RESUMO
In the past, the administration of medicines for children mainly involved changes to adult dosage forms, such as crushing tablets or opening capsules. However, these methods often led to inconsistent dosing, resulting in under- or overdosing. To address this problem and promote adherence, numerous initiatives, and regulatory frameworks have been developed to develop more child-friendly dosage forms. In recent years, multiparticulate dosage forms such as mini-tablets, pellets, and granules have gained popularity. However, a major challenge that persists is effectively masking the bitter taste of drugs in such formulations. This review therefore provides a brief overview of the current state of the art in taste masking techniques, with a particular focus on taste masking by film coating. Methods for evaluating the effectiveness of taste masking are also discussed and commented on. Another important issue that arises frequently in this area is achieving sufficient dissolution of poorly water-soluble drugs. Since the simultaneous combination of sufficient dissolution and taste masking is particularly challenging, the second objective of this review is to provide a critical summary of studies dealing with multiparticulate formulations that are tackling both of these issues.
Assuntos
Composição de Medicamentos , Solubilidade , Paladar , Humanos , Composição de Medicamentos/métodos , Preparações Farmacêuticas/química , Preparações Farmacêuticas/administração & dosagem , Formas de Dosagem , Química Farmacêutica/métodos , Comprimidos , Administração Oral , Criança , Excipientes/química , Liberação Controlada de FármacosRESUMO
Paediatric practice requires various dosing forms that are acceptable for children of different ages and abilities. A straw prefilled with a drug formulation might serve as a dosing form, especially for children and patients with swallowing difficulties. Using a two-step procedure, we developed granulated coated particles of bitter tasting paracetamol that are appropriate for use in a newly developed straw with two valves to assure liquid flow towards the oral cavity. The paracetamol crystals were coated with five different polymers (water-soluble, entero-soluble) to assure the duration of the taste-masking properties for several minutes during sipping of the drug. As none of these polymer coats assured small enough liquid volumes needed to empty the straw (20 mL) or low enough vacuum for easy drug consumption (130 mbar), the coated crystals were granulated with trehalose-erythritol powder mixture. Acceptable results were obtained with these granulated coated paracetamol particles when polyvinyl alcohol/polyethylene glycol graft copolymer (Kollicoat IR) or a mixture of this polymer with polyvinyl alcohol (Kollicoat Protect) were used. Dissolution tests in water and acidic media confirmed the taste-masking functionality of these particles during drinking simulation and immediate release of paracetamol in the stomach (85% in <30 min at pH 1.2, 4.5).