PMCCPMCCPMCC

Search tips
Search criteria 

Advanced

 
Logo of aapspharmspringer.comThis journalToc AlertsSubmit OnlineOpen Choice
 
AAPS PharmSciTech. 2003 September; 4(3): 142–148.
Published online 2003 March 4. doi:  10.1208/pt040347
PMCID: PMC2750640

Chemometric evaluation of pharmaceutical properties of antipyrine granules by near-infrared spectroscopy

Abstract

The purpose of this research was to apply near-infrared (NIR) spectroscopy with chemometrics to predict the change of pharmaceutical properties of antipyrine granules during granulation by regulation of the amount of water added. The various kinds of granules (mean particle size, 70–750 μm) were obtained from the powder mixture (1 g of antipyrine, 6 g of hydroxypropylcellulose, 140 g of lactose, and 60 g of potato starch) by regulation of the added water amount (11–19 wt/wt%) in a high-speed mixer. The granules were characterized by mean particle size, angle of repose, compressibility, tablet porosity, and tablet hardness as parameters of pharmaceutical properties. To predict the pharmaceutical properties, NIR spectra of the granules were measured and analyzed by principal component regression, (PCR) analysis. The mean particle size of the granules increased from 81 μm to 650 μm with an increase in the amount of water, and it was possible to make larger spherical granules with narrow particle size distribution using a high-speed mixer. Angle of repose, compressibility, and porosity of the tablets decreased with an increase of added water, but tablet hardness increased. The independent calibration models to evaluate particle size, angle of repose, and tablet porosity and hardness were established by using PCR based on NIR spectra of granules, respectively. The correlation coefficient constants of calibration curves for prediction of mean particle size, angle of repose, tablet porosity, and tablet hardness were 0.9109, 0.8912, 0.7437, and 0.8064, respectively. It is possible that the pharmaceutical properties of the granule, such as mean particle size, angle of repose, tablet porosity, and tablet hardness, could be predicted by an NIR-chemometric method.

Keywords: agitating granulating, physical properties, near-infrared spectroscopy, chemomemetrics, principle component regression analysis

Full Text

The Full Text of this article is available as a PDF (301K).

