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Intravenous anesthetics 2,6-diisopropyl phenol microemulsion composition and method of making the same

A technology of diisopropylphenol and composition, applied in the field of intravenous anesthetics, can solve the problems that are not conducive to improving patient compliance and reducing pain, and achieve good emulsification effect, low requirements for storage conditions, and reasonable price Effect

Active Publication Date: 2009-04-22
BEIJING SHIQIAO BIOPHAM +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the composition has the advantage of thermodynamic stability, microorganisms can be removed by sterile filtration, it is easy to prepare, and side effects such as embolism and hemolysis can be reduced, but we have found through research that free 2, 6-Diisopropylphenol concentration is higher, and still has stronger hemolytic property (see experimental example 3,4), its reason is that this composition is difficult to wrap 2,6-Diisopropylphenol in hydrophobic phase, resulting in a high concentration of free 2,6-diisopropylphenol in the aqueous phase, and causing it to have strong hemolytic properties. This technology is not conducive to reducing pain during injection and is not conducive to improving patient compliance

Method used

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  • Intravenous anesthetics 2,6-diisopropyl phenol microemulsion composition and method of making the same
  • Intravenous anesthetics 2,6-diisopropyl phenol microemulsion composition and method of making the same
  • Intravenous anesthetics 2,6-diisopropyl phenol microemulsion composition and method of making the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Composition prescription:

[0047]

[0048] Preparation method: Dissolve lecithin in MCT in a water bath at 65°C, add Solutol HS 15, 2,6-diisopropylphenol, and stir evenly to obtain an oil phase; combine glycocholic acid, sodium calcium ethylenediaminetetraacetate Disperse it with glycerin in about 60ml water, adjust the pH to 7 with sodium hydroxide solution to change glycocholic acid into sodium glycocholate to obtain the water phase; add the water phase to the oil phase under stirring at about 60°C, Continue to stir to obtain microemulsion, filter, add water to 100ml, potting, full nitrogen flow protection, and sterilization.

Embodiment 2

[0050] Composition prescription:

[0051]

[0052] Preparation method: Dissolve lecithin in MCT in a water bath at 60°C, add Solutol HS 15, 2,6-diisopropylphenol, and stir evenly to obtain an oil phase; disperse sodium glycocholate and glycerin in about 60ml water , Adjust the pH to 5 to obtain the water phase; add the water phase to the oil phase under stirring at about 60°C, pass the homogenizer 300Bar homogenization 2 cycles to quickly reach equilibrium, obtain microemulsion, filter, add water to 100ml, It is potted, protected by nitrogen flow throughout, and sterilized.

Embodiment 3

[0054] Composition prescription:

[0055]

[0056] Preparation method: Dissolve soybean phospholipids in soybean oil at 70°C in a water bath, add Solutol HS 15, 2,6-diisopropylphenol, and stir evenly to obtain an oil phase; Disperse sodium and glucose in about 60ml of water, adjust the pH to 6 with sodium hydroxide solution to change glycocholic acid into sodium glycocholate to obtain the water phase; add the water phase to the oil phase with stirring at about 70°C , Continue to stir to obtain microemulsion, filter, add water to 100ml, potting, and sterilizing.

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Abstract

The invention provides intravenous anesthetics 2, 6-diisopropyl phenol microemulsion composition, which is characterized by containing 2, 6-diisopropyl phenol, Solutol HS15, oil for injection, phospholipids or other aqueous components. The invention discloses a preparation method for the microemulsion composition at the same time. The grain diameter of the microemulsion composition is less than 100 nanometers, and the microemulsion composition is transparent in appearance, has slight opalescence, does not cause the occurrence of hemolysis, and can be used for intravenous injection and administration.

Description

Technical field [0001] The invention relates to an intravenous anesthetic 2,6-diisopropylphenol microemulsion composition and a preparation method thereof. Background technique [0002] 2,6-Diisopropylphenol (generic name: propofol, propofol) is a central anesthetic, which exerts sedative and hypnotic effects by activating the GABA receptor-chloride complex. 2,6-Diisopropylphenol is clinically suitable for various large and small operations of different ages and locations. It is generally welcomed by the clinic because of its characteristics of quick onset, rapid recovery, and few side effects. [0003] 2,6-Diisopropylphenol has a melting point of 19°C and a pKa of 11.2,6-Diisopropylphenol is highly fat-soluble, its LogP value is 3.842, and its solubility in water at room temperature is about 124mg / L. Due to the poor water solubility of 2,6-diisopropylphenol, it is often prepared using fat emulsion or microemulsion technology. [0004] 2,6-Diisopropylphenol injection is easy to c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/05A61K47/24A61K47/44A61P23/00A61K47/14
Inventor 金方蔡伟惠
Owner BEIJING SHIQIAO BIOPHAM
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