Effect of Disintegrants on Prolongation of Tablet Disintegration Induced by Immersion in Xanthan Gum-Containing Thickening Solution: Contribution of Disintegrant Interactions with Disintegration Fluids

In clinical practice, a thickening solution is frequently used to allow easy swallowing of tablets by patients suffering from dysphagia. This study investigated the effect of the thickening solution on tablet disintegration. Model tablets containing different disintegrants were prepared and their disintegration times (DTs) measured using standard methods. We also performed an additional disintegration test on the model tablets after immersing them for 1 min in thickening solution containing xanthan gum (XTG-SOL) (“modified disintegration test”). The DTs of the test tablets were substantially prolonged by immersion in XTG-SOL.

Furthermore, the effect of the XTG-SOL on the DTs differed depending on the type of disintegrant contained in the tablets. To investigate in more detail this prolongation of tablet disintegration, we examined the contribution of tablet properties to their DTs. The properties analyzed included contact angle, T₂ relaxation time, wetting time, and water absorption ratio. The contributions of these properties to the DTs were analyzed using multiple regression analysis. This analysis clarified that the tablet properties affecting DTs changed after immersion in XTG-SOL: wetting time significantly affected the DTs measured in the normal disintegration test, while T₂ was crucial for the DTs of tablets immersed in XTG-SOL. These findings provide valuable information for design of tablet formulations, and for clinical medication management for older patients with dysphagia.

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or continue reading here: Daisuke Sugiura, Yoshinori Onuki, Yoshiaki Fujita, Akihiro Nakamura, Tsutomu Harada, Effect of Disintegrants on Prolongation of Tablet Disintegration Induced by Immersion in Xanthan Gum-Containing Thickening Solution: Contribution of Disintegrant Interactions with Disintegration Fluids, Chemical and Pharmaceutical Bulletin, 2020, Volume 68, Issue 11, Pages 1055-1060, Released November 01, 2020, Online ISSN 1347-5223, Print ISSN 0009-2363, https://doi.org/10.1248/cpb.c20-00480

Materials
The disintegrants contained in the model tablets in this study:  Corn starch (CS) was was provided by Nihon Shokuhin Kako (Tokyo, Japan). Carmellose (CMC) [NS-300® (NS)] and carmellose calcium (CMC-Ca) [ECG®-505 (ECG)] were was provided by Gotoku Chemical (Tokyo, Japan). Low-substituted hydroxypropyl celluloses (L-HPC®) [LH-21] was provided by Shin-Etsu Chemical (Tokyo, Japan). Sodium starch glycolate [Glycolys® (GLY)] was provided by Roquette Japan (Tokyo, Japan). Crospovidone type A [Kollidon® CL-F (KO)] was provided by BASF Japan (Tokyo, Japan), while crospovidone type B [Polyplasdon™ XL-10 (PP)] was provided by ISP Technologies (Ashland, KY, U.S.A.). Mannitol (Parteck® M200) was provided by Merck Millipore (Billerica, MA, U.S.A.). Microcrystalline cellulose (MCC) (Ceolus® UF-F711) was provided by Asahi Kasei Chemicals (Tokyo, Japan). Magnesium stearate (Mg-St) was provided by Taihei Chemical Industrial (Osaka, Japan). XTG (ECO-GUM®) as a food thickening agent was provided by DSP Gokyo Food & Chemical Co., Ltd. (Tokyo, Japan).