Design and development of oro dispersible paediatric formulations of oseltamivir phosphate and meloxicam

Abstract

Present research worked was aimed at developing age appropriate dosage forms for paediatric and geriatric patients who often find it difficult to swallow the conventional solid dosage forms. Thus, present research was an attempt to mask the bitter taste and develop child friendly dosage forms like ODF and ODMT of oseltamivir phosphate (OST) and meloxicam (MX) for paediatric use. newlineOST is an antiviral drug used for treating influenza infection belongs to the class of neuraminidase inhibitors. newlineMX is a non-steroidal anti-inflammatory drug. It is a selective COX-2 inhibitor used in control of joint inflammation in patients with all forms of juvenile arthritis. newlineTaste masking for OST and MX was achieved by complexation with Kleptose Linecaps® (MLD), a novel maltodextrin polymer which is specifically used for masking the bitter taste of drugs. Mechanism by which MLD achieves the taste masking was extensively studied by running molecular dynamics studies (MD) using Schrodinger® Material Suite. newlineThe prepared complexes were characterised by FTIR, DSC, PXRD, HSM, SEM, 1H-NMR and 13C- NMR which confirmed the successful encapsulation of the drugs in the cavity of MLD. newlineTaste masked ODMT for OST and MX were prepared by direct compression method and optimised. In D-optimal mixture design, effect of formulation parameters like concentration of directly compressible excipients like Pharmaburst®, DCL 11 and Avicel PH 102 and their effect on hardness and friability was evaluated. newlineODF for OST and MX were formulated by solvent casting method and optimises for effect of polymer concentration and plasticizers on the mechanical properties of ODFs. Optimised ODFs were found be palatable and depicted fast disintegration times resulting in better efficacy. newlineIn vivo pharmacokinetic studies of MX ODMT and ODF formulated with ternary complexes of MX with MGL and MLD showed faster absorption and depicted 2 times enhancement in Cmax and Tmax when compared with marketed tablet formulation of MX. newline newline