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Oxiracetam lipid micro-bubble and preparation method thereof

A technology of lipid microbubbles and phospholipids, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of insufficient pharmacological effects, low drug concentration, and rare research To achieve the effect of prolonging drug action time, reducing degradation, and fast delivery efficiency

Inactive Publication Date: 2016-05-11
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 lipid micro-bubble and preparation method thereof
  • Oxiracetam lipid micro-bubble and preparation method thereof
  • Oxiracetam lipid micro-bubble and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] 2) Preparation of Oxiracetam Albumin Nanoparticles

[0070] 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.

[0071] 3) Preparation of Oxiracetam-loaded Albumin Nanoparticle Lipid Microbubbles

[0072] Get the lecithin mixed solution 4mL that step 1 makes and the oxiracetam albumin nanoparticle 1mL that step 2 makes and mix evenly, heat and cultivate for 2 hours, then fill with nitro...

Embodiment 2-10

[0085] 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.

[0086] 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.

[0087] Example 11

[0088] The oxiracetam lipid microvesicle that embodiment 1 is made is made into freeze-dried powder injection preparation

Embodiment 11

[0090] Primary drying (sublimation drying)

[0091] 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 temperature of the product should be ≤-20°C, and the temperature of the condenser should be ≤-50°C. In case of abnormal conditions, slow down the heating speed, stop heating or lower the plate temperature.

[0092] Secondary drying (analytical drying)

[0093] Set the l...

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Abstract

The invention provides an oxiracetam lipid micro-bubble. The oxiracetam lipid micro-bubble comprises a phospholipid bi-layer membrane, a gas and an oxiracetam-supported alhumin nanoparticle, wherein the gas and the oxiracetam-supported alhumin nanoparticle are wrapped in the phospholipid bi-layer membrane, and the gas is a nitrogen and perfluoropropane mixed gas with the volume ratio of 1:2-5. The oxiracetam lipid micro-bubble has high drug loading capacity and entrapment rate, can improve the plasma concentration of a target position, prolongs the action time of drugs in the target position, reduces drug degradation and improves the drug stability, and the nanoparticle can promote selective distribution of the drugs, facilitation of delivery of the drugs to lesion tissues, increases the drug effects and reduces toxic and side effects. The invention also discloses a preparation method of the lipid micro-bubble. The preparation method has the advantages of simplicity, easy industrialization, no involving of chemical reactions in the preparation process, no use of highly toxic organic solvents, high safety and strong environmental protection property.

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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IPC IPC(8): A61K31/4015A61K9/00A61K9/19A61K47/42A61K47/24A61P25/00
Inventor 叶雷
Owner CHONGQING RUNZE PHARM CO LTD
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