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Perfluorination carbon emulsion and preparing method thereof

A technology of perfluorocarbons and emulsions, which is applied in the fields of active ingredients of fluorine compounds, pharmaceutical formulations, and emulsion delivery, etc. It can solve problems such as sudden blood pressure, complement activation, and insufficient biocompatibility, and achieves small particle size Effect

Inactive Publication Date: 2011-04-13
XIAN LIBANG PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the products studied in the above countries use poloxamer F-68 as the surfactant. Although some of them have achieved success, for example, Russia’s Perftoran is marketed in Russia, but its common side effect is that it can activate the body’s complement and cause blood pressure. Sudden increase in white blood cells
It shows that its biocompatibility is not good enough. At the same time, this type of product also has the disadvantages that it cannot be sterilized by circulating steam and needs to be frozen.

Method used

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  • Perfluorination carbon emulsion and preparing  method thereof
  • Perfluorination carbon emulsion and preparing  method thereof
  • Perfluorination carbon emulsion and preparing  method thereof

Examples

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preparation example Construction

[0034] The preparation method of its perfluorocarbon emulsion comprises the following steps:

[0035] (1) Dispersing a certain amount of phospholipids in water or a buffer containing a stabilizer and an osmotic pressure regulator to prepare a phospholipid dispersion.

[0036] (2) Mix perfluorodecalin (perfluorodecalin, PFD) and perfluoro-N-4-methylcyclohexylpiperidine (perfluoro-N-(4-methylcyclohexyl)-piperidine, PFMCP) in a certain volume ratio Preparation of fluorocarbon mixed liquid.

[0037] (3) Dispersing a certain amount of fluorocarbon mixture obtained in step (2) in the phospholipid dispersion obtained in step (1) to form colostrum.

[0038] (4) The colostrum obtained in the step (3) is homogenized or micro-jetted to form a stable emulsion under certain pressure conditions, and after completion, the emulsion is subpackaged and sterilized to obtain a perfluorocarbon emulsion;

[0039] Alternatively, the emulsion is mixed in proportion with a buffer containing a stabil...

Embodiment 1

[0052] prescription:

[0053] PFD60ml

[0054] PFMCP 40ml

[0055] Yolk Lecithin 5g

[0056] Disodium hydrogen phosphate 0.284g

[0057] Sodium dihydrogen phosphate 0.24g

[0058] Glycerin 25g

[0059] Appropriate amount of water for injection

[0060] Full volume 1000ml

[0061] Method one:

[0062] The whole process was carried out under nitrogen protection.

[0063] Take PFD and PFMCP, stir well, heat to 80°C±5°C, use as oil phase, and set aside. Take another appropriate amount of water for injection, heat to 80°C±5°C, add disodium hydrogen phosphate, sodium dihydrogen phosphate and glycerin, stir until dissolved, then add egg yolk lecithin, stir vigorously until evenly dispersed, slowly add the oil phase, add Stir for a while after finishing, then use a high-pressure homogenizer for homogenization, keep the homogenization temperature at 60°C±5°C, adjust the homogenization pressure and the number of homogenization, so that the average particle size is below 400nm, ...

Embodiment 2

[0069] prescription:

[0070] PFD 140ml

[0071] PFMCP 60ml

[0072] Egg yolk lecithin 20g

[0073] Disodium hydrogen phosphate 0.284g

[0074] Sodium dihydrogen phosphate 0.24g

[0075] Vitamin E 0.1g

[0076] Sodium chloride 7.92g

[0077] Appropriate amount of water for injection

[0078] Full volume 1000ml

[0079] Method one:

[0080] The whole process was carried out under nitrogen protection.

[0081] Take PFD and PFMCP, stir well, heat to 40°C±5°C, use as oil phase, and set aside. Take another appropriate amount of water for injection, heat to 40°C±5°C, add disodium hydrogen phosphate, sodium dihydrogen phosphate and sodium chloride, stir until dissolved, then add vitamin E and egg yolk lecithin, stir vigorously until dispersed evenly, slowly Add the oil phase, stir for a while after the addition, and then use a high-pressure homogenizer to homogenize, keep the homogenization temperature at 40°C±5°C, adjust the homogenization pressure and homogenization times...

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PUM

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Abstract

The invention discloses a fluorocarbon emulsion and a preparation method of the fluorocarbon emulsion. The average particle size of the prepared fluorocarbon emulsion is less than 400 nm; the pH value is 4 to 9.5 ; and the osmotic pressure is 270 m MOS to 320 m MOS. Wherein, the fluorocarbon emulsion contains perfluorodecalin and perfluoro-N-4-Cyclohexyl Methyl piperidine; the volume ratio between the perfluorodecalin and the perfluoro-N-4-Cyclohexyl Methyl piperidine is 100 percent : 0 to 0: 100 percent; the volume percent ratios of the perfluorodecalin and the perfluoro-N-4-Cyclohexyl Methyl piperidine in the fluorocarbon emulsion are 5 percent to 30 percent; the fluorocarbon emulsion also contains phospholipid used as emulsifier; and the weight percentage of the phospholipid is 0.5 percent to 4.0 percent. The fluorocarbon emulsion is prepared with the method of homogenizing under high pressure or micro-jet, and has the advantage that the fluorocarbon emulsion can be stored in the non-refrigerated state. Thus, the fluorocarbon emulsion is a novel artificial preparation for carrying oxygen.

Description

technical field [0001] The invention belongs to the technical field of medicine preparation, and in particular relates to a perfluorocarbon emulsion and a preparation method thereof. Background technique [0002] Perfluorocarbons are hydrophobic and oleophobic, and their magnetic susceptibility is close to that of water. They have high solubility for gas, high density, and easy diffusion. Its oxygen-carrying capacity is high, and it can release 82% of oxygen in a pathological state, which exceeds the oxygen supply capacity of the patient's own red blood cells. It has low surface tension, moderate viscosity, good fluidity, and high vapor pressure, which is easy to be discharged through the respiratory tract and does not participate in human metabolism. [0003] Fluorocarbon liquid has the important function of human blood, it can transport the oxygen inhaled from the lungs to various parts of the human body, and transport the carbon dioxide discha...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/24A61K33/16A61P7/08A61K47/34A61K9/107A61K47/10A61K47/26
Inventor 王九成胡忍乐王智军李红英欧根坭·马亚夫斯基
Owner XIAN LIBANG PHARMA TECH
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