RESUMEN
OBJECTIVES: The pharmacokinetics of commercial and liposome-encapsulated mepivacaine (MVC) injected intra-orally in healthy volunteers was studied. METHODS: In this double blind, randomized cross-over study, 15 volunteers received, at four different sessions, 1.8 ml of the following formulations: 2% MVC with 1 : 100 000 epinephrine (MVC(2%EPI) ), 3% MVC (MVC(3%) ), 2% and 3% liposome-encapsulated MVC (MVC(2%LUV) and MVC(3%LUV) ). Blood samples were collected pre dose (0 min) and at 15, 30, 45, 60, 90, 120, 180, 240, 300, 360 min after injections. Liquid chromatography-tandem mass spectrometry was used to quantify plasma MVC concentrations. RESULTS: Pharmacokinetic analysis showed that the maximum plasma concentration (Cmax) and the areas under the curves (AUC(0-360) and AUC(0-∞)) after MVC(2%LUV) and MVC(2%EPI) injections were smaller (P < 0.05) than the equivalent figures for MVC(3%) and MVC(3%LUV). The time to maximum plasma concentration (Tmax) and the half-life of elimination (t½beta) obtained after the treatment with MVC(2%LUV), MVC(2%EPI), MVC(3%) and MVC(3%LUV) presented no statistically significant differences (P > 0.05). Cmax, AUC(0-360) and AUC(0-∞) after injection of the 2% formulations (MVC(2%LUV) and MVC(2%EPI) ) did not exhibit statistically significant differences (P > 0.05). The pharmacokinetics of MVC(2%LUV) were comparable to the pharmacokinetics of MVC(2%EPI). CONCLUSION: The liposomal formulation of 2% MVC exhibits similar systemic absorption to the local anesthetic with vasoconstrictor.
Asunto(s)
Anestésicos Locales/farmacocinética , Liposomas/farmacocinética , Mepivacaína/farmacocinética , Administración Oral , Adulto , Análisis de Varianza , Anestésicos Locales/administración & dosificación , Área Bajo la Curva , Disponibilidad Biológica , Cromatografía Líquida de Alta Presión/métodos , Estudios Cruzados , Preparaciones de Acción Retardada/administración & dosificación , Preparaciones de Acción Retardada/farmacocinética , Método Doble Ciego , Epinefrina/administración & dosificación , Epinefrina/farmacocinética , Femenino , Semivida , Humanos , Inyecciones , Liposomas/administración & dosificación , Masculino , Mepivacaína/administración & dosificación , Persona de Mediana Edad , Vasoconstrictores/administración & dosificación , Vasoconstrictores/farmacocinética , Adulto JovenRESUMEN
The pharmacokinetics and the local toxicity of commercial and liposome-encapsulated mepivacaine formulations injected intra-orally in rats were studied. Animals were divided in groups (n = 4-6) and treated with 0.1 mL of the formulations: 2% mepivacaine with 1:100,000 epinephrine (MVC(2%EPI)), 3% mepivacaine (MVC(3%)), and 2% liposome-encapsulated mepivacaine (MVC(LUV)). The results showed that the 2% liposome-encapsulated mepivacaine reduced C(max), prolonged AUC(0-infinity) and t(1/2) compared with 3% plain and 2% vasoconstritor-associated mepivacaine, after intraoral injection. In addition, it was also observed that liposomal mepivacaine might protect the tissue against local inflammation evoked by plain or vasoconstrictors-associated mepivacaine, giving supporting evidence for its safety and possible clinical use in dentistry.
Asunto(s)
Anestésicos Locales/farmacocinética , Epinefrina/farmacocinética , Liposomas/administración & dosificación , Mepivacaína/farmacocinética , Anestésicos Locales/administración & dosificación , Animales , Química Farmacéutica , Técnicas de Laboratorio Clínico , Formas de Dosificación , Sistemas de Liberación de Medicamentos , Epinefrina/administración & dosificación , Membrana Dobles de Lípidos , Masculino , Bloqueo Nervioso/métodos , Ratas , Ratas Wistar , Investigación , SolucionesRESUMEN
En una población pediátrica de 20 niños se evalúa el comportamiento cinético y dinámico dela lidocaína y mepivacaína asociados con adrenalina, con referencia específica al período de latencia, profundidad y duración del efecto anestésico