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Application of aldenafil citrate in preparation of medicine for preventing and/or treating pulmonary arterial hypertension

A technology of pulmonary arterial hypertension and citric acid, which is applied in the field of preparation of edenafil citrate for the prevention and treatment of pulmonary arterial hypertension, and can solve problems such as unsatisfactory treatment effects

Pending Publication Date: 2022-07-19
YOUCARE PHARMA GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Bosentan is currently the first-line drug for the clinical treatment of pu

Method used

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  • Application of aldenafil citrate in preparation of medicine for preventing and/or treating pulmonary arterial hypertension
  • Application of aldenafil citrate in preparation of medicine for preventing and/or treating pulmonary arterial hypertension
  • Application of aldenafil citrate in preparation of medicine for preventing and/or treating pulmonary arterial hypertension

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0039] Example 1

[0040] In this example, from the perspective of preventing pulmonary arterial hypertension, a rat model of pulmonary arterial hypertension was established, and a preventive drug regimen was implemented.

[0041]EXAMPLES Animals 70 SPF SD rats with a body weight of 200-220 g were randomly divided into 7 groups with 10 rats in each group. The above 7 groups were set as normal control group, pulmonary hypertension model group and positive drug sildenafil group respectively. (30 mg / kg, oral administration, once a day), positive drug bosentan group (100 mg / kg, oral administration, once a day), edenafil citrate low-dose group (15 mg / kg, oral administration , once a day), edenafil citrate medium-dose group (30 mg / kg, orally, once a day) and edenafil citrate high-dose group (60 mg / kg, orally, once a day) . At the beginning of the experiment, except for the normal control group, which was given an equal amount of normal saline, other animals were given 50 mg / kg of ...

Example Embodiment

[0049] Example 2

[0050] In this example, from the perspective of preventing pulmonary arterial hypertension, the effect of aldenafil citrate on the survival rate of pulmonary arterial hypertension model rats was studied.

[0051] At the end of the experiment, the death of animals was counted. The results are shown in Table 1, 2 animals died in the model group, and there was no animal death in the blank group and each administration group, indicating that the administration of idinafil citrate can delay the development of pulmonary hypertension and play a preventive role. while reducing mortality.

[0052] Table 1 Survival rate of rats at the end of the preventive effect experiment

[0053]

Example Embodiment

[0054] Example 3

[0055] In this example, from the perspective of preventing pulmonary arterial hypertension, the effects of aldenafil citrate on cardiac function, right ventricular systolic pressure and right ventricular remodeling in pulmonary arterial hypertension model rats were studied.

[0056] At the end of the experiment, the rats were anesthetized with chloral hydrate, their limbs and heads were fixed on the mouse plate, and the animal body temperature was maintained by turning on the heating plate. The needle electrodes were subcutaneously inserted into the front and rear limbs, and the ECG changes in lead II were observed and recorded for 3 minutes.

[0057] On the basis of the existing neck incision in the rat, the right neck muscle was further exposed, the tissue was bluntly separated, the external jugular vein of about 1 cm in length was freed, 2 sutures were embedded, the distal end was ligated, and the proximal end was cut. V"-shaped incision, slowly push the...

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Abstract

The invention discloses an application of aldenafil citrate in preparation of a medicine for preventing and/or treating pulmonary arterial hypertension. The invention has the following advantages: the aldenafil citrate realizes cardio-pulmonary protection for patients with pulmonary arterial hypertension by inhibiting right ventricular remodeling, reducing cardiac hypertrophy, reducing heart index, inhibiting lung edema, inhibiting thickening of pulmonary artery blood vessel walls with different diameters and reducing lung index; the compound also has a therapeutic effect on pulmonary arterial hypertension, the survival rate of model animals with pulmonary arterial hypertension can be improved, the weight of the model animals can be increased, and the therapeutic effect is realized by inhibiting the activity of PDE5 to adjust the level of cGMP in a PDE5/cGMP/PKG pathway. Therefore, the aldipine citrate has good application and development prospects in prevention and/or treatment of the pulmonary arterial hypertension and the complications of the pulmonary arterial hypertension.

Description

technical field [0001] The invention belongs to the technical field of new pharmacological action of aldenafil citrate, in particular to the use of aldenafil citrate in the preparation of a medicine for preventing and or treating pulmonary hypertension. Background technique [0002] Pulmonary arterial hypertension (PAH) is a group of idiopathic pulmonary hemodynamic disorders caused by certain diseases, mainly manifested as increased pulmonary vascular resistance, pulmonary vascular remodeling, in situ thrombosis, and ultimately leading to right ventricular hypertrophy , and progressively develop into right heart failure until death, which is a very serious chronic pulmonary circulatory disease and a key link in pulmonary heart disease. [0003] The prevention and treatment of pulmonary arterial hypertension is a major problem that needs to be studied and solved urgently. There is still a lack of ideal drugs, and there is still a long-term problem of drug resistance in clini...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61P11/00A61P9/12A61P9/00
CPCA61K31/519A61P11/00A61P9/12A61P9/00
Inventor 杨磊杜冠华袁天翊赵晓悦马国栋燕柳艳宋俊科
Owner YOUCARE PHARMA GROUP