IP Library Granted Patent US 10,561,621
Granted Patent B2
US 10,561,621 · App. 13/825,026 · Granted Feb 18, 2020

Microencapsulation process and product

Inventors: Diane Goll (Grand Haven, MI); Cecil W. Propst (Norton Shores, MI)
A61K9/5057A61K9/5031A61K9/5036A61K9/5042A61K9/5052
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Quick Facts
Patent No.
US 10,561,621
App. No.
13/825,026
Granted
Feb 18, 2020
Kind
B2
Abstract

A composition comprising a core material, having a taste value and a polymeric coating. The polymeric coating substantially surrounds the core material and comprises a cationic polymer and optionally an anionic polymer. The polymeric coating has a uniform thickness ranging from 2 μm to 20 μm. The composition provides release of a portion of the core material which is taste masked over a time period ranging from 0.5 minute to 2 minutes in the oral cavity and provides a modified-release of the remaining core material in a gastrointestinal tract.

Claims (20)

1. A composition comprising:

a core material consisting of one or more active pharmaceutical ingredients, the core material having a taste value; and

a polymeric coating substantially surrounding the core material, said polymeric coating comprising a coacervated polymer material comprising a cationic polymer and an anionic polymer mixture, the anionic polymer mixture including medium chain polyphosphates and long chain polyphosphates in a ratio of about 60:40, wherein said polymeric coating has a uniform thickness ranging from 1 μm to 20 μm, and

wherein said composition provides a controlled release of a portion of the core material which is taste masked over a time period ranging from 0.5 minute to 2 minutes in the oral cavity and provides modified-release of the remaining core material in a gastrointestinal tract.

2. The composition of claim 1 , wherein the composition has a microcapsule form.

3. The composition of claim 1 , wherein the polymeric coating is hydrophilic.

4. The composition of claim 1 , wherein said uniform thickness of the polymeric coating ranges from 2 μm to 5 μm.

5. The composition of claim 1 , wherein said polymeric coating further comprises a crosslinking agent.

6. The composition of claim 1 , wherein said one or more active pharmaceutical ingredients include an active pharmaceutical ingredient selected from the group consisting of: acetaminophen, ibuprofen, dexibuprofen lysinate, naproxen, loperamide, dimenhydrinate, doxylamine, dextromethorphan and chlorpheniramine.

7. The composition of claim 1 , wherein said cationic polymers are independently selected from the group consisting of: gelatin type A, gelatin type B, gelatin hydrolysates, gelatin succinylates, ovalbumin, serum albumin, casein, chitin, polyvinylamine, cellulose derivatives, and mixtures thereof.

8. The composition of claim 7 , wherein the cationic polymer is independently selected from the group consisting of: gelatin type A, gelatin type B, gelatin hydrolysates, gelatin succinylates and mixtures thereof.

9. The composition of claim 1 , wherein the core material has a water solubility taste threshold and an associated pH of less than or equal to 6; and wherein the polymeric coating is derived from a material having a pH value less than or equal to the associated pH of the water solubility taste threshold.

10. The composition of claim 9 , wherein the water solubility taste threshold ranges from 1×10 −4 mol/L to 1×10 −1 mol/L.

11. The composition of claim 1 , wherein the core material has a water solubility taste threshold and an associated pH of greater than or equal to 6; and wherein the polymeric coating is derived from a material having a pH value less than or equal to the associated pH of the water solubility taste threshold.

12. The composition of claim 11 , wherein the water solubility taste threshold ranges from 1×10 −4 mol/L to 1×10 −1 mol/L.

13. A pharmaceutical formulation comprising the composition according to claim 1 and further comprising one or more pharmaceutically acceptable ingredients independently selected from the group consisting of: excipients, binders, lubricants, disintegrating agents, sugar alcohols, colors, flavors and combinations thereof.

14. The composition of claim 1 , wherein the ratio of cationic polymer to the anionic polymer mixture ranges from 8:1 to 20:1.

15. The composition of claim 1 , wherein the ratio of cationic polymer to the anionic polymer mixture ranges from 9:1 to 11:1.

16. The composition of claim 1 , wherein the core material consisting of one or more active pharmaceutical ingredients makes up 80 wt. % to 95 wt. % of the composition.

17. The composition of claim 16 , wherein the polymeric coating makes up 5 wt. % to 20 wt. % of the composition.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 20, 2014
From: GOLL, DIANE; PROPST, CECIL W.
To: SPI PHARMA, INC.
Reel/Frame 032713/0389 →
Continuity (2)
Provisional Application 61384351 · Sep 20, 2010
Related Publication 20140044793A1 · Feb 13, 2014