Composition for preventing or treating osteoporosis and preparation and application thereof

A technology for osteoporosis and composition, applied in the direction of drug combination, medical preparations containing active ingredients, applications, etc., can solve the problems of increasing the risk of osteosarcoma, many side effects, toxic side effects, etc., and achieve the purpose of inhibiting osteoclasts Proliferation, improvement of osteoporosis, and promotion of osteoblast differentiation activity

Active Publication Date: 2022-03-25
完美(广东)日用品有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, long-term use of these drugs has many side effects, such as long-term use of bisphosphonates can cause toxic side effects on tissues...

Method used

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  • Composition for preventing or treating osteoporosis and preparation and application thereof
  • Composition for preventing or treating osteoporosis and preparation and application thereof
  • Composition for preventing or treating osteoporosis and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1: Effect of Composition on Osteoclast Activity

[0032] Excessive proliferation and activation of osteoclasts can cause increased bone resorption, reduce bone mass, reduce bone density, increase bone fragility and fracture risk. Therefore, inhibiting the differentiation of bone marrow mononuclear macrophages into osteoclasts is helpful for the prevention and treatment of osteoporosis.

[0033] Bone marrow mononuclear cells were isolated from the femur and tibia of 1-month-old mice (purchased from Guangdong Provincial Medical Experimental Animal Center), and evenly spread into 24-well plates, 1 × 10 per well. 5 After the cells adhered to the wall, they were cultured with α-MEM medium containing 25ng / ml M-CSF, 25ng / ml RANKL cytokines and 10% fetal bovine serum. For different pharmaceutical compositions, the culture medium was changed every 3 days. After 6 days, the data of osteoclasts in each group were calculated by using TRAP staining. The positive number of...

Embodiment 2

[0039] Example 2: Effect of composition on bone mineral density and trabecular bone in ovariectomized mice

[0040] Animals used in this example, female C57BL / 6 mice, were purchased from Guangdong Medical Experimental Animal Center. The mice were kept at a temperature of 23±2°C, a humidity of 55±5%, a ventilation frequency of 12-15 times / hour, and a lighting time of 12 hours / day (7:00-19:00 light), 5 / breeding cage ( 235×325×170H mm), feeding conditions: solid feed (Guangdong Medical Experimental Animal Center), free diet. When the mice were 3 months old, the mice were randomly divided into a sham operation group, a model group and an administration group. Mice were fasted for 12 hours before surgery, without food or water. Mice were anesthetized using isoflurane, then the skin was washed and sterilized with 75% ethanol. The mice in each group were operated by ventral incision. Except the sham operation group, the ovaries were not removed, and the mice in the other groups we...

Embodiment 3

[0046] Example 3: Effect of the composition on the antioxidant capacity of bone tissue in ovariectomized mice

[0047] The antioxidant capacity of mouse bone tissue was determined by oxidative radical absorbance capacity (Oxygen Radical Absorbance Capacity, ORAC) experiment.

[0048] Bone tissue sample pretreatment: in embodiment 2, take left hind limb of mouse, after stripping muscle and connective tissue, collect in centrifuge tube after grinding in liquid nitrogen, add perchloric acid solution (3%) to prepare 2% bone tissue The tissue homogenate was centrifuged at 10,000 r / min for 15 min at 4°C, and the supernatant was taken as a sample solution for ORAC determination.

[0049] ORAC experiment process: Add 20 μL bone tissue homogenate supernatant and 20 μL phosphate buffer saline of different groups of mice to the 96-well plate, then add 20 μL sodium fluorescein, and finally add 140 μL AAPH, and quickly place the 96-well plate in The assay was started in a fluorescent micr...

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Abstract

The invention belongs to the field of medicines, and particularly relates to a composition for preventing or treating osteoporosis, a preparation of the composition and application of the composition in preventing or treating osteoporosis. Specifically, the composition disclosed by the invention is mainly composed of a GPX4 agonist and a lipoxygenase 15 (Alox-15) inhibitor, and vitamin E is supplemented to play a synergistic effect. In one embodiment, the GPX4 agonist is prepared from one or more of 6-gingerol, 8-gingerol, 10-gingerol and PKUMDL-LC-101-D04, and the GPX4 agonist is prepared from one or more of 6-gingerol, 8-gingerol, 10-gingerol and PKUMDL-LC-101- And the Alox-15 inhibitor is prepared from one or more of quercetin, ferulic acid, baicalein, hesperetin, nobiletin, PD146176, orange flavone and ML351. In another embodiment, the composition comprises a ginger extract, a sea buckthorn extract, and a wheat germ extract. Pharmacological experiment results show that the composition can effectively prevent, improve and treat osteoporosis and clinical related symptoms.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a composition for preventing or treating osteoporosis and its preparation and application. Background technique [0002] Osteoporosis (OP) is a systemic bone metabolic disease whose main pathological features are decreased bone mineral density (BMD), impaired bone microarchitecture / mineralization, and increased fracture risk. Modern society is an aging society. With the aging of the population and the extension of life expectancy, the incidence of osteoporosis and osteoporotic fractures continues to rise. Osteoporosis has become a global health problem. According to incomplete statistics, more than 200 million people worldwide suffer from osteoporosis. In addition, the epidemiological survey data of the National Health Commission in 2018 showed that the prevalence of osteoporosis among people over 65 years old in my country was as high as 32%. Fragility fractures of the spin...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K31/355A61K31/12A61K31/352A61K36/9068A61P19/10A23L33/105A23L33/15
CPCA61K45/00A61K31/355A61K31/12A61K31/352A61K36/9068A61K36/185A61K36/899A61P19/10A23L33/105A23L33/15A23V2002/00A61K2300/00A23V2200/306A23V2250/21A23V2250/21168A23V2250/2132A23V2250/712
Inventor 何蓉蓉李怡芳栗原博张琼谊江曼亚
Owner 完美(广东)日用品有限公司
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