Lipid multiparticulate formulations

Patent metadata

Field	Value
Publication number	US-2017354599-A1
Application number	US-201515523711-A
Country	US
Kind code	A1
Filing date	Nov 24, 2015
Priority date	Dec 4, 2014
Publication date	Dec 14, 2017
Grant date	—

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.

First claim

1 . A composition comprising a plurality of particles that at solid at ambient temperature have a generally spherical shape, and have a mean diameter ranging from 40 μm to 3000 μm, said particles comprising at least one active agent, and a matrix, wherein said matrix comprises
a) at least one low flow point excipient and
b) at least one high flow point excipient.

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 2:1.

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 4:1.

4 . 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.

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

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

7 . The composition of claim 1 wherein the composition further comprises from 0.01 wt % to 20 wt % of a dispersing agent.

8 . The composition of claim 1 wherein said composition further comprises from 0.01 wt % to 20 wt % of an antioxidant.

9 . The composition of claim 1 wherein said composition further comprises a flow aid.

10 . The composition of claim 9 wherein said flow aid comprises 0.01 wt % to 5 wt % of the composition.

11 . A composition comprising:
a plurality of particles that are solid at ambient temperature, have a mean diameter ranging from 40 μm to 3000 μm, said particles comprising at least one active agent, and a matrix, wherein said matrix comprises a) at least one low flow point excipient; b) at least one high flow point excipient; and
wherein said composition has an in vivo AUC value, wherein the AUC value divided by the amount dosed is at least 1.25-fold an AUC value of a control dosage form divided by the amount dosed.

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

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

14 . A process for making a composition comprising:
(a) forming a molten mixture comprising at least one active agent, a low flow point excipient, and a high flow point excipient, (b) directing the molten mixture to a spinning disk atomizer to form droplets, (c) cooling said droplets to form solid particles, and (d) collecting said particles.

15 . The product of the process of claim 14 .

16 . The composition of claim 11 wherein the active agent is a carotenoid.

17 . The composition of claim 16 wherein the carotenoid comprises lutein, astaxanthin, zeaxanthin, alpha-carotene, beta-carotene, cryptoxanthin, lycopene, and any mixture thereof.

Assignees

• Capsugel Belgium Nv

Inventors

• Diorio Christopher
• Lokhnauth John
• Lee Chang

Classifications

• B01J2/02

  by dividing the liquid material into drops, e.g. by spraying, and solidifying the drops · CPC title

• A61K9/5123 Primary

  Organic compounds, e.g. fats, sugars · CPC title

• A61K31/045

  Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates · CPC title

• A61K31/122

  having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin · CPC title

• A61K9/143

  with inorganic compounds · CPC title