Combined preparation of a thiazide diuretic and a loop diuretic

A technology of diuretics and thiazides, applied in the field of pharmaceutical preparations, can solve problems such as hyperkalemia, achieve the effects of prolonging the action time, preventing hypokalemia, and improving excretion

Inactive Publication Date: 2008-08-27
海因里希·克瑙夫
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this fixed combination also poses a problem due to the risk of hyperkalemia in patients with elevated plasma creatinine (and in older persons with pseudonormal plasma creatinine)

Method used

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  • Combined preparation of a thiazide diuretic and a loop diuretic
  • Combined preparation of a thiazide diuretic and a loop diuretic
  • Combined preparation of a thiazide diuretic and a loop diuretic

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Experimental program
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Effect test

Embodiment

[0037] 1. Method

[0038] The ethically justified experiments were performed in 12 healthy volunteers (age 28-48 years, 6 males, 6 females) who had given their written consent to the study. Prior to dosing, participants were clinically tested. Participants maintained a standard diet, receiving defined fluid (1.5 L / day) and salt intake (6 g NaCl; 100 mmol Na + / sky).

[0039] According to an earlier study (35), urine was collected prior to the treatment period, ie 24 hours to 12 hours and 12 hours to 0 hours (8 am) before oral administration. From this time point, urine was collected at 2-hour intervals until the 6th hour after administration, then from the 6th to the 9th hour, from the 9th to the 12th hour and from the 12th to the 24th hour. Samples of defined volumes during the respective collections were frozen and analyzed for Na using the "MODULAR" analyzer (Roche Comp., Switzerland). + 、K + , Cl - , Ca 2+ , Mg 2+ and creatinine.

[0040] All data are expressed as...

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PUM

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Abstract

The invention relates to pharmaceutical preparations which contain a combination of a thiazide diuretic and a low dose of a loop diuretic and which is particularly suitable for treating hypertension and heart failure. It is not only the natriuretic / diuretic effects which are increased due to said combination of thiazide diuretic and loop diuretic, but also the undesired secondary effects in relation to potassium and magnesium losses are also significantly reduced. As a result, the desired hypocalciuric effect of the thiazide is maintained despite the presence of the loop diuretic.

Description

technical field [0001] The present invention relates to pharmaceutical formulations containing a fixed combination of a low dose loop diuretic and a thiazide diuretic. Background technique [0002] Free combinations of loop diuretics / thiazide diuretics have been and are being used successfully in patients with so-called diuretic resistance (ie, patients in whom even high doses of loop diuretics are ineffective or insufficiently effective) , and in patients with severe renal failure. In 1971, the use of high-dose infusions of loop diuretics (eg, furosemide) in patients with severe cardiac disease with the addition of a thiazide diuretic (eg, chlorthalidone) was first reported. Re-establish diuresis in patients who no longer respond to treatment. In patients with severe renal disease, the combination of diuretics may reduce the often required ultra-high doses of loop diuretics and thus reduce the occurrence of side effects. However, in both cases, due to the risk of serious...

Claims

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Application Information

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IPC IPC(8): A61K31/64A61K31/549A61P7/10
CPCA61K31/549A61K31/64A61P7/10A61P9/00A61P9/04A61P9/12A61K2300/00
Inventor 海因里希·克瑙夫恩斯特·穆奇勒
Owner 海因里希·克瑙夫
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