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Quantitative measurement of crystalline impurity in a pharmaceutical tablet by X-ray powder diffraction and method validation

Published online by Cambridge University Press:  05 June 2013

R. Casella*
Affiliation:
AstraZeneca Pharmaceuticals Inc., 35 Gatehouse Drive, Waltham, Massachusetts 02451
S. Boudreau
Affiliation:
AstraZeneca Pharmaceuticals Inc., retired
James A. Wesley
Affiliation:
Eli Lilly and Company, Lilly Research Laboratories, Drop Code 3832 -LTC North, North Indianapolis, Indianapolis 46285
Robert D'Aloise
Affiliation:
AstraZeneca Pharmaceuticals Inc., retired
*
a)Author to whom correspondence should be addressed. Electronic mail: robert.casella@astrazeneca.com

Abstract

A powder X-ray diffraction method was developed and validated to measure the crystalline impurity 4-(5-cyclopentyloxy-carbonylamino-1-methyl-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide hydrate in a pharmaceutical tablet ranging from 0.6 to 3% (w/w). The calibration plot was found to be linear with a correlation coefficient (r2) of 0.996, and was reproducible among operators. The detection limit was determined to be 0.6% with a signal-to-noise ratio of 3:1. The quantitation limit was determined to be 1% with a signal-to-noise ratio of 5:1. Instrument precision at the quantitation limit was 5.8%. Method precision was 6.1% at the quantitation limit and 7.4% at the detection limit. Intermediate precision at the quantitation limit was 7.3% during a 6-month study. Accuracy measurements using crystalline impurity standards prepared in an excipient mixture ranged from 89.3 to 105.5%. Accuracy measurements using tablets containing spiked quantities of crystalline impurity ranged from 72.0 to 92.7%. Accuracy measurements using spiked tablets were complicated because the crystalline impurity was lost during the manufacturing process and a correction factor was used. Ruggedness was assessed by evaluating repetitive assay, repetitive packing, sample packing, and sample stability. Repetitive assays show the exposure of standards to a relative humidity in excess of 57% caused displacement error because of an increase in sample volume and a peak-position shift. Repetitive-packing studies show the analyte was extracted from the sample at a low relative humidity because of a static-charge induction. Sample-packing studies show that two subjective packing techniques were equivalent, and that under- and over-packing samples cause changes in sample density which would not affect results within ±16%. Sample-stability studies show that the quantitation-limit standard was stable as long as the sample was exposed to a relative humidity below 57%.

Type
Technical Articles
Copyright
Copyright © International Centre for Diffraction Data 2013 

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References

Cullity, B. D. (1978). Elements of X-ray Diffraction (Addison-Wesley Publishing Company, Inc., Reading, MA), p. 13.Google Scholar
Lachman, L.Lieberman, H. A., and Kanig, J. L. (1986). The Theory and Practice of Industrial Pharmacy (Lea and Febiger, Philadelphia, PA), 3rd ed., pp. 7071.Google Scholar