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Compound antihypertensive preparation and application of compound antihypertensive preparation

A technology of high blood pressure and receptor antagonists, which is applied in the field of pharmaceutical compositions with metolazone as the active ingredient and angiotensin Ⅱ receptor antagonists, to achieve enhanced synergistic antihypertensive effect, a wide range of drug users, and improved compliance Effect

Inactive Publication Date: 2015-02-04
XIAN LIBANG ZHAOXIN BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The patent does not mention the drug users. We know that candesartan may worsen liver function in patients with liver dysfunction. It should be used with caution in clinical practice, and it should also be used with caution in patients with severe renal impairment

Method used

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  • Compound antihypertensive preparation and application of compound antihypertensive preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Embodiment 1: Preparation of compound pharmaceutical composition 1 (tablet) (calculated in 1000 tablets)

[0077] Tablet core prescription :

[0078] Valsartan 80

[0079] Metolazone 0.5

[0080] Microcrystalline Cellulose 60

[0081] starch 20

[0082] Crospovidone 10

[0083] Croscarmellose Sodium 4.5

[0084] Micronized silica gel 3

[0085] Magnesium Stearate 2.5

[0086] Coating prescription

[0087] Opadry Coating Powder 4g

[0088] Purified water 45g

[0089] Preparation:

[0090] (1) Weigh the prescribed amount of valsartan and metolazone, crush them through an 80-mesh sieve, and mix them evenly by using the method of equal increments.

[0091] (2) Weigh the prescribed amount of microcrystalline cellulose, starch, crospovidone, croscarmellose sodium, and micropowder silica gel, crush them through a 60-mesh sieve, and mix well.

[0092] (3) Mix (1) and (2) evenly, then add magnesium stearate, and mix evenly to obtain an intermediate.

[0093]...

Embodiment 2

[0096] Embodiment 2: Preparation of compound pharmaceutical composition 2 (tablet) (calculated in 1000 tablets)

[0097] Tablet prescription:

[0098] Valsartan 160g

[0099] Metolazone 0.25

[0100] Microcrystalline Cellulose 80g

[0101] Starch 26.5g

[0102] Crospovidone 15g

[0103] Croscarmellose Sodium 10g

[0104] Micronized silica gel 6g

[0105] Magnesium Stearate 2.5g

[0106] Coating prescription:

[0107] Opadry Coating Powder 4g

[0108] Purified water 45g

[0109] Preparation :

[0110] (1) Weigh the prescribed amount of valsartan and metolazone, crush them through an 80-mesh sieve, and mix them evenly by using the method of equal increments.

[0111] (2) Weigh the prescribed amount of microcrystalline cellulose, starch, crospovidone, croscarmellose sodium, and micropowder silica gel, crush them through a 60-mesh sieve, and mix well.

[0112] (3) Mix (1) and (2) evenly, then add magnesium stearate, and mix evenly to obtain an intermediate.

[0...

Embodiment 3

[0116] Embodiment 3, the preparation of compound pharmaceutical composition 3 (capsules) (in 1000 grains)

[0117] prescription :

[0118] Valsartan 40g

[0119] Metolazone 1g

[0120] Microcrystalline Cellulose 50 g

[0121] Crospovidone 15g

[0122] Povidone K30 12g

[0123] Sodium Lauryl Sulfate 0.8g

[0124] Magnesium stearate 1.2g

[0125] Preparation:

[0126] (1) Raw materials and auxiliary materials are passed through 80-mesh sieve respectively, and set aside.

[0127] (2) Take povidone K30 and sodium lauryl sulfate, dissolve in warm water to 50ml, and use it as a binder;

[0128] (3) Weigh valsartan, metolazone, microcrystalline cellulose, and crospovidone, mix them uniformly in equal increments, add binders to make soft materials, and granulate with 18 mesh sieves. Dry at ℃.

[0129] (4) After the granules are dried, sieve the granules with a 20-mesh sieve, then add magnesium stearate, and mix well.

[0130] (5) Calculate the content of intermediates...

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Abstract

The invention provides a medicine composition for treating hypertension. The medicine composition is characterized in that the medicine composition comprises (1) angiotensin II receptor antagonists, (2) diuretic metolazone and (3) acceptable auxiliary materials on pharmaceutical science. The weight proportion of the angiotensin II receptor antagonists to the metolazone is 20-200:0.5-10; the angiotensin II receptor antagonists and the metolazone are combined to strengthen the collaboration antihypertensive effect; untoward effects are reduced; the compliance of patients is improved; the medication crowds are wide; and the medicine composition can be used by the patients with the seriously-damaged renal function. The medicine composition is suitable for treating mild and moderate primary hypertension, and is particularly suitable for treating secondary hypertension caused by kidney damage.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a pharmaceutical composition with an angiotensin II receptor antagonist and metolazone as active ingredients and an application thereof. Background technique [0002] With the rapid growth of my country's economy and drastic changes in people's lifestyles, cardiovascular disease has become the biggest killer threatening human health. Hypertension is one of the most common cardiovascular diseases and 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 arterial systolic blood pressure (SBP) and / or diastolic blood pressure (DBP), especially the damage to target organs such as the heart, brain, and kidneys induced by...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/517A61P9/12
Inventor 张婉直陈涛余惟平
Owner XIAN LIBANG ZHAOXIN BIOTECH CO LTD
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