Antibacterial compositions for drug administration
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Publication Number
US-9114069-B2
Publication Date
2015-08-25
Expiration Date
Abstract
Non-toxic aqueous compositions are provided having antibacterial activity. Specifically, the invention provides aqueous alkyl glycoside or saccharide alkyl ester compositions which meet the antimicrobial effectiveness test criteria set forth in USP 31 <51> in preventing growth of specified bacteria and fungi.
Core Innovation
The invention relates to non-toxic aqueous pharmaceutical compositions that inhibit microbial growth. The compositions include at least one alkylsaccharide having antibacterial activity and ethylenediaminetetraacetic acid (EDTA) or a salt thereof, combined in amounts sufficient to inhibit microbial growth.
The alkylsaccharide is an alkyl chain length from 2 to 14 carbon atoms linked by glycosidic linkage to a maltose, specifically n-Dodecyl-4-O-α-D-glucopyranosyl-β-D-glucopyranoside. The compositions further comprise at least one therapeutic peptide comprising a parathyroid hormone (PTH) or analog thereof, including PTH (1-31), PTH (1-34) or PTH (3-34).
The pharmaceutical compositions are described as being useful with minimal mucosal irritation while stabilizing drugs and increasing bioavailability. Administration routes described include oral, ocular, intranasal, pulmonary, transmucosal, transdermal, and central nervous system delivery such as CSF, and the document includes therapeutic peptide and antibody examples showing improved absorption and/or stability.
Claims Coverage
The partial content provides one independent claim describing an aqueous pharmaceutical composition that combines an alkylsaccharide, a specified parathyroid hormone therapeutic peptide or analog, and EDTA or a salt thereof to inhibit microbial growth. Dependent claims refine the composition with concentration ranges, a pH threshold, and specified administration or formulation routes.
Aqueous microbial growth inhibition by admixing alkylsaccharide, PTH peptide, and EDTA
Admixing an alkylsaccharide having antibacterial activity with a therapeutic peptide that is a parathyroid hormone (PTH) or analog thereof and EDTA or a salt thereof in an aqueous pharmaceutical composition, wherein the alkylsaccharide consists of an alkyl chain length from 2 to 14 carbon atoms linked by glycosidic linkage to a maltose, and wherein the amounts are sufficient to inhibit microbial growth of Aspergillus niger, Candida albicans, Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa.
Specific alkylsaccharide as n-Dodecyl-4-O-α-D-glucopyranosyl-β-D-glucopyranoside
Using the alkylsaccharide as n-Dodecyl-4-O-α-D-glucopyranosyl-β-D-glucopyranoside as the antibacterial alkylsaccharide component of the aqueous pharmaceutical composition.
PTH or specified PTH analog therapeutic peptide component
Including as the therapeutic peptide a parathyroid hormone (PTH) or analog thereof, where the PTH analog is PTH (1-31), PTH (1-34) or PTH (3-34).
EDTA (or salt) included to enable microbial growth inhibition
Including EDTA or a salt thereof in the aqueous pharmaceutical composition such that the alkylsaccharide and EDTA or salt are present in an amount sufficient to inhibit microbial growth.
Concentration range for the alkylsaccharide
Carrying out the method with an alkylsaccharide concentration of about 0.05% to 0.5% by weight, with a narrower refinement of about 0.125% to 0.25% by weight.
Concentration range for EDTA
Using EDTA at a concentration ranging from about 0.01% to 2% by weight.
pH threshold for the aqueous composition
Performing the method at a pH of about 7.0 or lower.
Specified administration/formulation routes
Formulating the composition for administration transmucosally, transdermally, optically, or by injection.
Across the independent and dependent claims, the method is centered on inhibiting microbial growth in an aqueous pharmaceutical composition by admixing a defined antibacterial alkylsaccharide, a PTH or specified PTH analog therapeutic peptide, and EDTA or a salt, with further claim limitations on alkylsaccharide concentration, EDTA concentration, a pH threshold, and specified administration or formulation routes.
Stated Advantages
Inhibits microbial growth while being non-toxic.
Stabilizes drugs and increases bioavailability.
Provides minimal mucosal irritation.
Exhibits antimicrobial activity against the listed microorganisms.
Documented Applications
Used as an aqueous pharmaceutical composition with administration routes including oral, ocular, intranasal, pulmonary, transmucosal, transdermal, and CSF/central nervous system delivery.
Therapeutic use with peptide drugs including insulin, GLP-1, exenatide, PTH, and PYY, where improved absorption and/or stability is described.
Therapeutic use with monoclonal antibodies including adalimumab, trastuzumab, infliximab, and etanercept, where improved absorption and/or stability is described.
Antibacterial/microbial efficacy testing against USP <51> organisms using aqueous formulations combining specific alkylsaccharides with EDTA and described microbial log-reduction/no-increase criteria.
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