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MAGNESIUM-CONTAINING COMPOSITIONS FOR MODULATION OF THE PHARMACOKINETICS AND PHARMACODYNAMICS OF INSULIN AND ANALOGUES OF INSULIN AND PAIN FEELINGS IN THE PLACE OF INJECTION
MAGNESIUM-CONTAINING COMPOSITIONS FOR MODULATION OF THE PHARMACOKINETICS AND PHARMACODYNAMICS OF INSULIN AND ANALOGUES OF INSULIN AND PAIN FEELINGS IN THE PLACE OF INJECTION
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机译:注射部位的含镁组合物,用于调节胰岛素的药代动力学和药动学以及胰岛素和疼痛感的类似物
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摘要
1. A pharmaceutically acceptable injectable composition comprising: insulin; an effective amount of a first compound that chelates zinc to dissociate insulin hexamers to insulin monomers and dimers; an effective amount of a second compound that stabilizes insulin monomers and dimers resulting from dissociation; and an effective amount of one or more magnesium compounds to reduce discomfort at the injection site, compared with discomfort at the injection site of the dosage form in the absence of one or more magnesium compounds. 2. The composition of claim 1, wherein the insulin is human recombinant insulin. The composition of claim 1, wherein the insulin is an insulin analogue. The composition of claim 1, wherein the insulin concentration is 100, 200, 400, or 500 IU / ml. A composition according to claim 1 or 2, wherein one or more magnesium compounds are selected from the group consisting of inorganic magnesium salts, organic magnesium salts, and combinations thereof. The composition of claim 4, wherein the inorganic magnesium salts are selected from the group consisting of magnesium hydroxide (Mg (OH)), magnesium sulfate (Mg (SO)), magnesium halides such as magnesium chloride (MgCl), magnesium bromide (MgBr ) and magnesium iodide (MgI); magnesium pyrophosphate, magnesium sulfate heptahydrate, magnesium oxide (MgO), and combinations thereof. 7. The composition of claim 4, wherein the organic magnesium salts are selected from the group consisting of EDTA magnesium salt, magnesium lactate, amino acid chelating compounds such as magnesium aspartate; magnesium acetate, magnesium carbonate (Mg (CO)), magnesium citrate and magnesium gluconate. 8. The composition according to any one of paragraphs. 1-6, in which one or more magnesium compounds are Mg (OH), MgSO, EDTA magnesium salt, or combinations thereof. 9. The composition according to any one of paragraphs. 1-7, in which
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