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Propofol self-micro-emulsifying composition and preparation method thereof

A technology of self-microemulsification and propofol, which is applied to the active ingredients of hydroxyl compounds, drug combinations, drug delivery, etc., can solve the problems of injection pain and low oral bioavailability, to promote absorption, improve oral bioavailability, Good patient compliance

Inactive Publication Date: 2010-03-24
WUXI APPTEC (TIANJIN) CO LTD +3
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to solve the technical problems of injection pain and extremely low oral bioavailability in the existing fat emulsion formulation of propofol, and provide a self-microemulsifying composition of propofol and its preparation method

Method used

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  • Propofol self-micro-emulsifying composition and preparation method thereof
  • Propofol self-micro-emulsifying composition and preparation method thereof
  • Propofol self-micro-emulsifying composition and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Proportion: Propofol 10g

[0027] Polyoxyethylene Hydrogenated Castor Oil 40 60g

[0028] Divinyl glycol monoethyl ether 20g

[0029] Isopropyl Myristate 10g

[0030] Butylated Hydroxyanisole 0.02%

[0031] Preparation method: Weigh an appropriate amount of propofol, add the prescribed amount of oil phase, emulsifier, co-emulsifier and antioxidant, stir to make it evenly mixed at room temperature, protected from light and filled with nitrogen to obtain isopropofol Phenolic self-microemulsifying compositions.

Embodiment 2

[0033] Proportion: Propofol 10g

[0034] Polyoxyethylene Hydrogenated Castor Oil 40 56g

[0035] Isopropanol 19g

[0036] Isopropyl Myristate 15g

[0037] tert-butylhydroquinone 0.02%

[0038] Preparation method: Weigh an appropriate amount of propofol, add the prescribed amount of oil phase, emulsifier, co-emulsifier and antioxidant, stir to make it evenly mixed at room temperature, protected from light and filled with nitrogen to obtain isopropofol Phenolic self-microemulsifying compositions. The prepared self-emulsifying microemulsion composition is prepared into a reservoir layer of a transdermal patch, which is sequentially compounded with a backing layer and a pressure-sensitive layer on one side, and then sequentially compounded with a controlled-release layer and a protective layer on the other side, A transdermal patch containing self-emulsifying microemulsion is obtained.

Embodiment 3

[0040] Proportion: Propofol 10g

[0041] Polyoxyethylene castor oil 35 45g

[0042] Isopropanol 30g

[0043] Ethyl oleate / corn oil (2:1) 15g

[0044] Butylated Hydroxyanisole 0.02%

[0045] Preparation method: Weigh an appropriate amount of propofol, add the prescribed amount of oil phase, emulsifier, co-emulsifier and antioxidant, stir to make it evenly mixed at room temperature, protected from light and filled with nitrogen to obtain isopropofol Phenolic self-microemulsifying compositions.

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Abstract

The invention relates to a propofol self-micro-emulsifying composition and a preparation method thereof, mainly aiming at solving the technical problems of injection pain and extremely low oral bioavailability of the existing fat emulsion. The invention has the technical scheme that the propofol self-micro-emulsifying composition comprises the components by weight percent: 1-15% of propofol, 10-70% of emulsifying agent, 0-50% of auxiliary emulsifying agent and 0-30% of oil phase. The new formulation of propofol has the characteristics of low gastrointestinal metabolism, higher bioavailability,good stability and easy preparation.

Description

technical field [0001] The invention relates to a propofol self-microemulsifying composition and a preparation method thereof. Background technique [0002] Propofol, namely 2,6-diisopropylphenol, is a new type of systemic intravenous anesthetic. It has the advantages of quick onset, short action time, quick and complete recovery, few adverse reactions, no sequelae, wide application range (can be used for anesthesia induction, maintenance and auxiliary epidural anesthesia), and easy-to-control dosage. Therefore, since its anesthetic activity was discovered in 1977, many researches have been carried out on the formulation, and clinical application has been more and more extensive. In recent years, the drug has been widely used in clinical anesthesia induction and anesthesia maintenance, and sedation of intensive care patients. It can be used for intensive monitoring of adult patients receiving mechanical ventilation and sedation during surgery, and can also be used for cons...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/66A61K31/05A61P23/00
Inventor 王高森高萍郭庆海王宇邦
Owner WUXI APPTEC (TIANJIN) CO LTD
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