Preparation method and application of paclitaxel intravenous fat emulsion

A paclitaxel and fat emulsion technology, applied in the field of medicine, can solve the problems of toxic reaction, influence on the clinical safe application of taxane drugs, anaphylactic shock, etc., and achieve the effects of enhanced compliance, simple preparation method, and uniform quality and appearance.

Inactive Publication Date: 2013-06-19
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are many defects in this type of paclitaxel preparation itself, mainly in the severe adverse reactions caused by polyoxyethylene castor oil, such as anaphylactic shock, bronchospasm, etc.; Phthalates cause toxic reactions and affect the clinical safety application of traditional taxane drugs

Method used

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  • Preparation method and application of paclitaxel intravenous fat emulsion
  • Preparation method and application of paclitaxel intravenous fat emulsion
  • Preparation method and application of paclitaxel intravenous fat emulsion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1: Preparation of paclitaxel fat emulsion with seal oil as oil phase and polyoxyethylene 40 hydrogenated castor oil as emulsifier

[0049] Accurately weigh 0.1g paclitaxel and dissolve in 1.0g seal oil as the oil phase; weigh 0.25g polyoxyethylene 40 hydrogenated castor oil (HCO-40) and 0.20g glycerin in 10ml water for injection (0.1% sodium hydroxide to adjust pH Mix evenly in 8.5) and use it as the water phase; slowly add the oil phase to the water phase dropwise, and stir for 30 minutes with magnetic force to form a primary emulsion. fat milk.

Embodiment 2

[0050] Example 2: Preparation of paclitaxel fat emulsion with seal oil as oil phase and lecithin as emulsifier

[0051] Accurately weigh 0.02g of paclitaxel and dissolve in 1.0g of seal oil as the oil phase; weigh 0.25g of lecithin and 0.225g of glycerin in 10ml of water for injection (0.1% sodium hydroxide to adjust the pH to 8.5) and mix evenly as the water phase Then slowly drop the oil phase into the water phase, stir it magnetically for 30 minutes to form a primary emulsion, and circulate the high-pressure emulsion 5 times under a pressure of 800-1200 bar to obtain paclitaxel intravenous fat emulsion.

Embodiment 3

[0052] Example 3: Observation of Microscopic Morphology of Paclitaxel Fat Emulsion

[0053] Take the paclitaxel fat emulsion sample solution, dilute it with distilled water, take 10ul and put it on the surface of the copper mesh, line it with filter paper, and dry it naturally, then prepare for transmission electron microscope observation. Fix the electron beam voltage of the electron microscope at 80kV, move the coordinates, adjust the magnification, find and observe the particles and take pictures. See attached figure 1 . At the same time, 20ul of the diluted sample was dropped on the cover glass, evaporated to dryness naturally, sprayed with gold, and observed by scanning electron microscope. See attached figure 2 .

[0054] In the present invention, it can be seen through a transmission electron microscope that a single nanostructured lipid carrier is a spherical particle with relatively uniform size and relatively uniform distribution; the above results are also con...

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Abstract

The invention relates to a preparation method and application of paclitaxel intravenous fat emulsion. The paclitaxel fat emulsion comprises (1) 5-30% of marine organism fat rich in omega-3 fatty acid, (2) 0.5-7.5% of emulsifying agents, (3) 1.5-3.5% of glycerol, (4) 0.02-12% of paclitaxel and the balance of water for injection. The paclitaxel intravenous fat emulsion has good stability and slow release effect, shows excellent anti-tumor effects inside and outside the animal bodies, avoids the adverse effects caused by cremophor EL in the paclitaxel preparations clinically applied at present and provides a good carrier for paclitaxel.

Description

technical field [0001] The invention belongs to the field of medicine and relates to the preparation of paclitaxel intravenous injection fat emulsion with seal oil as the base. The invention mainly relates to the solubilization effect of the fat emulsion on medicine, its stability and the application of anti-tumor. Background technique [0002] For a long time, fat emulsion has been mainly used in clinical practice in the form of nutritional fat emulsion. Because the emulsion has the advantages of small size, high energy, small venous irritation, and peripheral intravenous administration, more and more attention has been paid to the choice of As a new drug carrier, venous milk encapsulates the drug in the inner phase or interface layer. Compared with other particulate carriers, the advantages of venous milk are: the drug is encapsulated in the inner phase or interface layer, the encapsulation rate is high, the stability of the drug is improved and the irritation and toxicit...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/337A61K47/44A61P35/00
Inventor 崔国辉崔纯莹敬婷婷
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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