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Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone

College of Pharmacy, Chung-Ang University, Seoul 06974, Korea
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These authors contributed equally to this work.
Pharmaceutics 2019, 11(6), 271; https://doi.org/10.3390/pharmaceutics11060271
Received: 25 April 2019 / Revised: 27 May 2019 / Accepted: 3 June 2019 / Published: 10 June 2019
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Abstract

In this study, we aimed to design a highly swellable and mechanically robust matrix tablet (SMT) as a gastroretentive drug-delivery system (GRDDS) capable of improving the dissolution behavior of β-lapachone with low aqueous solubility. For the preparation of SMTs, the cogrinding technique and freeze–thaw method were used to disperse β-lapachone in SMTs in an amorphous state and to enhance the swelling and mechanical properties of SMTs, respectively. As a result, the crystallinity of coground β-lapachone incorporated in the SMTs was found to be considerably decreased; thereby, the dissolution rates of the drug in a simulated gastric fluid could be substantially increased. The SMTs of β-lapachone also demonstrated significantly enhanced swelling and mechanical properties compared to those of a marketed product. The reason for this might be because the physically crosslinked polymeric networks with a porous structure that were formed in SMTs through the freeze–thaw method. In addition, β-lapachone was gradually released from the SMTs in 6 h. Therefore, SMTs of β-lapachone developed in this study could be used as GRDDS with appropriate swelling and mechanical properties for improving the dissolution behavior of hydrophobic drugs such as β-lapachone. View Full-Text
Keywords: swelling gastroretentive system; cogrinding technique; freeze–thawing method; β-lapachone; dissolution behavior; mechanical strength swelling gastroretentive system; cogrinding technique; freeze–thawing method; β-lapachone; dissolution behavior; mechanical strength
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Kim, H.; Lee, C.-L.; Lee, S.; Lee, T.J.; Haleem, I.; Lee, Y.; Hwang, N.J.; Shim, K.; Kim, D.; Lee, J. Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone. Pharmaceutics 2019, 11, 271.

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