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Compound of losartan compound or its medical salt and calcium channel blocker or its medical salt

A technology of calcium channel blocker and medicinal salt, which is applied in the field of medicine to achieve the effect of lowering blood pressure, less side effects, and a wide range of applications

Inactive Publication Date: 2009-01-21
BEIJING INSTITUTE OF TECHNOLOGYGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

one of the articles [1] In the clinical trials to demonstrate the rationality of single-drug and combined drug therapy, it w

Method used

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  • Compound of losartan compound or its medical salt and calcium channel blocker or its medical salt
  • Compound of losartan compound or its medical salt and calcium channel blocker or its medical salt
  • Compound of losartan compound or its medical salt and calcium channel blocker or its medical salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1 Compound I and Amlodipine Combined Therapeutic Effect Observation on Moderate to Severe Hypertension

[0033] 1. Materials and methods

[0034] 1. Research object

[0035] 1.1 Case selection: A total of 90 outpatients and hospitalized 18-70-year-old patients with mild, moderate and high blood pressure who have not been treated or have used antihypertensive drugs, including 35 males and 35 females, with a body mass index of 30, took placebo The diastolic blood pressure in sitting position is 95-109mnHg (1mmHg=0.133kPa), and the systolic blood pressure in sitting position is 180Hg. Exclusion criteria: secondary hypertension, history of cardiovascular and cerebrovascular disease attacks, arrhythmia requiring drug treatment, allergies to drug ingredients, drug abuse or alcoholism, pregnancy and lactation, type 2 diabetes, low and high blood pressure Potassium symptoms, thyroid dysfunction, severe liver and kidney insufficiency.

[0036] Two research methods

...

Embodiment 2

[0049] Example 2 Observation and treatment of compound I and amlodipine combined medication on synergistic effect in spontaneously hypertensive rats

[0050] 1. Materials and methods

[0051] 1. Test drug

[0052] (2-n-propyl-4-methyl-1H-benzimidazole)-6-yl]formamido-1-yl]methylbiphenyl tetrazolium compound, off-white powder (manufactured), content 99.8% ( w / w); Amlodipine, white powder, provided by Changzhou Yabang Pharmaceutical Co., Ltd. The two medicines are prepared into a suspension solution from 0.3% CMC, and the storage solutions are stored in accordance with the concentration of intragastric administration, and stored in a refrigerator away from light.

[0053] 2. Experimental animals

[0054]5 groups of spontaneously hypertensive rats (SHR), 8 in each group, purchased from: Department of Animal Experiments, Beijing Fuwai Hospital, Academy of Sciences, Chinese Academy of Medicine, in line with the first-class standard, body weight (250±30) g; animal certificate: 01...

Embodiment 3

[0061] Example 3 Compound I and Garopamil Combined Medication Treatment Observation on Diabetes Combined with Hypertension Rats

[0062] A representative study was performed with a combination of I and a non-DHP representative of CCB, such as garopamil.

[0063] There is a good antihypertensive synergistic effect between I and Garopamil, especially for diabetes combined with hypertension, that is, the combined effect of the two is higher than the algebraic sum of the effects of the two components alone .

[0064] At present, diabetes combined with hypertension is an important factor for the development and deterioration of diabetes. Lowering blood pressure can well control urinary protein and nephropathy factors in diabetic patients. Currently, among the first-line CCB drugs for the treatment of hypertension, there is no evidence that they have a protective and therapeutic effect on renal hypertension. However, this experiment confirmed that the combined therapy of this drug ...

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Abstract

The invention relates to a formula of a sartan compound or a pharmaceutically acceptable salt thereof and a calcium channel blocker or a pharmaceutically acceptable salt, which belong to the technical field of medicine. The formula comprises the following components by weight proportion: 5-200 parts of [(2-n-propyl-4-methyl-1H-benzimidazole)-6-carboxamide-1-radical] methyl biphenyl tetrazolium and a carboxylic acid compound and salt thereof and 0.5-60 parts of a calcium ion retarder; the preferable scheme is 20-100 parts of the [(2-n-propyl-4-methyl-1H-benzimidazole)-6-carboxamide-1-radical] methyl biphenyl tetrazolium and the carboxylic acid compound and the salt thereof and 1-30 parts of the calcium ion retarder; the administration forms can be one of the following forms such as oral administration, inhalation, subcutaneous administration, sublingual administration, intramuscular administration, intravenous administration, transdermal administration, local administration or rectal administration. In the formula of the invention, an antihypertensive I and the calcium channel blocker or the pharmaceutically acceptable salt are studied; thus a preparation with a new formula for treating hypertension is provided. The preparation is characterized by low dosage, obvious blood pressure lowering effect and little adverse reaction.

Description

technical field [0001] The invention relates to a compound of a sartan compound or a pharmaceutically acceptable salt thereof and a calcium channel blocker or a pharmaceutically acceptable salt, belonging to the technical field of medicine. Background technique [0002] Hypertension is the most common cardiovascular disease, and its complications are one of the leading causes of human death. It is an issue of major public commitment on a global scale. my country is in a period of rapid social and economic development. With the transformation of society and the intensification of population aging, people's living standards and behaviors have undergone tremendous changes, and the prevalence of hypertension has also shown a rapid upward trend. According to the prediction of the World Health Organization, cardiovascular diseases will become prevalent in certain parts of Asia, Latin America, the Middle East and Africa on a large scale. In China, by 2020, non-communicable diseas...

Claims

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Application Information

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IPC IPC(8): A61K31/4184A61K45/00A61K31/4422A61P9/12
Inventor 周智明董美伶薛为哲章军
Owner BEIJING INSTITUTE OF TECHNOLOGYGY
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