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Publication Number
US-12048691-B2
Publication Date
2024-07-30
Expiration Date
Abstract
The disclosure provides a tebipenem pivoxil HBr formulation in the form of a tablet core comprising at least 70% (w/w) tebipenem pivoxil HBr, and in certain embodiment more than 80% (w/w) tebipenem pivoxil HBr. The disclosure provides a tebipenem pivoxil HBr tablet core comprising at least 70% w/w tebipenem pivoxil HBr, 5-25% w/w of a diluent, 0.5 to 5% w/w of a glidant, 0.5 to 5% w/w of a lubricant, and optionally 0.5 to 5% w/w of disintegrant. The disclosure provides methods of treating a patient who has a bacterial infection such as complicated urinary tract infection (cUTI), acute and chronic pyelonephritis, an upper or lower respiratory infection, or bacteremia by administering a formulation of the disclosure to the patient.
Core Innovation
The invention relates to a tebipenem pivoxil HBr tablet core consisting of at least 70% w/w tebipenem pivoxil HBr. The core further includes 15–25% w/w of a binder/diluent, wherein the binder/diluent is microcrystalline cellulose, and also includes crospovidone disintegrant, silicon dioxide glidant, and magnesium stearate.
A major aspect of the invention is the selection of excipients and their specified weight ranges to form a high drug-load tebipenem pivoxil HBr tablet core. The description addresses limitations of prior dosage forms in which more than 60% drug can cause large tablets and related manufacturing issues, and discusses crystalline and amorphous salt forms and polymorphs of tebipenem pivoxil HBr, including HBr Form B and HBr Form C.
The invention emphasizes control of API particle size distribution to avoid capping and sticking during compression while enabling compression. The disclosed tablet embodiments also include coating options, including immediate-release aqueous film coatings, and report pharmacokinetic and bioequivalence assessment for a reduced-size tablet formulation under fasted versus fed conditions.
The disclosed clinical and microbiological scope includes treatment of bacterial infections, including complicated urinary tract infection and acute pyelonephritis with bacteremia, resistant Gram-negative pathogens, and nontuberculous mycobacterial infections.
Claims Coverage
The claim set includes one independent claim directed to a tebipenem pivoxil HBr tablet core composition, with dependent claims refining the core formulation and adding performance and use coverage. Across the independent-claim family, the coverage comprises formulation composition, optional solid-state form specifications, dissolution performance constraints, coating narrowing to immediate-release aqueous film coating, and treatment of specified infections in a human patient by administering the tablet.
High drug-load tebipenem pivoxil HBr tablet core with specified excipients
A tebipenem pivoxil HBr tablet core consisting of at least 70% w/w tebipenem pivoxil HBr; 15–25% w/w of a binder/diluent wherein the binder/diluent is microcrystalline cellulose; 0.5 to 2% w/w of a disintegrant wherein the disintegrant is crospovidone; 0.5 to 2% w/w of a glidant wherein the glidant is silicon dioxide; and 0.5 to 2% w/w of magnesium stearate.
Claim coverage centers on a high drug-load tebipenem pivoxil HBr tablet core defined by specified microcrystalline cellulose binder/diluent, crospovidone disintegrant, silicon dioxide glidant, and magnesium stearate. The dependent claim set further narrows to specific solid-state forms, includes dissolution performance constraints, specifies an immediate-release aqueous film coating in some embodiments, and supports treatment of specified bacterial and nontuberculous mycobacterial infections in a human patient by administering the claimed tablet.
Stated Advantages
Addresses limitations of prior dosage forms in which more than 60% drug can cause large tablets and related manufacturing issues.
Uses control of API particle size distribution to avoid capping and sticking during compression while enabling compression.
Includes coating options, including immediate-release aqueous film coatings.
Reports pharmacokinetic and bioequivalence assessment for a reduced-size tablet formulation under fasted versus fed conditions.
Documented Applications
Treatment of a bacterial infection in a human patient by administering a tebipenem pivoxil HBr tablet.
Treatment of complicated urinary tract infection and acute pyelonephritis with bacteremia.
Treatment of resistant Gram-negative pathogens.
Treatment of a nontuberculous mycobacterial infection in a human patient by administering a tebipenem pivoxil HBr tablet.
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