Evaluation of Different Particle Size Reduction Techniques in Application of Formulation Preparation

Authors

  • Darrin Lau University of California, Berkeley Berkeley, CA 94720
  • Minli Xie Small Molecule Technical Operation, Medivation, 525 Market St #36
  • Yingqing Ran Small Molecule Pharmaceutical Sciences, Genentech DNA Way,

Keywords:

Particle size, size reduction, Avicel PH 101, Naproxen, Dibasic calcium phosphate dihydrate

Abstract

Several commonly used particle size reduction techniques were evaluated in this study.  Two excipients Avicel PH 101, calcium phosphate dihydrate and a poorly soluble compound naproxen were used for evaluation. All the techniques tested in this study: tissue grinder, glass beads, Glen Mills high speed mixer, polytron and sonication showed different degree of particle size reduction. The polytron in combination with the sonicator proved to be the most suitable technique for particle size reduction in discovery with limited API available. The processed particle sizes from the polytron technique were comparable to the glass tissue grinders while minimizing the loss of sample. Glass beads created small particle sizes (under 20 microns) depending on the length of time, but it was overly time consuming. Glen-mill needs about hundreds of milligram material to work with despite the comparable particle size reduction.


References

Fincher, J.H., “particle size and its relationship to absorption and activityâ€, J. Pharm. Sci. vol.57, pp. 1825-1835, 1968.

Hinz, R.J., Johnson, K.C., “The effect of particle size distribution on dissolution rate and oral absorptionâ€, Int. J. Pharm. vol. 51, pp. 9-17, 1989.

Johnson, K.C. and Swindell, A. C., “Guidance in the setting of drug particle size specifications to minimize variability in absorptionâ€. Pharm. Res. vol. 13, no.12, pp. 1795-1798, 1996.

Yalkowsky, S.H., Bolton, S., “Particle size and content uniformityâ€. Pharm. Res. vol.7, pp. 962-966. 1990.

Jinno, J., Kamada, N., Miyake, M., Yamada, K., Mukai, T., Odomi, M., Toguchi, H., Liversidge, G.G., Higaki, K., Kimura, T., “effect of particle size reduction on dissolution and oral absorption of a poorly water-soluble drug, cilostazol, in beagle dogsâ€, J. of Control. Release. vol.111, pp. 56-64. 2006.

Clement, S., Purutyan, H., “Narrowing down equipment choices for particle-size reductionâ€, Chem. Eng. Prog. vol. 98, no.6, pp.50-54. 2002.

W. Wu, G. H. Nancollas, “The dissolution and growth of sparingly soluble inorganic salts: A kinetics and surface energy approachâ€, Pure &App Chem., vol.70, no. 10, pp. 1867-1872, 1998.

Chou,K.J., Bao L., Kam K. R., Gu C., Chiang P., “ Evaluation of nanoparticle formation feasibility upon wet milling based on physicochemical properties of drug moleculesâ€, Let. in Appl. NanoBio. vol.4 no.1, pp. 231-235. 2015.

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Published

2016-08-15

How to Cite

Lau, D., Xie, M., & Ran, Y. (2016). Evaluation of Different Particle Size Reduction Techniques in Application of Formulation Preparation. Asian Journal of Applied Sciences, 4(4). Retrieved from https://ajouronline.com/index.php/AJAS/article/view/3999

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