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Lipid microsphere composition and preparation method thereof

A technology of lipid microspheres and compositions, which is applied in the direction of active ingredients of heterocyclic compounds, pharmaceutical formulations, medical preparations of non-active ingredients, etc. Leakage and other issues to achieve the effect of improving encapsulation rate and stability

Active Publication Date: 2021-01-08
NKD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

If the drug has strong water solubility or poor water solubility and oil solubility, it is difficult to make lipid microspheres, or the encapsulation efficiency is low after making lipid microspheres, the stability is poor, and the drug is easy to leak

Method used

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  • Lipid microsphere composition and preparation method thereof
  • Lipid microsphere composition and preparation method thereof
  • Lipid microsphere composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Example 1 Preparation of norcantharidin lipid microsphere composition

[0045] Prescription composition:

[0046]

[0047]

[0048]Preparation of norcantharidin phospholipid complex: dissolve egg yolk lecithin E80 with 20 ml of ethanol, add norcantharidin, control temperature at 10-15°C, stir for 2 hours, and dry under reduced pressure to remove ethanol.

[0049] Preparation of norcantharidin lipid microsphere composition:

[0050] (1) Norcantharidin phospholipid complex, oleic acid and egg yolk phosphatidylglycerol were added to a mixed solvent of soybean oil and medium chain triglyceride, and stirred at 70° C. until completely dissolved to obtain an oil phase.

[0051] (2) Poloxamer 188, glycerin and sodium metabisulfite were added to water for injection, and stirred at 70° C. until dissolved to obtain an aqueous phase.

[0052] (3) adding the water phase to the oil phase under high-speed shearing at 15,000 rpm to obtain colostrum.

[0053] (4) Using a high-p...

Embodiment 2

[0056] The preparation of embodiment 2 docetaxel lipid microspheres

[0057] Prescription composition:

[0058]

[0059]

[0060] Preparation of docetaxel phospholipid complex: dissolve egg yolk lecithin E80 with 10 ml of ethanol, add docetaxel, control temperature at 2-8°C, stir for 4 hours, and dry under reduced pressure to remove ethanol.

[0061] Preparation of Docetaxel Lipid Microsphere Composition:

[0062] 1) Add docetaxel phospholipid complex, oleic acid and egg yolk phosphatidylglycerol into soybean oil, stir at 40° C. until the dissolution is complete, and prepare an oil phase.

[0063] (2) Poloxamer 188 and glycerin were added to water for injection, and stirred at 40° C. until dissolved to obtain an aqueous phase.

[0064] (3) adding the water phase to the oil phase under high-speed shearing at 10,000 rpm to obtain colostrum.

[0065] (4) Using a high-pressure homogenizer, the colostrum was homogenized at a high pressure of 5000 psi for 2 times and at a h...

Embodiment 3

[0068] Example 3 Preparation of paclitaxel lipid microsphere composition

[0069] Prescription composition:

[0070] Element Dosage (g) paclitaxel 0.02 Egg yolk lecithin E80 0.10 egg yolk phosphatidylglycerol 0.01 Phosphatidylinositol 1.8 Poloxamer 188 0.8 Corn oil 6 Oleic acid 0.06 glycerin 1.8 Sodium bisulfite 0.01 Phosphoric acid Moderate Water for Injection to 100ml

[0071] Preparation of paclitaxel phospholipid complex: dissolve egg yolk lecithin E80 with 5 ml of ethanol, add paclitaxel, control the temperature to 25°C and stir for 1 hour, and then dry under reduced pressure to remove ethanol.

[0072] Preparation of paclitaxel lipid microsphere composition:

[0073] (1) Add paclitaxel phospholipid complex, oleic acid, phosphatidylinositol and egg yolk phosphatidylglycerol to corn oil, stir at 50° C. until the dissolution is complete, and obtain an oil phase.

[0074] (2) Poloxamer 188, ...

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Abstract

The invention relates to a lipid microsphere composition and a preparation method thereof. The lipid microsphere composition contains a pharmaceutical phospholipid complex, and contains egg yolk phosphatidylglycerol as a stabilizer, wherein phospholipid is egg yolk lecithin E80. According to the embodiment of the invention, the egg yolk lecithin E80 is selected to prepare the pharmaceutical phospholipid complex, and the egg yolk phosphatidylglycerol is selected as the stabilizer, so that the prepared lipid microsphere can remarkably improve the encapsulation efficiency and stability, and particularly has a better effect on medicines with poorer fat solubility.

Description

technical field [0001] The present invention relates to a lipid microsphere composition and a preparation method thereof. Background technique [0002] Compared with oral preparations, injections have the advantages of fast onset of action and high bioavailability. However, because the drug directly enters the circulatory system, there is no process of release and absorption, the injection of ordinary intravenous administration is likely to cause too high concentration at the initial stage of administration, causing toxic reactions; the drug itself, excipients or solvents are easily irritating to the injection site or blood vessels. Reduce patient compliance. [0003] Lipid microspheres are a kind of microparticle dispersion system with fatty oil as soft matrix and encapsulated by phospholipid membrane. The lipid core part encapsulated in lipid microspheres. Because the drug is wrapped by phospholipid membrane and does not directly contact with blood, water and tissue, li...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/337A61K31/34A61K31/365A61K31/4745A61K45/00A61K47/24A61K47/54
CPCA61K9/107A61K47/24A61K47/544A61K45/00A61K31/365A61K31/34A61K31/337A61K31/4745
Inventor 左保燕马丽端陈成军张超尚丽霞陶秀梅
Owner NKD PHARMA CO LTD
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