Continuous monitoring of the hydration behavior of hydrophilic matrix tablets using time-domain NMR

Tsuji, Takahiro and Ono, Takashi and Taguchi, Hiromu and Leong, Kok Hoong and Hayashi, Yoshihiro and Kumada, Shungo and Okada, Kotaro and Onuki, Yoshinori (2023) Continuous monitoring of the hydration behavior of hydrophilic matrix tablets using time-domain NMR. Chemical & Pharmaceutical Bulletin, 71 (7). pp. 576-583. ISSN 1347-5223, DOI https://doi.org/10.1248/cpb.c23-00214.

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Abstract

Time-domain NMR (TD-NMR) was used for continuous monitoring of the hydration behavior of hydro-philic matrix tablets. The model matrix tablets comprised high molecular weight polyethylene oxide (PEO), hydroxypropyl methylcellulose (HPMC), and polyethylene glycol (PEG). The model tablets were immersed in water. Their T2 relaxation curves were acquired by TD-NMR with solid-echo sequence. A curve-fitting analysis was conducted on the acquired T2 relaxation curves to identify the NMR signals corresponding to the nongelated core remaining in the samples. The amount of nongelated core was estimated from the NMR signal intensity. The estimated values were consistent with the experiment measurement values. Next, the model tablets immersed in water were monitored continuously using TD-NMR. The difference in hydration behaviors of the HPMC and PEO matrix tablets was then characterized fully. The nongelated core of the HPMC matrix tablets disappeared more slowly than that of the PEO matrix tablets. The behavior of HPMC was significantly affected by the PEG content in the tablets. It is suggested that the TD-NMR method has potential to be utilized to evaluate the gel layer properties, upon replacement of the immersion medium: purified (nondeuterated) water is replaced with heavy (deuterated) water. Finally, drug-containing matrix tablets were tested. Diltiazem hydrochloride (a highly water-soluble drug) was employed for this experiment. Reasonable in vitro drug dissolution profiles, which were in accordance with the results from TD-NMR ex-periments, were observed. We concluded that TD-NMR is a powerful tool to evaluate the hydration proper-ties of hydrophilic matrix tablets.

Item Type: Article
Funders: Japan Society for the Promotion of Science [Grant no. 20K06986]
Uncontrolled Keywords: Hydrophilic matrix tablet; Time-domain NMR; Hydration; Continuous monitoring; Extended drug; Release
Subjects: R Medicine > RS Pharmacy and materia medica
Divisions: Faculty of Pharmacy > Department of Pharmaceutical Chemistry
Depositing User: Ms. Juhaida Abd Rahim
Date Deposited: 30 Oct 2025 04:01
Last Modified: 30 Oct 2025 04:01
URI: http://eprints.um.edu.my/id/eprint/48710

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