Selected References

These references are in PubMed. This may not be the complete list of references from this article.
1. Otsuka M, Gao J, Matsuda Y. Effect of amount of added water during extrusion-spheronization process of pharmaceutical properties of granules. Drug Dev Ind Pharm. 1994;20:2977–2992. doi: 10.3109/03639049409041962. [Cross Ref]
2. Terashita K, Ohike A, Kato M, Miyanami K. Granulation process and end-point in high speed mixer granulation. Yakugaku Zasshi. 1987;107:377–383.
3. Aoki S, Okamoto A, Nemoto M, Yoshida T, Danjjo K, Sunada H, Otsuka A. Optimization of granulation in a vertical high-speed mixer: effect of process variables on mean granule diameter and its distribution. Yakuzaigaku. 1993;53(3):194–199.
4. Sunada H, Hoshi N, Hasegawa M. Standard Formulation Research Association. Particulate Des Pharm Technique. 1993;213–222.
5. Toyoshima S, Watanabe S, Matsuo K, Ksai M. Studies on wet granulation, I: the effect of amount of binder on granulating state and properties of granules. Yakugaku Zasshi. 1971;91:1088–1091. [PubMed]
6. Horisawa E, Yamada M, Danjyo K, Otsuka A. Effect of binder solution on properties of wet masses and granules prepared by extruding granulation. Yakuzaigaku. 1992;52(1):13–24.
7. Kristensen HG, Holm P, Jaegerskou A, Schaefer T. Granulation in high speed mixers, IV: effect of liquid saturation on the agglomeration. Pharm Ind. 1984;46:763–767.
8. Ueda H, Ueda J, Sato T. Relationship between water-holding capacity of powder and physical properties of granules prepared by agitating granulation. J Soc Powder Technol Japan. 2001;38:84–89.
9. Holm P, Jungersen O, Schaefer T, Kristensen HG. Granulation in high speed mixters, II effects of process variables during keading. Pharm Ind. 1983;45:806–811.
10. Holm P, Jungersen O, Schaefer T, Kristensen HG. Granulation in high speed mixers, II: effects of process variables during kneading. Pharm Ind. 1984;46:97–101.
11. Jaegerskou A, Holm P, Schaefer T, Kristensen HG. Granulation in high speed mixers, III: effects of process variables on the intragranular porosity. Pharm Ind. 1984;46:310–314.
12. Iwamoto M, Kawano S, Uozumi J. Introduction of Near-Infrared Spectroscopy. Tokyo, Japan: Saiwai Shobou; 1994.
13. Martents H, Næs T. Multivariate Calibration. New York, NY: John Wiley & Sons; 1989.
14. Morisseau KM, Rhodes CT. Near-infrared spectroscopy as a nondestructive alternative to conventional tablet hardness testing. Pharm Res. 1997;14:108–111. doi: 10.1023/A:1012071904673. [PubMed] [Cross Ref]
15. Drennen JK, Lodder RA. Nondestructive near-infrared analysis of intact tablets for determination of degradation products. J Pharm Sci. 1990;79:622–627. doi: 10.1002/jps.2600790717. [PubMed] [Cross Ref]
16. Buchanan BR, Baxter MA, Chen TS, Qin XZ, Robinson PA. Use of near-infrared spectroscopy to evaluate an active in a film coated tablet. Pharm Res. 1996;13:616–621. doi: 10.1023/A:1016014625418. [PubMed] [Cross Ref]
17. Norris T, Aldridge PK, Sekulic SS. Determination of end-points for polymorph conversions of crystalline organic compounds using on-line near-infrared spectroscopy. Analyst. 1997;122:549–552. doi: 10.1039/a700782e. [Cross Ref]
18. Saver RW, Meulman PA, Bowerman DK, Havens JL. Factor analysis of infrared spectra for solid-state forms of delavirdine mesylate. Int J Pharm. 1998;167:105–120. doi: 10.1016/S0378-5173(98)00051-9. [Cross Ref]
19. Patl AD, Luner PE, Kemper MS. Quantitative analysis of polymorphs in binary and multi-component powder mixtures by near-infrared reflectance spectroscopy. Int J Pharm. 2000;206:63–74. doi: 10.1016/S0378-5173(00)00530-5. [PubMed] [Cross Ref]
20. Otsuka M, Kato F, Matsuda Y. Comparative evaluation of the degree of indomethacin crystallinity by chemoinfometrical Fourier-transformed near-infrared spectroscopy and conventional powder X-ray diffractometry. AAPS Pharm Sci. 2000;2:9–9. doi: 10.1208/ps020109. [PMC free article] [PubMed] [Cross Ref]
21. Otsuka M, Kato F, Matsuda Y. Determination of indomethacin polymorphic contents by chemometric near-infrared spectroscopy and conventional powder X-ray diffractometry. Analyst. 2001;126:1578–1582. doi: 10.1039/b103498g. [PubMed] [Cross Ref]
22. Bull CR. Compensation for particle size effects in near infrared reflectance. Analyst. 1991;116:781–786. doi: 10.1039/an9911600781. [Cross Ref]
23. Aucott LS, Garthwaite PH. Transformations, to reduce the effect of particle size in near-infrared spectra. Analyst. 1988;113:1849–1854. doi: 10.1039/an9881301849. [Cross Ref]
24. Norris KH, Williams PC. Optimization of mathematical treatments of raw near-infrared signal in the measurement of protein in hard red spring wheat, I: influence of particle size. Cereal Chem. 1984;61:158–165.
25. Franke P, Gill I, Luscombe CN, Rudd DR, Waterhouse J, Jayasooriya A. Near-infrared mass median particle size determination of lactose monohydrate: evaluating several chemometric approaches. Analyst. 1998;123:2043–2046. doi: 10.1039/a802532k. [PubMed] [Cross Ref]

Articles from AAPS PharmSciTech are provided here courtesy of American Association of Pharmaceutical Scientists