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Variable-focus microscopy and UV surface dissolution imaging as complementary techniques in intrinsic dissolution rate determination.

Abstract：

:This work reports a novel approach to the assessment of the surface properties of compacts used in Surface Dissolution Imaging (SDI). SDI is useful for determining intrinsic dissolution rate (IDR), an important parameter in early stage drug development. Surface topography, post-compaction and post-SDI run, have been measured using a non-contact, optical, three-dimensional microscope based on focus variation, the Alicona Infinite Focus Microscope, with the aim of correlating the IDRs to the surface properties. Ibuprofen (IBU) was used as a model poorly-soluble drug. DSC and XRD were used to monitor possible polymorphic changes that may have occurred post-compaction and post-SDI run. IBUs IDR decreased from 0.033mg/min/cm2 to 0.022mg/min/cm2 from 10 to 20min, respectively, during the experiment. XRD and DSC showed no form changes during the SDI run. The surface topography images showed that a distinct imprint was embossed on the surfaces of some compacts which could affect IDRs. Surface parameter values were associated with the SDI experiments which showed strong correlations with the IDR values. The variable-focus microscope can be used as a complimentary tool in the determination of IDR values from the SDI.

journal_name

Int J Pharm

journal_title

International journal of pharmaceutics

authors

Ward A,Walton K,Box K,Østergaard J,Gillie LJ,Conway BR,Asare-Addo K

doi

10.1016/j.ijpharm.2017.07.053

subject

Has Abstract

pub_date

2017-09-15 00:00:00

pages

139-144

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(17)30661-0

journal_volume

530

pub_type

杂志文章

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