Preparation of an enteric release system
View Patent ↗Hydrophobic liquids are microencapsulated by an enteric matrix in an environment substantially free of organic solvents, the process including forming an emulsion of the enteric material and hydrophobic liquid in water, the emulsion titrated with an acid to form a particulate precipitate of the microencapsulated hydrophobic liquid in an enteric matrix.
1. A method of microencapsulating an active ingredient with an enteric matrix, the method comprising:
a) agitating a combination of water, an enteric matrix material, and an emulsifier at a pH above a solubility of the enteric matrix material to maintain complete dissolution of the enteric matrix material, the combination substantially free of organic solvents, wherein the enteric matrix material is selected from the group consisting of non-deamidated zein, shellac, and mixtures thereof;
b) adding a hydrophobic liquid to the combination;
c) homogenizing the hydrophobic liquid and the combination to create an emulsion; and
d) acid titrating the emulsion under agitated conditions in an amount effective to form a particulate precipitate having enteric functionality, wherein the acid is a food grade acid, and wherein the emulsion is free of oppositely charged particles.
2. The method of claim 1 wherein the emulsion is acid titrated to a pH in the range of about 3.0 to about 6.5.
3. The method of claim 1 further comprising (e) filtering, washing and drying the particulate precipitate to produce a dry powder.
4. The method of claim 1 further comprising (b1) agitating the hydrophobic liquid and combination to create a coarse emulsion prior to homogenization.
5. The method of claim 1 further comprising (d1) adding a surface oil remover to the particulate precipitate in an amount effective to reduce residual surface oil.
6. The method of claim 1 further comprising (a1) adding a base in an amount effective to adjust the pH to about 7.1 to about 12.0.
7. The method of claim 6 wherein the base is sodium hydroxide.
8. The method of claim 6 wherein the base is potassium hydroxide.
9. The method of claim 6 wherein the base is ammonium hydroxide.
10. The method of claim 1 , wherein the enteric matrix material is selected for providing a specific release rate.
11. The method of claim 1 wherein the emulsifier is a food grade emulsifier.
12. The method of claim 1 wherein the emulsifier is selected from the group consisting of polysorbate, polyglycerol ester, sucrose stearate, sucrose esters, protein, lecithin and mixtures thereof.
13. The method of claim 1 wherein the hydrophobic liquid comprises an essential oil.
14. The method of claim 1 wherein the hydrophobic liquid comprises linalool and thymol.
15. The method of claim 1 wherein the hydrophobic liquid comprises alpha-pinene, para-cymene, linalool and thymol.
16. The method of claim 15 wherein the hydrophobic liquid includes a triglyceride.
17. The method of claim 1 wherein the hydrophobic liquid comprises linalyl ester and thymyl ester.
18. The method of claim 1 wherein the hydrophobic liquid comprises unsaturated and polyunsaturated fatty acids.
19. The method of claim 1 wherein the hydrophobic liquid comprises unsaturated and polyunsaturated lipids.
20. The method of claim 1 wherein the hydrophobic liquid comprises beta-carotene.
21. The method of claim 1 wherein the hydrophobic liquid comprises oil soluble vitamins.
22. The method of claim 1 wherein the hydrophobic liquid comprises a triglyceride.
23. The method of claim 22 wherein the triglyceride is soybean oil.
24. The method of claim 21 wherein the triglyceride is canola oil.
25. The method of claim 1 wherein the acid is citric acid.
26. The method of claim 1 wherein the combination includes from about 0.01 to about 5.0 percent by weight emulsifier.
27. The method of claim 1 wherein the emulsion comprises from about 2.0 to about 7.0 percent by weight hydrophobic liquid.
28. The method of claim 1 , wherein the particle precipitate has a particle size ranging from about 1.0 to 1000.0 microns.
29. A method of microencapsulating an active ingredient with an enteric matrix, the method comprising:
a) agitating a combination of water, an enteric matrix material, and an emulsifier at a pH above a solubility of the enteric matrix material to maintain complete dissolution of the enteric matrix material, the combination substantially free of organic solvents, wherein the enteric matrix material is selected from the group consisting of non-deamidated zein, shellac, and mixtures thereof;
b) adding a hydrophobic liquid to the combination;
c) homogenizing the hydrophobic liquid and the combination to create an emulsion; and
d) acid titrating the emulsion to a pH at or below an isoelectric point of the enteric matrix material under agitated conditions with a food grade acid in an amount and for a time effective to form a particulate precipitate having enteric functionality, without substantial degradation of the enteric functionality, and wherein the emulsion is free of oppositely charged particles.
30. The method of claim 1 , wherein the particulate precipitate includes the hydrophobic liquid homogeneously dispersed throughout a matrix of the enteric matrix material.
31. The method of claim 29 , wherein the particulate precipitate includes the hydrophobic liquid homogeneously dispersed throughout a matrix of the enteric matrix material.