IP Library Granted Patent US 11,324,699
Granted Patent B2
US 11,324,699 · App. 15/523,711 · Granted May 10, 2022

Lipid multiparticulate formulations

Inventors: Christopher Diorio (Campbell Hall, NY); John Lokhnauth (Fair Lawn, NJ); Chang Lee (Bethesda, MD)
Assignee: Capsugel Belgium NV
A61K9/145A61K9/143A61K9/148A61K9/5123A61K31/045A61K31/122
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Quick Facts
Patent No.
US 11,324,699
App. No.
15/523,711
Granted
May 10, 2022
Kind
B2
Abstract

Disclosed are various embodiments of lipid multiparticulate compositions comprising at least one active agent, a low flow point excipient, and a high flow point excipient.

Claims (22)

1. A composition comprising a plurality lipid of particles that are solid at ambient temperature, have a generally spherical shape, and have a mean diameter ranging from 100 μm to 3000 μm, said lipid particles comprising at least one active agent, and a matrix, wherein said matrix comprises

a) at least one low flow point excipient wherein the low flow point excipient has a melting point of less than 50° C., wherein the low flow point excipient consists of one or more of polyglycolized glycerides, a mixture of C 10 -C 18 triglycerides, stearoyl polyoxylglycerides, lauroyl macrogol-32 glycerides, fatty acid esters of glycols, fatty acid esters of poly glycols, fatty acid esters of polyglycerols, myristyl alcohol, lauryl alcohol, capric alcohol, lauric acid, oleic acid, and mixtures thereof; and

b) at least one high flow point excipient wherein the high flow point excipient has a melting point of 50° C. or greater;

wherein a mass ratio of the at least one low flow point excipient and the at least one high flow point excipient is greater than 4:1.

2. The composition of claim 1 wherein a mass ratio of said at least one low flow point excipient and said at least one high flow point excipient is at least 10:1.

3. The composition of claim 1 wherein a mass ratio of said at least one low flow point excipient and said at least one high flow point excipient is at least 15:1.

4. The composition of claim 1 comprising from 1 wt % to 60 wt % of the active agent.

5. The composition of claim 1 wherein the high flow point excipient comprises at least 2 wt % of the composition.

6. The composition of claim 1 wherein the particles further comprise from 0.01 wt % to 20 wt % of a dispersing agent.

7. The composition of claim 1 wherein said particles further comprise from 0.01 wt % to 20 wt % of an antioxidant.

8. The composition of claim 1 wherein said composition further comprises 0.01 wt % to 5 wt % of a flow aid.

9. A composition comprising:

a plurality of lipid particles that are solid at ambient temperature, have a mean diameter ranging from 100 μm to 3000 μm, said lipid particles comprising at least one active agent, and a matrix, wherein said matrix comprises

a) at least one low flow point excipient, wherein the low flow point excipient consists of one or more of polyglycolized glycerides, a mixture of C 10 -C 18 triglycerides, stearoyl polyoxylglycerides, lauroyl macrogol-32 glycerides, fatty acid esters of glycols, fatty acid esters of poly glycols, fatty acid esters of polyglycerols, myristyl alcohol, lauryl alcohol, capric alcohol, lauric acid, oleic acid, and mixtures thereof, and wherein the low flow point excipient has a melting point of less than 50° C.;

b) at least one high flow point excipient, wherein the high flow point excipient has a melting point of 50° C. or greater; and

wherein a mass ratio of the at least one low flow point excipient and the at least one high flow point excipient is greater than 4:1;

wherein said composition has an in vivo AUC value, wherein the AUC value divided by the amount dosed is at least 1.25-fold compared to an AUC value of a control dosage form divided by the amount dosed.

10. The composition of claim 1 wherein said active agent is a carotenoid.

11. The composition of claim 10 wherein said carotenoid comprises lutein, astaxanthin, zeaxanthin, alpha-carotene, beta-carotene, cryptoxanthin, lycopene, and mixtures thereof.

12. The composition of claim 9 wherein the active agent is a carotenoid.

13. The composition of claim 12 wherein the carotenoid comprises lutein, astaxanthin, zeaxanthin, alpha-carotene, beta-carotene, cryptoxanthin, lycopene, and any mixture thereof.

14. The composition of claim 1 wherein the high flow point excipient comprises glycerol behenate, glycerol dibehenate, glycerol palmitate, hydrogenated castor oil, stearyl alcohol, behenyl alcohol, palmitic acid, stearic acid, paraffin wax, beeswax, candelilla wax, carnauba wax, and mixtures thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 19, 2025
From: CAPSUGEL BELGIUM NV
To: LONZA SALES AG
Reel/Frame 071157/0636 →
Continuity (2)
Provisional Application 62087766 · Dec 4, 2014
Related Publication 20170354599A1 · Dec 14, 2017
Cited By (1)
US 12,697,303