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A compound antihypertensive drug combination containing metofazong and its application

The technology of a drug and a composition is applied in the field of pharmaceutical compositions of metofazone and calcium channel antagonists, which can solve the problem of not weakening the diuretic effect, and achieve the effects of improving drug efficacy, reducing adverse reactions, and widening the number of drug users.

Active Publication Date: 2019-05-03
XIAN LIBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The adverse reactions of Metorfazon are also similar to those of hydrochlorothiazide, such as palpitations, chest pain, ventricular fibrillation, etc., but different from hydrochlorothiazide, it not only does not damage the renal function, but also has a low glomerular filtration rate due to renal dysfunction. In addition to the distal convoluted tubule and the distal end of the ascending branch of the loop, the diuretic effect may also be applied to the proximal convoluted tubule. The diuretic effect is stronger than that of hydrochlorothiazide and the diuretic period is longer

Method used

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  • A compound antihypertensive drug combination containing metofazong and its application
  • A compound antihypertensive drug combination containing metofazong and its application
  • A compound antihypertensive drug combination containing metofazong and its application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Embodiment 1: the preparation of compound pharmaceutical composition 1 (tablet) (in 1000 pieces)

[0039] Tablet prescription:

[0040] Amlodipine

5g

Methodox

0.5g

lactose

40g

microcrystalline cellulose

60g

Calcium hydrogen phosphate

20g

Sodium carboxymethyl starch

4.5g

Magnesium stearate

1g

[0041] Coating prescription

[0042] Opadry Coating Powder 4g

[0043] Purified water 45g

[0044] Preparation:

[0045] (1) Weigh the prescribed amount of amlodipine and metofazon, crush them through an 80-mesh sieve, and mix them uniformly by the method of equal increments.

[0046] (2) Weigh microcrystalline cellulose, lactose, calcium hydrogen phosphate, sodium carboxymethyl starch, and magnesium stearate in the prescribed amount, pulverize them through a 60-mesh sieve, and mix well.

[0047] (3) Mix (1) and (2) uniformly to obtain an intermediate.

[0048] (4) Check the intermediate content, ca...

Embodiment 2

[0051] Embodiment 2: the preparation of compound pharmaceutical composition 2 (tablet) (in 1000 pieces)

[0052] Tablet prescription:

[0053] Amlodipine

10g

Methodox

0.25g

microcrystalline cellulose

105g

Calcium hydrogen phosphate

50g

pregelatinized starch

30g

Sodium carboxymethyl starch

3g

Micropowder silica gel

0.5g

Magnesium stearate

1.25g

[0054] Coating prescription:

[0055] Opadry Coating Powder 4g

[0056] Purified water 45g

[0057] Preparation:

[0058] (1) Weigh the prescribed amount of amlodipine and metofazon, crush them through an 80-mesh sieve, and mix them uniformly by the method of equal increments.

[0059] (2) Weigh microcrystalline cellulose, calcium hydrogen phosphate, pregelatinized starch, sodium carboxymethyl starch, micropowder silica gel, and magnesium stearate in the prescribed amount, pulverize them through a 60-mesh sieve, and mix well.

[0060] (3) Mix (1...

Embodiment 3

[0064] Embodiment 3, the preparation of compound pharmaceutical composition 3 (capsules) (in 1000 grains)

[0065] prescription:

[0066] Amlodipine

2.5g

Methodox

1g

microcrystalline cellulose

30g

Calcium hydrogen phosphate

15g

[0067] Povidone K30

12g

Sodium dodecyl sulfate

0.8g

Magnesium stearate

0.75g

[0068] Preparation:

[0069] (1), raw materials and auxiliary materials are respectively passed through 80 mesh sieves, and set aside.

[0070] (2), get povidone K30, sodium lauryl sulfate, add warm water and dissolve to 50ml, as adhesive;

[0071] (3) Weigh amlodipine, metorfazon, microcrystalline cellulose, and calcium hydrogen phosphate, mix them uniformly with equal increments, add binders to make soft materials, granulate with 18 mesh sieves, and granulate at 80°C Set aside to dry.

[0072] (4), after the granules are dried, sieve the granules with 20 meshes, then add magnesium ste...

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Abstract

A pharmaceutical composition for treating hypertension is provided. The composition includes (1) a calcium channel antagonist, (2) a diuretic metolazone and (3) pharmaceutically acceptable accessories, wherein the weight ratio of the calcium channel antagonist to the metolazone is 1-40:0.1-2. By combination of the calcium channel antagonist and the metolazone, synergistic antihypertensive effects are improved, untoward effects are reduced, patient compliance is improved, and the medicine taking population is wide. The composition is particularly suitable for patients with renal function injury, and diuretic resistance is not liable to generate.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a pharmaceutical composition of metofazone and a calcium channel antagonist and an application thereof. Background technique [0002] Hypertension is the most common chronic disease and the most important risk factor for cardiovascular and cerebrovascular diseases. Its major complications such as stroke, myocardial infarction, heart failure and chronic kidney disease not only cause disability and high mortality, but also seriously consume medical and social resources, resulting in a heavy burden on the family and the country. [0003] Hypertension has become a major public health problem worldwide. According to statistics from the national health department, by the end of 2010, the number of hypertensive patients in my country has reached 200 million, and more than 3 million people are added every year. Hypertension is a clinical syndrome characterized by elevated systemic arter...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/517A61P9/12A61K31/4422A61K31/4545
Inventor 安龙王汝涛陈涛
Owner XIAN LIBANG PHARMA