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[Toward a second generation of fluorocarbon emulsions. Methodologies: synthesis of fluorocarbons, formulation, preparation and control of emulsions].

The fluorocarbons to be used as intravascular gas carriers may be prepared: by fluorination of hydrocarbons, by means of gaseous fluorine or of metallic fluorides or by electrolysis in anhydrous hydrogen fluoride; by selective synthesis from small fluorinated molecules. Selective synthesis seems preferable because of the high purity of the compounds thus obtained, allowing fairly simple purification and detoxification procedures. The adequacy of fluorocarbons for intravascular use (limited by the values of some of their crucial physicochemical properties such as vapour pressure, gas dissolving power, viscosity) was found dependent of their molecular weight range, preferably between 460 and 540 dalton. Ionic balance, osmolarity, viscosity, mean particle size and particle size distribution are among the most important criteria to be respected in the preparation of biocompatible emulsions. Several physicochemical methods were developed for selecting the best ingredients and the best emulsification procedures and for evaluating the stability of the emulsions to storage and to thermal stress. The combination of these physicochemical measurements may be used as a methodology for the optimisation and control of fluorocarbon emulsions as well as a way of evaluating new ingredients and formulations.

Biocompatible Materials↗

[Fatty emulsions in parenteral feeding following liver transplantation. A study of the neurotropic effect of MCT/LCT emulsions using EEG].

In the early postoperative period after liver transplantation a possible neurotropic side effect of middle-chain triglycerides used for total parenteral nutrition (TPN) was evaluated by EEG and Glasgow Coma Scale. Group I: no fat for TPN; Group II: 0.7 g/kg body weight (BW) and day, of MCT/LCT emulsion; Group III: 1.5 g/kg BW and day, of MCT/LCT emulsion. Only on postoperative day 5/6 significant differences in distribution of background activity in the EEG were seen between Group I and II. Patients in Group I showed more pathological EEG patterns (Mann-Whitney-U-test p less than 0.05). Per discriminant analysis an influence of applicated fatty acids on the registered background activity could be excluded. Instead an underlying rejection of the graft in 7 of 10 patients could be made responsible for deterioration of the EEG pattern. Following the presented data a negative neurotropic effect of MCT/LCT emulsions in the described dosages can be negated.

Adult↗

A new intravenous emulsion containing medium-chain triglyceride: studies of its metabolic effects in the perioperative period compared with a conventional long-chain triglyceride emulsion.

The effects of carbohydrate, lipid, and nitrogen metabolism of recently available lipid emulsions containing either 50% medium-chain triglyceride (MCT) and 50% long-chain triglyceride (LCT) or 100% LCT were compared in elective surgical patients. Postoperative urinary urea excretion was similar during isocaloric MCT/LCT and LCT infusions (1.9 mg/kg/min) and was decreased compared with a standard infusion of 5% glucose (1 mg/kg/min). Plasma glucose and insulin concentrations were similar during both lipid and low dose glucose infusions. However, plasma triglyceride and nonesterified fatty acid concentrations were decreased during the MCT/LCT infusion compared with the LCT infusion, suggesting that the MCT/LCT emulsion was cleared from the circulation faster than pure LCT. Ketone body concentrations were similar during all three infusions. MCT/LCT emulsion can be safely infused perioperatively and has similar nitrogen conserving properties to LCT in these circumstances.

Blood Glucose↗

Is the antiemetic effect of the emulsion formulation of propofol due to the lipid emulsion?

The hypothesis that the lipid emulsion of the emulsion formulation of propofol is responsible for the low frequency of nausea, retching, and vomiting after propofol anesthesia was tested. A randomized, prospective, and comparative study was performed to evaluate the antiemetic effect of 10% lipid solution in 60 women, ASA physical status I and II, scheduled for ambulatory laparoscopic procedures. Two groups of patients were studied. Induction of anesthesia (thiopental) and maintenance of anesthesia (enflurane, nitrous oxide) were similar in both groups. At induction the study group received 10% Intralipid (3 mL/min for 20 min). The control group received 5% dextrose in lactated Ringer's solution at the same rate. Other drugs administered during or after anesthesia were similar among the groups. The groups were similar with respect to duration of anesthesia, characteristics of early and intermediate recovery, as well as pain scores in the postanesthesia care unit. There were no differences in the amount of antiemetic medications administered or postoperative nausea, retching, or vomiting when the patients were evaluated objectively by a blinded observer or subjectively by patient self-evaluation. It is concluded that 10% Intralipid, the lipid in the emulsion formulation of propofol, does not possess significant antiemetic effects.

Adult↗

Drop Coalescence during Emulsion Formation in a High-Pressure Homogenizer for Tetradecane-in-Water Emulsion Stabilized by Sodium Dodecyl Sulfate.

