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Drug combination containing raloxifene and application thereof

A technology for raloxifene hydrochloride and a drug, which is applied to a drug compatibility combination containing raloxifene and its application field, and can solve the problems of increased risk and great cardiovascular benefit in the treatment group

Inactive Publication Date: 2011-08-17
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the results of the prospective randomized double-blind placebo-controlled clinical trial Women's Health initiative (WHI) were published in JAMA in July 2002. Compared with the placebo group, the treatment group (estrogen + pregnancy The relative risk of invasive breast cancer, coronary heart disease and stroke increased, and the value of HRT as a preventive treatment for postmenopausal women was challenged unprecedentedly. In early 2003, the North American Menopause Society revised the guidelines for the application of HRT: in the short term It is appropriate to use HRT to relieve menopausal symptoms, and it is not recommended to use HRT to prevent disease
In July 2005, Michael E Mendelsohn et al. mentioned the time hypothesis using HRT in an article published in "Science". In June 2007, JoAnn E. Manson et al. published a large-scale The results of WHI-CACS (WHI Coronary-Artery Calcium Study), a randomized clinical trial of women's health initial project, support the hypothesis that there is a time effect of HRT, that is, the application of HRT in early menopausal women aged 50-59 years Prevention of cardiovascular disease is beneficial. Traditional estrogen replacement therapy has greater cardiovascular benefits than estrogen + progesterone replacement therapy, but estrogen therapy alone brings some terrible side effects, such as breast cancer, intrauterine membranous carcinoma, venous thrombosis
According to the novelty search by authoritative organizations, there are no reports at home and abroad on the combination of raloxifene, estrogen, and aspirin and its application in the prevention and treatment of postmenopausal atherosclerosis

Method used

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  • Drug combination containing raloxifene and application thereof
  • Drug combination containing raloxifene and application thereof
  • Drug combination containing raloxifene and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0085] Example 1 The preparation of the drug compatibility composition containing raloxifene

[0086] Get drug raloxifene hydrochloride, estradiol valerate and aspirin, take by weighing respectively (unit: gram) according to the mass ratio of raloxifene hydrochloride, estradiol valerate and aspirin (unit: gram) by raloxifene hydrochloride, estradiol valerate and aspirin Evenly, subpackage or press into tablets in a conventional way, and set aside.

Embodiment 2

[0087] Example 2 Application of the drug combination containing raloxifene described in the present invention as a drug for preventing and treating atherosclerosis in postmenopausal women.

[0088] (1) Preparation and treatment of animal models of postmenopausal atherosclerosis:

[0089] Eighty 3-month-old purebred female New Zealand white rabbits with an average weight of 2.25 kg were adaptively fed with common feed for 1 week, then intravenously anesthetized with 3% pentobarbital sodium, and underwent bilateral ovariectomy. The sham operation group only opened The abdominal cavity, without ovariectomy, was fed with high-fat diet containing 1.5% cholesterol for 12 weeks after ovariectomy. They were randomly divided into 8 groups (n=10), which were group A (control group), group B (raloxifene + estrogen + aspirin), group C (raloxifene + estrogen), group D (estrogen ), group E (raloxifene group), group F (estrogen + progesterone group), group G (aspirin group) and group H (sha...

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Abstract

The invention discloses a drug combination containing raloxifene and application thereof in preparing drugs for preventing and curing atherosclerotic diseases of postmenopausal women. The combination comprises raloxifene hydrochloride, estradiol valerate and aspirin in a mass ratio of 105:1:43.75. Postmenopausal atherosclerotic animal models verify that the combination of the invention can betterinhibit postmenopausal atherosclerosis and alleviate the side effects compared with the single drug and the traditional hormone replacement therapy, and indicate that the combination has more attractive development prospect in the development and application in preparing the new drugs for preventing and curing atherosclerotic diseases of postmenopausal women.

Description

technical field [0001] The invention relates to a drug compatibility combination containing raloxifene and its application in the preparation of drugs for preventing and treating atherosclerotic diseases in postmenopausal women. Background technique [0002] Globally, about 17.5 million people die of cardiovascular disease every year, about half of whom are women. On average, 16 women die of cardiovascular and cerebrovascular diseases every minute in the world. Cardiovascular disease is the single cause of death among women. Causes of death by disease, in many developed countries, including the United States, the number of women who die of cardiovascular disease exceeds that of men every year. Previous epidemiological observational studies have shown that the age of onset of coronary heart disease and stroke in women is 10 years later than that in men. The prevalence of coronary heart disease in postmenopausal women is 2-3 times higher than that of premenopausal women, and ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/616A61K31/565A61K31/4535A61P9/10
Inventor 贺红杨发林户可庆王欣李继福
Owner SHANDONG UNIV
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