Swelling and Salt Formation in Ibuprofen and Tranexamic Acid-Containing Tablets during High-Temperature Storage

Ibuprofen (IBP)- and Tranexamic acid (TXA)-containing tablets are known to swell when stored at high temperatures, but the mechanism of swelling is unknown. In this study, we investigated the possible mechanism of swelling with high-temperature storage. Differential scanning calorimetry (DSC) and po...

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Main Authors: Yuto Kawano, Yoshiharu Tanaka, Nanami Hata, Yuki Yoshiike, Masato Nakajima, Etsuo Yonemochi, Nobuhiro Ishihara
Format: Article
Language:English
Published: MDPI AG 2022-10-01
Series:Crystals
Subjects:
Online Access:https://www.mdpi.com/2073-4352/12/10/1420
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author Yuto Kawano
Yoshiharu Tanaka
Nanami Hata
Yuki Yoshiike
Masato Nakajima
Etsuo Yonemochi
Nobuhiro Ishihara
author_facet Yuto Kawano
Yoshiharu Tanaka
Nanami Hata
Yuki Yoshiike
Masato Nakajima
Etsuo Yonemochi
Nobuhiro Ishihara
author_sort Yuto Kawano
collection DOAJ
description Ibuprofen (IBP)- and Tranexamic acid (TXA)-containing tablets are known to swell when stored at high temperatures, but the mechanism of swelling is unknown. In this study, we investigated the possible mechanism of swelling with high-temperature storage. Differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD) analyses showed that a new complex was formed in swollen tablets, when stored at 50 °C for 60 days. Additionally, we prepared single crystals of IBP and TXA, and analyzed them using single crystal X-ray diffractometry (SCXRD), to identify the new complex formed during storage. This revealed that the single crystal was a salt consisting of IBP and TXA. The PXRD peak of the salt simulated by SCXRD matched that of the PXRD peak of the swollen tablet after storage. These results suggest a close relationship between the swelling and crystal structures of IBP and TXA.
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spelling doaj.art-6c99e5e82dbc4d059046dfb129c72e112023-11-23T23:38:09ZengMDPI AGCrystals2073-43522022-10-011210142010.3390/cryst12101420Swelling and Salt Formation in Ibuprofen and Tranexamic Acid-Containing Tablets during High-Temperature StorageYuto Kawano0Yoshiharu Tanaka1Nanami Hata2Yuki Yoshiike3Masato Nakajima4Etsuo Yonemochi5Nobuhiro Ishihara6R&D Center, Zenyaku Kogyo Co., Ltd., 4-7-1 Minamiosawa, Tokyo 192-0364, JapanR&D Center, Zenyaku Kogyo Co., Ltd., 4-7-1 Minamiosawa, Tokyo 192-0364, JapanR&D Center, Zenyaku Kogyo Co., Ltd., 4-7-1 Minamiosawa, Tokyo 192-0364, JapanR&D Center, Zenyaku Kogyo Co., Ltd., 4-7-1 Minamiosawa, Tokyo 192-0364, JapanR&D Center, Zenyaku Kogyo Co., Ltd., 4-7-1 Minamiosawa, Tokyo 192-0364, JapanDepartment of Physical Chemistry, School of Pharmacy and Pharmaceutical Sciences, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, JapanR&D Center, Zenyaku Kogyo Co., Ltd., 4-7-1 Minamiosawa, Tokyo 192-0364, JapanIbuprofen (IBP)- and Tranexamic acid (TXA)-containing tablets are known to swell when stored at high temperatures, but the mechanism of swelling is unknown. In this study, we investigated the possible mechanism of swelling with high-temperature storage. Differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD) analyses showed that a new complex was formed in swollen tablets, when stored at 50 °C for 60 days. Additionally, we prepared single crystals of IBP and TXA, and analyzed them using single crystal X-ray diffractometry (SCXRD), to identify the new complex formed during storage. This revealed that the single crystal was a salt consisting of IBP and TXA. The PXRD peak of the salt simulated by SCXRD matched that of the PXRD peak of the swollen tablet after storage. These results suggest a close relationship between the swelling and crystal structures of IBP and TXA.https://www.mdpi.com/2073-4352/12/10/1420ibuprofentranexamic acidsaltcrystal structureswell
spellingShingle Yuto Kawano
Yoshiharu Tanaka
Nanami Hata
Yuki Yoshiike
Masato Nakajima
Etsuo Yonemochi
Nobuhiro Ishihara
Swelling and Salt Formation in Ibuprofen and Tranexamic Acid-Containing Tablets during High-Temperature Storage
Crystals
ibuprofen
tranexamic acid
salt
crystal structure
swell
title Swelling and Salt Formation in Ibuprofen and Tranexamic Acid-Containing Tablets during High-Temperature Storage
title_full Swelling and Salt Formation in Ibuprofen and Tranexamic Acid-Containing Tablets during High-Temperature Storage
title_fullStr Swelling and Salt Formation in Ibuprofen and Tranexamic Acid-Containing Tablets during High-Temperature Storage
title_full_unstemmed Swelling and Salt Formation in Ibuprofen and Tranexamic Acid-Containing Tablets during High-Temperature Storage
title_short Swelling and Salt Formation in Ibuprofen and Tranexamic Acid-Containing Tablets during High-Temperature Storage
title_sort swelling and salt formation in ibuprofen and tranexamic acid containing tablets during high temperature storage
topic ibuprofen
tranexamic acid
salt
crystal structure
swell
url https://www.mdpi.com/2073-4352/12/10/1420
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