Abstract
The present study was aimed to develop gastric floating in-situ gels of meloxicam (MLX) mainly to enhance anti-inflammatory activity and alleviate gastric ulceration potential of meloxicam. Ternary inclusion complex of meloxicam containing hydroxyl propyl beta cyclodextrin (HPβCD) and diethylamine (DEA) in 1:1:1 molar ratio was used as chief component in the development of gastric floating in-situ gel formulations of meloxicam. Box-Behnken design was utilized to design and optimize gastric floating in-situ gels of meloxicam. Independent variables (concentrations of sodium alginate, calcium carbonate, and ternary inclusion complex of meloxicam respectively) were optimized in order to achieve the desired responses. The response surface plots and the possible interactions between the independent variables were analyzed using the Design Expert Software 11.0.3.0 (Stat-Ease, Inc, USA). The results showed that the optimized gastric floating in-situ gels with short floating lag time (41 seconds), low viscosity (190 cps), and high in-vitro drug release at 6th hour (77%) was obtained using an optimized combination of calcium carbonate (0.75%w/v), sodium alginate (1.25%w/v) and MLX-HPβCD-DEA ternary complex (equivalent to 11.25mg of meloxicam), respectively. Moreover, the optimized gastric floating in-situ gel formulation of meloxicam ternary complex exhibited significantly ameliorated anti-inflammatory activity (84.38 % (p
Highlights
Oral liquids offer several advantages over other oral pharmaceutical formulations such as tablets, capsules, and pills but they often suffer from abrupt gastrointestinal transit
The results showed that the optimized gastric floating in-situ gels with a short floating lag time (41 seconds), low viscosity (190 cps), and high in vitro drug release at sixth hour (77%) was obtained using an optimized combination of calcium carbonate (0.75% w/v), sodium alginate (1.25% w/v), and MLX-HPβCD-DEA ternary complex, respectively
Meloxicam is purchased from the UFC Biotechnology New York (USA), Sodium alginate and calcium carbonate were purchased from the Research Lab Fine Chemicals, Mumbai (India), while other ingredients used were of analytical research grade
Summary
Oral liquids offer several advantages over other oral pharmaceutical formulations such as tablets, capsules, and pills but they often suffer from abrupt gastrointestinal transit. This could be a serious concern for the majority of drugs, weakly acidic drugs as they are absorbed from the stomach and/or upper part of the small intestine (El-Kamel et al, 2001; Rouge et al, 1996). The gastric retention of oral solutions containing these drugs could be favorably achieved through a radical approach of the liquid insitu gelling system Except our past work (Jafar et al, 2017), there is a lack of major evidences in the literature about the meloxicam ternary complex (prepared using cyclodextrins and alkali substance combination) incorporated gastric floating in-situ gels, even though this has been considered to be very beneficial from the therapeutic point of view
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