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Blocky calcium diphosphonate complex and preparation method thereof

A technology of calcium bisphosphonate and complex, applied in the field of biomedical materials, can solve the problems of adverse reactions, low concentration threshold, etc., and achieve the effects of simple preparation method, moderate crystal growth rate and low stress

Inactive Publication Date: 2021-04-13
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current bisphosphonic acid (or sodium salt) is relatively water-soluble, and the concentration threshold for its effective effect is very low, and it is easy to cause adverse reactions if it exceeds the threshold, so it can only be directly injected or loaded with a delivery system for sustained release. To some extent, it limits the application of bisphosphonates, which have significant osteogenic effects, in bone regeneration and repair.

Method used

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  • Blocky calcium diphosphonate complex and preparation method thereof
  • Blocky calcium diphosphonate complex and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0018] Weigh 1-hydroxyl-2-(imidazol-1-yl)-ethylene-1,1-diphosphoric acid (0.0272g, 0.10mmol) with a purity of 98%, calcium chloride (0.0110g , 0.10mmol), add 10mL water, slowly drop into 0.1mol / LNaOH solution, stir at the same time to make the solution clear and transparent and adjust the pH to 2.5, then transfer the solution to a vial, cover it, tighten it, and place the vial at a constant temperature box, react at 20°C for 60 days, then filter, wash, and dry to obtain large, regular-shaped, colorless and transparent block crystals, which are block calcium bisphosphonate complexes. Among them, the reaction time of the preparation process is negatively correlated with the reaction temperature, that is, the higher the temperature, the shorter the reaction time; As the pH increases, the size becomes smaller and smaller.

[0019] figure 1 It is an optical microscope picture of blocky calcium bisphosphonate complex crystals, from which it can be seen that the blocky calcium bisp...

Embodiment 2

[0022] Weigh 1-hydroxyl-2-(imidazol-1-yl)-ethylene-1,1-diphosphoric acid (0.0408g, 0.15mmol) with a purity of 98%, calcium hydroxide (0.0074g , 0.1mmol), add 10mL water, slowly drop into 0.1mol / LNaOH solution, stir at the same time to make the solution clear and transparent and adjust the pH to 3, then transfer the solution to a vial, cover it, tighten it, and place the vial at a constant temperature In the box, react at 25°C for 40 days, then filter, wash, and dry to obtain large regular-shaped colorless transparent block crystals, which are block calcium bisphosphonate complexes.

Embodiment 3

[0024] Weigh 1-hydroxyl-2-(imidazol-1-yl)-ethylene-1,1-diphosphoric acid (0.0544g, 0.20mmol) with a purity of 98%, calcium nitrate (0.0164g, 0.1mmol), add 10mL water, slowly drop into 0.1mol / LNaOH solution, stir at the same time to make the solution clear and transparent and adjust the pH to 3, then transfer the solution to a vial, cover it, tighten it, and place the vial in an incubator , reacted at 25°C for 30 days, then filtered, washed, and dried to obtain moderate, colorless, transparent block crystals with regular shapes, which are block calcium bisphosphonate complexes.

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Abstract

The invention discloses a blocky calcium bisphosphonate complex and a preparation method thereof. The chemical formula is Ca(2Zol)(2H2O), wherein Ca represents calcium, Zol represents 1-hydroxy-2- (imidazole-1-yl)-ethylidene-1, 1-diphosphoric acid, H2O represents water, the crystal system is a triclinic system, the space group is P-1, the lattice constants are alpha=105.648, beta=109.149 degrees, gamma=97.8570 degrees, and z=1. The preparation method comprises the following steps: taking calcium salt and 1-hydroxy-2-(imidazole-1-yl)-ethylidene-1, 1-diphosphoric acid as raw materials and deionized water as a solvent, adjusting the pH value to 2.5-3.5 by using a sodium hydroxide solution, standing at 20-30 DEG C for 20-60 days, and performing filtering, washing and drying to obtain a blocky transparent crystal, namely, the blocky calcium bisphosphonate complex. The preparation method disclosed by the invention is extremely simple, moderate in crystal growth speed, small in stress, good in uniformity and very complete in appearance, and has important potential application prospects in the fields of drug sustained release, targeted delivery, bone tissue repair and the like.

Description

technical field [0001] The invention relates to the technical field of biomedical materials, in particular to a block-shaped calcium bisphosphonate complex and a preparation method thereof. Background technique [0002] Coordination polymers are a class of compounds formed by the combination of metal ions and organic ligands through coordination bonds. In recent years, the development of coordination polymer chemistry has endowed it with new explorations and applications in the fields of design, synthesis, structure, and performance, and has gradually become a frontier and hot topic in organic, inorganic, materials, biology, and medical disciplines. Using the principle of molecular self-assembly to design and construct complexes with novel structures, so that they have specific biological functions, has important practical significance for their wide application in the field of biomedicine. [0003] 1-Hydroxy-2-(imidazol-1-yl)-ethylene-1,1-diphosphate is a bisphosphonic aci...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G83/00C07F9/6506
CPCC08G83/008C07F9/6506C07B2200/13
Inventor 施雪涛壮琛柴牧原林佳义杨夕冉
Owner SOUTH CHINA UNIV OF TECH
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