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Risedronate calcium complex and preparation method thereof

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

Inactive Publication Date: 2021-04-30
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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  • Risedronate calcium complex and preparation method thereof
  • Risedronate calcium complex and preparation method thereof
  • Risedronate calcium complex and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Take by weighing risedronic acid (0.0085g, 0.03mmol) with a purity of 98%, and calcium chloride (0.0033g, 0.03mmol) with a purity of 98%, add it to 10mL of water, slowly drop into 0.1mol / L NaOH solution, and 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 72 hours, then filter, wash, and dry to obtain Larger, regular-shaped long strips of transparent crystals are risedronate 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; With the increase of pH, the morphology becomes finer and finer.

[0020] figure 1 These are the optical microscope and scanning electron microscope pictures of the risedronate calcium complex crystal respectively, and it can be seen from the figure t...

Embodiment 2

[0024] Take by weighing risedronic acid (0.0142g, 0.05mmol) with a purity of 98%, and calcium hydroxide (0.0074g, 0.1mmol) with a purity of 98%, add it to 10mL of water, slowly drop into 0.1mol / L NaOH solution, and 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 54 hours, then filter, wash, and dry to obtain Larger, regular-shaped long strips of transparent crystals are risedronate calcium complexes.

Embodiment 3

[0026] Take by weighing risedronic acid (0.0283g, 0.1mmol) with a purity of 98%, and calcium phosphate (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 constant temperature box, react at 150°C for 36 hours, then filter, wash, and dry to obtain Moderate, regular-shaped long strips of transparent crystals are risedronate calcium complexes.

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Abstract

The invention discloses a risedronate calcium complex and a preparation method thereof, the chemical formula of the risedronate calcium complex is Ca (Ris) (H2O), Ca represents calcium, Ris represents risedronate, H2O represents water, the crystal system is an orthorhombic system, the space group is P212121, and the lattice constant z is 4. The preparation method comprises the following steps: by taking calcium salt and risedronate or risedronate sodium as raw materials and deionized water as a solvent, adjusting the pH value to 3-7 by using a sodium hydroxide solution, standing at 20-200 DEG C for 12-72 hours, filtering, washing and drying to obtain a strip-shaped transparent crystal, namely the risedronate 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 risedronate 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] Risedronic acid is a bisphosphonic acid small-molecule drug widely used clinically in the t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F9/58C08G83/00A61P19/10A61P19/00A61P29/00A61P35/00
CPCA61P19/00A61P19/10A61P29/00A61P35/00C07B2200/13C07F9/58C08G83/008
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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