4.4 Article

The quaternary structure of insulin glargine and glulisine under formulation conditions

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BIOPHYSICAL CHEMISTRY
卷 253, 期 -, 页码 -

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ELSEVIER
DOI: 10.1016/j.bpc.2019.106226

关键词

Insulin; Glargine; Glulisine; Quaternary structure; SAXS

资金

  1. iNEXT - Horizon 2020 program of the European Union [653706, 2861]

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The quaternary structures of insulin glargine and glulisine under formulation conditions and upon dilution using placebo or water were investigated using synchrotron small-angle X-ray scattering. Our results revealed that insulin glulisine in Apidra (R) is predominantly hexameric in solution with significant fractions of dodecamers and monomers. Upon dilution with placebo, this equilibrium shifts towards monomers. Insulin glargine in Lantus (R) and Toujeo (R) is present in a stable hexamer/dimer equilibrium, which is hardly affected by dilution with water down to 1 mg/ml insulin concentration. The results provide exclusive insight into the quaternary structure and thus the association/dissociation properties of the two insulin analogues in marketed formulations.

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