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Incadronate calcium complex and preparation method thereof

A technology of calcium incadronate and incadronic acid, which is applied in the field of calcium incadronate complexes and their preparation, can solve problems such as adverse reactions and low concentration thresholds, and achieve simple preparation methods, moderate crystal growth speed, The effect of less stress

Inactive Publication Date: 2021-04-09
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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  • Incadronate calcium complex and preparation method thereof
  • Incadronate calcium complex and preparation method thereof
  • Incadronate calcium complex and preparation method thereof

Examples

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Effect test

Embodiment 1

[0019] Take by weighing the incadronic acid (0.0086g, 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 hydrochloric acid solution, simultaneously Stir to make the solution clear and transparent and adjust the pH to 2, then transfer the solution to a vial, cover it, and tighten it, place the vial in an incubator, react at 20°C for 48 hours, then filter, wash, and dry to obtain Larger colorless transparent flaky crystals are incadronate calcium complexes; among them, the reaction time and reaction temperature are negatively correlated, that is, the higher the temperature, the shorter the reaction time. The prepared calcium incadronate complex was in the form of colorless transparent flaky crystals in aqueous solution, and as the pH increased, the rectangles became smaller and smaller.

[0020] figure 1 It is a scanning electron microscope picture of the calcium incadronate complex crystal, an...

Embodiment 2

[0024] Take by weighing the incadronic acid (0.0144g, 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 36 hours, then filter, wash, and dry to obtain Larger colorless transparent flaky crystals are incadronate calcium complexes.

Embodiment 3

[0026] Take by weighing the incadronic acid (0.0287g, 0.1mmol) that purity is 98%, the calcium nitrate (0.0082g, 0.05mmol) that purity is 98%, add in 10mL water, slowly drip into 0.1mol / L NaOH solution, stir simultaneously 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 constant temperature box, react at 150°C for 24 hours, then filter, wash, and dry to obtain Moderate colorless transparent flaky crystals, that is, calcium incadronate complex.

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Abstract

The invention discloses an incadronate calcium complex and a preparation method thereof. The chemical formula of the incadronate calcium complex is Ca(Inc)(H2O), Ca represents calcium, Inc represents incadronic acid, H2O represents water, the crystal system is a triclinic system, the space group is P-1, and the lattice constants are as follows: alpha=84.6480 degrees, beta=89.3220 degrees, gamma=71.4520 degrees and z=2. The preparation method comprises the following steps: taking calcium salt and incadronic acid as raw materials and deionized water as a solvent, adjusting the pH value to 2-8 by using a sodium hydroxide (or hydrochloric acid) solution, standing for 12-48 hours at 20-200 DEG C, filtering, washing and drying to obtain colorless transparent flaky crystals, namely the incadronate calcium complex. The disclosed preparation method 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 an incadronate 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] Incadronic acid is a bisphosphonic acid small-molecule drug widely used clinically in the ...

Claims

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Application Information

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IPC IPC(8): C08G83/00C07F9/38
CPCC07B2200/13C07F9/3817C08G83/008
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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