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Fructose-1,6-diphosphate calcium preparation and uses

A technology of diphosphoric acid and fructose diphosphate, applied in the field of fructose-1, can solve the problems of poor absorption, difficult absorption, large dosage, etc.

Active Publication Date: 2009-09-02
NANJING TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] Current research shows that many of the above calcium preparations still have some common disadvantages of poor absorption and large dosage.
Calcium supplementation focuses on absorption, but the calcium contained in plant foods and many calcium salt drugs are often not easily absorbed by the body

Method used

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  • Fructose-1,6-diphosphate calcium preparation and uses
  • Fructose-1,6-diphosphate calcium preparation and uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Configure 58L of FDP solution (concentration 86g / L), adjust pH to 5.0. Add 2L CaCl 2 The solution, the molar concentration of 7.2mol / L, was stirred at 250rpm for 30min, concentrated in vacuo, slowly added 2 times the volume of the solution to obtain alcohol, stirred for 30min, vacuum filtered, washed with a small amount of 80% alcohol water, and then washed with anhydrous The alcohol was dehydrated twice, vacuum filtered, and spray-dried to obtain 5.1 kg of fructose-1,6-diphosphate monocalcium salt with a purity of 99.0% and a yield of 95% of the theoretical value.

Embodiment 2

[0052] Prepare 50L of FDP solution (concentration is 34.5g / L), adjust pH to 2.0. Add 5L Ca(NO 3 ) 2 (concentration is 5.04mol / L), under the condition of 250rpm, stirring reaction for 4h, vacuum concentration, adding ethanol of twice the solution volume, and stirring for 15min, after fructose-1,6-diphosphate monocalcium salt crystallizes, vacuum filtration , washed with a small amount of 80% alcohol water, then dehydrated twice with anhydrous alcohol, vacuum filtered, crystallized in 3 times alcohol, freeze-dried fructose-1,6-diphosphate monocalcium salt 1.76kg, purity 99.0 %, the yield is 96% of the theoretical value.

Embodiment 3

[0054] Prepare 5L of FDP solution (concentration is 92g / L), adjust pH to 6.0 and add 500ml CaCl 2 The solution (concentration is 2.7mol / L), stirred and reacted for 4h, added 2.5 volumes of acetone, and stirred for 15min, vacuum filtered after crystallization, washed with a small amount of 80% alcohol water, then dehydrated with anhydrous alcohol for 2 times, vacuumed After suction filtration, the spray-dried fructose-1,6-diphosphate monocalcium salt was 501.1 g, the purity was 99.0%, and the yield was 95% of the theoretical value.

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Abstract

The invention relates to the preparation of fructose-1,6-diphosphate monocalcium salt and its application in the preparation of medicines for treating or preventing osteoporosis or fracture. 1,6-diphosphate fructose and CaCl2, Ca(NO3)2 solution at a molar ratio of 1:1, the concentration of calcium salt is lower than 10mol / L, and the pH of the reaction solution is controlled under the condition of 2.0 to 6.5 under sufficient stirring to react and crystallize Drying produces fructose-1,6-diphosphate monocalcium salt. Fructose-1,6-diphosphate monocalcium salt is a water-soluble calcium salt with high solubility. It enters the gastrointestinal tract after oral administration and is in an ion state in the small intestinal fluid, which greatly increases the absorption in the body and improves the bioavailability. The parent FDP acts as a high-energy matrix to provide the energy required for metal ion calcium to enter tissues and cells through active transport, which improves the biological efficacy of calcium.

Description

technical field [0001] The invention relates to a chemical synthesis method and application thereof, in particular to the preparation and application of fructose-1,6-diphosphate monocalcium salt Background technique [0002] Calcium (Ca) is a major element in the human body, containing 1200g in the human body, 99% of which is concentrated in bones and teeth, mainly in the form of hydroxyapatite, and the remaining 1% in the free or bound ionic state. Soft tissue cells and blood. Normal plasma calcium concentration is 2.25 to 2.27 mmol / L. Stabilization of blood calcium concentration plays a pivotal role in physiological processes such as nerve and muscle stress, transmission of nerve impulses, maintenance of cardiac rhythm, blood coagulation, and cell adhesion. There is a blood calcium homeostasis system in the human body, including a huge bone calcium store and parathyroid hormone, calcitonin, vitamin D, etc., which are involved in the regulation of bone calcium-blood calci...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H11/04A61K31/7024A61P19/10A61P19/08
Inventor 应汉杰吕浩赵谷林
Owner NANJING TECH UNIV