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Publication Number
US-12239740-B2
Publication Date
2025-03-04
Expiration Date
Abstract
A solid dosage form for injection and a method of making said dosage form wherein the dosage form has a moisture content of 5% (w/w) or less. The solid dosage form comprises a dried matrix including a first excipient and 0.01 to 50% (w/w) or more than 50% and up to 80% (w/w) of a therapeutic peptide; and one or more additional excipients and at least 5% (w/w) of CMC, based on the total weight of the solid dosage form, wherein the dosage form has a width of 0.5 mm to 2 mm.
Core Innovation
The invention relates to a solid dosage form for injection of therapeutic peptides. The solid dosage form includes a freeze dried matrix comprising a therapeutic peptide and a first excipient, and a bulk component comprising the freeze dried matrix with one or more additional excipients. The bulk component further includes at least 5% (w/w) carboxymethyl cellulose (CMC) based on the total weight of the solid dosage form.
The dosage form is defined to have a moisture content of 5% (w/w) or less. The solid dosage form is injectable and is shaped to facilitate skin penetration without a needle. The dosage form has a maximum width from 0.5 mm to 2 mm and includes a pointed end configured to facilitate skin penetration, where the pointed end is formed as a cone or as a beveled tip formed from two or more intersecting surfaces meeting at a common point.
The first excipient and the one or more additional excipients are selected from polyols, sugars, surfactants, amino acids, EDTA and/or stabilising agents. The therapeutic peptide is present in the freeze dried matrix in an amount of 0.01 to 50% (w/w). The described formulation is configured such that the inclusion of CMC in the bulk component contributes to compressive strength enabling skin penetration.
The problem addressed is providing a needle-free injectable solid dosage form for therapeutic peptides that is dry and shaped for skin penetration while maintaining sufficient mechanical integrity. The documented examples include therapeutic peptides such as octreotide, PTH 1-34, exenatide, and liraglutide formulated in freeze dried matrices and bulk components containing CMC, with stated moisture levels and compressive strength measurements to support the described performance.
Claims Coverage
The document provides one independent claim (clm-00001). The independent claim comprises inventive features covering a freeze dried matrix containing a therapeutic peptide, a bulk component with at least 5% (w/w) CMC, defined dry moisture content, and a needle-free skin-penetrating geometry with specified pointed end forms and maximum width constraints.
Freeze dried matrix with therapeutic peptide
A solid dosage form comprising a freeze dried matrix including a first excipient and 0.01 to 50% (w/w) of a therapeutic peptide.
Bulk component with at least 5% (w/w) carboxymethyl cellulose
A bulk component comprising the freeze dried matrix, one or more additional excipients and at least 5% (w/w) carboxymethyl cellulose (CMC), based on the total weight of the solid dosage form.
Dry injectable solid dosage form with moisture content ≤5% (w/w)
The solid dosage form is injectable and has a moisture content of 5% (w/w) or less.
Needle-free skin penetration geometry with pointed end
The dosage form has a maximum width of 0.5 mm to 2 mm and has a pointed end configured to facilitate skin penetration.
Pointed end geometry as cone or beveled tip formed by intersecting surfaces
The pointed end is in the form of a cone or in the form of a beveled tip that is formed from two or more intersecting surfaces meeting at a common point.
Excipient selection from polyols, sugars, surfactants, amino acids, EDTA, and stabilising agents
The first excipient is a polyol, sugar, surfactant, amino acid, EDTA and/or stabilising agent, and the one or more additional excipients is at least one of a polyol, sugar, surfactant, amino acid, EDTA and/or stabilising agent.
Overall, the claim coverage centers on a needle-free injectable solid dosage form that combines a freeze dried therapeutic peptide matrix with a bulk component containing at least 5% (w/w) CMC, maintained at moisture content of 5% (w/w) or less, and shaped with a maximum width of 0.5–2 mm and a pointed end (cone or beveled tip formed from intersecting surfaces meeting at a common point) configured for skin penetration.
Stated Advantages
CMC increases compressive strength enabling skin penetration without a needle.
Documented Applications
Needle-free injection/skin penetration delivery of therapeutic peptides using an injectable solid dosage form.
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