Insoluble compositions for controlling blood glucose

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/44 (2006.01) A61K 38/28 (2006.01)

Patent

CA 2315300

The present invention relates to insoluble compositions comprising a protein selected from the group consisting of insulin, insulin analogs, and proinsulins; a derivatized protein selected from the group consisting of derivatized insulin, derivatized insulin analog, and derivatized proinsulin; a complexing compound; a hexamer-stabilizing compound; and a divalent metal cation. Formulations of the insoluble composition are suitable for both parenteral and non-parenteral delivery for treating hyperglycemia and diabetes. Microcrystal forms of the insoluble precipitate are pharmaceutically analogous to the neutral protamine Hagedorn (NPH) insulin crystal form. Surprisingly, it has been discovered that suspension formulations of such insoluble compositions possess unique and controllable dissolution properties that provide therapeutically advantageous glucodynamics compared with insulin NPH formulations.

L'invention porte: sur des compositions insolubles comportant une protéine sélectionnée parmi l'insuline, des analogues de l'insuline et des proinsulines; sur une protéine dérivée sélectionnée parmi de l'insuline dérivée, un analogue de l'insuline dérivée et de la proinsuline dérivée; sur un composé de complexion; sur composé stabilisateur d'hexamère; et sur un cation de métal divalent. Les préparations contenant ces compositions, administrables par voie parentérale ou non parentérale, servent à traiter l'hyperglycémie et le diabète. Les formes microcristallines du précipité insoluble sont pharmaceutiquement analogues à la forme cristalline de l'insuline isophane (NPH). On a eu la surprise de découvrir que les préparations en suspension desdites compositions insolubles avaient des propriétés singulières et contrôlables de dissolution présentant une glucodynamique thérapeutiquement avantageuse par rapport aux préparations d'insuline isophane.

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