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The dehydration behavior and non-isothermal dehydration kinetics of donepezil hydrochloride monohydrate (Form I)
Received date: 13 May 2013
Accepted date: 10 Aug 2013
Published date: 05 Mar 2014
Copyright
Powders of donepezil hydrochloride monohydrate (Form I) underwent isomorphic dehydration, losing 3% w/w water between 90% and 10% relative humidity (RH) without changing its powder X-ray pattern. Below 10% RH, additional dehydration occurred in conjunction with a reversible phase transition between the monohydrate state and a dehydrated state, with a 4.0% w/w loss to 0% RH. A combination of methods was used to understand the structural changes occurring during the desolvation process, including dynamic vapor sorption measurements, thermal analysis and powder X-ray diffraction. Form I showed the characteristics of the channel hydrate, whose non-isothermal dehydration behavior proceeds in two steps: (1) the loss of non-crystalline water adsorbed on the surface, and (2) the loss of one crystalline water in the channel. Dehydrated Form I is structurally similar to the monohydrate Form I. According to the heat of fusion and the crystal density criteria, the two crystal forms belonged to the univariant system, and the anhydrate (Form III) is stable. The dehydration kinetics was achieved from the TG-DTG curves by both the Achar method and the Coats-Redfern method with 15 frequently cited basic kinetic models. The dynamic dehydration processes for steps 1 and 2 were best expressed by the Zhuralev-Lesokin-Tempelman equation, suggesting a three-dimensional diffusion-controlled mechanism.
Key words: dehydration; thermal analysis; transformation; dehydration kinetics
Tiantian LIU , Yuanyuan RAN , Bochao WANG , Weibing DONG , Songgu WU , Junbo GONG . The dehydration behavior and non-isothermal dehydration kinetics of donepezil hydrochloride monohydrate (Form I)[J]. Frontiers of Chemical Science and Engineering, 2014 , 8(1) : 55 -63 . DOI: 10.1007/s11705-013-1352-3
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