the capsule shell size 3 or 4 encapsulates a blended pimavanserin composition comprising granules comprising 40 mg pimavanserin tartrate and one or more pharmaceutically acceptable excipients.
Overall, the independent claims define a size 3 or 4 capsule encapsulating a blended pimavanserin composition where granules contain 40 mg pimavanserin tartrate with pharmaceutically acceptable excipients and have bulk density greater than 0.4 g/ml determined by USP<616>, method 1.
Stated Advantages
Increases bulk density, flowability, and compressibility for reproducible high-speed capsule filling.
Documented Applications
Oral delivery of pimavanserin using pharmaceutically acceptable capsules, including capsule shell size 3 or 4, containing a blended pimavanserin composition with granules having a defined bulk density.
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