IP Library › Granted Patent US 12,521,352
Granted Patent B2
US 12,521,352 · App. 17/313,408 · Granted Jan 13, 2026

Taste masking drug formulations

Inventors: Cory Berkland (Lawrence, KS); Milind Singh (Apex, NC)
Assignee: Adare Pharmaceuticals USA, Inc.
A61K9/5026A61K9/0053A61K9/5015A61K9/5063A61K9/5089A61K31/426A61K31/573A61K47/10
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Quick Facts
Patent No.
US 12,521,352
App. No.
17/313,408
Granted
Jan 13, 2026
Kind
B2
Abstract

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.

Claims (21)

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 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,

wherein the hydrophobic matrix comprises one or more hydrophobic matrix components,

wherein at least one of the one or more hydrophobic matrix components is a wax, a lipid, or a glycerol fatty acid ester,

wherein the shell portion encapsulates the core portion, and

wherein upon encountering the acidic environment of the stomach and/or gastrointestinal tract, the active pharmaceutical ingredient is fully released from the composition by about 30 minutes.

2 . The composition of claim 1 , wherein the hydrophilic excipient is one or more selected from the group consisting of polyethylene glycol, polyols, poloxamer block copolymers, and lutrol block copolymers.

3 . The composition of claim 1 , wherein the active pharmaceutical ingredient is hydrophobic.

4 . The composition of claim 1 , wherein the hydrophobic matrix further comprises one or more of a stearyl alcohol, a high weight molecular weight glycol with a minimum of 20 repeating units, a cellulose ether, a cellulose ester, a poloxamer, a starch, a gelatin, or a stearic acid.

5 . 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, hypromellose phthalate, polyacrylate derivative or polymethacrylate derivative.

6 . The composition of claim 1 , comprising a plurality of the microcapsules having a mean particle diameter from about 50 μm to about 500 μm, wherein at least 80% of the microcapsules have a particle diameter within 25% of the mean particle diameter of the plurality of microcapsules.

7 . 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.

8 . The composition of claim 1 , comprising a plurality of the microcapsules in a liquid suspension.

9 . The composition of claim 1 , comprising a plurality of the microcapsules formulated as a dry powder.

10 . The composition of claim 1 , wherein the shell portion comprises from about 1% to about 50% by weight of the pH-responsive material.

11 . The composition of claim 1 , wherein the shell portion comprises from about 1% to about 10% by weight of the hydrophobic matrix components.

12 . The composition of claim 1 , wherein the active pharmaceutical ingredient and the hydrophilic excipient present in the core are in the form of a co-melt.

13 . The composition of claim 1 , wherein the composition is formulated as a liquid suspension, a chewable tablet, or an effervescent tablet.

14 . The composition of claim 1 , wherein the shell portion is free of the active pharmaceutical ingredient.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 6, 2021
From: BERKLAND, CORY; SINGH, MILIND
To: ORBIS BIOSCIENCES, INC.
Reel/Frame 056159/0804 →
CHANGE OF NAME Recorded May 6, 2021
From: ORBIS BIOSCIENCES, INC.
To: ADARE PHARMACEUTICALS USA, INC.
Reel/Frame 056166/0506 →
Continuity (5)
Continuation 16542986 · Aug 16, 2019
Division 15244455 · Aug 23, 2016
Continuation PCTUS2015017485 · Feb 25, 2015
Provisional Application 61944152 · Feb 25, 2014
Related Publication 20210251909A1 · Aug 19, 2021
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