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.
Highlights
Unpleasant taste mainly bitterness had lead to dilemma for modern pharmaceutical science
Ofloxacin-Ion exchange resin complexation involves the exchange of ionizable drug and metal ions in resin, which in turn depends on the pKa of drug and resin
A maximum of 95.51 ± 1.42% w/w and 94.15 ± 2.08 % w/w drug loading was obtained for Tulsion 335 and Indion 204 respectively at pH 6
Summary
Unpleasant taste mainly bitterness had lead to dilemma for modern pharmaceutical science. Methods of taste masking employ pH sensitive polymers like Eudragit E 100 (aminoalkylmethacrylate copolymers) (Shishu, Kapoor, Kamalpreet, 2009), polyacrylic acid ion exchange resin Indion 204, Indion 214, Indion 234, Indion CRP 244 and CRP 254, Tulsion 335, Amberlite IRP64 (Cation exchange resins) (Venkatesh, Jha, Karki, 2009; Mundada et al, 2008; Avari, Bhalekar, 2008; Pisal et al, 2004; Manek, Kamat, 1981; Tawakkul, 2009; Amin et al, 2005; Leonard, Cooper, 1998; Metcalf, Purdy, 2001). Amberlite IRP69 was evaluated for taste masking, improvement of physicochemical properties of actives and subsequently formed resinate for sustaining the drug release (Khan et al, 2007; Junyaprasert, Manwiwattanakul, 2008). Taste masking of oral pharmaceuticals has become potential tool to improve patient compliance and commercial success of product (Nanda, Kandarapu, Garg, 2008; Wagh, Ghadlinge, 2009; Hiremath, Shastry, Shrinath, 2004)
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