Preparation and evaluation of non-effervescent gastroretentive tablets containing pregabalin for once-daily administration and dose proportional pharmacokinetics

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Graphical abstractThe main purpose of this study was to develop gastroretentive tablets with floating and swelling properties for once-daily administration of pregabalin. The non-effervescent floating and swelling tablets were prepared using wet granulation and compaction, which are widely used and easily accessible. All formulations showed sustained release patterns and maintained buoyancy for over 24 h. The amount of hydroxypropyl methylcellulose and crospovidone were found to be critical factors affecting in vitro dissolution and floating properties of the prepared tablets. The optimized tablets containing 300 mg of pregabalin started to float within 3 min and swelled above 12.8 mm, the reported pyloric sphincter diameter during the fed state, in all dimensions including length, width, and thickness. In vivo results in beagle dogs indicated that the optimized formulations are suitable as once-daily dosage forms, and dose proportionality was observed in doses ranging from 75 to 300 mg. Additionally, the dogs administered with the formulation having poor in vitro gastroretentive properties showed highly variable and reduced extent of absorption, signifying the necessity of the gastroretentive drug delivery system. In conclusion, the developed non-effervescent floating tablets are promising candidates for once-daily delivery of pregabalin.

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