In situ determination of delavirdine mesylate particle size in solid oral dosage forms.

Abstract:

PURPOSE:The in-situ particle size of delavirdine mesylate in dry mix and tablets was determined. METHODS:Optical microscopy and fluorescence microscopy combined with image analysis were used for qualitative and quantitative measurements. RESULTS:Using optical microscopy, it was demonstrated qualitatively that fragmentation of the large drug particles was occurring during tablet compression. Quantitative comparisons between dry mix and tablet samples showed that in the dry mix, drug particles remain intact, with particle lengths exceeding 200 microm. In the tablets, no particles longer than 100 microm had been observed. Analysis of multiple tablet lots revealed consistent in-situ drug particle size distributions, regardless of the original bulk drug particle size. CONCLUSIONS:Bulk drug particle size of delavirdine mesylate is not predictive of the particle size in the tablet due to fragmentation of particles during compression. Optical and fluorescence microscopy are valuable tools for probing in-situ particle size in complex matrices.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

White JG

doi

10.1023/a:1018875130152

subject

Has Abstract

pub_date

1999-04-01 00:00:00

pages

545-8

issue

4

eissn

0724-8741

issn

1573-904X

journal_volume

16

pub_type

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