Pharmacodynamic Evaluation and Physical/Chemical Analysis of Two Formulations of Propofol used in Target-Controlled Infusion

• Published in: Brazilian journal of anesthesiology (Elsevier) Vol. 63; no. 1; pp. 59 - 65
• Main Authors: Simoni, Ricardo Francisco, Miziara, Luiz Eduardo de Paula Gomes, Esteves, Luis Otávio, D’Castro, João Gilberto Ribeiro, Morales, Carlos Alberto, Sandrin, Carlos Eduardo Esqueapatti, Contente, Thaís Costa, Oliveira-Silva, Diogo
• Format: Journal Article
• Language: English
• Published: Brazil Elsevier Editora Ltda 01.01.2013; Elsevier
• Subjects: Adult; Anesthesia; Anesthetics, Intravenous - administration & dosage; Anesthetics, Intravenous - pharmacokinetics; Chemical Phenomena; Chemistry, Pharmaceutical; Clinical; Consciousness Monitors; Double-Blind Method; Humans; Infusions, Intravenous - methods; Intravenous; Male; Pharmacology; Propofol; Propofol - administration & dosage; Propofol - pharmacokinetics; Clinical; Anesthesia; Pharmacology; Propofol; Intravenous; Consciousness Monitors
• ISSN: 0104-0014; 0104-0014
• DOI: 10.1016/j.bjane.2012.03.003

There are several formulations of propofol available to the anesthesiologist for clinical use. The aim of this study was to analyze the physicochemical properties, pharmacodynamic effect, and pharmaceutical and clinical equivalence of the reference drug propofol as well as a similar formulation. Sixteen volunteers were enrolled in this randomized, double-blind, and paired study of Diprivan® and Propovan® formulations. Formulations were given as target-controlled infusion with target concentration of 3.0μg.mL-1 for 15minutes. Variables studied were the area under the curve (AUC) of the bispectral index (BIS) graph regarding time, minimum BIS reached and time to reach it, and recovery time. The two formulations were sent to analysis of particle size of lipid emulsion, surface potential, and active principle quantification. There was no difference between the formulations when comparing AUC, minimum BIS reached and time to reach it. The similar formulation recovery time was lower compared to the reference formulation (eight and 10min, respectively, p = 0.014). Mean particle size of lipid emulsion, surface potential, and active ingredient quantification were similar for both formulations. There was no clinically significant difference between the use of propofol, reference Diprivan®, and the similar Propovan® during infusion. However, the recovery time was longer with the reference drug. Although analysis of both formulations studied show similar results regarding its physicochemical characterization, further studies should be conducted to justify this difference.