Antibiotic product, use and formulation thereof
Inventors
Burnside, Beth A. • Flanner, Henry H. • Rowlings, Colin
Assignees
Shionogi Inc • MiddleBrook Pharmaceuticals Inc
Publication Number
US-8460710-B2
Publication Date
2013-06-11
Expiration Date
2024-09-14
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Abstract
An antibiotic product is comprised of at least three dosage forms, each of which has a different release profile, with the Cmax for the antibiotic product being reached in less than about twelve hours after the initial release of antibiotic. In one embodiment, there are two delayed release dosage forms, as well as a delayed sustained release dosage form, with each of the dosage forms having a different release profile, wherein each reaches a Cmax at different times.
Core Innovation
The invention concerns an antibiotic product composed of at least three different dosage forms, each formulated to provide a distinct release profile of at least one antibiotic. These dosage forms are assembled into a single or unitary product that, when administered, achieves a maximum serum concentration (Cmax) of the total antibiotic released in less than about twelve hours from the time the first dosage form initiates release. The preferred embodiment utilizes two delayed release dosage forms and one delayed sustained release dosage form, with each dosage form beginning its release at either the same or at different intervals after administration, ensuring that each achieves Cmax at different times.
The problem addressed by this invention is the challenge of administering antibiotics, which typically require repeated dosing of immediate release forms, leading to poor compliance, or using controlled release formulations at higher doses. Existing approaches do not provide optimal release timing for antibiotics with short half-lives and may not maintain effective serum concentrations throughout the dosing period. The invention aims to allow once-a-day administration while providing sequential or pulsed antibiotic delivery to better maintain therapeutic levels over a 24-hour period.
The formulation of the antibiotic product can include various release mechanisms, such as delayed release, delayed sustained release, and coatings that are pH sensitive or non-pH sensitive, tailored to control the initiation and rate of antibiotic release from each dosage form. This flexibility in release profiles enables efficient coverage with antibiotics that possess elimination half-lives of 2–10 hours. The product can be configured for multiple routes of administration, but is preferably designed as an oral dosage form where all dosage forms are combined in a tablet or capsule, ensuring all antibiotic for a full day is given in a single administration.
Claims Coverage
There are three main inventive features in the independent claims of this patent.
Once-a-day antibiotic product comprising specific delayed and sustained release dosage forms
An oral antibiotic product composed of first, second, and third dosage forms, each containing at least one antibiotic and a pharmaceutically acceptable carrier. The first and second dosage forms are delayed release, while the third is a delayed sustained release form. The third dosage form initiates release at about the same time as, or later than, the second dosage form, and the second starts release after the first. The product contains the full daily dose of an antibiotic with a half-life of 2–10 hours, achieves Cmax in less than 12 hours from initial release, and is free of immediate release dosage forms.
Antibiotic product with four dosage forms for controlled sequential release
An oral antibiotic product comprising first, second, third, and fourth dosage forms, where the fourth dosage form is either a sustained or delayed release dosage form, each containing at least one antibiotic and a pharmaceutically acceptable carrier. The antibiotic released from the fourth dosage form achieves a Cmax after that achieved by each of the first, second, and third dosage forms.
Process for treating bacterial infection using the once-a-day antibiotic product
A method for treating bacterial infection by administering to a host, once-a-day, the antibiotic product comprising the specific configuration of delayed and sustained release dosage forms as disclosed above, such that the entire daily dose is delivered in a single administration.
The inventive features center on a once-daily antibiotic product utilizing at least three dosage forms with distinct delayed and sustained release profiles, designed for oral administration without immediate release forms, as well as the corresponding method of treating infection by administering this product.
Stated Advantages
Provides an improvement over twice-a-day administration and once-a-day single-profile administration of antibiotics.
Allows once-a-day dosing with controlled sequential or pulsed release, reducing the number of administrations required and potentially improving patient compliance.
Enables optimal therapeutic activity for antibiotics with short half-lives (2–10 hours) by maintaining effective serum concentrations over 24 hours.
Documented Applications
Treatment of bacterial infections in a host via once-a-day administration of the antibiotic product.
Oral administration in the form of capsules, tablets, or sachets containing at least two or three differing release profile dosage forms.
Formulation for topical administration, including oil-in-water or water-in-oil emulsions.
Formulation for administration in the eye or ear, such as liquid emulsions.
Formulation as nose drops, rectal or vaginal creams, emulsions, or dissolvable dosage forms.
Formulation for inhalation therapy using coated and micronized particles.
Formulation for transdermal patch containing dosage forms with different release profiles.
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