Tebipenem pivoxil immediate and modified release oral dosage forms

Inventors

Jain, Akash • Lu, Enxian • Lyu, Shaoqiong • Li, Shoufeng • KEUTZER, Timothy • UTLEY, Luke • Fraczkiewicz, Grazyna • MACWAN, Joyce

Assignees

Spero Therapeutics Inc

Abstract

Immediate and modified release oral dosage forms of tebipenem pivoxil including dosage form cores are provided. The dosage form core includes tebipenem pivoxil in free base or salt form, and excipients including a binder, a lubricant, optionally a diluent, and optional additional excipients. The weight to weight ratio of tebipenem pivoxil to the excipients in the dosage form core is from 30:60 to 60:30. The disclosure includes methods of treating bacterial infections including complicated urinary tract infections.

Core Innovation

The invention relates to a tebipenem pivoxil HBr tablet core for oral solid dosage forms. The tablet core comprises at least 60% (w/w) tebipenem pivoxil, and tebipenem is the only therapeutic active agent.

The invention addresses release performance for the tablet core using dissolution testing and defined performance targets. In vitro dissolution performance is described using a USP Paddle in pH 5.0 acetate buffer, with immediate release variants showing more than 85% release in 15 min and modified release variants showing no more than 50% release in 30 min, with at least 85% release after 2–4 h for modified/short modified variants.

The invention further includes compositions for the tablet core, including excipients and optional release control elements. A binder, disintegrant, and lubricant are described as being present in certain tablet cores, with examples including microcrystalline cellulose and/or silicified microcrystalline cellulose, crospovidone including PVPP XL-10, and magnesium stearate, and optional coatings including enteric coatings using Eudragit-type polymers.

Claims Coverage

The independent claim set includes one independent composition claim and one independent method-of-treatment claim. Across these independent claims, the coverage focuses on a tebipenem pivoxil HBr tablet core composition with high drug loading and tebipenem as the only therapeutic active agent, and administering that tablet core dosage form for treating bacterial infections in at-risk or affected subjects.

The claims coverage centers on a tebipenem pivoxil HBr tablet core where tebipenem pivoxil comprises at least 60% (w/w) and is the sole therapeutic active agent, and on a method of treating a bacterial infection by administering the corresponding tablet-core dosage form to a subject at risk for or already having the bacterial infection.

Stated Advantages

Documented Applications