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Publication Number
US-11311503-B1
Publication Date
2022-04-26
Expiration Date
Abstract
Disclosed are sterile aqueous choline salt compositions, their preparation, and methods of use. Also disclosed are methods to treat choline deficiency, intestinal failure associated liver disease (IFALD), and fatty liver disease. Additionally disclosed is a method of synthesis of choline salts.
Core Innovation
The invention relates to a sterile composition for intravenous injection that comprises choline chloride in an aqueous medium, wherein the choline chloride is present at 25-75% by weight/volume. The composition is defined by sterilization and sterility performance parameters, including gamma irradiation at a dose of at least 20 kGy and a sterility assurance level of at least 10^-6.
The composition further includes defined formulation properties that may include or exclude preservative, and may contain at least one amino acid, at least one vitamin, and/or at least one fatty acid. The invention defines ionic strength of the composition as 0.3-7 Molar or about 7 Molar, and additionally defines a pH of about 4-7.
The document also includes an approach for synthesizing choline chloride using gaseous trimethylamine with 2-chloroethanol under pressure in ethanol/MTBE, with high-purity specifications and low residuals/impurities.
Claims Coverage
The claim set includes two independent claims that both require a sterile composition for intravenous injection comprising choline chloride in an aqueous medium at 25-75% (w/v) and sterilization by gamma irradiation at at least 20 kGy. Across the independent claims and their dependents, the coverage is refined with additional inventive features including sterility assurance level, microbial CFU/mL limits for specified organisms, and defined formulation parameters such as optional preservative content, ionic strength, and pH.
Sterile intravenous choline chloride aqueous composition at 25-75% (w/v)
A sterile composition for intravenous injection comprising choline chloride in an aqueous medium, wherein the choline chloride is present at 25-75% by weight/volume%.
Gamma irradiation sterilization at least 20 kGy
The composition has been sterilized by gamma irradiation at a dose of at least 20 kGy.
Sterility assurance level at least 10^-6
The composition has a sterility assurance level of at least 10^-6.
Microbial CFU limit for S. aureus, G. stearothermophilus, and/or B. pumilus
The composition contains less than 10^-1 CFU/mL of S. aureus, G. stearothermophilus, and/or B. pumilus.
Optional preservative and optional amino acid, vitamin, or fatty acid components
The composition does not contain a preservative; and/or contains a preservative; and/or contains at least one amino acid, at least one vitamin, and/or at least one fatty acid.
Defined ionic strength 0.3-7 Molar or about 7 Molar
The composition has an ionic strength of 0.3-7 Molar; or has an ionic strength of about 7 Molar.
Defined pH about 4-7
The composition has a pH of about 4-7.
Overall, the claims cover sterile intravenous injection compositions of choline chloride in an aqueous medium at 25-75% (w/v) that are gamma-irradiation sterilized at at least 20 kGy and meet defined sterility assurance and microbial CFU limits. The coverage is further qualified by optional preservative and optional amino acid/vitamin/fatty acid content, and by formulation constraints on ionic strength and pH.
Stated Advantages
Gamma irradiation sterilization provides sterilized compositions meeting sterility assurance and microbial contamination limits for specified organisms at defined CFU thresholds.
Terminal heat sterilization is stated to be impractical for 50% choline chloride due to high D121.
Documented Applications
Sterile composition for intravenous injection.
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