Drug compound for AT1 receptor antagonist/diuretic/folate coupling and uses thereof

The technology of a receptor antagonist and a composition is applied in the field of pharmacy to achieve the effects of reducing target organ damage, taking medicines conveniently, and reducing medical expenses

Active Publication Date: 2008-06-18
SHENZHEN AUSA PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that β-blockers combined with thiazide diuretics are no longer the first-line treatment for all hypertensive patients

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Protective effect of telmisartan / hydrochlorothiazide+folic acid on reducing blood pressure and target organ damage in spontaneously hypertensive rats

[0036] Spontaneously hypertensive rats (SHR) were purchased from Shanghai Slack Experimental Animal Co., Ltd. (permit number: SCXK (Shanghai) 2003-0003), Beijing Weitong Lihua Experimental Animal Technology Co., Ltd. (permit number: SCXK) (Beijing) 2002-0003), and bred and bred in this room, spare. After 8 to 10 weeks of age, the blood pressure of the rats increased, and the blood pressure of the rats was measured for 1 week (days 1 and 6), and the rats with stable blood pressure were used for the experiment. The grouping and dosage of hypertensive rats are shown in Table 1. A WKY normal control group was also set up, with 20 rats in each group. Oral administration, once a day, weighed once a week, adjust the dose according to body weight, for 26 consecutive weeks. Observation indicators:

[0037] (1) Measu...

Embodiment 2

[0076] Example 2: Protective effect of irbesartan / hydrochlorothiazide+folic acid on target organ damage in spontaneously hypertensive rats

[0077] The blood pressure of white-haired hypertensive rats (SHR) increased after 8 to 10 weeks of age, and the blood pressure of the rats was measured for 1 week, and the rats with stable blood pressure were used for the experiment. According to the blood pressure value, SHR was divided into model group, irbesartan / hydrochlorothiazide (15+1.25mg / kg) group, irbesartan / hydrochlorothiazide+folic acid (15+1.25+0.04mg / kg), irbesartan / Hydrochlorothiazide + folic acid (15 + 1.25 + 0.08 mg / kg) group, folic acid group (0.08 mg / kg), and WKY normal control group, 20 rats in each group, administered by intragastric administration, once a day, for 26 consecutive weeks. At the end of the 26th week, blood was taken to measure serum nitric oxide (NO) and endothelin (ET) levels; urine was collected to measure 24h urine α1 microglobulin and urine creatin...

Embodiment 3

[0079] Example 3: Protective effect of candesartan / hydrochlorothiazide+folic acid on target organ damage in stroke-susceptible spontaneously hypertensive rats (SHRsp)

[0080] SHRsp aged 8 to 10 weeks were purchased from Shanghai Institute of Hypertension and Experimental Animal Center of Fuwai Hospital, and were kept at room temperature (23±2)°C, relative humidity (50±10)%, light and dark for 12 hours each, free to eat The standard feed and solid feed were provided by the Experimental Animal Breeding Farm of the Chinese Academy of Medical Sciences, and the drinking water was purified water. Blood pressure was measured before the test, and SHRsp was divided into model group, candesartan / hydrochlorothiazide (1.6mg / kg+1.25mg / kg) group, candesartan / hydrochlorothiazide+folic acid (1.6mg / kg+1.25mg / kg+0.08mg / kg) group, and a WKY control group, 30 rats in each group. Oral administration, once a day, weighed once a week, adjust the dose according to body weight, for 20 consecutive w...

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PUM

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Abstract

The invention relates to a drug combination of applying jointly angiotensin II receptor antagonist / diuretic / folacin and the purpose. The combination includes: officinal dose of angiotensin II receptor antagonist, officinal dose of diuretic, officinal does of folic acid compound and pharmacy-acceptable carrier. The invention provides the purpose of the combination in preparing the medicine used for preventing, treating or delaying hypertension, target organ damage caused by hypertension or hypertension-related diseases; the invention also provides the purpose of the drug combination in preparing the medicine used for reducing the danger of cardiovascular and cerebrovascular events caused by hypertension. The implementation of the invention, which provides the patient with the drug combination, can improve the curative effect, increase the compliance of the patient, convenience the drug administration and reduce the medical expenses.

Description

technical field [0001] The invention relates to an angiotensin II receptor (AT1 receptor) antagonist / diuretic / folic acid combined pharmaceutical composition and application thereof, belonging to the field of pharmacy. Background technique [0002] As one of the common diseases that endanger human health, essential hypertension is the main cause of serious cardiovascular and cerebrovascular diseases such as myocardial infarction, stroke, and kidney disease. The main purpose of treating hypertension is to minimize the total risk of death and disability from cardiovascular disease. Lowering blood pressure with drugs can effectively reduce the morbidity and mortality of cardiovascular complications and prevent stroke, coronary heart disease, and heart failure. and the occurrence and development of kidney disease. The first-line antihypertensive drugs recommended by WHO and my country’s guidelines for the prevention and treatment of hypertension are: diuretics, β-adrenergic rece...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/549A61K31/519A61K9/16A61K9/20A61K9/48A61P9/10A61P9/12A61P13/12A61P27/02A61K31/4184A61K31/4178
Inventor 陈光亮王琳琳李莉吕红霞刘海鹏胡容峰段炎炎孙聪王媛媛徐希平
Owner SHENZHEN AUSA PHARMA
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