Crystal Structures and Vapor-Induced Crystalline Transformation of 7-Ethyl-10-Hydroxycamptothecin Pseudopolymorphs.

Abstract:

:Solvent-induced 3 frameworks (the monohydrate, methanol solvate, and dimethyl formamide [DMF] solvate) of an anticancer drug, 7-ethyl-10-hydroxycamptothecin (SN38), were constructed. The crystal structures of the 3 pseudopolymorphs were characterized by single-crystal X-ray diffraction technique for the first time. Crystal structure analysis of all these polymorphs revealed that the monohydrate showed 3D frameworks linked by hydrogen bonds. In the methanol solvate, the 1D molecular chains were linked by the methanol molecules through intermolecular hydrogen bonds to form a 2D sheet. The DMF solvate exhibits the 1D hydrogen bonding-linked chains along b-axis. Vapor-induced transformation has been investigated for the monohydrate, the methanol solvate, and the DMF solvate. The conversion relationships among the 3 solid frameworks are illustrated. Insights regarding transformation mechanisms have been established from consideration of the crystal structures.

journal_name

J Pharm Sci

authors

Fang L,Wang L,Yao C,Song S,Wu Z,Tao X

doi

10.1016/j.xphs.2017.03.020

subject

Has Abstract

pub_date

2017-10-01 00:00:00

pages

2998-3004

issue

10

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(17)30206-X

journal_volume

106

pub_type

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