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Oxiracetam preparation and method of preparing the same

A preparation and nanoparticle technology, applied in the field of medicine, can solve the problems of low blood-brain barrier permeability, improve oxiracetam, increase the amount of drug entering the brain, etc., to prolong the circulation time, increase the dose, inhibit Effects of uptake by efficient efflux pumps

Active Publication Date: 2008-04-02
CSPC OUYI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although some lipophilic drugs with appropriate molecular weight can pass through the BBB, they are quickly absorbed back into the blood by the high-efficiency efflux pump on the cell membrane, so the amount of drugs in the brain is very small
And oxiracetam is a kind of very polar small molecular substance, very hydrophilic, the partition coefficient in organic solvent is very small, the blood-brain barrier permeability is low, in addition, the efficient efflux pump on the cell membrane Ingestion, so that the amount of oxiracetam in the brain is very small, which affects the efficacy of the drug
The Chinese patent publication number is CN1555794, and the name is "oxiracetam dispersible tablet and its preparation method"; the Chinese patent publication number is CN1424034, and the name is "a preparation method and product of oxiracetam injection preparation"; the Chinese patent Publication No. CN1390543, titled "Oxiracetam Medicine for Injection"; Chinese Patent Publication No. CN1486693, titled "Preparation Method and Product of Oxiracetam Freeze-dried Powder Injection" respectively recorded oxiracetam different dosage forms, but these dosage forms did not mention how to improve the blood-brain barrier permeability of oxiracetam and increase the amount of drug entering the brain

Method used

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  • Oxiracetam preparation and method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] a, take by weighing 80mg oxiracetam and dissolve in acetone, form the solution of 80mg / ml, take by weighing the chitin of 1520mg and dissolve in the methylene chloride and form the solution of 20mg / ml, then mix these two kinds of organic solutions;

[0022] b. Add the mixed organic solution to a 2% PVA solution 4 times its volume, use a probe ultrasonic instrument under ice bath conditions, and ultrasonically treat it for 2 minutes to form an emulsion;

[0023] c. Volatilize under normal pressure for 2 hours, evaporate under reduced pressure for 30 minutes, remove the organic solvent, centrifuge at 10°C, 23,000 r / min at high speed for 30 minutes, collect the solidified nanoparticles, wash with an appropriate amount of distilled water, centrifuge twice, and freeze-dry to obtain nanoparticles ;

[0024] d. Weigh 32 mg of glucosamide, add distilled water to form a 5 mg / ml solution, and then add nanoparticles. Sonicate for 60 s in an ice bath to evenly suspend the nanopart...

Embodiment 2

[0026] a, take by weighing 120mg oxiracetam and dissolve in acetone to form a solution of 80mg / ml, take by weighing 1080mg of chitin and dissolve in dichloromethane to form a solution of 20mg / ml, then mix these two organic solutions;

[0027] b. Add the mixed organic solution to a 2% PVA solution 4 times its volume, use a probe ultrasonic instrument under ice bath conditions, and ultrasonically treat it for 2 minutes to form an emulsion;

[0028] c. Volatilize under normal pressure for 2 hours, evaporate under reduced pressure for 30 minutes, remove the organic solvent, centrifuge at 10°C, 23,000 r / min at high speed for 30 minutes, collect the solidified nanoparticles, wash with an appropriate amount of distilled water, centrifuge twice, and freeze-dry to obtain nanoparticles ;

[0029] d. Weigh 36 mg of methylglucosamide, add distilled water to form a 5 mg / ml solution, and then add nanoparticles. Sonicate for 60 s in an ice bath to evenly suspend the nanoparticles. 10°C, 23...

Embodiment 3

[0031] a. Weigh 160mg of oxiracetam and dissolve it in acetone to form a solution of 80mg / ml, weigh 906mg of glucosamidooligosaccharide and dissolve it in dichloromethane to form a solution of 20mg / ml, and then mix the two organic solutions ;

[0032] b. Add the mixed organic solution to a 2% PVA solution 4 times its volume, use a probe ultrasonic instrument under ice bath conditions, and ultrasonically treat it for 2 minutes to form an emulsion;

[0033] c. Volatilize under normal pressure for 2 hours, evaporate under reduced pressure for 30 minutes, remove the organic solvent, centrifuge at 10°C, 23,000 r / min at high speed for 30 minutes, collect the solidified nanoparticles, wash with an appropriate amount of distilled water, centrifuge twice, and freeze-dry to obtain nanoparticles ;

[0034] d. Weigh 42 mg of glucosamide, add distilled water to form a 5 mg / ml solution, and then add nanoparticles. Sonicate for 60 s in an ice bath to evenly suspend the nanoparticles. 10°C...

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Abstract

The invention provides an oxiracetam agent and the preparation method, which relates to medical technical field and is used to induce the drug to penetrate through blood-brain barrier and to improve treatment effects. The agent contains oxiracetam nano-particle and excipientpharmaceutical excipient. After improved, the oxiracetam nano-particle and excipientpharmaceutical excipient contains drug core and a modified layer. The drug core mainly comprises principal agent and carrier, wherein the carrier is polymer material containing amino polysaccharide with a content of 70 to 95 percent, and the principal agent is oxiracetam with a content of 5 to 30 percent. The invention adopts polymer material containing amino polysaccharide as carrier to carry the oxiracetam and endow the oxiracetam with good brain targeting function. And the invention adopts surfactant to modify the nano surface of the carrier and lengthens the recycling time of the carrier nano-granule and the nano-particle in the recycling system. Tests show that the blood-brain barrier transmittance is 24h, which is 36.75 percent higher than ordinary oxiracetam agent and greatly enhances the dosage of oxiracetam passing through the blood-brain barrier.

Description

technical field [0001] The invention relates to a method for preparing a pharmaceutical preparation, in particular to an oxiracetam preparation with relatively high blood-brain barrier permeability, which belongs to the technical field of medicine. Background technique [0002] Oxiracetam is a synthetic cyclic derivative of hydroxyaminobutyric acid (GABOB), which only acts on the central nervous system, mainly distributed in the cerebral cortex and hippocampus, and can activate, protect or promote the functional recovery of nerve cells , to improve the memory and learning functions of mentally handicapped patients, and the drug itself has no direct vasoactive or central stimulating effect, and the effect on the learning and memory ability is a lasting promotion effect. [0003] Since oxiracetam mainly acts on the cerebral cortex and hippocampus, it needs to pass through the blood-brain barrier. The blood-brain barrier (BBB) ​​is a barrier between blood and brain tissue form...

Claims

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Application Information

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IPC IPC(8): A61K31/4015A61K9/16A61K47/36A61P25/00
Inventor 郭卫芹张育李国聪
Owner CSPC OUYI PHARM CO LTD
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