Pharmaceutical formulations comprising naltrexone and/or bupropion
Inventors
Churchill, Rob • Chesnut, Aaron
Assignees
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Publication Number
US-12303604-B1
Publication Date
2025-05-20
Expiration Date
Abstract
Described are pharmaceutical formulations comprising naltrexone and/or bupropion. Such pharmaceutical formulations can comprise extended-release, multilayer beads. Also described are methods of administering such formulations, such as for the treatment of overweight or obesity.
Core Innovation
The disclosed invention relates to treating overweight or obesity by administering an oral, capsule-based, extended-release naltrexone and bupropion treatment regimen with once-daily dosing that escalates over a sequence of weeks. The regimen provides a first, second, third, and fourth oral dosage form, where each weekly dosage form is administered once a day and the fourth and subsequent weeks continue at a highest dose level.
The oral dosage forms include capsules in which the bupropion extended-release formulation exhibits defined in vitro dissolution performance in a dissolution test of USP Apparatus 1 Basket Method at 100 rpm in water at 37 °C. The dissolution profile is specified by release percentages within one hour, two hours, and four hours, thereby defining the extended-release behavior for bupropion in the capsule dosage forms.
The disclosed formulation content further includes extended-release multilayer beads within the capsule dosage forms, including bead architectures with a drug-free core particle and multiple coatings. The bead structures include a drug layer, a non-aqueous barrier coating, an extended release polymer coating, and an optional top coating, optionally including a seal coating, to support the extended-release performance.
The patent text further ties formulation performance to naltrexone and bupropion exposure targets and/or bioequivalence. It describes steady-state pharmacokinetic targets (Cmax and AUC0-24h) and states that once-daily oral formulations are bioequivalent to the FDA-approved CONTRAVE® trilayer tablet given twice daily, using 90% confidence interval ranges for AUC and Cmax.
Claims Coverage
The independent claim coverage centers on 2 inventive features: a once-daily four-week escalating capsule regimen for treating overweight or obesity, and a bupropion extended-release dissolution profile defined by USP Apparatus 1 at 37 °C.
Once-daily four-week escalating capsule regimen for overweight or obesity
Administering a first oral dosage form once a day for a first week, a second oral dosage form once a day for a second week, a third oral dosage form once a day for a third week, and a fourth oral dosage form once a day for a fourth and subsequent weeks, each oral dosage form comprising naltrexone (or salt thereof) and bupropion (or salt thereof), wherein each oral dosage form is a capsule.
Bupropion extended-release dissolution profile defined by USP Apparatus 1 at 37 °C
A capsule comprises a bupropion extended-release formulation having an in vitro bupropion dissolution profile in a dissolution test of USP Apparatus 1 Basket Method at 100 rpm in water at 37 °C, with release percentages within one hour, two hours, and four hours.
Overall, the claim coverage focuses on a once-daily escalating treatment over four weeks using capsule dosage forms containing naltrexone and bupropion, together with a specified bupropion extended-release in vitro dissolution profile. Dependent material further ties selected dosage forms to naltrexone dissolution thresholds, steady-state pharmacokinetic ranges for Cmax and AUC0-24h, and bioequivalence to the FDA-approved CONTRAVE® trilayer tablet.
Stated Advantages
Provides once-daily oral formulations that are stated to be bioequivalent to the FDA-approved CONTRAVE® trilayer tablet given twice daily.
Defines extended-release performance via specified USP Apparatus 1 dissolution release ranges for bupropion at 37 °C and 100 rpm.
Provides described steady-state pharmacokinetic exposure targets (Cmax and AUC0-24h) for naltrexone and bupropion.
Documented Applications
Treating overweight or obesity in a subject in need thereof using a once-daily escalating oral capsule regimen comprising naltrexone (or salt) and bupropion (or salt).
Using a fourth and subsequent weekly highest-dose oral dosage form administered once daily as a basis for described bioequivalence to CONTRAVE® (twice-daily) and/or described steady-state pharmacokinetic exposure targets.
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