Abstract

To illustrate the effects of premixing propofol lipid emulsion (PLE) and fentanyl citrate (FC) on acute toxicity, sedation, and analgesia, sixty female mice were randomly assigned to individual and premixed groups. The median lethal dose (LD50), median effective dose (ED50) of loss of righting reflex, and ED50of tail flick test in both groups were determined using the up and down procedure (FC : PLE = 1 μg : 2 mg). PLE was immediately administered to the mice from the individual group via the tail vein after injecting FC. By contrast, FC was mixed with PLE before injection from the premixed group. No significant differences in LD50, histopathological examination, and ED50sedation value were found between the groups. However, ED50of analgesia in the premixed group decreased to half of that in the individual group. Transmission electron microscopic observation revealed ~10 nm fusiform particles at the juncture of 200–300 nm particles in the mixture of PLE and FC compared with the single PLE and its mixture with saline, which may be attributed to the structure of FC. In conclusion, premixing PLE and FC enhanced synergic analgesia twofold but did not influence toxicity and sedation compared with individual injections.

Highlights

  • Propofol (2,6-diisopropylphenol) is widely used to induce and maintain sedation during operation and intensive care

  • The estimated LD50 in the premixed group was 34.84 mg/kg propofol combined with 17.42 μg/kg fentanyl, and LD50 in the individual group was 34.84 mg/kg propofol + 17.42 μg/kg fentanyl, which showed no significant difference between the two groups (Table 1)

  • Propofol is prepared into propofol lipid emulsion, whereas fentanyl is prepared into fentanyl citrate

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Summary

Introduction

Propofol (2,6-diisopropylphenol) is widely used to induce and maintain sedation during operation and intensive care. Propofol is an important clinical intravenous anesthetic that presents rapid action and short-term effects. Propofol is injected in clinical settings as a lipid emulsion with a particle size of 200–259 nm [1]. Propofol lipid emulsion is commonly prepared as follows: 1% propofol, 10% soybean oil, 1.2% purified egg phospholipids (emulsifier), and 2.25% glycerol (tonicity-adjusting agent); sodium hydroxide is added to adjust the pH. The large amount of soybean oil long-chain triglyceride increases the serum triglyceride level and induces hypertriglyceridemia [2]. A new type of propofol medium/long-chain lipid emulsion has been developed, in which half of the soybean oil long-chain triglyceride is replaced with medium-chain triglycerides to reduce the abovementioned risks [3]

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