Bioavailability of an extemporaneous suspension of propafenone made from tablets.
Propafenone is an effective antiarrhythmic agent used in children, while in Mexico no specific formulation for children is available, which causes errors in adequate dosage. The aim of this study was to determine the bioavailability of a suspension prepared extemporaneously using commercial tablets of propafenone. The bioavailability was determined in two groups of rabbits (n = 8): the first group received a single intravenous dose of 2 mg/kg of propafenone; the second was orally administered an extemporaneous suspension of propafenone prepared from commercial tablets. Blood samples were drawn at several times during the next 24 h and analysed by HPLC to determine drug levels. The extemporaneous suspension was tested previously with satisfactory results regarding physicochemical and microbiologic stability. The area under the curve (AUC) for the i.v. route was 5600.6 ng/ml.h and for oral administration the AUC was 3327.6 ng/ml.h. The bioavailability was calculated at 59.41%. These results are consistent with previous reports for solid dosage forms. The propafenone suspension prepared extemporaneously using commercial tablets is bioavailable using an animal model; nevertheless, it is necessary to carry out human studies either in volunteers or in patients to confirm these results.
Olguín
Hugo Juárez
HJ
Laboratorio de Farmacología, Instituto Nacional de Pediatría (INP), México, Colonia Cuicuilco, Mexico City.
Pérez
Carmen Flores
CF
Pérez
Janett Flores
JF
Mendiola
Blanca Ramírez
BR
Portugal
Miriam Carrasco
MC
Chávez
Jesús Bobadilla
JB
D000284:Administration, Oral; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D004355:Drug Stability; D007275:Injections, Intravenous; D008297:Male; D011405:Propafenone / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D011817:Rabbits; D013535:Suspensions; D013607:Tablets
D000889:Anti-Arrhythmia Agents; D013535:Suspensions; D013607:Tablets; D011405:Propafenone