Oxiracetam phospholipid-coated microbubble and preparation method thereof

A technology of lipid microbubbles and phospholipids, which is used in pharmaceutical formulations, medical preparations with non-active ingredients, and non-active ingredients of polymer compounds, etc. To achieve the effect of prolonging the action time of the drug, reducing the degradation, and enhancing the immune function

Inactive Publication Date: 2016-04-27
CHONGQING RUNZE PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although the research on microbubbles in contrast agents is becoming more and more mature, it is rare to study microbubbles as a new type of drug carrier
Although microbubbles have unique advantages in targeted drug delivery and promotion of drug absorption at the target site, there are many technical problems that cannot be overcome at present: for example, as a drug carrier, the drug loading capacity of microbubbles is low, resulting in the delivery to the target site. The drug concentration is low, not enough for most drugs to produce effective pharmacological effects, etc.
At present, drug-loaded microbubbles are only suitable for a small amount of drugs with strong drug effects, such as recombinant human endostatin, buserelin, paclitaxel, etc.

Method used

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  • Oxiracetam phospholipid-coated microbubble and preparation method thereof
  • Oxiracetam phospholipid-coated microbubble and preparation method thereof
  • Oxiracetam phospholipid-coated microbubble and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] 2) Preparation of Oxiracetam Albumin Nanoparticles

[0071] Oxiracetam albumin nanoparticles were prepared by desolvation method, accurately weighed 20mg of bovine serum albumin and dissolved in 2mL of water, and another 200mg of oxiracetam was dissolved in 12mL of absolute ethanol at a volume flow rate of 1mL / min Add oxiracetam ethanol solution dropwise to albumin aqueous solution, add 100mL of glutaraldehyde with a concentration of 0.25%, and stir for 4 hours in the dark to solidify, and remove ethanol by rotary evaporation at 35°C to obtain oxiracetam albumin nanoparticle mixture. Suspension, see results figure 1 . The encapsulation efficiency was determined to be 88.48% by centrifugation.

[0072] 3) Preparation of Oxiracetam-loaded Albumin Nanoparticle Lipid Microbubbles

[0073] Take 4 mL of the lecithin mixture prepared in step 1 and mix evenly with 1 mL of oxiracetam albumin nanoparticles prepared in step 2, heat and incubate for 2 hours, then fill with perf...

Embodiment 2-10

[0086] Experimental results show: the kind of phospholipid, the proportioning relationship of phospholipid, glycerol and phosphate buffer solution, and the selection of glutaraldehyde have very important influence on the present invention.

[0087] The experimental results of Examples 1-7 of the present invention show that: through the cooperation of various parameters of the present invention, an encapsulation rate of 82.3% to 92% can be realized, and the diameter of the obtained oxiracetam lipid microbubbles is 4 to 7 microns. The imaging effect in vitro and in vivo is good, and the drug release rate in vivo is 80-92% within 24 hours, which has a good application prospect.

[0088] Example 11

[0089] The oxiracetam lipid microvesicle that embodiment 1 is made is made into freeze-dried powder preparation

Embodiment 11

[0091] Primary drying (sublimation drying)

[0092] Refrigerate the back box, and when the temperature of the back box reaches -40°C, turn on the vacuum pump, and then open the small butterfly valve after 2 seconds to evacuate the back box. When the vacuum of the rear box is ≤90Pa, open the middle partition valve. When the vacuum of the front box is ≤12pa, set the temperature of the heat transfer oil to 0°C, the limited leakage to 8±2pa, heat the product for 180min, and set the temperature of the heat transfer oil to 10°C , the limited amount of leakage is 8±2pa, until the product is completely whitened. During the entire sublimation process, the vacuum degree of the front and rear boxes should be ≤30Pa, the product temperature should be ≤-20°C, and the condenser temperature should be ≤-50°C. If there is an abnormal situation, slow down the heating speed, stop heating or lower the plate temperature.

[0093] Secondary drying (analytical drying)

[0094] Set the layer temper...

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Abstract

The invention provides an oxiracetam phospholipid-coated microbubble. The oxiracetam phospholipid-coated microbubble comprises a phospholipid bilayer membrane, gas and albumin nano particles carrying oxiracetam, wherein the gas and the albumin nano particles are wrapped in the phospholipid bilayer membrane. The oxiracetam phospholipid-coated microbubble has the advantages that the oxiracetam phospholipid-coated microbubble has relatively high drug loading capacity and entrapment efficiency and can increase the plasma concentration of a target position, prolong the action time of drugs at the target position, reduce drug degradation and increase drug stability, and the nano particles can promote the selective distribution of the drugs, favorably deliver the drugs into lesion tissue, increase drug effect and reduce toxic and side effects. The invention further discloses a preparation method of the oxiracetam phospholipid-coated microbubble. The preparation method has the advantages that the method is simple in preparation process, easy in industrialization, high in safety and high in environmental friendliness, chemical reactions are not involved in the preparation process, and no organic solvents with high toxicity are used.

Description

technical field [0001] The invention relates to oxiracetam, in particular to oxiracetam lipid microvesicles and a preparation method thereof. Background technique [0002] Oxiracetam is a nootropic drug synthesized for the first time in 1974 by the Italian Shi Kebichem Company. It is composed of two isomers (S)-oxiracetam ((S)-oxiracetam) and (R)- Racemate of oxiracetam ((R)-oxiracetam). The nootropic drug oxiracetam is a synthetic hydroxyaminobutyric acid (GABOB) derivative, which is a central nervous system drug that can promote learning, enhance memory, and protect damaged nerve cells. [0003] Patent CN102525899A announced a kind of oxiracetam injection, CN1555794A announced a kind of oxiracetam dispersible tablet, CN102579386A announced a kind of oxiracetam capsule and film-coated tablet, CN101732251A announced a kind of oxiracetam lipid Plastid injection; these preparations all have problems such as short drug target action time, insufficient drug stability, and fast...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4015A61K47/42A61K47/24A61K9/00A61K9/19A61P25/00
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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