Propofol microemulsion composition

Abstract

The invention discloses a propofol microemulsion composition which does not contain phosphatide and fatty acid triglycerides. The propofol microemulsion composition provided by the invention comprises 0.8-1.2 % (w / v) of propofol, 20-25 % (w / v) of Pluronic F 68, 20-30 % (w / v) of propylene glycol and the balance being water. The invention provides the propofol microemulsion composition which can be administered through gastrointestinal tracts, skins, mucous membranes or injection, and the composition has advantageous of simple technology conditions, greatly improved stability and convenient usage, and is easy to realize productization and be clinically accepted.

Description

Technical field: [0001] The invention relates to a microemulsion preparation of propofol, which belongs to the field of pharmaceutical preparations. Background technique: [0002] Propofol (Propofol), also known as propofol, is an intravenous anesthesia drug. It was approved by the US FDA in 1989 and recommended for clinical use. With the wide application in clinical practice, it has been found that propofol, as an anesthetic, has unique advantages: quick onset, short maintenance time, rapid recovery, no accumulation, and small side effects. The characteristics of propofol can be summarized as follows: rapid and stable induction of anesthesia, no involuntary muscle movement, coughing, and hiccups during induction, fast metabolism in the body, easy control, no accumulation, rapid recovery after drug withdrawal, stable recovery, and patient consciousness after recovery Clear, no drowsiness, dizziness and other phenomena. In addition, propofol can still inhibit the laryngeal ...

AI Technical Summary

Problems solved by technology

[0004] At present, the clinical preparation of propofol is fat emulsion. The existing clinical and preclinical research results show that the disadvantages that may be related to fat emulsion include: 1) poor physical stability, easy to aggregate into large oil droplets; Unstable system, not resistant to heat and freezing, requires high storage temperature

2) poor dilution resistance; 3) the fat component in the auxiliary material is easy to infect bacteria, and the anesthetic with lipid as the carrier cannot be used under strict aseptic conditions, so the incidence of infection is higher; Lipid components provide a good living environment for bacteria, so infection is prone to occur when propofol is used, and there are continuous reports of infection with propofol

In order to reduce the incidence of infection, the manufacturer added ethylenediaminetetraacetic acid (EDTA) to propofol injection in 1996, which effectively reduced the incidence of infection; Sexual bacterial infection, which brings risks to surgery, etc.

4) Injection is easy to cause pain; 5) Potential safety hazards of auxiliary materials (phospholipids are oxidized); emulsions made of lecithin will be hydrolyzed during storage and transportation, and can form lysophospholipids, which are conducive to the formation and stability of fat emulsions, but have a higher The hemolytic property should be controlled at a low level

6) Due to the fatty solvent of propofol emulsion, long-term infusion will cause hypertriglyceridemia, followed by acute pancreatitis

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