Granted Patent B2

US 12,636,289 · App. 18/170,185 · Granted May 26, 2026

Inventors: Paul Sudhakar (Shawnee, KS); Scott Boyer (West Chicago, IL)

A61K31/53A61K9/0053A61K47/02A61K47/06A61K47/10A61K47/26A61K47/34A61K47/36A61K47/38

Abstract

Claims (97)

1 . An oral liquid suspension comprising:

3,5-diamino-6-(2,3-dichlorophenyl)-as-triazine (lamotrigine);

water;

glycerin;

propylene glycol;

polyethylene glycol;

methylparaben;

sodium benzoate;

sorbitol;

saccharin;

sucralose;

xanthan gum;

carboxymethyl cellulose;

sodium phosphate;

microcrystalline cellulose; and

colloidal silicon dioxide

wherein,

the lamotrigine comprises less than about 8 wt % lamotrigine hydrate;

the oral liquid suspension has a viscosity at 25° C. of 100-200 mP;

the oral liquid suspension is packaged in a glass or plastic bottle and the packaging further includes a syringe or cup, marked in mL, ounces, or both;

the oral liquid suspension is packaged in a glass or plastic bottle configured for use to administer multiple doses of lamotrigine;

the oral liquid suspension, while packaged in the container, is free from microbial contamination for at least 90 days under ambient conditions, wherein the microbial contamination includes less than 0.1 wt. % Escherichia coli ( E. coli ) and less than 0.1 wt. % Burkholderia cepacia complex (BCC); and

the oral liquid suspension is an immediate release dosage form that exhibits in-vitro dissolution rate more than 85% of drug release within 15 minutes, when said dosage form is placed in a dissolution vessel filled with 900 ml of 0.1N HCl, pH 1.2 maintained at 37±0.5° C. and stirred at a paddle speed of 50 rpm using a USP Type II (paddle) apparatus.

2 . The oral liquid suspension of claim 1 , wherein the lamotrigine is present in 10 mg/mL.

3 . The oral liquid suspension of claim 1 , wherein the lamotrigine present in the oral liquid suspension has the following particle size distribution (PSD):

D 90 of not more than 200 microns,

D 50 of not more than 100 microns, and

D 10 of not more than 30 microns.

4 . The oral liquid suspension of claim 1 , wherein the lamotrigine present in the oral liquid suspension has the following particle size distribution (PSD):

D 90 of not more than 140 microns,

D 50 of not more than 63 microns, and

D 10 of not more than 26 microns.

5 . The oral liquid suspension of claim 1 , having a viscosity at 25° C. of 117.5±10 mPs.

6 . The oral liquid suspension of claim 1 , having a pH of 6.5-8.0.

7 . The oral liquid suspension of claim 1 , having a pH of 7.1-7.2.

8 . The oral liquid suspension of claim 1 , having a specific gravity of not more than 1.2.

9 . The oral liquid suspension of claim 1 , having a specific gravity of not more than 1.03.

10 . The oral liquid suspension of claim 1 , further comprising a flavoring agent.

11 . The oral liquid suspension of claim 1 , further comprising cherry flavor as a flavoring agent.

12 . The oral liquid suspension of claim 1 , further comprising a coloring agent.

13 . The oral liquid suspension of claim 1 , further comprising FD&C red #40 and FD&C yellow #6 as a coloring agent.

14 . The oral liquid suspension of claim 1 , comprising:

1±0.1% (w/v) 3,5-diamino-6-(2,3-dichlorophenyl)-as-triazine (lamotrigine);

84.75±8.5% (w/v) water;

3.25±0.33% (w/v) glycerin (99% natural);

2.25±0.23% (w/v) propylene glycol;

3.00±0.3% (w/v) polyethylene glycol 400;

0.1±0.01% (w/v) methylparaben;

0.03±0.003% (w/v) sodium benzoate powder;

2.1±0.21% (w/v) sorbitol (3% of 70% solution);

0.08±0.008% (w/v) saccharin sodium dihydrate powder;

0.75±0.08% (w/v) sucralose;

0.20±0.02% (w/v) xanthan gum;

0.10±0.01% (w/v) sodium carboxymethyl cellulose (medium viscosity 2% aqueous solution at 25° C. 400-800 cPs);

0.03±0.01% (w/v) sodium phosphate dibasic (dried);

1.26±0.15% (w/v) microcrystalline cellulose and colloidal silicon dioxide;

0.2±0.02% (w/v) cherry flavor;

0.002±0.0002% (w/v) FD&C red #40; and

0.0002±0.00002% (w/v) FD&C yellow #6.

