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Sodium 4-hydroxybutyrate formulations

IP.com Disclosure Number: IPCOM000240274D
Publication Date: 2015-Jan-20
Document File: 4 page(s) / 33K

Publishing Venue

The IP.com Prior Art Database

Abstract

Sodium 4-hydroxybutyrate formulations

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This is the abbreviated version, containing approximately 55% of the total text.

Page 01 of 4

SODIUM 4-HYDROXYBUTYRATE FORMULATIONS


[0001] Sodium oxybate is an active pharmaceutical substance with a molecular formula of C4H7NaO3 and a molecular weight of 126.09 g/mole. Sodium oxybate is the international commonly accepted non-proprietary name for sodium 4-hydroxybutyrate, which is represented by Formula (I):


(I)


[0002] Sodium oxybate is an effective treatment of cataplexy and of excessive daytime sleepiness (EDS) in narcolepsy. It was approved by the FDA in 2002 under the brand name of XYREM™ in the form of 500mg/ml oral solution. Each mL of XYREM™ contains 500 mg of sodium oxybate in purified water, neutralized to pH 7.5 with malic acid.


[0003] The present document discloses oral solutions of sodium oxybate comprising 200mg/ml, 250mg/ml, 300mg/ml, 800mg/ml or 900mg/ml of sodium oxybate in purified water, neutralized with a weak acid, preferably malic acid.


[0004] In an embodiment of the present invention, the oral solution of sodium oxybate can further comprise a base for the pH adjustment. Preferably, the base is sodium hydroxide.


[0005] In another embodiment of the present invention, the oral solution of sodium oxybate can further comprise other pharmaceutical acceptable excipients such as preservatives, antioxidants, sweeteners and/or flavoring agents.


Page 02 of 4

EXAMPLES

EXAMPLE 1:

The following table illustrates a formulation for 200mg/ml sodium oxybate oral solution in a bottle containing 300 mL of solution:

Ingredient

Quantity per

Quantity per

mL

bottle

Sodium oxybate

200 mg

60 g

 Acetic acid q.s. pH 7.5 q.s. pH 7.5 Purified water q.s. 1 mL q.s. 300 mL

EXAMPLE 2:

The following table illustrates a formulation for 250mg/ml sodium oxybate oral solution in a bottle containing 300 mL of solution:

Ingredient

Quantity per

Quantity per

mL

bottle

Sodium oxybate

250 mg

75 g

 Malic acid q.s. pH 7.5 q.s. pH 7.5 Purified water q.s. 1 mL q.s. 300 mL

EXAMPLE 3:

The f...