Avaliação farmacodinâmica e análise físico-química de duas formulações de propofol usadas em infusão alvo-controlada

Ricardo Francisco Simoni; Luiz Eduardo de Paula Gomes Miziara; Luis Otávio Esteves; João Gilberto Ribeiro D; Carlos Alberto Morales Jr; Carlos Eduardo Esqueapatti Sandrin; Thaís Costa Contente; Diogo Oliveira-Silva

doi:10.1590/S0034-70942013000100005

Scientific Article

Avaliação farmacodinâmica e análise físico-química de duas formulações de propofol usadas em infusão alvo-controlada

Pharmacodynamic evaluation and physical/chemical analysis of two formulations of propofol used in target-controlled infusion

Ricardo Francisco Simoni; Luiz Eduardo de Paula Gomes Miziara; Luis Otávio Esteves; João Gilberto Ribeiro D'Castro; Carlos Alberto Morales Jr; Carlos Eduardo Esqueapatti Sandrin; Thaís Costa Contente; Diogo Oliveira-Silva

http://dx.doi.org/10.1590/S0034-70942013000100005 Braz J Anesthesiol, vol.63, n1, p.66-72, 2013

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Resumo

JUSTIFICATIVA E OBJETIVOS: Existem várias formulações de propofol para uso clínico à disposição do anestesiologista. O objetivo desse estudo foi analisar as propriedades físico-químicas, o efeito farmacodinâmico e a equivalência farmacêutica e clínica do fármaco referência de propofol e uma formulação similar. MÉTODOS: Dezesseis voluntários participaram desse estudo aleatório, duplamente encoberto e pareado entre as formulações Diprivan® e Propovan®. As formulações foram administradas em regime de infusão alvo-controlada com concentração-alvo de 3,0 µg.mL-1 por 15 minutos. As variáveis estudadas foram a área sob a curva (ASC) do gráfico do índice bispectral (BIS) em relação ao tempo, o BIS mínimo atingido e o tempo para tal e o tempo de recuperação. As duas formulações foram submetidas às análises de tamanho de partículas da emulsão lipídica, potencial de superfície e quantificação de princípio ativo. RESULTADOS: Não houve diferença entre as formulações quando se comparou a ASC, BIS mínimo atingido e o tempo decorrido para tal. O tempo de recuperação com a formulação similar foi menor em relação à referência (oito e 10 min, respectivamente, p = 0,014). O tamanho médio de partículas da emulsão lipídica, potencial de superfície e a quantificação de princípio ativo foram semelhantes nas duas formulações. CONCLUSÃO: Não houve diferença clínica significativa entre o uso de propofol referência Diprivan® e seu similar Propovan® durante a infusão. Entretanto, o tempo de recuperação foi mais prolongado com o fármaco referência. Embora as análises com as duas formulações estudadas mostrarem resultados semelhantes quanto a sua caracterização físico-química, outros estudos devem ser realizados para justificar tal diferença.

Palavras-chave

ANESTÉSICOS, Venoso, propofol, FARMACOLOGIA, MONITORAÇÃO, Índice Bispectral, TÉCNICAS ANESTÉSICAS, Geral, Venosa

Abstract

BACKGROUND AND OBJECTIVES: 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. METHOD: 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 3.0 μg.mL-1 for 15 minutes. 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. RESULTS: 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 10 min, respectively, p = 0.014). Mean particle size of lipid emulsion, surface potential, and active ingredient quantification were similar for both formulations. CONCLUSION: 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.

Keywords

Anesthesia, Intravenous, Consciousness Monitors, Pharmacology, Clinical, Propofol

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Avaliação farmacodinâmica e análise físico-química de duas formulações de propofol usadas em infusão alvo-controlada

Pharmacodynamic evaluation and physical/chemical analysis of two formulations of propofol used in target-controlled infusion

Ricardo Francisco Simoni; Luiz Eduardo de Paula Gomes Miziara; Luis Otávio Esteves; João Gilberto Ribeiro D'Castro; Carlos Alberto Morales Jr; Carlos Eduardo Esqueapatti Sandrin; Thaís Costa Contente; Diogo Oliveira-Silva

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