ACIDIFYING COATINGS AND DISINTEGRATION-RESISTANT SUBSTRATES COATED THEREWITH

• US 20190314286A1
• Filed: 03/29/2019
• Published: 10/17/2019
• Est. Priority Date: 04/12/2018
• Status: Active Grant

• Current Assignee: BPSI Holdings, LLC
• Original Assignee: BPSI Holdings, LLC
• Inventors: Mehta, Raxitkumar Y., Reyes, George, Teckoe, Jason, To, Daniel
• Granted Patent: US 10,758,489 B2
• Time in Patent Office: Days
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2846 Poly(meth)acrylates
• CPC Class Codes: A61K 9/2853 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2886 having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer of the type active core-drug layer-inactive layer A61K9/209
• CPC Class Codes: A61K 9/2893 Tablet coating processes mechanical aspects A61J3/06
• CPC Class Codes: C08K 2003/2241 Titanium dioxide
• CPC Class Codes: C08K 5/09 Carboxylic acids; Metal salts thereof; Anhydrides thereof
• CPC Class Codes: C08K 5/092 Polycarboxylic acids
• CPC Class Codes: C08K 5/51 Phosphorus bound to oxygen
• CPC Class Codes: C08L 1/04 Oxycellulose; Hydrocellulose , e.g. microcrystalline cellulose
• CPC Class Codes: C08L 1/284 with hydroxylated hydrocarbon radicals
• CPC Class Codes: C08L 3/02 Starch; Degradation products thereof, e.g. dextrin
• CPC Class Codes: C09D 101/284 with hydroxylated hydrocarbon radicals
• CPC Class Codes: C09D 101/286 substituted with acid radicals C09D101/282 takes precedence
• CPC Class Codes: C09D 7/63 organic

Abstract

The present invention includes acidifying film coating compositions containing a polymer and an acidic component for use on orally-ingestible substrates such as tablets and the like. The acidifying coating compositions can be applied as an aqueous dispersion to an enteric-coated substrate to increase the disintegration resistance to aqueous media of up to pH 5.0. In preferred aspects, the acidic component is citric acid, lactic acid, stearic acid or mixtures thereof. Methods of preparing the dry film coatings, methods of preparing corresponding aqueous dispersions, methods of applying the coatings to substrates and the coated substrates themselves are also disclosed.

Claims

1. A dry, acidifying coating composition comprising a polymer and an acidic component.

2. The composition of claim 1, wherein the polymer is selected from the group consisting of hypromellose (hydroxypropylmethyl cellulose or HPMC), hydroxypropyl cellulose (HPC), sodium carboxymethyl cellulose, polyvinyl alcohol (PVA), polyvinyl alcohol-polyethylene glycol graft copolymer, other copolymers based on PVA and mixtures thereof.

3. The composition of claim 1, wherein the acidic component comprises ionizable hydrogen ions.

4. The composition of claim 3, wherein the acidic component is selected from the group of citric acid, lactic acid, stearic acid and mixtures thereof.

5. The composition of claim 1, wherein the polymer is about 10-90% by weight of the composition.

6. The composition of claim 5, wherein the polymer is about 25-85% by weight of the composition.

7. The composition of claim 6, wherein the polymer is about 30-80% by weight of the composition.

8. The composition of claim 1, wherein the acidic component is about 5-50% by weight of the composition.

9. The composition of claim 8, wherein the acidic component is about 8-45% by weight of the composition.

10. The composition of claim 1, further comprising one or more of a plasticizer, detackifier, pigment or surfactant.

11. A composition of claim 10, wherein the polymer is present in an amount of from about 25 to about 85% by weight of the composition;

the amount of the acidic component is present in an amount of from about 8 to about 45% by weight of the composition;

the plasticizer is present in an amount of from about 2 to about 18% by weight of the polymer; and

the detackifier is present in an amount of from about 5 to about 45% by weight of the composition.

12. An aqueous dispersion comprising the composition of claim 1 and water.

13. The aqueous dispersion of claim 12, further comprising one or more of a plasticizer, a detackifier, a pigment and a surfactant, added as part of the dry coating composition.

14. The aqueous dispersion of claim 12, further comprising one or more of a plasticizer, a detackifier, a pigment and a surfactant, added separately to the aqueous dispersion.

15. An orally-ingestible substrate coated with the aqueous dispersion of claim 12.

16. The orally-ingestible substrate of claim 15, further comprising an enteric coating beneath the acidifying coating.

17. The orally-ingestible substrate of claim 16, further comprising a subcoat between the orally-ingestible substrate and the enteric coating.

18. The orally-ingestible substrate of claim 17, wherein the enteric coating comprises a partially neutralized enteric polymer.

19. The orally-ingestible substrate of claim 18, wherein the partially neutralized enteric polymer is a partially neutralized methacrylic acid copolymer.

20. The orally-ingestible substrate of claim 19, wherein the partially neutralized methacrylic acid copolymer comprises about 40 to 75% by weight of the enteric coating composition on a dry basis.

21. An orally-ingestible substrate, substantially resistant to disintegration in a pH 5.0 medium, comprising:

i) a core portion containing a drug or active ingredient;

ii) an enteric coating portion, substantially enveloping said core portion, the enteric coating comprising a partially neutralized enteric polymer; and

iii) an acidifying topcoat substantially enveloping said enteric coating portion.

22. The orally-ingestible substrate of claim 21, further comprising a subcoat between the drug containing core and enteric coating comprising a partially neutralized enteric polymer.

23. The orally-ingestible substrate of claim 21, wherein the partially neutralized enteric polymer is a partially neutralized methacrylic acid copolymer.

24. An orally-ingestible substrate of claim 21, wherein the core portion comprises from about 50 to about 90% by weight;

the enteric coating portion comprises from about 8 to about 40% by weight and the acidifying topcoat comprises from about 2 to about 30% by weight.

25. The orally-ingestible substrate of claim 24, wherein the acidifying topcoat comprises from about 3 to about 25% by weight.

26. A method of preparing an orally-ingestible substrate which is substantially resistant to disintegration in a pH 5.0 medium comprising the steps of:

i) providing a drug containing core;

ii) applying an enteric coating on the drug containing core; and

iii) applying an acidifying topcoat over the enteric coating.

27. The method of claim 26, further comprising the step of applying a subcoat between the drug containing core and enteric coating.