Controlled release dosage forms for high dose, water soluble and hygroscopic drug substances
Inventors
Allphin, Clark • Pfeiffer, James
Assignees
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Publication Number
US-10813885-B1
Publication Date
2020-10-27
Expiration Date
Abstract
Controlled release dosage forms are described herein. The controlled release formulations described herein provide prolonged delivery of high dose drugs that are highly water soluble and highly hygroscopic. In specific embodiments, controlled release dosage forms for delivery of a drug selected from GHB and pharmaceutically acceptable salts, hydrates, tautomers, solvates and complexes of GHB. The controlled release dosage forms described herein may incorporate both controlled release and immediate release formulations in a single unit dosage form.
Core Innovation
The invention relates to controlled-release dosage forms for high-dose, water-soluble and hygroscopic drugs, including gamma-hydroxybutyrate and pharmaceutically acceptable salts of gamma-hydroxybutyrate. A sustained release portion includes a core and a functional coating deposited over the core to provide a defined dissolution-based release profile.
The sustained release portion is defined by the functional coating composition and the sustained release performance in dissolution testing. The functional coating comprises one or more methacrylic acid-methyl methacrylate co-polymers from about 20% to about 50% by weight of the functional coating, and the core contains gamma-hydroxybutyrate or pharmaceutically acceptable salts of gamma-hydroxybutyrate.
The problem addressed is delivering gamma-hydroxybutyrate from a sustained release portion with reduced early release while maintaining extended release performance, including dissolution behavior under specified apparatus conditions. The disclosed formulations release greater than about 40% of gamma-hydroxybutyrate by about 4 to about 6 hours in dissolution apparatus 2 in deionized water at 37°C and 50 rpm, and the document further describes optional moisture-barrier/cosmetic coatings and resistance to dose dumping, including dissolution in vodka.
Claims Coverage
The partial content identifies one independent claim. It has a sustained release portion with a core and a functional coating deposited over the core, where the functional coating includes methacrylic acid-methyl methacrylate copolymers and where sustained release is defined by dissolution testing release thresholds at about 4 to about 6 hours under specified apparatus conditions.
Sustained release portion with deposited functional coating over a core
The sustained release portion comprises a functional coating deposited over the core, wherein the core comprises at least one pharmaceutically active ingredient selected from gamma-hydroxybutyrate and pharmaceutically acceptable salts of gamma-hydroxybutyrate.
Methacrylic acid-methyl methacrylate co-polymers in the functional coating at specified weight fraction
The functional coating comprises one or more methacrylic acid-methyl methacrylate co-polymers that are from about 20% to about 50% by weight of the functional coating.
Dissolution release threshold defined for sustained release performance
The sustained release portion releases greater than about 40% of its gamma-hydroxybutyrate by about 4 to about 6 hours when tested in a dissolution apparatus 2 in deionized water at a temperature of 37°C and a paddle speed of 50 rpm.
High-dose gamma-hydroxybutyrate or pharmaceutically acceptable salts in the sustained release portion
The formulation comprises a sustained release portion comprising about 500 mg to 12 g of at least one pharmaceutically active ingredient selected from gamma-hydroxybutyrate and pharmaceutically acceptable salts of gamma-hydroxybutyrate.
Across the independent claim, the inventive coverage centers on a sustained release formulation having a coated core, methacrylic acid-methyl methacrylate copolymer content within a specified weight range in the functional coating, and a dissolution-tested release performance defined by release of more than about 40% by about 4 to about 6 hours under specified dissolution apparatus conditions.
Stated Advantages
Documented Applications
No documented applications found
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