Novel formulations

Abstract

There is provided inter aliaan aqueous liquid pharmaceutical formulationcomprising (i) an insulincompound at a concentration of 500-1000 U / ml, (ii) ionic zinc, (iii) a zinc binding species at a concentration of 1 mM or more selected from species having a logK with respect to zinc ion binding in the range 4.5-12.3 at 25 DEG C, and (iv) a non-ionic surfactant; and wherein the formulation is substantially free of EDTA and any other zinc binding species havinga logK with respect to zinc ion binding of more than 12.3at 25 DEG C.

Description

field of invention [0001] In particular, the present invention relates to rapid-acting aqueous liquid formulations of insulin and insulin analogues. Such compositions are suitable for the treatment of patients suffering from diabetes, especially type I diabetes. Background of the invention [0002] Diabetes mellitus is a metabolic disorder associated with poor control of blood sugar levels, leading to hypoglycemia or hyperglycemia. Untreated diabetes can lead to serious microvascular and macrovascular complications, including coronary artery disease, peripheral artery disease, stroke, diabetic nephropathy, neuropathy, and retinopathy. The two main types of diabetes are (i) type 1 diabetes, which results from the pancreas not producing insulin, and the usual treatment is insulin replacement therapy, and (ii) type 2 diabetes, in which the patient produces insufficient insulin or is insulin resistant, which Treatment consists of insulin sensitizers (such as metformin or piogl...

AI Technical Summary

Problems solved by technology

[0020] However, a known problem associated with the use of formulations containing higher concentrations of insulin compounds, especially rapid-acting insulin compounds, is the reduced rapid-acting effect observed in low-concentration (or low-strength) formulations such as 100 U / ml of insulin compound up

Thus, increasing concentrations of insulin compounds have been observed to result in slower onset of action, even though the same dose is delivered, see e.g. de la "Pharmacokinetics and Pharmacodynamics of High-Dose Human Regular U-500 Insulin Versus Human Regular U -100 Insulin in Healthy Obese Subjects), Diabetes Care, 34, pp. 2496-2501, 2011

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