Dexmedetomidine nano preparation and preparation method thereof

A technology of dexmedetomidine and nano-preparation, applied in the field of medicine, can solve the problems of easy occurrence of adverse reactions, limiting the scope of clinical application, reducing the anesthesia time of dexmedetomidine and the like

Inactive Publication Date: 2019-02-26
THE FIRST AFFILIATED HOSPITAL OF ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, patients over 65 years old are more likely to have adverse reactions when using dexmedetomidine, and the dosage needs to be halved
After reducing the dosage, the anesthesia time of dexmedetomidine will be reduced, and the dosage window will be reduced, which will limit its clinical application range

Method used

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  • Dexmedetomidine nano preparation and preparation method thereof
  • Dexmedetomidine nano preparation and preparation method thereof
  • Dexmedetomidine nano preparation and preparation method thereof

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preparation example Construction

[0024] A preparation method of dexmedetomidine nano-preparation, the preparation steps of dexmedetomidine nano-preparation are as follows:

[0025] (1) dexmedetomidine and polylactic acid-polyglycolic acid copolymer are dissolved with an organic solvent;

[0026] (2) polyvinyl alcohol is made into 1% aqueous solution, and another part of polyvinyl alcohol is made into 0.3% aqueous solution;

[0027] (3) slowly adding the 1% polyvinyl alcohol aqueous solution of step (2) in the organic solution of step (1), cooling in an ice bath, and then ultrasonically emulsifying with a probe to obtain a nano-preparation emulsion of dexmedetomidine;

[0028] (4) Add the solution obtained in (3) to the polyvinyl alcohol solution, then magnetically stir for several hours at a certain temperature, and volatilize and remove the organic solvent to obtain a dexmedetomidine nano-preparation suspension;

[0029] (5) The nano-preparation suspension in step (4) was centrifuged at 8000 rpm, and washed...

Embodiment 1

[0041] Dissolve 10 mg of dexmedetomidine and 50 mg of polylactic acid-polyglycolic acid copolymer (the ratio of polylactic acid and polyglycolic acid is 75:25, and the average molecular weight of the copolymer is 10,000) with 1 ml of dichloromethane, and add it to a 50 ml tip in a bottom centrifuge tube;

[0042] Slowly add 10.0ml of 1% polyvinyl alcohol solution into the dichloromethane solution, and perform ultrasonic emulsification for 2 minutes after cooling in an ice bath; Stir for 2 hours to evaporate the organic solvent;

[0043]Centrifuge the nano-suspension at 8000rpm for 10min, discard the supernatant; wash the nano-preparation with deionized water three times, each time the volume of deionized water is 15ml, then centrifuge at 8000rpm for 10min, discard the supernatant, and obtain a solidified Nano-formulation of dexmedetomidine.

Embodiment 2

[0045] With 7.5mg dexmedetomidine and 50mg polylactic acid-polyglycolic acid copolymer (the ratio of polylactic acid and polyglycolic acid is 50:50, polymer average molecular weight 15000), dissolve with 0.7ml dichloromethane, and add to 50ml conical bottom centrifuge tube;

[0046] Slowly add 8.4ml of 1% polyvinyl alcohol solution into the methylene chloride solution, and perform ultrasonic emulsification for 1 minute after cooling in an ice bath; add the ultrasonically completed emulsion into a beaker containing 36ml of 0.3% PVA solution, and magnetic Stir for 3 hours to evaporate the organic solvent;

[0047] The nanosuspension was centrifuged at 8000rpm for 10min, and the supernatant was discarded; the nano-preparation was washed three times with deionized water, each deionized water volume was 18.2ml, and then separated by centrifugation at 8000rpm for 10min, and the supernatant was discarded, to obtain Cured dexmedetomidine nanoformulations.

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Abstract

The invention discloses a dexmedetomidine nano preparation which is prepared by wrapping dexmedetomidine by a polylactic acid-polyglycolic acid copolymer and by taking polyvinyl alcohol as an emulsifier. The nano preparation is of a spherical structure and has a particle size of 250-350 nanometers. A preparation method comprises the following steps: dissolving the dexmedetomidine and the polylactic acid-polyglycolic acid copolymer; slowly putting a 1% polyvinyl alcohol solution into an organic solvent so as to obtain a dexmedetomidine nano preparation suspension; separating the nano preparation suspension in a centrifuge, and washing with water, thereby obtaining a cured dexmedetomidine nano preparation. The dexmedetomidine nano preparation disclosed by the invention has high dispersibility and a good slow release function, the anesthesia time of the dexmedetomidine is effectively prolonged, and a tolerance dosage is increased, so that the application range of the dexmedetomidine is widened. The dexmedetomidine nano preparation is simple in preparation method and easy to popularize.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a dexmedetomidine nano-preparation and a preparation method thereof. Background technique [0002] Dexmedetomidine is a highly selective α2-adrenoceptor agonist, white powder, insoluble in water. It acts on the α2AR of the brain and spinal cord to inhibit neuronal discharge, and has the characteristics of sedation, analgesia, anxiolysis, inhibition of sympathetic nerve activity, and mild respiratory depression. The structural formula of dexmedetomidine is shown in the figure below: [0003] [0004] Dexmedetomidine is poorly soluble in water, and water-soluble dexmedetomidine hydrochloride is commonly used clinically. Dexmedetomidine is used as an adjuvant drug for general anesthesia and an adjuvant drug in regional blockade. It is used in cardiac surgery, pediatrics, and intensive care units. be widely applied. The adult dosage of dexmedetomidine hydrochloride is to slowly inject 4...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/4174A61K47/34A61K47/32A61P23/00
CPCA61P23/00A61K9/5138A61K9/5146A61K31/4174
Inventor 罗旭倪容蓉谷露张定林孙凤军胡俊
Owner THE FIRST AFFILIATED HOSPITAL OF ARMY MEDICAL UNIV
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