Immediate release formulations and dosage forms of gamma-hydroxybutyrate
Inventors
ROURKE, ANDREA MARIE • MURPHY, MAURA PATRICIA • PFEIFFER, JAMES FREDERICK • ALLPHIN, CLARK PATRICK • MCGINLAY, ALYA KHAN
Assignees
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Publication Number
US-8778398-B2
Publication Date
2014-07-15
Expiration Date
Abstract
The present invention provides a solid immediate release dosage form adapted for oral administration of GHB. The solid immediate release dosage form includes an immediate release formulation comprising a relatively high weight-percentage of GHB with a bioavailability similar to that of a liquid GHB dosage form.
Core Innovation
The invention provides an immediate release compressed tablet for oral delivery of gamma-hydroxybutyrate (GHB). The tablet comprises GHB in an amount of about 90-98% by weight, at least one binder in an amount of about 1-5% by weight, and at least one lubricant in an amount of about 1-5% by weight, and it releases at least 90% of the GHB contained therein within a period of less than one hour after administration.
The invention further covers an immediate release compressed tablet for oral delivery of a pharmaceutically acceptable salt of GHB selected from sodium oxybate and calcium oxybate. In this tablet, the salt of GHB is present in an amount of about 90-98% by weight, together with at least one binder in an amount of about 1-5% by weight and at least one lubricant in an amount of about 1-5% by weight, and the tablet releases at least 90% of the pharmaceutically acceptable salt of GHB contained therein within a period of less than one hour after administration.
The immediate release formulations are solid dosage forms intended to provide rapid dissolution and substantial release, with delivery rate defined by at least 90% release in less than one hour after administration. The description also reports solid formulations containing sodium oxybate and calcium oxybate with relative bioavailability and dissolution performance compared to liquid Xyrem®, together with definitions and performance metrics including immediate release, delivery rate, AUC, and Cmax.
Claims Coverage
The independent claims define immediate release compressed tablets for oral delivery of GHB or pharmaceutically acceptable salts of GHB, together with a rapid release performance threshold. Across these independent claims, the core coverage centers on about 90-98% by weight of the GHB entity or its salt, about 1-5% by weight binder, about 1-5% by weight lubricant, and at least 90% release within less than one hour after administration.
Immediate release compressed tablet composition and rapid release threshold
An immediate release compressed tablet for oral delivery of GHB, comprising GHB in an amount of about 90-98% by weight, at least one binder in an amount of about 1-5% by weight, and at least one lubricant in an amount of about 1-5% by weight, wherein the tablet releases at least 90% of the GHB contained therein within a period of less than one hour after administration.
Immediate release compressed tablet of sodium oxybate or calcium oxybate with rapid release threshold
An immediate release compressed tablet for oral delivery of a pharmaceutically acceptable salt of GHB selected from sodium oxybate and calcium oxybate, comprising about 90-98% by weight of a pharmaceutically acceptable salt of GHB, at least one binder in an amount of about 1-5% by weight, and at least one lubricant in an amount of about 1-5% by weight, wherein the tablet releases at least 90% of the pharmaceutically acceptable salt of GHB contained therein within a period of less than one hour after administration.
Method of treating cataplexy and excessive daytime sleepiness using immediate release sodium oxybate formulation
A method for treating an individual afflicted with cataplexy and excessive daytime sleepiness associated with narcolepsy, restless leg syndrome, essential tremor, fibromyalgia, or chronic fatigue syndrome, comprising administering an immediate release formulation for oral delivery of sodium oxybate with the same composition and rapid release threshold.
The independent claims collectively cover immediate release compressed tablets formulated with GHB or a salt of GHB, limited binder and lubricant ranges, and a requirement that at least 90% is released within less than one hour. The same formulation framework is also claimed in an oral treatment method for cataplexy and excessive daytime sleepiness associated with specified conditions.
Stated Advantages
Provides an immediate release tablet that releases at least 90% of the contained GHB within less than one hour after administration.
Documented Applications
Treating an individual afflicted with cataplexy and excessive daytime sleepiness associated with narcolepsy, restless leg syndrome, essential tremor, fibromyalgia, or chronic fatigue syndrome by administering an immediate release formulation for oral delivery of sodium oxybate.
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