Stabilizing alkylglycoside compositions and methods thereof
Inventors
Assignees
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Publication Number
US-8133863-B2
Publication Date
2012-03-13
Expiration Date
Abstract
The present invention relates to alkylglycoside-containing compositions and methods for increasing the stability, reducing the aggregation and immunogenicity, increasing the biological activity, and reducing or preventing fibrillar formation of a peptide, polypeptide, or variant thereof, for example amylin, a monoclonal antibody, insulin, Peptide T or analog thereof, gastrin, gastrir releasing peptides, gastrin releasing peptide-like (GRP) proteins, epidermal growth factor or analog thereof.
Core Innovation
The invention relates to liquid pharmaceutical compositions for increasing the stability, reducing aggregation or reducing immunogenicity of octreotide or a variant thereof. The compositions include octreotide or a variant thereof and a stabilizing agent comprising at least one alkylglycoside, and the compositions are free of naturally occurring variants of octreotide.
The invention further provides a method for increasing the stability of octreotide or a variant thereof by admixing octreotide or a variant thereof, a stabilizing agent, and a buffering agent to form a liquid composition. The stabilizing agent is at least one alkylglycoside surfactant, thereby increasing the stability of the octreotide or the variant, with the proviso that the liquid composition is free of naturally occurring variants of octreotide.
In the described scope, alkylglycoside surfactants and saccharide alkyl ester surfactants are used to increase stability and reduce aggregation and fibril formation while preserving biological activity, and to reduce immunogenicity. The document also discusses aggregation and fibrillation behavior as dependent on concentration, temperature, and ionic strength, and refers to improved stabilization duration.
Claims Coverage
The partial content includes two independent claims: one composition claim and one method claim. Both claims center on using alkylglycoside surfactants for stability enhancement under the restriction that the composition is free of naturally occurring variants of octreotide.
Liquid pharmaceutical composition with alkylglycoside stabilizing agent
A liquid pharmaceutical composition for increasing the stability, reducing aggregation or reducing immunogenicity of octreotide or a variant thereof comprising octreotide or a variant thereof and a stabilizing agent comprising at least one alkylglycoside, with the proviso that the composition is free of naturally occurring variants of octreotide.
Admixing alkylglycoside surfactant stabilizing agent with buffering agent
A method for increasing the stability of octreotide or a variant thereof comprising admixing octreotide or a variant thereof, a stabilizing agent and a buffering agent to form a liquid composition, with the proviso that the composition is free of naturally occurring variants of octreotide, wherein the stabilizing agent is at least one alkylglycoside surfactant, thereby increasing the stability of the octreotide or variant thereof.
Across the independent claims, the coverage is directed to liquid formulations of octreotide or a variant that include at least one alkylglycoside surfactant as a stabilizing agent and that exclude naturally occurring octreotide variants. The method claim mirrors the composition structure by requiring admixing the octreotide or variant with the alkylglycoside surfactant stabilizing agent and a buffering agent in a liquid composition.
Stated Advantages
Increasing stability of octreotide or a variant thereof.
Reducing aggregation.
Reducing immunogenicity.
Preserving biological activity.
Reducing fibril formation.
Reducing anti-insulin antibody titers.
Maintaining glucose-lowering activity after storage.
Documented Applications
Liquid pharmaceutical formulations containing octreotide or a variant thereof, including delivery-mode constraints for intranasal, pulmonary, or buccal delivery.
Therapeutic liquid formulations using peptide and protein examples described in the document for stability and aggregation control, including insulin, amylin/IAPP, monoclonal antibodies, growth hormone, Peptide T/DAPTA, and HIV CCR5 entry inhibitor analogs.
Assessing stability by determining bioactivity of octreotide or variants using in vivo or in vitro assays.
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