IP Library Granted Patent US 12661360
Granted Patent B2
US 12661360 · App. 18/767,610 · Granted Jun 23, 2026

Ready to use non-aqueous solutions of lamotrigine

Inventors: Yu-Hsing Tu (West Windsor, NJ); Yingjun Fan (Plainsboro, NJ); Kalyan Kathala (Monroe, NJ); Ashok Perumal (South Brunswick, NJ); James A. Lee (West Windsor, NJ)
Assignee: Tulex Pharmaceuticals Inc.
A61K31/53A61K9/08A61K47/10
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Quick Facts
Patent No.
US 12661360
App. No.
18/767,610
Granted
Jun 23, 2026
Kind
B2
Abstract

Disclosed are ready to use non-aqueous solutions of lamotrigine. The lamotrigine is dissolved in a solvent, wherein the solvent comprises propylene glycol and optionally at least one co-solvent, and wherein if water is present in the ready to use non-aqueous solution, the water is not at least one co-solvent. Also disclosed are methods for treating a neurological disorder or a mental disorder by administering the ready to use non-aqueous solutions of lamotrigine, processes for preparing ready to use non-aqueous solutions of lamotrigine, and kits containing lamotrigine to prepare ready to use non-aqueous solutions of lamotrigine.

Claims (39)

1 . A ready to use solution, comprising lamotrigine dissolved in a solvent,

wherein the solvent comprises propylene glycol and at least one co-solvent comprising glycerin,

wherein the ready to use solution has a water content of equal to or less than about 20% w/w of the ready to use solution, and

wherein water is not the at least one co-solvent.

2 . The ready to use solution of claim 1 , wherein a concentration of lamotrigine in the ready to use solution is about 0.01 mg/mL to about 40 mg/mL.

3 . The ready to use solution of claim 1 , wherein a concentration of lamotrigine in the ready to use solution is about 20 mg/mL.

4 . The ready to use solution of claim 1 , wherein the water content is equal to or less than about 1% w/w of the ready to use solution.

5 . The ready to use solution of claim 1 , wherein the at least one co-solvent further comprises at least one selected from the group consisting of polypropylene glycol, polyethylene glycol, and ethanol.

6 . The ready to use solution of claim 1 , wherein water is not present in the ready to use solution.

7 . The ready to use solution of claim 1 , wherein a weight ratio of propylene glycol to glycerin is 80:20 to 20:80.

8 . The ready to use solution of claim 1 , wherein a propylene glycol content is about 45% to about 87% w/w of the ready to use solution.

9 . The ready to use solution of claim 1 , wherein a glycerin content is about 11% to about 60% w/w of the ready to use solution.

10 . The ready to use solution of claim 1 , wherein a propylene glycol content is about 45% to about 55% w/w of the ready to use solution and a glycerin content is about 45% to about 55% w/w of the ready to use solution.

11 . The ready to use solution of claim 1 , further comprising ethyl maltol.

12 . The ready to use solution of claim 1 , wherein the ready to use solution has a pH meter reading from about 7.5 to about 7.8.

13 . The ready to use solution of claim 1 , wherein the ready to use solution has a viscosity from 200 centipoise to about 300 centipoise.

14 . The ready to use solution of claim 1 , wherein the ready to use solution has a density from about 1.1 g/mL to about 1.2 g/mL.

15 . A ready to use solution, comprising:

about 15 mg/mL to about 25 mg/mL of lamotrigine; and

a solvent, the solvent comprising:

about 45% to about 55% w/w of propylene glycol; and

about 45% to about 55% w/w of glycerin,

wherein the ready to use solution has a water content of equal to or less than about 20% w/w of the ready to use solution, and

wherein water is not the solvent.

16 . The ready to use solution of claim 15 , wherein a concentration of lamotrigine in the ready to use solution is about 20 mg/mL.

17 . A method for treating a disorder, comprising administering orally to a human subject in need thereof a ready to use solution, wherein the ready to use solution includes about 2 mg to about 700 mg of lamotrigine dissolved in a solvent, wherein the solvent comprises propylene glycol and at least one co-solvent comprising glycerin, wherein the ready to use solution has a water content of equal or less than about 20% w/w of the ready to use solution, wherein water is not the at least one co-solvent, and wherein the disorder is epilepsy or bipolar disorder.

18 . The method of claim 17 , wherein the disorder is epilepsy.

19 . The method of claim 17 , wherein the disorder is bipolar disorder.

20 . The method of claim 18 , wherein the epilepsy disorder includes partial seizures, tonic-clonic seizures, and/or seizures of Lennox-Gastaut syndrome.

21 . The method of claim 19 , wherein the bipolar disorder is a bipolar I disorder.

22 . The method of claim 17 , comprising administering about 2 mg to about 500 mg of lamotrigine.

23 . The method of claim 17 , wherein the administering results in a C max value from about 800 ng/ml to about 1,000 ng/ml of lamotrigine in the subject.

24 . The method of claim 17 , wherein the administering results in an AUC value from about 35,000 ng/mL*hr to about 40,000 ng/mL*hr of lamotrigine in the subject.

25 . The method of claim 21 , wherein the therapeutically effective amount is administered after fasting.

26 . The method of claim 21 , wherein the therapeutically effective amount is administered after a meal.

27 . The method of claim 17 , wherein a concentration of lamotrigine in the ready to use solution is about 0.01 mg/mL to about 40 mg/mL.

28 . The method of claim 17 , wherein a concentration of lamotrigine in the ready to use solution is about 20 mg/mL.

29 . The method of claim 17 , wherein water is not present in the ready to use solution.

30 . The method of claim 17 , wherein a propylene glycol content is about 45% to about 55% w/w of the ready to use solution and a glycerin content is about 45% to about 55% w/w of the ready to use solution.