Development and evaluation of ofloxacin orally disintegrating tablets

Abstract

Bitter taste of ofloxacin, a broad spectrum bactericidal agent, is masked and orally disintegrating tablets were formulated. The bitter taste is masked by forming complex between drug and weak cation exchange resins, Tulsion 335 and Indion 204. Effect of pH and drug:resin ratio on the drug loading was studied. Maximum drug loading was observed at pH 6. Ratio of 1:2 of drug:resin masked almost complete bitterness of ofloxacin. Formation of complexes was confirmed by IR spectroscopy. Physical characterization of taste masked complexes was carried out. Present work envisages the taste masking of ofloxacin and development of orally disintegrating tablets. The effect of pH and resin quantities on drug loading were studied to find the optimum conditions of drug loading for complete taste masking. Effect of superdisintegrants like sodium starch glycolate, croscarmellose sodium and polyplasdone XL at varying level on physical parameters of compressed tablets was also assessed. The formulations containing 5 % w/w polyplasdone XL showed about 90 % of drug release within 5 minutes. No significant differences were observed in the physical parameters of resinates as well as tablets prepared from Tulsion 335 and Indion 204. O gosto amargo de ofloxacina, agente bactericida de largo espectro, é mascarado e formularam-se comprimidos dispersíveis. O sabor amargo é mascarado pela formação de complexo entre o fármaco e resinas de troca catiônica fraca, Tulsion 335 e Indion 204. Efeito do pH e da proporção fármaco: resina sobre a carga de fármaco foi estudada. Carga de fármaco máxima foi observada em pH 6. Proporção 1:2 do fármaco: resina mascarou quase completamente o gosto amargo de ofloxacina. A formação de complexos foi confirmada por espectroscopia no IV. Caracterização física dos complexos de sabor mascarado foi realizada. O presente trabalho preconiza o mascaramento do gosto de ofloxacina e desenvolvimento decomprimidos por via oral, se desintegrando. O efeito do pH e da resina quantidades de carga de fármaco foram estudadas paraencontrar as condições óptimas de carga de fármaco para dissimulação do saborcompleto. Efeito da superdisintegrants como amido glicolato de sódio, croscarmelose sódica e Polyplasdone XL em diferentes níveis de parâmetros físicos de comprimidos também avaliados foi avaliada. As formulações contendo 5 %w/w Polyplasdone XL mostraram cerca de 90% de libertação do fármaco no prazo de 5 minutos. Não foram observadas diferenças significativas nos parâmetros físicos de resinatosbem como comprimidos preparados a partir de Tulsion 335 e Indion 204.

Improved therapeutic potential of tapentadol employing cationic exchange resins as carriers in neuropathic pain: evidence from pharmacokinetic and pharmacodynamics study

“…However, further increase in pH (pH 12.0) had reduced drug loading due to reduced selectivity coefficient of amine drug (TAP) towards resin 24 , 30 . While strong affinity of H + ions for binding to the –COO − group of resin compared to drug contributed to lower drug loading at lower pH 25 .…”

“…Thus, the adsorption-desorption features of KyronT-134 and Tulsion335 can be utilized in development of DRCs of pharmaceutical importance. Further DRCs can be dispensed in a variety of dosage forms like powder, chewing gums, suspension, conventional tablets or capsules 25 – 28 . Extended release resinates can maintain steady plasma drug levels, reduce frequency of multiple dosing, allows dose adjustment according to patient need and enhance adherence of patients to therapy 18 , 20 .…”