Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate

The dissolution rate is the rate-limiting step for Biopharmaceutics Classification System (BCS) class II drugs to enhance their in vivo pharmacokinetic behaviors. There are some factors affecting the dissolution rate, such as polymorphism, particle size, and crystal habit. In this study, to improve...

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Main Authors:	Chi Uyen Phan, Jie Shen, Kaxi Yu, Jianming Mao, Guping Tang
Format:	Article
Language:	English
Published:	MDPI AG 2021-06-01
Series:	Molecules
Subjects:	crystal habit sorafenib tosylate dissolution rate pharmacokinetics
Online Access:	https://www.mdpi.com/1420-3049/26/11/3469

id	doaj-db4ca8a4411f43eb9640b2efb9d67d70
record_format	Article
spelling	doaj-db4ca8a4411f43eb9640b2efb9d67d702021-06-30T23:32:00ZengMDPI AGMolecules1420-30492021-06-01263469346910.3390/molecules26113469Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib TosylateChi Uyen Phan0Jie Shen1Kaxi Yu2Jianming Mao3Guping Tang4Faculty of Chemical Technology—Environment, The University of Danang—University of Technology and Education, Danang 550000, VietnamDepartment of Chemistry, Zhejiang University, Hangzhou 310028, ChinaDepartment of Chemistry, Zhejiang University, Hangzhou 310028, ChinaDepartment of Chemistry, Zhejiang University, Hangzhou 310028, ChinaDepartment of Chemistry, Zhejiang University, Hangzhou 310028, ChinaThe dissolution rate is the rate-limiting step for Biopharmaceutics Classification System (BCS) class II drugs to enhance their in vivo pharmacokinetic behaviors. There are some factors affecting the dissolution rate, such as polymorphism, particle size, and crystal habit. In this study, to improve the dissolution rate and enhance the in vivo pharmacokinetics of sorafenib tosylate (Sor-Tos), a BCS class II drug, two crystal habits of Sor-Tos were prepared. A plate-shaped crystal habit (ST-A) and a needle-shaped crystal habit (ST-B) were harvested by recrystallization from acetone (ACN) and n-butanol (BuOH), respectively. The surface chemistry of the two crystal habits was determined by powder X-ray diffraction (PXRD) data, molecular modeling, and face indexation analysis, and confirmed by X-ray photoelectron spectroscopy (XPS) data. The results showed that ST-B had a larger hydrophilic surface than ST-A, and subsequently a higher dissolution rate and a substantial enhancement of the in vivo pharmacokinetic performance of ST-B.https://www.mdpi.com/1420-3049/26/11/3469crystal habitsorafenib tosylatedissolution ratepharmacokinetics
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Chi Uyen Phan Jie Shen Kaxi Yu Jianming Mao Guping Tang
spellingShingle	Chi Uyen Phan Jie Shen Kaxi Yu Jianming Mao Guping Tang Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate Molecules crystal habit sorafenib tosylate dissolution rate pharmacokinetics
author_facet	Chi Uyen Phan Jie Shen Kaxi Yu Jianming Mao Guping Tang
author_sort	Chi Uyen Phan
title	Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate
title_short	Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate
title_full	Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate
title_fullStr	Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate
title_full_unstemmed	Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate
title_sort	impact of crystal habit on the dissolution rate and in vivo pharmacokinetics of sorafenib tosylate
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2021-06-01
description	The dissolution rate is the rate-limiting step for Biopharmaceutics Classification System (BCS) class II drugs to enhance their in vivo pharmacokinetic behaviors. There are some factors affecting the dissolution rate, such as polymorphism, particle size, and crystal habit. In this study, to improve the dissolution rate and enhance the in vivo pharmacokinetics of sorafenib tosylate (Sor-Tos), a BCS class II drug, two crystal habits of Sor-Tos were prepared. A plate-shaped crystal habit (ST-A) and a needle-shaped crystal habit (ST-B) were harvested by recrystallization from acetone (ACN) and n-butanol (BuOH), respectively. The surface chemistry of the two crystal habits was determined by powder X-ray diffraction (PXRD) data, molecular modeling, and face indexation analysis, and confirmed by X-ray photoelectron spectroscopy (XPS) data. The results showed that ST-B had a larger hydrophilic surface than ST-A, and subsequently a higher dissolution rate and a substantial enhancement of the in vivo pharmacokinetic performance of ST-B.
topic	crystal habit sorafenib tosylate dissolution rate pharmacokinetics
url	https://www.mdpi.com/1420-3049/26/11/3469
work_keys_str_mv	AT chiuyenphan impactofcrystalhabitonthedissolutionrateandinvivopharmacokineticsofsorafenibtosylate AT jieshen impactofcrystalhabitonthedissolutionrateandinvivopharmacokineticsofsorafenibtosylate AT kaxiyu impactofcrystalhabitonthedissolutionrateandinvivopharmacokineticsofsorafenibtosylate AT jianmingmao impactofcrystalhabitonthedissolutionrateandinvivopharmacokineticsofsorafenibtosylate AT gupingtang impactofcrystalhabitonthedissolutionrateandinvivopharmacokineticsofsorafenibtosylate
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Impact of Crystal Habit on the Dissolution Rate and In Vivo Pharmacokinetics of Sorafenib Tosylate

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