IP Library Granted Patent US 10,463,738
Granted Patent B2
US 10,463,738 · App. 15/807,389 · Granted Nov 5, 2019

Oral composition for delivery of drugs and other substances

Inventors: Walter A Shaw (Birmingham, AL); Stephen W Burgess (Chelsea, AL); Shengrong Li (Birmingham, AL)
Assignee: Avanti Polar Lipids, Inc.
A61K47/24A61K9/1617A61K31/05A61K31/12A61K31/661A61K47/10A61K47/12A61K9/0095
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Quick Facts
Patent No.
US 10,463,738
App. No.
15/807,389
Granted
Nov 5, 2019
Kind
B2
Abstract

The present disclosure provides for a composition which may be used for the solublization of an agent or the oral administration of an agent, the composition comprising, a lyosphosphatidyl compound and at least one of a monoglyceride and a free fatty acid. In certain embodiments, the composition comprises a lyosphosphatidyl compound, a monoglyceride and a free fatty acid. In certain embodiments, the composition comprises an agent, a lyosphosphatidyl compound, a monoglyceride and a free fatty acid.

Claims (26)

1. A composition for solubilizing an agent, the composition comprising:

a lysophosphatidyl compound of the general formula IJ, a monoglyceride of the general formula IV and a free fatty acid of the general formula V:

wherein,

one of R 4 , R 5 and R 6 is —C(O)—R 7 and the remaining of R 4 , R 5 and R 6 are each independently selected from H or R 8 ;

R 7 and R 9 are each independently a saturated or unsaturated carbon chain from 1 to 21 carbons in length; and

R 8 is saturated or unsaturated carbon chain from 1 to 10 carbons in length.

2. The composition of claim 1 further comprising the agent.

3. The composition of claim 1 , wherein R 7 and R 9 are each independently a saturated carbon chain from 13 to 21 carbons in length.

4. The composition of claim 1 , wherein R 7 and R 9 are each independently a saturated carbon chain from 6 to 12 carbons in length.

5. The composition of claim 1 , wherein the monoglyceride has the general formula IVA or IVB and R 7 is a saturated carbon chain from 13 to 21 carbons in length:

6. The composition of claim 1 , wherein the monoglyceride has the general formula IVC

7. The composition of claim 1 , wherein the free fatty acid has the general formula VA

8. The composition of claim 1 , wherein R9 is a saturated carbon chain from 13 to 15 carbons in length and the monoglyceride has the general formula IVC

9. The composition of claim 1 , wherein the free fatty acid and monoglyceride are present in the composition in a molar ratio of between 2:1 and 1:2.

10. The composition of claim 1 , wherein the free fatty acid and the monoglyceride comprise from about 70 mole percent to 99 mole percent of the composition, with the lysophosphatidyl compound comprising from about 30 mole percent to 1 mole percent of the composition, wherein the mole percentage values are expressed with regard to the lysophosphatidyl compound, the monoglyceride and the free fatty acid of the composition.

11. The composition of claim 1 , wherein the ratios of the components of the composition are 1:4:2, 1:3:3, 2:4:2, or 1:2:4 mole percent lysophosphatidyl compound:monoglyceride:free fatty acid.

12. The composition of claim 1 further comprising the agent, wherein the composition forms a eutectic.

13. The composition of claim 12 , wherein the agent is present at molar concentration of 1:1 or less with respect to the lysophosphatidyl compound.

14. The composition of claim 1 , wherein the composition forms a eutectic.

15. A composition for solubilizing an agent, the composition comprising: a lysophosphatidyl compound of the general formula IJ, a monoglyceride of the general formula IVC and a free fatty acid of the general formula VA:

wherein the free fatty acid and monoglyceride are present in the composition in a molar ratio of between 2:1 and 1:2 and the free fatty acid and the monoglyceride comprise from about 70 mole percent to 99 mole percent of the composition, with the lysophosphatidyl compound comprising from about 30 mole percent to 1 mole percent of the composition, wherein the mole percentage values are expressed with regard to the lysophosphatidyl compound, the monoglyceride and the free fatty acid of the composition.

16. The composition of claim 15 , wherein the ratios of the components of the composition are 1:4:2, 1:3:3, 2:4:2, or 1:2:4 mole percent lysophosphatidyl compound:monoglyceride:free fatty acid.

17. The composition of claim 15 further comprising the agent.

18. The composition of claim 15 further comprising the agent, wherein the composition forms a eutectic.

19. The composition of claim 18 , wherein the agent is present at molar concentration of 1:1 or less with respect to the lysophosphatidyl compound.

20. The composition of claim 15 , wherein the composition forms a eutectic.

Assignments (2)
CHANGE OF NAME Recorded Aug 31, 2022
From: AVANTI POLAR LIPIDS, INC.
To: AVANTI POLAR LIPIDS, LLC
Reel/Frame 061364/0407 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 2, 2019
From: BURGESS, STEPHEN W; SHAW, WALTER A; LI, SHENGRONG
To: AVANTI POLAR LIPIDS, INC.
Reel/Frame 049654/0001 →
Continuity (3)
Continuation 14822289 · Aug 10, 2015
Provisional Application 62035393 · Aug 9, 2014
Related Publication 20180064813A1 · Mar 8, 2018