Visualizing fluid transport inside orally disintegrating tablets and changes in tablets using real-time X-ray radiography and X-ray computed tomography

Abstract

Objective

To investigate the disintegration of wet- and dry-compressed orally disintegrating (OD) tablets, with synchrotron radiation as the X-ray source.

Significance

Pharmaceutical tablets are vital for the treatment of various diseases. Therefore, they are constantly developed to ensure desirable characteristics. In particular, OD tablets need to disintegrate immediately after absorbing saliva. How these tablets absorb saliva is key to enhancing rapid product development. Recently, absorption processes have been investigated using various noninvasive techniques, including X-ray radiography and X-ray computed tomography. However, X-ray radiography studies on how water without a contrast agent is absorbed, moves, and causes a tablet to swell are scarce. The use of a contrast agent is associated with some shortcomings, including complex data analysis in some instances, alterations in the viscosity of water, and potential influence on fluid transport inside the tablet, thus possibly affecting the disintegration process.

Methods

Real-time X-ray radiography was used to monitor the disintegration of various tablets, while X-ray computed tomography and software were used to create 3 D images.

Results

We demonstrated how pure water penetrated the wet-compressed tablet faster than inside the dry-compressed tablet, and how the latter swelled more. X-ray computed tomography showed the presence of voids in the tablets following water absorption.

Conclusion

Our methods are promising for nondestructive fluid absorption and transport investigations inside OD tablets.

Keywords:

• Orally disintegrating tablet
• disintegration
• X-ray radiography
• X-ray computed tomography
• real-time

Acknowledgements

The synchrotron radiation experiments were performed at the BL14B2 of SPring-8 with the approval of the Japan Synchrotron Radiation Research Institute (JASRI) (Proposal No. 2021A1639).

Author contributions

K. S. designed the experiments, performed the experiments, analyzed and interpreted the data, contributed reagents, materials, analysis tools or data, and wrote the paper. M. Y. designed the experiments, performed the experiments, analyzed and interpreted the data, contributed reagents, materials, analysis tools or data. N. N. performed the experiments, analyzed and interpreted the data, and contributed reagents, materials, analysis tools or data. T. H. conceived and designed the experiments, interpreted the data, contributed reagents, materials, analysis tools or data. Y. F. designed the experiments, interpreted the data, contributed reagents, materials, analysis tools or data. Y. T. conceived and designed the experiments, interpreted the data, contributed reagents, materials, analysis tools or data. T. Y. designed the experiments, interpreted the data, contributed reagents, materials, analysis tools or data. T. T. conceived and designed the experiments, interpreted the data, contributed reagents, materials, analysis tools or data. All authors have reviewed and agree to the contents of the manuscript.

Disclosure statement

Kazuhiro Suzuki, Norio Nishikawa, and Yuji Terui are employees of Toshiba Nanoanalysis Corporation. Masahiko Yoshiki is an employee of Toshiba Corporation. The other authors declare no conflicts of interest.

Data availability statement

No datasets were generated or analyzed during the current study.

Additional information

Funding

This work was supported by the Grants-in-aid for scientific research program (KAKENHI) of the Japan Society for the Promotion of Science (grant number JP19K11283).