Silica-based antimicrobial oral compositions

Patent metadata

Field	Value
Publication number	US-10959922-B2
Application number	US-201615275541-A
Country	US
Kind code	B2
Filing date	Sep 26, 2016
Priority date	Sep 28, 2015
Publication date	Mar 30, 2021
Grant date	Mar 30, 2021

Abstract

Oral compositions containing a carrier, a cationic antimicrobial compound, and a silica and/or silicate material are disclosed. These compositions can provide a controlled release of the antimicrobial compound.

First claim

We claim:

1. An oral composition comprising:
(i) a carrier;
(ii) from about 0.02 to about 2 wt. % of a cationic antimicrobial compound; and
(iii) from about 0.5 to 3 wt. % of a silica and/or silicate material characterized by:
an average particle size in a range from about 0.1 to about 20 μm;
a CTAB surface area in a range from about 250 to about 350 m 2 /g; and
an absorptive capacity of the cationic antimicrobial compound in a range from about 200 to about 400 mg of the cationic antimicrobial compound per gram of the silica and/or silicate material.

2. The composition of claim 1 , wherein:
the silica and/or silicate material comprises a precipitated silica having an absorptive capacity of the cationic antimicrobial compound in a range from about 210 to about 325 mg/g; and
the cationic antimicrobial compound comprises an antimicrobial quaternary ammonium compound.

3. The composition of claim 1 , wherein the silica and/or silicate material comprises an alkali metal aluminosilicate characterized by:
an average particle size in a range from about 0.5 μm to about 10 μm;
a CTAB surface area in a range from about 250 m 2 /g to about 350 m 2 /g; and
a BET surface area in a range from about 200 m 2 /g to about 800 m 2 /g.

4. The composition of claim 1 , wherein the silica and/or silicate material comprises a precipitated silica characterized by:
an average particle size in a range from about 0.5 μm to about 6 μm; and
a BET surface area in a range from about 250 m 2 /g to about 700 m 2 /g.

5. The composition of claim 4 , wherein the cationic antimicrobial compound comprises cetylpyridinium chloride (CPC).

6. The composition of claim 1 , wherein:
the carrier comprises water; and
the composition comprises from about 0.1 to about 1 wt. % of the cationic antimicrobial compound and from about 0.5 to 3 wt. % of the silica and/or silicate material.

7. The composition of claim 1 , wherein:
the carrier comprises a dentifrice composition; and
the oral composition comprises from about 0.1 to about 1 wt. % of the cationic antimicrobial compound and from about 0.5 to 3 wt. % of the silica and/or silicate material.

8. The composition of claim 1 , wherein the composition is in the form of a mouthwash, a mouth rinse, a mouth spray, a chewing gum, a breath strip, a lozenge, a candy, a tablet, a mint, a toothpaste, a gel, an edible film, or a whitening strip.

9. The composition of claim 1 , wherein the composition further comprises an additive comprising a humectant, a binder, a flavoring agent, an anti-cavity agent, a colorant, a sweetener, a surfactant, a thickener, a preservative, or combinations thereof.

10. The composition of claim 1 , wherein the composition further comprises an abrasive silica material characterized by:
a CTAB surface area in a range from about 1 to about 60 m 2 /g; and
an absorptive capacity of the cationic antimicrobial compound in a range from about 2 to about 100 mg of the cationic antimicrobial compound per gram of the abrasive silica material.

11. The composition of claim 10 , wherein the composition comprises from about 5 to about 25 wt. % of the abrasive silica material.

12. A method of reducing or inhibiting microbial growth in an oral cavity of a subject, the method comprising administering an effective amount of the composition of claim 1 to the oral cavity of the subject.

13. The method of claim 12 , wherein:
the subject is a human; and
the effective amount is in a range from about 0.25 to about 25 grams.

14. The method of claim 12 , wherein:
the subject is a human; and
the effective amount is an amount sufficient for a controlled release of at least 1 ppm of the cationic antimicrobial compound for a controlled release time period in a range from about 15 min to about 12 hr.

15. An oral composition comprising:
(a) a carrier; and
(b) from about 0.5 to 4.5 wt. % of treated particles comprising:
(I) a silica and/or silicate material; and
(II) 0.1 to 1 wt. % of a cationic antimicrobial compound comprising cetylpyridinium chloride; wherein:

the silica and/or silicate material has an absorptive capacity of the cationic antimicrobial compound in a range from about 200 to about 400 mg of the cationic antimicrobial compound per gram of the silica and/or silicate material; and
the treated particles comprise the cationic antimicrobial compound at an amount in a range from about 50% to about 200% of the absorptive capacity; and
the silica and/or silicate material is characterized by:
an average particle size in a range from about 0.5 μm to about 6 μm;
a CTAB surface area in a range from about 250 m 2 /g to about 350 m 2 /g; and
a BET surface area in a range from about 250 m 2 /g to about 700 m 2 /g.

16. The composition of claim 15 , wherein the treated particles comprise the cationic antimicrobial compound at an amount in a range from about 75% to about 150% of the absorptive capacity.

17. The composition of claim 15 , wherein:
the silica and/or silicate material comprises a precipitated silica having an absorptive capacity of the cationic antimicrobial compound in a range from about 210 to about 325 mg/g; and
the composition comprises from about 1 to 3 wt. % of the precipitated silica.

18. The composition of claim 15 , wherein the composition further comprises from about 5 to about 15 wt. % of an abrasive silica material characterized by:
a CTAB surface area in a range from about 1 to about 35 m 2 /g; and
an absorptive capacity of the cationic antimicrobial compound in a range from about 5 to about 40 mg of the cationic antimicrobial compound per gram of the abrasive silica material.

19. A method of reducing or inhibiting microbial growth in an oral cavity of a subject, the method comprising administering an effective amount of the composition of claim 15 to the oral cavity of the subject; wherein:
the effective amount is in a range from about 0.25 to about 25 grams; and/or
the effective amount is an amount sufficient for a controlled release of at least 1 ppm of the cationic antimicrobial compound for a controlled release time period in a range from about 30 min to about 8 hr.

20. The composition of claim 1 , wherein said composition is capable of providing a controlled release of at least 1 ppm of the cationic antimicrobial compound for a controlled release time period in a range from about 15 min to about 12 hr.

21. The composition of claim 20 , wherein the composition, when the antimicrobial compound is cetylpyridinium chloride and such composition is administered to the oral cavity of a subject, achieves a controlled release of greater or equal to two times the MIC of 1 ppm of the cetylpyridinium chloride for all nineteen washes.

Assignees

• Evonik Operations Gmbh

Inventors

• Nassivera Terry
• Gallis Karl
• Lundquist Eric
• Mauller Linda

Classifications

• A61K8/26

  Aluminium; Compounds thereof · CPC title

• A61K8/4926

  having six membered rings · CPC title

• A61K9/0053 Primary

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61K9/143

  with inorganic compounds · CPC title

• A61K8/04

  Dispersions; Emulsions · CPC title