Alkaline phosphatase formulations and uses thereof
Inventors
Kaleko, Michael • STAPLETON, Ray • Bristol, Andrew • Hubert, Steven • FREIRE, Cristina
Assignees
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Publication Number
US-12691077-B2
Publication Date
2026-07-28
Expiration Date
Abstract
The present invention provides, in part, formulations comprising an alkaline phosphatase. Particularly, modified-release formulations comprising an alkaline phosphatase are provided, which release a substantial amount of the alkaline phosphatase in the intestines. Therapeutic uses of the alkaline phosphatase formulations are also provided.
Core Innovation
The invention relates to a modified-release formulation comprising at least one modified-release pellet comprising an alkaline phosphatase (AP)-based agent contained in a capsule. The formulation is defined by specific weight percentages of an AP-based agent, sucrose sphere, hydroxypropylcellulose, buffer salt, enteric polymer, and a coating system additive mixture of glyceryl monostearate, polysorbate-80, and triethyl citrate.
The formulation maintains at least 80% AP-based agent activity when stored at 2-8°C for at least 6 months. The modified-release coating provides stability in gastric fluid and release in intestinal fluid and/or environments associated with microbial enzyme degradation, with pH-dependent solubility and a time-dependent erosion profile.
The disclosed compositions are positioned for therapeutic use in preventing or treating gastrointestinal disorders, including Clostridioides difficile infection (CDI/CDAD/CDD) and antibiotic-associated GI dysbiosis. The document also describes radiation-induced gastrointestinal injury and enteropathy, including radiation enteritis/proctitis and acute radiation syndrome (ARS), using an AP-based agent delivered in the modified-release capsule-contained dosage form.
Claims Coverage
The provided material presents one independent claim relating to a modified-release capsule-contained formulation. The inventive features include a defined composition with specific weight ranges, a defined coating system additive mixture, and a storage-stability/activity retention requirement at 2-8°C for at least 6 months.
Modified-release capsule-contained AP-based agent formulation with specified component ranges
A modified-release formulation comprising at least one modified-release pellet comprising an alkaline phosphatase (AP)-based agent contained in a capsule, with about 5-15% by weight AP-based agent, about 35-45% by weight sucrose sphere, about 15-25% by weight hydroxypropylcellulose, about 0.1-1% by weight buffer salt, about 20-30% by weight enteric polymer, and about 1-10% by weight coating system additive.
Defined coating system additive mixture
The coating system additive is a mixture of glyceryl monostearate, polysorbate-80, and triethyl citrate.
Storage stability and activity retention
The formulation maintains at least 80% AP-based agent activity when stored at 2-8°C for at least 6 months.
Modified-release behavior by pH-dependent solubility and time-dependent erosion
The modified-release formulation includes a coating with solubility that depends on pH and includes a time-dependent erosion profile.
Therapeutic prevention or treatment of radiation-induced disorder by administration
A method of treating or preventing a radiation-induced disorder by administering the formulation to a subject in need.
Overall, the claim coverage centers on a specific modified-release capsule-contained composition for an AP-based agent with defined weight ranges, a defined coating additive mixture, and an activity retention requirement under storage conditions, with further functional coating behavior and an explicit radiation-induced disorder use context in dependent subject-matter.
Stated Advantages
Maintains at least 80% AP-based agent activity when stored at 2-8°C for at least 6 months.
Documented Applications
Preventing or treating radiation-induced gastrointestinal disorders by administering the modified-release formulation to a subject in need.
Preventing or treating Clostridioides difficile infection (CDI/CDAD/CDD) and antibiotic-associated GI dysbiosis.
Preventing or treating radiation-induced GI injury/enteropathy, including radiation enteritis/proctitis and acute radiation syndrome (ARS).
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