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Molecular compound of 17 beta-estradiol and vitamin C as well as preparation method and application thereof

A technology of molecular complexes and vitamins, which is used in medical preparations, pharmaceutical formulations, and drug combinations containing active ingredients.

Active Publication Date: 2021-08-13
ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these findings did not ultimately overcome the adverse effects of 17β-estradiol therapy, and even conjugated estrogens still have 17β-estradiol-like adverse effects

Method used

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  • Molecular compound of 17 beta-estradiol and vitamin C as well as preparation method and application thereof
  • Molecular compound of 17 beta-estradiol and vitamin C as well as preparation method and application thereof
  • Molecular compound of 17 beta-estradiol and vitamin C as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1: Preparation of a molecular complex of 17β-estradiol and vitamin C with a molar ratio of 1:1

[0042] 2720 ​​mg of 17β-estradiol and 1760 mg of vitamin C were dissolved in 60 ml of 30% V / V ethanol aqueous solution to prepare a clear solution, and the clear solution was lyophilized to obtain 4480 mg of lyophilized powder.

Embodiment 2

[0043] Example 2: Preparation of a molecular complex of 17β-estradiol and vitamin C with a molar ratio of 1:1

[0044] 2720mg of 17β-estradiol was mixed with 1760mg of vitamin C, dissolved in 50ml of 40% V / V ethanol aqueous solution to prepare a clear solution, and the clear solution was distilled and dried under reduced pressure at room temperature to obtain 4480mg of powder.

Embodiment 3

[0045] Example 3: Preparation of a molecular complex of 17β-estradiol and vitamin C with a molar ratio of 1:1

[0046] 2720mg of 17β-estradiol was mixed with 1760mg of vitamin C, dissolved with 40ml of 50% V / V ethanol aqueous solution to prepare a clear solution, and the clear solution was distilled and dried under reduced pressure at room temperature to obtain 4480mg of powder.

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Abstract

The invention discloses a molecular compound of 17 beta-estradiol and vitamin C as well as a preparation method and application thereof. The molecular compound is formed by compounding 17 beta-estradiol molecules and vitamin C in a molar ratio of 0.25: 1, 0.5: 1, 0.75: 1, 1: 1, 1: 0.25, 1: 0.5 or 1: 0.75. The invention further provides a method for preparing the molecular compound of 17 beta-estradiol and vitamin C. The molecular compound of 17beta-estradiol and vitamin C provided by the invention can be distributed to bone tissues in a bone targeting manner, so that not only the anti-osteoporosis activity of 17beta-estradiol is remarkably improved, but also the side effects of hyperplasia endometrii and thrombosis caused by treating with 17 beta-estradiol and conjugated estrogens can be effectively avoided.

Description

technical field [0001] The present invention relates to a molecular complex of 17β-estradiol and vitamin C, in particular to a molecule of 17β-estradiol and vitamin C compounded by 17β-estradiol and vitamin C with a molar ratio of 1:1 Composite and its preparation method, the present invention further relates to the use of the molecular compound in the preparation of anti-osteoporosis drugs, and the present invention belongs to the technical field of medicine. Background technique [0002] 17β-Estradiol (17β-Estradiolum, E2) participates in the physiological and pathological activities of animals and humans. For example, 17β-estradiol improves the survival and activation of new neurons in the hippocampus of adult female rats in response to spatial memory, improves cognitive function in humans and animals, and attenuates changes in cardiomyocyte contractile function induced by ovariectomy. Another example is that for 17β-estradiol-treated mice, melatonin supplementation can ...

Claims

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Application Information

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IPC IPC(8): A61K31/375A61K31/565A61P19/10A61P15/00
CPCA61K31/375A61K31/565A61P19/10A61P15/00A61K2300/00A61K9/19
Inventor 彭师奇吴国峰赵明
Owner ZHEJIANG MEDICINE CO LTD XINCHANG PHAMACEUTICAL FACTORY
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