Oral composition for delivery of drugs and other substances
The present disclosure provides for a composition which may be used for the solubilization of an agent or the oral administration of an agent, the composition comprising, a lysophosphatidyl compound and at least one of a monoglyceride and a free fatty acid. In certain embodiments, the composition comprises a lysophosphatidyl compound, a monoglyceride and a free fatty acid. In certain embodiments, the composition comprises an agent, a lysophosphatidyl compound, a monoglyceride and a free fatty acid.
1. A composition for solubilizing an agent, the composition comprising:
a lysophosphatidyl compound of the general formula ID and a monoglyceride of the general formula IV:
wherein:
one or more of the lysophosphatidyl compound and the monoglyceride are present as a salt;
R 1 is a carbon chain of 12, 13, 14, 15 or 16 carbons;
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 is a saturated or unsaturated carbon chain from 1 to 21 carbons in length; and
R 8 is a 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 further comprising a free fatty acid of the general formula V:
wherein:
R 9 is a saturated or unsaturated carbon chain from 1 to 21 carbons in length.
4. The composition of claim 1 , wherein the lysophosphatidyl compound is a compound of the general formula IJ:
5. 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 a saturated carbon chain from 6 to 12 carbons in length.
6. 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:
7. The composition of claim 1 , wherein the monoglyceride has the general formula IVC:
8. The composition of claim 3 , wherein the free fatty acid has the general formula VA:
9. The composition of claim 3 , 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 3 , wherein the free fatty acid and the monoglyceride comprise from about 70 mole percent to 99 mole percent of the composition and the lysophosphatidyl compound comprises 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 3 , wherein the free fatty acid and monoglyceride are present in the composition in a molar ratio of 1:2, the free fatty acid and the monoglyceride comprise from about 70 mole percent to 99 mole percent of the composition, and the lysophosphatidyl compound comprises 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.
12. The composition of claim 3 , wherein the ratios of the components of the composition are 1:4:2 mole percent lysophosphatidyl compound:monoglyceride:free fatty acid.
13. The composition of claim 1 further comprising the agent, wherein the composition forms a eutectic.
14. The composition of claim 2 , wherein the agent is present at a molar concentration of 1:1 or less with respect to the lysophosphatidyl compound, and wherein the composition further comprises a free fatty acid of the general formula V:
wherein:
R 9 is a saturated or unsaturated carbon chain from 1 to 21 carbons in length.
15. The composition of claim 14 , wherein the ratios of the components of the composition are 1:4:2:1, 1:4:2:0.8, 1:4:2:0.5, or 1:4:2:0.1 mole percent lysophosphatidyl compound:monoglyceride:free fatty acid:agent.
16. The composition of claim 1 , wherein the agent is a BCS class II, class Ill or class IV compound.