• Journal of the Korea Academia-Industrial cooperation Society
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• v.16 no.11
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• pp.7549-7554
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• 2015

The aim of this study was to develop gastric retentive bi-layered tablet using floating drug delivery technique. Metformin was selected as a model drug due to its narrow absorption window as well as very highly water solubility. These properties of metformin led to be difficult controlling the drug release. The bi-layered tablet was prepared with bi-layered compression machine to minimize interference between floating part and controlling part. The tablet weight, appearance and hardness were evaluated after compression process. The times of 'time to floating' and 'Floating duration' were tested for floating ability and drug release study was also carried out to understand drug release behavior. Furthermore, the drug release of bi-layered tablet was compared with marketed metformin tablet with sustained release pattern (Glucopharge XR$^{(R)}$).The floating ability and drug release behaviors were well controlled by changing amounts of $NaHCO_3$ (floating substance) and hydroxypropyl methylcellulose (HPMC; release control material). Bi-layered tablet had 13s of time to float, over 10h of floating duration and very similar drug release behavior compared with Glucopharge XR$^{(R)}$($f_2$: 89.6). Consequently, the bi-layered tablet with floating ability was successfully prepared and these properties can maximize the efficacy of metformin.

• Journal of Life Science
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• v.33 no.3
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• pp.268-276
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• 2023

This study was conducted to optimize the formulation conditions of the immediate-release layer of carvedilol in the development of a two-layer tablet formulation for carvedilol and ivabradine. Using a 2⁴+3 full-factorial design of experiments, excipients (microcrystalline cellulose, citric acid, and crospovidone) of the carvedilol immediate-release layer (wet granulation part) and process parameters for the tablet compression process (main compression) were optimized, and seven types of each dependent variable (assay, content uniformity, hardness, friability, disintegration, and dissolution [pH 1.2 and 6.8]) were evaluated using design expert software. The analysis of variance results confirmed that the main compression has a significant effect on hardness, friability, and disintegration time and that microcrystalline cellulose has a major effect on friability and dissolution. In addition, it was confirmed that citric acid has a significant effect on friability. Crospovidone affects friability and dissolution. According to the design space from the design of the experiment results, the optimized range is microcrystalline cellulose (~18.0-32.0 mg), citric acid (~0.5-12 mg), and main compression (~615-837 kgf). Consequently, this study confirmed the availability of manufacturing the carvedilol immediate-release layer in which all risk factors evaluated in the initial risk assessment are removed.