Oral liquid compositions of guanfacine

Patent metadata

Field	Value
Publication number	US-2016346235-A1
Application number	US-201615144026-A
Country	US
Kind code	A1
Filing date	May 2, 2016
Priority date	May 1, 2014
Publication date	Dec 1, 2016
Grant date	—

Abstract

The present invention relates to oral liquid compositions of guanfacine. The liquid. compositions can be immediate release or extended release compositions. The compositions comprise guanfacine in a concentration from about 0.1 mg/mL to about 12.0 mg/mL of the composition. The liquid compositions can be in the form of ready-to use liquid compositions or reconstituted liquid compositions. It further relates to processes for the preparation of said oral liquid compositions.

First claim

1 . An oral liquid composition comprising guanfacine in a pharmaceutically acceptable carrier.

2 . An oral liquid composition comprising guanfacine in a pharmaceutically acceptable carrier, wherein the composition comprises guanfacine in a concentration from about 0.1 mg/mL to about 12.0 mg/mL of the composition.

3 . The oral liquid composition of claim 2 , wherein the composition comprises guanfacine in a concentration from about 1.0 mg/mL to 7.0 mg/mL of the composition.

4 . An oral liquid composition comprising guanfacine in a pharmaceutically acceptable carrier, wherein the composition is a stable composition.

5 . The oral liquid composition of claim 4 , wherein the composition comprises less than about 1.0% w/w of 2,6-dichlorophenyl acetic acid.

6 . The oral liquid composition of claim 5 , wherein the composition comprises less than about 0.7% w/w of 2,6-dichlorophenyl acetic acid.

7 . The oral liquid composition of claim 4 , wherein the composition comprises less than about 3.0% w/w of total related substances.

8 . The oral liquid composition of claim 7 , wherein the composition comprises less than about 2.0% w/w of total related substances.

9 . The oral liquid composition of claim 1 , wherein the composition has a pH of less than about 6.8.

10 . The oral liquid composition of claim 1 , wherein the composition is a ready-to-use liquid composition or a reconstituted liquid composition.

11 . The oral liquid composition of claim 10 , wherein the ready-to-use liquid composition comprises a solution, a suspension, a syrup, a concentrate, an elixir, or an emulsion.

12 . The oral liquid composition of claim 10 , wherein the reconstituted liquid composition comprises a solution and/or a suspension reconstituted from powder comprising granules, pellets, or beads.

13 . The oral liquid composition of claim 1 , wherein guanfacine is present in an immediate release form.

14 . The oral liquid composition of claim 13 , wherein guanfacine is present as powder, pellets, granules, beads.

15 . The oral liquid composition of claim 13 , wherein guanfacine is present as guanfacine-resin complex.

16 . The oral liquid composition of claim 13 , wherein guanfacine is layered over inert cores.

17 . The oral liquid composition of claim 1 , wherein guanfacine is present in an extended release form.

18 . The oral liquid composition of claim 17 , wherein the composition comprises:
(i) cores comprising guanfacine and a release-controlling agent; and (ii) a pharmaceutically acceptable carrier.

19 . The oral liquid composition of claim 18 , wherein guanfacine is present in the core or layered over an inert particle to form a core.

20 . The oral liquid composition of claim 18 , wherein release-controlling agent is present in the core or coated over the guanfacine core or both.

21 . The oral liquid composition of claim 20 , wherein the release-controlling agent is selected from the group consisting of a pH-dependent release-controlling agent, a pH-independent release-controlling agent, and mixtures thereof.

22 . The oral liquid composition of claim 21 , wherein the pH-dependent release-controlling agent is selected from the group consisting of acrylic copolymers, methacrylic acid and ethyl acrylate copolymers; cellulosic polymers; vinyl polymers; polyvinyl derivatives; zein; shellac; and combinations thereof.

23 . The oral liquid composition of claim 21 , wherein the pH-independent release-controlling agent is selected from the group consisting of cellulosic polymers; acrylic copolymers; polyethylene derivatives; polyvinyl alcohol; polyvinyl acetate; gums; triglycerides; waxes; lipids; fatty acids or their salts/derivatives; polyvinyl polymers; polyvinyl acetate and polyvinyl pyrrolidone mixtures; and combinations thereof.

24 . The oral liquid composition of claim 18 , wherein the core further comprises pharmaceutically acceptable excipients selected from the group consisting of acids, osmogents, binders, glidants, and combinations thereof.

25 . The oral liquid composition of claim 17 , wherein the composition further comprises guanfacine in an immediate release form.

26 . The oral liquid composition of claim 1 , wherein the pharmaceutically acceptable carrier comprise one or more liquid adjuvants and other pharmaceutically acceptable excipients.

27 . The oral liquid composition of claim 26 , wherein the other pharmaceutically acceptable excipients are selected from the group comprising acids, osmogents, buffering agents, suspending agents, glidants, sweetening agents, flavors, colorants, anti-caking agents, wetting agents, preservatives, antioxidants, chelating agents, binders, viscosity modifiers, emulsifiers and combinations thereof.

28 . A method of treating Attention Deficit Hyperactivity Disorder or Hypertension by administering the oral liquid composition of claim 1 .

29 . A method of treating Attention Deficit Hyperactivity Disorder or Hypertension, wherein the oral liquid composition of claim 1 is administered once daily.

Assignees

• Sun Pharmaceutical Ind Ltd

Inventors

• Singh Romi Barat
• Ramaraju Kalaiselvan
• Mondal Balaram
• Kumar Ashish
• Kaushik Suchitra

Classifications

• A61P9/12

  Antihypertensives · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P25/14

  for treating abnormal movements, e.g. chorea, dyskinesia · CPC title

• A61P31/12

  Antivirals · CPC title

• A61P31/04

  Antibacterial agents · CPC title