15 . The oral liquid suspension of claim 1 , having a volume of 0.2 mL, 0.5 mL, 2.5 mL, 10 mL, 15 mL, or 20 mL.

16 . The oral liquid suspension of claim 1 , while packaged in a container, is essentially free from microbial growth for at least 24 months under ambient conditions.

17 . The oral liquid suspension of claim 1 , while packaged in a container, is essentially free from Escherichia coli ( E. coli ) for at least 24 months under ambient conditions.

18 . The oral liquid suspension of claim 1 , while packaged in a container, is essentially free from Burkholderia cepacia complex (BCC) for at least 24 months under ambient conditions.

19 . The oral liquid suspension of claim 1 , which is an immediate release dosage form.

20 . The oral liquid suspension of claim 1 , wherein the oral liquid suspension exhibits redispersibility, such that upon turning over 3 times, the oral liquid suspension exhibits at least 90% redispersibility.

21 . The oral liquid suspension of claim 1 , wherein the oral liquid suspension exhibits redispersibility, such that upon turning over 3 times, the oral liquid suspension exhibits at least 95% redispersibility.

22 . The oral liquid suspension of claim 1 , wherein the oral liquid suspension is packaged in a glass bottle, an amber colored polyethylene terephthalate (PET) bottle, a high density polyethylene (HDPE) bottle, a low density polyethylene (LDPE) bottle, or a polypropylene (PP) bottle.

23 . The oral liquid suspension of claim 1 , wherein the oral liquid suspension is packaged in a glass or plastic bottle with a child proof closure.

24 . An oral liquid suspension comprising:

1±0.1% (w/v) 3,5-diamino-6-(2,3-dichlorophenyl)-as-triazine (lamotrigine);

84.75±8.5% (w/v) water;

3.25±0.33% (w/v) glycerin (99% natural);

2.25±0.23% (w/v) propylene glycol;

3.00±0.3% (w/v) polyethylene glycol 400;

0.1±0.01% (w/v) methylparaben;

0.03±0.003% (w/v) sodium benzoate powder;

2.1±0.21% (w/v) sorbitol (3% of 70% solution);

0.08±0.008% (w/v) saccharin sodium dihydrate powder;

0.75±0.08% (w/v) sucralose;

0.20±0.02% (w/v) xanthan gum;

0.10±0.01% (w/v) sodium carboxymethyl cellulose (medium viscosity 2% aqueous solution at 25° C. 400-800 cPs);

0.03±0.01% (w/v) sodium phosphate dibasic (dried); and

1.26±0.15% (w/v) microcrystalline cellulose and colloidal silicon dioxide; wherein,

the lamotrigine comprises less than about 8 wt % lamotrigine hydrate;

the oral liquid suspension has a viscosity at 25° C. of 100-200 mP;

the oral liquid suspension is packaged in a glass or plastic bottle and the packaging further includes a syringe or cup, marked in mL, ounces, or both;

the oral liquid suspension is packaged in a glass or plastic bottle configured for use to administer multiple doses of lamotrigine;

the oral liquid suspension, while packaged in the container, is free from microbial contamination for at least 90 days under ambient conditions, wherein the microbial contamination includes less than 0.1 wt. % Escherichia coli ( E. coli ) and less than 0.1 wt. % Burkholderia cepacia complex (BCC);

the oral liquid suspension is an immediate release dosage form that exhibits in-vitro dissolution rate more than 85% of drug release within 15 minutes, when said dosage form is placed in a dissolution vessel filled with 900 ml of 0.1N HCl, pH 1.2 maintained at 37±0.5° C. and stirred at a paddle speed of 50 rpm using a USP Type II (paddle) apparatus;

the oral liquid suspension exhibits redispersibility, such that upon turning over 3 times, the oral liquid suspension exhibits at least 90% redispersibility;

the oral liquid suspension is packaged in a glass bottle, an amber colored polyethylene terephthalate (PET) bottle, a high density polyethylene (HDPE) bottle, a low density polyethylene (LDPE) bottle, or a polypropylene (PP) bottle;

the oral liquid suspension is packaged in a glass or plastic bottle with a child proof closure; and

the lamotrigine present in the oral liquid suspension has the following particle size distribution (PSD):

D 90 of not more than 200 microns,

D 50 of not more than 100 microns, and

D 10 of not more than 30 microns.

25 . The oral liquid suspension of claim 24 , having a viscosity at 25° C. of 117.5±10 mP.

Assignments (2)

Continuity (3)

References Cited (24)