Add time:09/27/2019         Source:sciencedirect.com

The objective of this study was to develop the dextromethorphan hydrobromide sustained-release (DMB-SR) tablets using floating technique to prolong the gastric residence time and compared their pharmacokinetic behavior with conventional sustained release tablets. DMB-SR floating tablets were prepared employing hydroxypropyl methylcellulose (HPMC) as hydrophilic gel material, sodium bicarbonate as gas-generating agent and hexadecanol as floating assistant agent. An orthogonal experiment design method was used to select the optimized formulation. The floating tablets were evaluated for uniformity of weight, hardness, friability, drug content, floating characteristics, in vitro release and in vivo bioavailability. The optimized tablets were prepared with HPMC K4M 25 mg, sodium bicarbonate 20 mg and hexadecanol 18 mg. The prepared tablets could float within 3 min and maintain for more than 24 h. The data of physical parameters were all lie within the limits. Drug release at 12 h was more than 85%. The comparative pharmacokinetic study was performed by administration of the DMB-SR floating tablets and conventional DMB-SR tablets. The area under curve of plasma concentration–time (AUC) of floating tablets was slightly higher than that of reference tablets, Tmax was prolonged apparently. The results showed the floating tablets are a feasible approach for the sustained-release preparation of drugs, which have limited absorption sites in the stomach.

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