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Pharmaceutical composition of alfacalcidol and medical application of pharmaceutical composition

A technology of alfacalcidol and its compounds, which is applied in the field of biomedicine, can solve the problems that have not been reported related to alfacalcidol, and achieve the effect of highlighting substantive features, significant progress, and improved therapeutic effect

Inactive Publication Date: 2016-08-10
陈斌
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] So far, there has been no report on the correlation between alfacalcidol and its pharmaceutical composition and renovascular hypertension

Method used

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  • Pharmaceutical composition of alfacalcidol and medical application of pharmaceutical composition
  • Pharmaceutical composition of alfacalcidol and medical application of pharmaceutical composition
  • Pharmaceutical composition of alfacalcidol and medical application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: Compound (I) Separation Preparation and Structure Confirmation

[0023] Sources of reagents: ethanol, petroleum ether, ethyl acetate, n-butanol, and dichloromethane were of analytical grade, purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd. Methanol, of analytical grade, were purchased from Jiangsu Hanbang Chemical Reagent Co., Ltd.

[0024] Separation method: (a) Grind the dried tubers (2kg) of Gastrodia elata, extract with 85% ethanol under heat reflux (15L×3 times), combine the extracts, concentrate until no alcohol smell (3L), and then use petroleum ether (3L×3 times) 3 times), ethyl acetate (3L × 3 times) and water-saturated n-butanol (3L × 3 times) were extracted to obtain petroleum ether extract, ethyl acetate extract and n-butanol extract respectively; (b) step (a) The ethyl acetate extract in (a) was removed with D101 type macroporous resin, first eluted with 30% ethanol for 6 column volumes, then eluted with 85% ethanol for 12 column volum...

Embodiment 2

[0028] Embodiment 2: pharmacological action

[0029] 1. Materials and methods

[0030] 1.1 Animals

[0031] Normal male SD rats (provided by the Experimental Animal Center of Guangzhou University of Traditional Chinese Medicine), weighing 90-120 g.

[0032] 1.2 Reagents and samples

[0033] Alfacalcidol was purchased from China Institute for the Control of Pharmaceutical and Biological Products. Compound (I) is self-made, and the preparation method is shown in Example 1. Captopril: Changzhou Pharmaceutical Factory.

[0034] 1.3 Rat grouping and model preparation

[0035] The classic renal artery clamp method was used. If the postoperative blood pressure was greater than 3 standard deviations before the operation and higher than 115mmHg, the model was determined to be established. In the sham operation group, only the renal artery was dissociated without silver clips. The renovascular hypertensive rats (RHR) were randomly divided into 6 groups: sham operation group, mod...

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Abstract

The invention discloses a pharmaceutical composition of alfacalcidol and its medical application. The pharmaceutical composition of alfacalcidol provided by the invention contains alfacalcidol and a kind of The natural product compound (Ⅰ) with a novel structure, when alfacalcidol and compound (Ⅰ) act alone, can interfere with myocardial fibrosis in rats with renovascular hypertension by reducing the concentration of collagen; When pyridoxol and compound (I) act in combination, the intervention effect is better, and it can be developed into a drug for preventing and treating myocardial fibrosis in patients with renovascular hypertension, which has outstanding substantive features and significant progress compared with the prior art.

Description

technical field [0001] The invention belongs to the field of biomedicine and relates to a new application of alfacalcidol, in particular to a pharmaceutical composition of alfacalcidol and its application in myocardial fibrosis caused by renovascular hypertension. Background technique [0002] The chemical name of alfacalcidol is (5Z,7E)-9,10-cyclocholesta-5,7,10(19)-triene-1α,3β-diol. [0003] Alfacalcidol is rapidly converted in the liver to 1,25-dihydroxyvitamin D3, a metabolite of vitamin D3 that regulates calcium and phosphate metabolism. Because of the rapid conversion process, the clinical effect of alfacalcidol is basically the same as that of 1,25-dihydroxyvitamin D3. Its main function is to increase the intestinal absorption of calcium and phosphate by increasing the level of 1,25-dihydroxyvitamin D3 in the blood circulation in the body, promote bone mineralization, reduce the level of plasma parathyroid hormone, and reduce bone calcium dissolution. It is suitabl...

Claims

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Application Information

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IPC IPC(8): C07D493/08A61K31/365A61K31/592A61P9/00A61P9/12A61P13/12
CPCC07D493/08A61K31/365A61K31/592
Inventor 陈斌
Owner 陈斌
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