Taste masking drug formulations
The present disclosure relates to a taste-masking microcapsule composition. The composition comprises a core portion encapsulated by a shell portion. The core portion comprises an active pharmaceutical ingredient (API) and one or more excipients. The shell portion comprises a hydrophobic matrix and a pH-responsive material. The microcapsule compositions prevent API release at the more neutral pH levels in the oral cavity, but upon exposure to pH levels of the stomach, the pH-responsive material becomes soluble thereby permitting release of the API.
1. A composition comprising: a microcapsule comprising a core portion and a shell portion, wherein the core portion comprises an active pharmaceutical ingredient and a hydrophilic excipient, wherein the shell portion comprises a mixture of a hydrophobic matrix and from about 1% to 25% by weight of a pH-responsive material, wherein the pH-responsive material is insoluble at a pH of greater than 5.0 or is otherwise insoluble in saliva and is soluble at a pH of less than 5.0, the balance of the shell portion comprising the hydrophobic matrix, wherein the hydrophobic matrix comprises one or more hydrophobic matrix components, wherein at least one of the hydrophobic matrix components is a wax or a lipid, wherein the shell portion encapsulates the core portion.
2. The composition of claim 1 , wherein the hydrophilic excipient is one or more selected from the group consisting of polyethylene glycol, polyols, and poloxamer and lutrol block copolymers.
3. The composition of claim 1 , wherein the hydrophilic excipient is polyethylene glycol.
4. The composition of claim 3 wherein the active pharmaceutical ingredient is hydrophobic.
5. The composition of claim 1 wherein pH-responsive material is a butylated methacrylate copolymer.
6. The composition of claim 1 , wherein the one or more hydrophobic matrix components further comprises stearic acid.
7. The composition of claim 6 , wherein the one or more hydrophobic matrix components comprises the wax, and wherein the wax is a combination of carnauba wax and beeswax.
8. The composition of claim 1 wherein the pH-responsive material comprises methacrylate copolymer, butylated methacrylate copolymer, basic butylated methacrylate copolymer, poly(methacrylic acid), amino methacrylate copolymer, aminoalkyl methacrylate copolymer, hydroxypropylmethyl cellulose phthalate, hypomellose phthalate, polyacrylate derivative or polymethacrylate derivative, and the hydrophobic matrix comprises a wax, lipid or combination thereof.
9. The composition of claim 8 , wherein the one or more hydrophobic matrix components further comprises stearic acid.
10. The composition of claim 9 , wherein the one or more hydrophobic matrix components comprises the wax, and wherein the wax is a combination of carnauba wax and beeswax.
11. The composition of claim 10 , wherein the pH-responsive material is a butylated methacrylate copolymer.
12. The composition of claim 2 , wherein the pH-responsive material comprises a butylated methacrylate copolymer and the one or more hydrophobic matrix components further comprises stearic acid.
13. The composition of claim 12 , wherein the one or more hydrophobic matrix components comprises the wax, and wherein the wax is selected from the group consisting of carnauba wax, beeswax, and a combination thereof.
14. The composition of claim 1 , wherein the active pharmaceutical ingredient is selected from the group consisting of prednisone and ritonavir, and the one or more hydrophobic matrix components comprises a lipid.
15. The composition of claim 14 wherein the pH-responsive material comprises a butylated methacrylate copolymer.
16. The composition of claim 1 comprising a plurality of the microcapsules having a mean particle diameter from about 100 μm to about 400 μm wherein at least 80% of the microcapsules have a particle diameter within 25% of the mean particle diameter of the plurality of microcapsules.
17. The composition of claim 1 comprising a plurality of the microcapsules in a liquid suspension.
18. The composition of claim 1 comprising a plurality of the microcapsules formulated as a dry powder.
19. The composition of claim 1 wherein the shell portion comprises from about 1% to 10% by weight of the pH-responsive material.
20. The composition of claim 1 wherein the hydrophobic matrix further comprises a glycerol fatty acid ester, a cellulose ether, or a cellulose ester.
21. The composition of claim 1 wherein the one or more hydrophobic matrix components comprises carnauba wax or glycerol monostearate.
22. The composition of claim 21 wherein the one or more hydrophobic matrix components further comprises a sorbitan ester.
23. The composition of claim 21 wherein the one or more hydrophobic matrix components further comprises sorbitan oleate.
24. The composition of claim 1 wherein the one or more hydrophobic matrix components further comprises a sorbitan ester.
25. The composition of claim 1 wherein the one or more hydrophobic matrix components further comprises sorbitan oleate.