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Zoledronic acid for preparing medicaments for preventing and treating osteoporosis

A technology for osteoporosis and zoledronic acid, which can be used in drug combinations, medical preparations containing active ingredients, bone diseases, etc., can solve the problem of inability to promote bone formation, poor effect of compact bone fractures, and limited clinical application. And other issues

Inactive Publication Date: 2008-09-10
王洪 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Current therapies for osteoporosis (eg, vitamin D, hormone replacement) prevent bone resorption rather than bone formation
Estrogen replacement therapy is limited in clinical application because of its potential cancer risk and adverse reactions; although parathyroid hormone can stimulate bone formation, one of the disadvantages is that it must be injected; calcitonin can improve bone formation in the short term. Pain in osteoporotic patients, but less effective in preventing compact bone loss and skeletal fractures

Method used

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  • Zoledronic acid for preparing medicaments for preventing and treating osteoporosis
  • Zoledronic acid for preparing medicaments for preventing and treating osteoporosis
  • Zoledronic acid for preparing medicaments for preventing and treating osteoporosis

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0009] Example 1: Effect of Zoledronate on Bone Mineral Density of Retinoic Acid-Induced Osteoporosis Rats

[0010] Rats (250-320g), half male and half male, totally 50. They were randomly divided into 5 groups: normal control group, model control group, three dose groups of zoledronic acid 0.4932 mg / kg, 1.5364 mg / kg, and 4.8761 mg / kg. Except for the normal control group, the other groups were fed with retinoic acid 65 mg / kg once a day for 2 consecutive weeks. Simultaneously with modeling, each administration group was intragastrically administered 0.15ml / kg according to the set dose, once a day, the control group was given the same amount of vehicle, and the model control group was fed normally for 4 consecutive weeks. The next day after the last administration, rats were anesthetized with 10% chloral hydrate (350 mg / kg, i.p.), placed under the probe of a dual-energy line bone densitometer, and fixed on the detection table in a supine position, with the head and body in a st...

example 2

[0016] Example 2: Effects of Zoledronate on Femur Length, Weight and Bone Calcium Content in Rats with Osteoporosis Caused by Retinoic Acid

[0017] Rats (250-320g), half male and half male, totally 50. They were randomly divided into 5 groups: normal control group, model control group, three dose groups of zoledronic acid 0.4932 mg / kg, 1.5364 mg / kg, and 4.8761 mg / kg. Except for the normal control group, the other groups were fed with retinoic acid 65 mg / kg once a day for 2 consecutive weeks. Simultaneously with modeling, each administration group was intragastrically administered 0.15ml / kg according to the set dose, once a day, the control group was given the same amount of vehicle, and the model control group was fed normally for 4 consecutive weeks. The day after the last administration, the rats were sacrificed and dissected, the left femur was stripped, the length of the femur was measured with a vernier caliper, the femur was baked to constant weight, and the weight of ...

example 3

[0024] Example 3: Effect of Zoledronate on Femur Length, Weight and Bone Calcium Content in Ovariectomized Rats

[0025] The occurrence of menopause with osteoporosis has been confirmed by many epidemiological studies. Menopause can cause disturbance of glucose metabolism and insulin resistance, and disturbance of glucose metabolism is the main reason for the increase of advanced glycation end products. High levels of advanced glycation end products can lead to decreased number and activity of osteoblasts, decreased bone formation, and ultimately osteoporosis.

[0026] At present, hormone replacement therapy is mainly used in the treatment of postmenopausal osteoporosis. Although it has a certain effect on osteoporosis, it can cause the occurrence of breast cancer and endometrial cancer. The invention adopts the method of ovariectomy to make rat osteoporosis model, and proves the prevention and treatment effect of zoledronic acid on postmenopausal osteoporosis.

[0027] Rats...

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Abstract

The invention discloses applications of zoledronic acid in preventing osteoporosis; the zoopery is providence that zoledronic acid has good preventing effect and therapeutical action to osteoporosis; zoledronic acid can be prepared into any clinically acceptable oral preparations such as tablets, capsules, granules, suspensions, dry suspensions and oral liquid, etc. so as to clinically prevent and treat osteoporosis.

Description

technical field [0001] Osteoporosis is a systemic bone disease characterized by damage to the microstructure of bone tissue, a decrease in the proportion of bone mineral components and bone matrix, bone thinning, a decrease in the number of bone trabeculae, increased bone fragility, and increased risk of fracture. Diseases of metabolic disorders. Osteoporosis is the most common disease of the elderly. The invention relates to the application of zoledronic acid in preventing and treating osteoporosis. Zoledronic acid is the first bisphosphonate approved for the treatment of multiple myeloma, breast cancer, prostate cancer, lung cancer and other solid tumors related complications of bone metastasis. It blocks the resorption of bone and cartilage by osteoclasts by combining with bone, inhibits the activity of osteoclasts, induces apoptosis of osteoclasts, and inhibits the release of calcium from bones induced by various stimulating factors released by tumors, thereby reducing s...

Claims

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Application Information

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IPC IPC(8): A61K31/675A61P19/10
Inventor 王洪韩静
Owner 王洪
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