Application of Carbopol/PVP interpolymer complex to prepare mucoadhesive floating granule

摘要

Novel mucoadhesive floating granule was prepared using Carbopol/PVP interpolymer complex to deliver hydrophilic drugs in a controlled manner. Acetaminophen was used as a model drug. Maximum floatability of the granules was obtained at the ratio of 1/1, where 95 % of the granules floated for 12 h. As the concentration of sodium bicarbonate increased, both the floating duration and the release rate of the drug increased. The granules without sodium bicarbonate floated only for 2 h and floating onset time was 15 min. The release rate of drug gradually increased as the drug content in the granule increased. As the drug content in the granules increased, duration of adhesion decreased. However, the decrease in adhesion duration was minimal up to 40 % of drug content. The release rate from the granules prepared by dry granulation method was faster than that by wet granulation. The granules prepared by dry granulation method led to formation of highly porous structure; whereas, that by wet granulation method showed non-porous structure. The optimum size of the granules to retard the release of the model drug was within the range of 3-4 mm. Based on both mucoadhesive and buoyant properties, the floating granules are expected to reside in the upper part of the stomach for sufficient period of time and release the drug in a sustained manner.