The present study investigates the effects of homogenizer pressure, surfactant concentration, ionic strength, and dispersed phase fraction on the coalescence rate of tetradecane-in-water emulsions during their formation in a high-pressure homogenizer. Experiments were conducted in a recirculating system consisting of a Rannie laboratory-scale single-stage homogenizer and a stirred vessel for tetradecane-in-water emulsions stabilized by sodium dodecyl sulfate (SDS). The initial evolution of the number concentration of droplets in the stirred tank was measured when subjected to a negative stepchange in the homogenizer pressure. The average drop coalescence rate constant in the homogenizer was inferred by fitting the experimental evolution of the number concentration of drops to a simple model accounting for the coalescence in the homogenizer under the assumption of a quasi steady state in the homogenizer. The residence time of the emulsion in the homogenizer was evaluated from the analysis of radial turbulent flow between disks. The step down homogenizer pressure was varied in the range 20.7-48.3 MPa, the drop size in the range 174-209 nm, the dispersed phase fraction in the range 5%-15%, SDS concentration in the range 0.0033-0.25 wt%, and ionic strength in the range 0.01-0.1 M. The coalescence rate constants were found to be in the range from 3.34x10(-17) to 2.43x10(-16) m(3) s(-1). The coalescence rate constant was found to be higher for higher homogenizer pressures, smaller drop sizes, lower dispersed phase fractions, and lower SDS concentrations and was insensitive to variations in ionic strength. Copyright 2001 Academic Press.

Journal Article↗

Comparison of a lower-lipid propofol emulsion with the standard emulsion for sedation during monitored anesthesia care.

BACKGROUND: The currently used emulsion formulations of 1% propofol contain 10% soybean oil. However, a new emulsion of 1% propofol (Ampofol) containing 50% less lipid has recently become available for clinical investigation. This study was designed to compare the pharmacodynamic properties of Ampofol with those of a standard formulation (Diprivan) when administered for intraoperative sedation. METHODS: Sixty healthy outpatients undergoing minor operations with local anesthesia were randomly assigned to receive either Ampofol (n = 31) or Diprivan (n = 29) for intravenous sedation. The sedation was initiated with an intravenous loading dose of propofol, 0.75 mg/kg, followed by an initial infusion rate of 50 microg x kg(-1) x min(-1) to achieve an Observer's Assessment of Alertness/Sedation score of 3. The targeted level of sedation was maintained with a variable-rate propofol infusion during the operation. The onset times to achieving a sedation score of 3, the severity of pain on injection of the loading dose, intraoperative hemodynamic variables, and electroencephalographic Bispectral Index values were recorded. In addition, recovery times, postoperative pain and nausea, and patient satisfaction with the sedative medication were assessed. RESULTS: There were no significant differences between Ampofol and Diprivan with respect to onset times, dosage requirements, Bispectral Index values, hemodynamic variables, recovery times, or patient satisfaction scores. The incidence of moderate pain on injection was higher in the Ampofol group (26%vs. 7% with Diprivan; P < 0.05). CONCLUSIONS: Ampofol was equipotent to Diprivan with respect to its sedative properties during monitored anesthesia care. Although both groups received pretreatment with intravenous lidocaine, Ampofol was associated with more pain on injection.

Adult↗

The pharmacodynamic effects of a lower-lipid emulsion of propofol: a comparison with the standard propofol emulsion.

UNLABELLED: Using a randomized, double-blind protocol design, we compared a new lower-lipid emulsion of propofol (Ampofol) containing propofol 1%, soybean oil 5%, and egg lecithin 0.6% with the most commonly used formulation of propofol (Diprivan) with respect to onset of action and recovery profiles, as well as intraoperative efficacy, when administered for induction and maintenance of general anesthesia as part of a "balanced" anesthetic technique in 63 healthy outpatients. Anesthesia was induced with sufentanil 0.1 microg/kg (or fentanyl 1 microg/kg) and propofol 2 mg/kg IV and maintained with a variable-rate propofol infusion, 120-200 microg x kg(-1) x min(-1). Onset times to loss of the eyelash reflex and dropping a syringe were recorded. Severity of pain on injection, speed of induction, intraoperative hemodynamic variables, and electroencephalographic bispectral index values were assessed. Recovery times to opening eyes and orientation were noted. The results demonstrated that there were no significant differences between Ampofol and Diprivan with respect to onset times, speed of induction, anesthetic dose requirements, bispectral index values, hemodynamic variables, recovery variables, or patient satisfaction. However, the incidence of pain on injection was more frequent in the Ampofol group (26% versus 6%, P < 0.05). We conclude that Ampofol is equipotent to Diprivan with respect to its anesthetic properties but was associated with a more frequent incidence of mild pain on injection. IMPLICATIONS: The pharmacodynamic profile of a lower-lipid containing emulsion of propofol (Ampofol) was compared with Diprivan when administered for induction and maintenance of general anesthesia. This preliminary study demonstrated that the two formulations of propofol were equivalent with respect to their induction and maintenance properties. However, Ampofol was associated with a more frequent incidence of pain on injection.

Adult↗

[Riems foot-and-mouth disease oil emulsion vaccines for swine. 2. Use of foot-and-mouth 2-component oil emulsion vaccines in practice].

Riems FMD two-component oil emulsion vaccine was subcutaneously applied (5 ml) under field conditions to 855 store pigs of different age groups (trivalent--O1, A5, C). It produced early onset of lasting strong immunity against the three above FMD virus types. General condition of the animals and their body weight development were not adversely affected. Pea-size to walnut-size vaccination granulomas were recorded on slaughter as locally delimited reactions in 15 to 20 percent of vaccinated animals and were found to be morphologically correlated to adjuvant action. They were easily removed from the carcasses by excision of the vaccination point, with only minor loss of slaughter substance.

Adjuvants, Immunologic↗