FORMULATIONS OF PIMAVANSERIN

• US 20190216791A1
• Filed: 03/25/2019
• Published: 07/18/2019
• Est. Priority Date: 08/30/2017
• Status: Active Grant

• Current Assignee: Acadia Pharmaceuticals Inc.
• Original Assignee: Acadia Pharmaceuticals Inc.
• Inventors: Tejwani, Ravi, Abele, Stephen Edward, Vizzotti, Emanuel Joseph
• Granted Patent: US 10,449,185 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/4468 having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/1688 resulting in pure drug agglomerate optionally containing up to 5% of excipient
• CPC Class Codes: A61K 9/1694 resulting in granules or microspheres of the matrix type containing more than 5% of excipient
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/4808 characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• CPC Class Codes: A61K 9/4833 Encapsulating processes; Filling of capsules mechanical aspects A61J3/07
• CPC Class Codes: A61K 9/485 Inorganic compounds
• CPC Class Codes: A61K 9/4858 Organic compounds
• CPC Class Codes: A61K 9/4866 Organic macromolecular compounds
• CPC Class Codes: C07B 2200/13 Crystalline forms, e.g. polymorphs

Abstract

Provided herein are capsules containing pimavanserin, processes for manufacturing said capsule, and pharmaceutical compositions containing pimavanserin.

Claims

1. A pharmaceutically acceptable capsule for orally delivering 34 mg of pimavanserin to a patient, wherein the capsule has a capsule shell that encapsulates a blended pimavanserin composition comprising:

40 mg granulated pimavanserin tartrate having a particle size distribution (D90) of 180 to 340 μ

m, wherein the bulk density of the granulated pimavanserin is 0.4 to 0.6 g/ml as determined by USP<

616>

, method 1;

59 mg microcrystalline cellulose having a particle size distribution (D90) of 180 to 340 μ

m; and

1 mg magnesium stearate;

wherein the particle size distribution is measured using laser light scattering with a Malvern Mastersizer 2000 LLS PS system, a Scirocco 2000 dry dispersion unit and a sample size of 2 to 10 g.

2. The pharmaceutically acceptable capsule of claim 1, wherein the capsule shell is a hard shell size 3 or size 4 capsule.

3. The pharmaceutically acceptable capsule of claim 1, wherein the capsule shell is a hard shell size 4 capsule.

4. A pharmaceutically acceptable capsule for orally delivering 34 mg of pimavanserin to patient, wherein the capsule has a size 4 capsule shell that contains a blended pimavanserin composition comprising:

40% w/w pimavanserin tartrate;

59% w/w microcrystalline cellulose;

wherein the D90 particle size distribution of the blended pimavanserin composition is 100 to 300 μ

m as measured using laser scattering particle size analysis.

5. The pharmaceutically acceptable capsule of claim 4, wherein the blended pimavanserin composition further comprises 1% w/w magnesium stearate.

6. The pharmaceutically acceptable capsule of claim 4, wherein the bulk density of the blended pimavanserin composition is 0.4 to 0.6 g/ml as determined by USP <

616>

, method 1.

7. The pharmaceutically acceptable capsule of claim 4, wherein the capsule releases at least 80% of the pimavanserin within 30 minutes in accordance with USP <

711>

dissolution apparatus 1.