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Publication Number
US-11135170-B2
Publication Date
2021-10-05
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 needle-free injection intended for parenteral delivery of a therapeutic protein or peptide in a solid, substantially dry formulation. The dosage form has a defined moisture content between 1 and 5% (w/w) and includes a dried matrix including at least a first excipient and 0.01 to 50% (w/w) of a therapeutic protein.
The formulation further includes one or more additional excipients and 5 to 95% (w/w), based on the total weight of the solid dosage form, of carboxymethylcellulose (CMC) blended in the dosage form. A key aspect is that the dosage form has a width of 0.5 mm to 2 mm and a compressive strength that is at least 80 MPa and is 168 MPa or less.
The document describes preparation and composition concepts for producing a dried matrix, including a freeze-dried matrix and/or drying approaches such as vacuum drying, with CMC blended to form the stated dosage form. The formulation optionally includes bulking agents, stabilising agents, surfactants, and other excipient options, and experimental examples indicate that reducing moisture via vacuum drying increases compressive strength while maintaining the defined moisture and CMC-containing solid dosage form characteristics.
Claims Coverage
The partial set includes one independent claim defining the solid dosage form for needle-free injection by specifying moisture content, dried matrix composition, therapeutic protein loading, carboxymethylcellulose (CMC) blend level, physical width, and compressive strength constraints.
Moisture-controlled needle-free injection solid dosage form
A solid dosage form for needle-free injection having a moisture content of between 1 and 5% (w/w).
Dried matrix with therapeutic protein and defined protein loading
A dried matrix including at least a first excipient and 0.01 to 50% (w/w) of a therapeutic protein.
Carboxymethylcellulose blended solid with defined CMC range
One or more additional excipients and 5 to 95% (w/w), based on the total weight of the solid dosage form, of carboxymethylcellulose (CMC) blended in the dosage form.
Defined dimensions and compressive strength for needle-free injection
The dosage form has a width of 0.5 mm to 2 mm, and the compressive strength of the dosage form is at least 80 MPa and is 168 MPa or less.
Across the independent claim, the claim coverage centers on a needle-free injection solid dosage form that is substantially dry, contains a dried matrix with a defined therapeutic protein amount, includes CMC in a defined range, and has defined width with compressive strength constrained to at least 80 MPa but not greater than 168 MPa.
Stated Advantages
Needle-free administration speed.
Reduced wastage.
Clinical tolerability, including sensory equivalence to a 27-gauge needle (Phase I).
Documented Applications
Treating intestinal tumours, metastatic carcinoid tumours, acromegaly, solitary bone cysts, hypoparathyroidism, or type 2 diabetes mellitus by administering to a subject a therapeutically effective amount of the solid dosage form.
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