Insulin analog formulations
First Claim
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1. A human insulin analog complex, which comprises:
- six molecules of a human insulin analog, two zinc ions, and at least three molecules of a phenolic derivative selected from the group consisting of m-cresol, phenol, or a mixture of m-cresol and phenol;
such that the insulin analog complex is a hexamer;
wherein the human insulin analog is human insulin wherein Pro at position B28 is substituted with Asp, Lys, Leu, Val, or Ala, and Lys at position B29 is Lys or Pro;
des(B28-B30)-human insulin;
or des (B27 )-human insulin.
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Abstract
The present invention discloses a human insulin analog hexamer complex and formulations. More specifically, the present invention relates to various parenteral formulations, which comprise: human insulin analogs in a hexamer conformation, zinc ions, and at least three molecules of a phenolic derivative selected from the group consisting of m-cresol, phenol, or a mixture of m-cresol and phenol. The formulation provides a rapid onset of action.
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13 Claims
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1. A human insulin analog complex, which comprises:
- six molecules of a human insulin analog, two zinc ions, and at least three molecules of a phenolic derivative selected from the group consisting of m-cresol, phenol, or a mixture of m-cresol and phenol;
such that the insulin analog complex is a hexamer;
wherein the human insulin analog is human insulin wherein Pro at position B28 is substituted with Asp, Lys, Leu, Val, or Ala, and Lys at position B29 is Lys or Pro;
des(B28-B30)-human insulin;
or des (B27 )-human insulin. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11)
- six molecules of a human insulin analog, two zinc ions, and at least three molecules of a phenolic derivative selected from the group consisting of m-cresol, phenol, or a mixture of m-cresol and phenol;
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12. A human insulin analog complex, consisting of:
- six molecules of a human insulin analog, two zinc ions, and at least three molecules of a phenolic derivative selected from the group consisting of m-cresol, phenol, or a mixture of m-cresol and phenol;
such that the insulin analog complex is a hexamer;wherein the human insulin analog is human insulin wherein Pro at position B28 is substituted with Asp, Lye, Leu, Val, or Ala, and Lys at position B29 is Lys or Pro;
des(B28-B30)-human insulin;
or des(B27)-human insulin.
- six molecules of a human insulin analog, two zinc ions, and at least three molecules of a phenolic derivative selected from the group consisting of m-cresol, phenol, or a mixture of m-cresol and phenol;
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13. A parenteral pharmaceutical formulation consisting of:
- about 3.5 mg/mL LysB28 ProB29 -human insulin, about 19.7 μ
g/mL zinc, about 7 mM sodium phosphate, about 16 mg/mL glycerin, and about 29 mM m-cresol;
wherein LysB28 ProB29 -human insulin is a hexamer.
- about 3.5 mg/mL LysB28 ProB29 -human insulin, about 19.7 μ
Specification