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Open AccessArticle

Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach

College of Pharmacy, Dongguk University-Seoul, Gyeonggi 10326, Korea
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Pharmaceutics 2018, 10(3), 161; https://doi.org/10.3390/pharmaceutics10030161
Received: 2 August 2018 / Revised: 8 September 2018 / Accepted: 12 September 2018 / Published: 17 September 2018
(This article belongs to the Special Issue New Approaches to Enhance Drug Solubility and Bioavailability)
To develop sustained release gastro-retentive effervescent floating tablets (EFT), a quality-based experimental design approach was utilized during the composing of a hydrophilic matrix loaded with a high amount of a highly water-soluble model drug, metformin HCl. Effects of the amount of polyethylene oxide WSR 303 (PEO), sodium bicarbonate, and tablet compression force were used as independent variables. Various times required to release the drug, tablet tensile strength, floating lag time, tablet ejection force, and tablet porosity, were selected as the responses. Polymer screening showed that PEO had the highest gel strength among the various tested polymers. Sodium bicarbonate had the most significant effect on the release rate and floating lag time by retarding the rate from the hydrophilic matrices, whilst tablet compression force and PEO exerted the greatest influence on tablet properties (p < 0.0001). The design space was built in accordance with the drug release profiles, tensile strength, and floating lag time, following failure probability analysis using Monte Carlo simulations. The kinetic modeling revealed that the release mechanism was best described by the Korsmeyer-Peppas model. Overall, the current study provided a perspective on the systematic approach of gastro-retentive EFT, loaded with highly water-soluble drugs by applying quality by design concepts. View Full-Text
Keywords: polyethylene oxide; sodium bicarbonate; gel strength; floating lag time; drug release kinetics; experimental design polyethylene oxide; sodium bicarbonate; gel strength; floating lag time; drug release kinetics; experimental design
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MDPI and ACS Style

Thapa, P.; Jeong, S.H. Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach. Pharmaceutics 2018, 10, 161. https://doi.org/10.3390/pharmaceutics10030161

AMA Style

Thapa P, Jeong SH. Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach. Pharmaceutics. 2018; 10(3):161. https://doi.org/10.3390/pharmaceutics10030161

Chicago/Turabian Style

Thapa, Prakash; Jeong, Seong H. 2018. "Effects of Formulation and Process Variables on Gastroretentive Floating Tablets with A High-Dose Soluble Drug and Experimental Design Approach" Pharmaceutics 10, no. 3: 161. https://doi.org/10.3390/pharmaceutics10030161

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