PARENTERAL LIQUID PREPARATION COMPRISING CARBAMATE COMPOUND

• US 20190314336A1
• Filed: 12/14/2017
• Published: 10/17/2019
• Est. Priority Date: 12/14/2016
• Status: Active Application

• Current Assignee: SK Biopharmaceuticals Co., Ltd. (SK Inc.)
• Original Assignee: SK Biopharmaceuticals Co., Ltd. (SK Inc.)
• Inventors: BAEK, Myoung Ki, LEE, Ji Hye, CHOI, So Young
• Application Number:
  US16/468,756
• Publication Number:
  US 20190314336A1
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/325 Carbamic acids; Thiocarbamic acids; Anhydrides or salts thereof thiurams A61K31/145
• CPC Class Codes: A61K 31/41 having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
• CPC Class Codes: A61K 31/4192 1,2,3-Triazoles
• CPC Class Codes: A61K 47/40 Cyclodextrins; Derivatives thereof
• CPC Class Codes: A61K 47/6951 using cyclodextrin cyclodextrins used as simple excipients A61K47/40
• CPC Class Codes: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/08 Solutions composition of solutions A61K47/00
• CPC Class Codes: A61P 25/08 Antiepileptics; Anticonvulsants

Abstract

The present invention relates to a parenteral liquid preparation containing, as active ingredients; a carbamate compound of chemical formula 1, an isomer thereof, or a pharmaceutically acceptable salt, a solvate or a hydrate thereof; and a cyclodextrin derivative.

Claims

1. A parenteral liquid formulation comprising as an active ingredient a carbamate compound of the following Formula 1 or an isomer thereof, or a pharmaceutically acceptable salt, solvate or hydrate thereof;

and a cyclodextrin derivative;

2. The parenteral liquid formulation according to claim 1, wherein R₁ and R₂ are each independently selected from the group consisting of hydrogen, halogen and C₁-C₈ alkyl.

3. The parenteral liquid formulation according to claim 1, wherein the carbamate compound of Formula 1 is carbamic acid (R)-1-(2-chlorophenyl)-2-tetrazol-2-yl)ethyl ester of the following Formula 2:

4. The parenteral liquid formulation according to claim 1, wherein the cyclodextrin derivative is a hydroxyalkyl-cyclodextrin or sulfoalkyl ether-cyclodextrin.

5. The parenteral liquid formulation according to claim 4, wherein the hydroxyalkyl-cyclodextrin is 2-hydroxypropyl-β

-cyclodextrin, and the sulfoalkyl ether-cyclodextrin is sulfobutyl ether-β

-cyclodextrin.

6. The parenteral liquid formulation according to claim 1, which contains the carbamate compounds of Formula 1 in a concentration of 0.5 mg/ml to 20 mg/ml.

7. The parenteral liquid formulation according to claim 1, wherein the weight ratio of the carbamate compounds of Formula 1 to the cyclodextrin derivatives is about 1:

2 to 1;

50.

8. The parenteral liquid formulation according to claim 1, which contains carbamic acid (R)-1-(2-chlorophenyl)-2-tetrazol-2-yl)ethyl ester and 2-hydroxypropyl-β

-cyclodextrin in the weight ratio of 1;

2 to 1;

50.

9. The parenteral liquid formulation according to claim 1, which contains carbamic acid (R)-1-(2-chlorophenyl)-2-tetrazol-2-yl)ethyl ester and sulfobutyl ether-β

-cyclodextrin in the weight ratio of 1;

2 to 1;

50.

10. The parenteral liquid formulation according to claim 1, which is used as an anticonvulsant.

11. The parenteral liquid formulation according to claim 1, which is used for the treatment of anxiety, depression, convulsion, epilepsy, migraine, bipolar disorder, drug abuse, smoking, attention deficit hyperactivity disorder (ADHD), obesity, sleep disorders, neuropathic pain, stroke, cognitive disorders, neurodegeneration and muscle spasm.

12. An injection composition comprising a parenteral liquid formulation according to claim 1.

13. A method for preparing a parenteral liquid formulation, comprising mixing a carbamate compound of Formula 1 as defined in claim 1 and cyclodextrin derivatives in a solvent.

14. The method for preparing a parenteral liquid formulation according to claim 13, wherein the carbamate compound of Formula 1 is carbamic acid (R)-1-(2-chlorophenyl)-2-tetrazol-2-yl)ethyl ester of the following Formula 2:

15. The method for preparing a parenteral liquid formulation according to claim 13, wherein the cyclodextrin derivative is a hydroxyalkyl-cyclodextrin or sulfoalkyl ether-cyclodextrin.