Modified Release Gamma-Hydroxybutyrate Formulations Having Improved Pharmacokinetics
Patent No. US11065224 (titled "Modified Release Gamma-Hydroxybutyrate Formulations Having Improved Pharmacokinetics") was filed by Rtw Investments Lp on Jul 31, 2019.
What is this patent about?
’224 is related to the field of modified-release pharmaceutical formulations, specifically those designed for the delivery of gamma-hydroxybutyrate (GHB) . The background of the invention lies in addressing the inconveniences associated with existing GHB treatments for conditions like narcolepsy, which often require multiple doses per night. The goal is to develop a once-nightly formulation with improved pharmacokinetic properties.
The underlying idea behind ’224 is to create a modified-release GHB formulation that mimics the bioavailability of a twice-nightly immediate-release solution, but with a single dose. This is achieved by carefully controlling the in vitro release profile to optimize in vivo absorption. The key insight is that a formulation releasing half its GHB rapidly in acidic conditions and the other half rapidly in a pH 6.8 buffer can approximate or exceed the bioavailability of a twice-nightly immediate-release solution.
The claims of ’224 focus on a pharmaceutical composition designed for once-nightly administration that releases GHB into the bloodstream. Claim 1 specifies that the composition must be effective in inducing sleep for at least six consecutive hours and, when administered after a standardized evening meal, must yield a plasma concentration versus time curve that is bioequivalent to those depicted in specific figures of the patent for various doses.
In practice, the invention uses a combination of immediate-release and modified-release portions within the formulation. The immediate-release portion provides an initial dose of GHB, while the modified-release portion is designed to release the remaining GHB later, maintaining therapeutic levels throughout the night. This is achieved through a coating on the modified-release portion that delays the release until it encounters a specific pH environment in the digestive tract.
This approach differs significantly from prior attempts at modified-release GHB formulations, which often suffered from reduced bioavailability compared to immediate-release solutions. The inventors discovered that a specific in vitro release profile, characterized by rapid release in both acidic and pH 6.8 buffer conditions, is crucial for achieving comparable or superior bioavailability. This dual-release mechanism is the key differentiator from previous approaches.
How does this patent fit in bigger picture?
Technical landscape at the time
In the mid-2010s when ’224 was filed, modified release formulations were being developed at a time when hardware or software constraints made achieving consistent drug bioavailability non-trivial. At a time when immediate release formulations were common, modified release formulations were being developed to improve patient compliance and reduce the frequency of dosing.
Novelty and Inventive Step
The examiner allowed the claims because an updated prior art search did not disclose a reference that teaches a pharmaceutical composition that releases gamma-hydroxybutyrate in the bloodstream of a human subject, wherein the composition is designed to be administered only once per night, as recited in the claims. The examiner was persuaded that the claimed invention was novel and unobvious over the prior art.
Claims
This patent contains 38 claims, with claim 1 being the only independent claim. Independent claim 1 is directed to a pharmaceutical composition that releases gamma-hydroxybutyrate in the bloodstream, designed for once-per-night administration to induce sleep, and characterized by specific bioequivalence to plasma concentration curves. The dependent claims generally elaborate on the characteristics of the pharmaceutical composition, such as dissolution profiles and blood concentrations at specific times.
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Date
Description
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US11065224
- Application Number
- US16527633
- Filing Date
- Jul 31, 2019
- Status
- Granted
- Expiry Date
- Dec 9, 2037
- External Links
- Slate, USPTO, Google Patents