Determinação do perfil farmacocinético do cetorolaco de trometamina comprimido de 30mg administrado por via sublingual em voluntários saudáveis

• Ano de defesa: 2011
• Autor(a) principal: Costa, Cléber Soares Pimenta
• Tipo de documento: Dissertação
• Tipo de acesso: Acesso aberto
• Idioma: por
• Palavras-chave em Português: Cetorolaco; Farmacocinética
• Link de acesso: http://www.repositorio.ufc.br/handle/riufc/2274

Ketorolac tromethamine (ketorolac) is a non-steroidal anti-inflammatory drug (NSAID) used in the treatment of pain. The use of a sublingual analgesic has several advantages such as increased bioavailability and ease of administration, especially in patients who have difficulty swallowing. Thus, the aim of this study was to evaluate the pharmacokinetic profile of a formulation of ketorolac in Brazilian male volunteers. This was an open, non-randomized, 01 period, 01 treatment, single dose under fasting conditions study where was administered 30 mg sublingual tablet formulation of ketorolac. Healthy Brazilians male were eligible for inclusion. After an overnight fast, subjects received a single sublingual dose of the formulation. Plasma samples were obtained over a 24-hour period after administration. Plasma ketorolac concentrations were analyzed by High Performance Liquid Chromatography coupled Mass Spectrometry for analysis of pharmacokinetic properties, including Cmax, AUC0-24, and AUC0-∞. Tolerability was assessed by vital sign monitoring, laboratory analysis results, anamnesis and physical examination. A total of 14 male subjects were enrolled and completed the study. The pharmacokinetics parameters values (mean ± standard deviation, except median for time to Tmax) calculated for formulation were as follows: AUC0-∞ (9682 ± 1908 ng*h/mL); AUC0-24 (9346 ± 1789 ng*h/mL); Cmax (2605 ± 465 ng/mL); Tmax (0,58 ± 0,22 h); t1/2 (5,76 ± 0,69 h) and Ke (0,12 ± 0,02 1/h). The ketorolac formulation was well tolerated at the administered dose and no adverse reactions were observed. The advantage of the use of the sublingual formulation of ketorolac is its practical administration. It can be the treatment of choice for moderate and severe pain, especially in patients where parenteral route is undesirable or impracticable, or those who have difficulty of swallowing. The methods were successfully applied, it is possible to analyze the pharmacokinetic parameters and assess the safety of the tablet formulation of 30 mg of ketorolac tromethamine administered sublingually in healthy volunteers.