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Drug for treating or preventing duplication of hypertension with serum hyperuricemia and/or hypercholesterolemia

A technology for hypercholesterolemia and hyperuricemia, applied in the field of drugs used to treat hypertension combined with serum hyperuricemia and/or hypercholesterolemia, and can solve problems such as lowering cholesterol

Inactive Publication Date: 2010-05-26
KOTOBUKI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For hypercholesterolemia, sometimes a single agent cannot achieve a sufficient cholesterol-lowering effect. In this case, the general clinical situation is to combine multiple cholesterol-lowering drugs

Method used

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  • Drug for treating or preventing duplication of hypertension with serum hyperuricemia and/or hypercholesterolemia
  • Drug for treating or preventing duplication of hypertension with serum hyperuricemia and/or hypercholesterolemia
  • Drug for treating or preventing duplication of hypertension with serum hyperuricemia and/or hypercholesterolemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Regarding the uric acid excretion-promoting action, the delay in disappearance of phenol red in blood was used as an index to evaluate. Specifically, for 6-week-old SD male rats, 0.5% methylcellulose (MC), 30 mg / kg or 100 mg / kg of prasartan was orally administered, and 75 mg of prasartan was administered intravenously 3 hours after administration. / kg of phenol red. One hour after the administration of phenol red, blood was collected from the abdominal aorta under ether anesthesia, and the amount of phenol red in the serum was measured. The amount of phenol red in the blood serum of the control group to which prasartan was not administered was regarded as 100%, and the delayed rate of disappearance of phenol red in the blood by administration of prasartan was evaluated as the uric acid excretion promotion rate (%) . Table 1 shows the composition of the groups, the test substances and their doses, and the uric acid excretion promotion rate (mean ± standard deviation). ...

Embodiment 2

[0027] The test was carried out on patients with mild and moderate essential hypertension. Prasartan was administered to 17 patients who also suffered from hyperuricemia, and the serum uric acid values ​​(mg / dL) (mean ± standard deviation) before administration and on the last day of administration were studied. The results are shown in Table 2. It should be noted that 40 mg / day to 160 mg / day of prasartan is administered orally at intervals of 4 weeks, and the dose is increased by increasing the dose if the antihypertensive effect is not obvious.

[0028] Table 2

[0029]

Embodiment 3

[0031] Using the Tail cuff method, the systolic blood pressure of 20-week-old male SHR (Spontaneously hypertensiverat, SPF grade, production unit; Hoshino Experimental Animal Breeding Institute: spontaneously hypertensive rats) was measured, and the animals were divided into 4 groups. The average value of the systolic blood pressure of animals in each group was uniform. Oral administration of 0.5% methyl cellulose (MC) or a solution formed by suspending the test substance in 0.5% methyl cellulose, once a day, for 28 days, before the start of administration and at the 1st, 7th, and 1st days of administration. Systolic blood pressure 5 hours after administration on the 14th and 28th. Table 3 shows the composition of the group, the test substance and its dosage. In addition, see Table 4 for the measured blood pressure (mmHg) (mean ± standard deviation) of the measurement results. It should be noted that the test substances are divided into hydrochlorothiazide (HCTZ), prasartan, ...

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Abstract

The purpose in this invention is to providing drugs for treating or preventing duplication of hypertension with serum hyperuricemia and / or hypercholesterolemia that is much frequency among the duplication onset in geriatric diseases. This invention is related to drugs for treating or preventing duplication of hypertension with serum hyperuricemia and / or hypercholesterolemia of which active principles are 2-propyl-3- {[2'-(1H-tetrazole -5-yl) biphenyl -4-yl]methyl}-5, 6, 7, 8-tetrahydrocyclohepta imidazole -4-(3H) - one and that prodrug or that salt. Pratosartan is able to use in combination with one or more than two diuretics chosen from sulfonamide-, phenoxyacetic acid- and thiazide-type diuretics, triamterene, amiloride, spironolactone, potassium canrenoate and traxanox sodium. Also, pratosartan is able to use in combination with one or more than two hypolipidemic drugs chosen from statins, fibrates, cholesterol absorption inhibitors, cholesterol sequestrants and cholesterol excretion enhancers.

Description

technical field [0001] The invention relates to a medicine for treating hypertension combined with serum hyperuricemia and / or hypercholesterolemia. Background technique [0002] In recent years, various studies have been conducted on the prevention and treatment of adult diseases. Examples of risk factors for adult diseases include hypertension, hypercholesterolemia, diabetes, obesity, and serum hyperuricemia. Moreover, it is known that when two or more of these risk factors occur in combination, the mortality rate will increase sharply. In addition, in such a combination of risk factors, it is known that the frequency of the combination of hypertension and hyperuricemia and the combination of hypertension and hypercholesterolemia is high. [0003] In the past, angiotensin II receptor antagonists have been widely used in the treatment of hypertension. Furthermore, it is known from animal experiments and the like that angiotensin II receptor antagonists have the effect of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D403/10A61K31/4184A61P3/06A61P9/12A61P19/06
CPCA61K31/4184A61P19/06A61P25/20A61P3/06A61P43/00A61P7/10A61P9/12A61K31/549C07D257/04
Inventor 富山格富山泰宫本英俊林启一郎望月诚一郎
Owner KOTOBUKI PHARMA CO LTD
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