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Minodronate calcium complex and preparation method thereof

A technology of calcium minodronate and minodronate, applied in the field of biomedical materials, can solve problems such as adverse reactions and low concentration thresholds

Inactive Publication Date: 2021-04-30
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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  • Minodronate calcium complex and preparation method thereof
  • Minodronate calcium complex and preparation method thereof
  • Minodronate calcium complex and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Take by weighing the minodronic acid (0.0096g, 0.03mmol) that purity is 98%, the calcium chloride (0.0033g, 0.03mmol) that purity is 98%, add in 10mL water, slowly drip into 0.1mol / L NaOH solution, simultaneously Stir to make the solution clear and transparent and adjust the pH to 3, then transfer the solution to a vial, cover it, and tighten it, place the vial in an incubator, react at 20°C for 24 hours, then filter, wash, and dry to obtain Larger regular shape colorless transparent parallelogram crystals are minodronate calcium 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 value increases, the rectangle becomes smaller and smaller.

[0020] figure 1 It is a scanning electron microscope picture of the minodronate calcium complex crystal, and it can be seen from the figure that the minodronate calcium complex is a par...

Embodiment 2

[0024] Take by weighing the minodronic acid (0.0161g, 0.05mmol) that purity is 98%, the calcium hydroxide (0.0074g, 0.1mmol) that purity is 98%, add in 10mL water, slowly drip into 0.1mol / L NaOH solution, simultaneously Stir to make the solution clear and transparent and adjust the pH to 4, then transfer the solution to a vial, cover it, and tighten it, place the vial in an incubator, react at 80°C for 18 hours, then filter, wash, and dry to obtain Larger regular shape colorless transparent parallelogram crystals are minodronate calcium complexes.

Embodiment 3

[0026] Take minodronic acid (0.0322g, 0.1mmol) with a purity of 98%, and calcium nitrate (0.0082g, 0.05mmol) with a purity of 98%, add it to 10mL of water, slowly drop into 0.1mol / L NaOH solution, and stir at the same time Make the solution clear and transparent and adjust the pH to 5, then transfer the solution to a 15mL reactor, cover it, and tighten it, place the reactor in a thermostat, react at 150°C for 12 hours, then filter, wash, and dry to obtain Moderate colorless transparent parallelogram crystals with regular shape are minodronate calcium complexes.

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Abstract

The invention discloses a minodronate calcium complex and a preparation method thereof, the chemical formula of the minodronate calcium complex is Ca (Min) 2 (2H2O), Ca represents calcium, Min represents minodronate, H2O represents water, the crystal system is a monoclinic system, the space group is C2 / C, the lattice constant beta is equal to 106.444 degrees, and z is equal to 4. The preparation method comprises the following steps: by taking calcium salt and minodronic acid as raw materials and deionized water as a solvent, adjusting the pH value to 3-5 by using a sodium hydroxide solution, standing at 20-200 DEG C for 3-24 hours, filtering, washing and drying to obtain a colorless transparent parallelogram crystal, namely the minodronate calcium 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 minodronate calcium 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] Minodronic acid is a bisphosphonic acid small molecule drug widely used clinically in anti-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/6561
CPCC07F9/65616C07B2200/13
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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