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Hot-melt granulation in a twin screw extruder: effects of processing on formulations with caffeine and Ibuprofen.
J Pharm Sci. 2013 Dec; 102(12):4330-6.JP

Abstract

Hot-melt granulation (HMG) by twin screw extrusion is a novel technology for the continuous processing of pharmaceuticals but confidence must still be gained regarding whether the environment affects drug properties. In this preliminary study, granulation was studied for a model product containing lactose monohydrate and active ingredients of differing water solubility, namely ibuprofen versus caffeine. The formulations were granulated at 220 rpm and 100°C with polyethylene glycol binders of differing molecular weights and at concentrations between 6.5% and 20%. In terms of granule properties, the low melting point of ibuprofen had a dominant influence by producing larger, stronger granules, whereas the caffeine products were more comparable to a blank containing no active ingredient. Drug degradation was study by differential scanning calorimetry, X-ray diffraction, and high-pressure liquid chromatography. The only detected change was the dehydration of lactose monohydrate for the caffeine and blank products, whereas the lubricating influence of the ibuprofen protected its granules. The short residence time (∼60 s) was consider to be influential in minimizing damage of the drug despite the high temperature and shear attributed to HMG inside a twin screw extruder.

Authors+Show Affiliations

MMRI/CAPPA-D, Department of Chemical Engineering, McMaster University, Hamilton, Ontario, L8S 4L7, Canada.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24114922

Citation

Weatherley, Sharleen, et al. "Hot-melt Granulation in a Twin Screw Extruder: Effects of Processing On Formulations With Caffeine and Ibuprofen." Journal of Pharmaceutical Sciences, vol. 102, no. 12, 2013, pp. 4330-6.
Weatherley S, Mu B, Thompson MR, et al. Hot-melt granulation in a twin screw extruder: effects of processing on formulations with caffeine and Ibuprofen. J Pharm Sci. 2013;102(12):4330-6.
Weatherley, S., Mu, B., Thompson, M. R., Sheskey, P. J., & O'Donnell, K. P. (2013). Hot-melt granulation in a twin screw extruder: effects of processing on formulations with caffeine and Ibuprofen. Journal of Pharmaceutical Sciences, 102(12), 4330-6. https://doi.org/10.1002/jps.23739
Weatherley S, et al. Hot-melt Granulation in a Twin Screw Extruder: Effects of Processing On Formulations With Caffeine and Ibuprofen. J Pharm Sci. 2013;102(12):4330-6. PubMed PMID: 24114922.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Hot-melt granulation in a twin screw extruder: effects of processing on formulations with caffeine and Ibuprofen. AU - Weatherley,Sharleen, AU - Mu,Bo, AU - Thompson,Michael R, AU - Sheskey,Paul J, AU - O'Donnell,Kevin P, Y1 - 2013/10/01/ PY - 2013/06/02/received PY - 2013/09/05/revised PY - 2013/09/11/accepted PY - 2013/10/12/entrez PY - 2013/10/12/pubmed PY - 2014/6/26/medline KW - X-ray diffractometry KW - caffeine KW - calorimetry (DSC) KW - chemical stability KW - continuous granulation KW - drug degradation KW - extrusion KW - granulation KW - hot-melt granulation KW - ibuprofen SP - 4330 EP - 6 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 102 IS - 12 N2 - Hot-melt granulation (HMG) by twin screw extrusion is a novel technology for the continuous processing of pharmaceuticals but confidence must still be gained regarding whether the environment affects drug properties. In this preliminary study, granulation was studied for a model product containing lactose monohydrate and active ingredients of differing water solubility, namely ibuprofen versus caffeine. The formulations were granulated at 220 rpm and 100°C with polyethylene glycol binders of differing molecular weights and at concentrations between 6.5% and 20%. In terms of granule properties, the low melting point of ibuprofen had a dominant influence by producing larger, stronger granules, whereas the caffeine products were more comparable to a blank containing no active ingredient. Drug degradation was study by differential scanning calorimetry, X-ray diffraction, and high-pressure liquid chromatography. The only detected change was the dehydration of lactose monohydrate for the caffeine and blank products, whereas the lubricating influence of the ibuprofen protected its granules. The short residence time (∼60 s) was consider to be influential in minimizing damage of the drug despite the high temperature and shear attributed to HMG inside a twin screw extruder. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/24114922/Hot_melt_granulation_in_a_twin_screw_extruder:_effects_of_processing_on_formulations_with_caffeine_and_Ibuprofen_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)30795-4 DB - PRIME DP - Unbound Medicine ER -