IQUIR   05412
INSTITUTO DE QUIMICA ROSARIO
Unidad Ejecutora - UE
congresos y reuniones científicas
Título:
Development of Praziquantel Oral Liquid Formulations for Treatment of Pediatric Patients
Autor/es:
LAURA CARRAU; NELSON G. STÜRTZ; PATRICIA M. CASTELLANO
Lugar:
Rosario
Reunión:
Congreso; 4 Reunión Internacional de Ciencias Farmacéuticas; 2016
Resumen:
Praziquantel (PZQ) is the active ingredient used to treat infections caused by Taenia saginata, T. solium, Hymenolepis nana, Diphyllobothrium latum, Schistosoma mansoni, S. haematobium and S. japonicum. It has been included in the WHO Model List of Essential Medicines for Children 5th edition, as Intestinal anthelminthic and as Antischistosomal. PZQ, which has no structural relationship with other anthelmintics, kills adults alike worms and larvae. It has very low solubility in water and unpalatable. The aim of this work is to develop a liquid formulation of PZQ that meets the requirements of acceptability for the treatment of pediatric patients. This involves improving the taste and swallowability. We sought to minimize the ethanol content in the formulation to suit the legislation and minimize the content of propylene glycol to enhance palatability. Seven formulations were prepared with different proportions of the excipients: Propylene Glycol, ethanolic hydrochloric acid solution (100 ml absolute ethanol, 100 ml; HCl 0,1N, 6,5 ml), water preserved (metilparaben, 0,03 %; propilparaben, 0,07 %), saccharin and orange essence. Different conditions were tested in the formulation process: orderof addition of reagents, temperature andstirring rate. PZQ content was quantified by high performance liquid chromatography.A Chromatographic system Agilent 1200 was used to perform the quantification. The chromatographic conditions were:mobile phase, Acetonitrilo-Agua (6:4); column, C18 250 x 4.60 mm 10µ 100 A; flow, 1,5 ml/min; wavelength, 210 nm, injection volume, 10 µl. The validated parameters for the API were: linearity, LOD, LOQ and precision. The system with concentrations of excipients permitted for pediatric use in which the active ingredient was completely dissolved was selected. Therefore, the selected formulation was: Propylene Glycol, 89,5 %; ethanolic hydrochloric acid solution, 1,5 %; water preserved, 9 %; saccharin and orange essence. A formulation suitable for pediatric administration was successfully achieved, with a concentration of 40 mg/ml of PZQ.