Tags

Type your tag names separated by a space and hit enter

Preparation and characterisation of ibuprofen-poloxamer 188 granules obtained by melt granulation.
Eur J Pharm Sci. 2002 Feb; 15(1):71-8.EJ

Abstract

The aim of this study was to prepare, by melt granulation, granules containing ibuprofen as a poorly water soluble model drug in order to improve its dissolution rate and its availability; lactose as a diluent and poloxamer 188 (Lutrol F68), as a new meltable hydrophilic binder, were used. The granules were prepared in a laboratory-scale high-shear mixer, using a jacket temperature of 50 degrees C and an impeller speed of 500 rpm. The particle size analysis shows that the main fraction was between 200 and 500 microm, while the determination of drug content indicated that ibuprofen was quite uniformly distributed in all the fractions. Scanning Electron Microscopy (SEM), image and fractal analysis revealed that the granules did not have a perfect spherical shape and a rugged surface (D(s)=2.6475). The in vitro dissolution tests showed an increase in the dissolution rate of granules compared to pure drug and physical mixture. The characterisation of the samples, performed by Differential Scanning Calorimetry (DSC) and X-ray powder diffraction (XRD), suggests that the improvement of dissolution rate could be correlated to the formation of a eutectic mixture between the drug and the binder. Stability studies indicated that the granule properties do not change, at least after 1 year of storage at 25 degrees C. In conclusion, the results of this work suggest that the melt granulation technique is an easy and fast method to improve the dissolution rate of ibuprofen, using poloxamer 188 as a new hydrophilic meltable binder.

Authors+Show Affiliations

Dipartimento di Scienze Farmaceutiche, Università degli Studi di Bologna, Via S. Donato 19/2, 40127 Bologna, Italy. passerin@biocfarm.unibo.itNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

11803133

Citation

Passerini, Nadia, et al. "Preparation and Characterisation of Ibuprofen-poloxamer 188 Granules Obtained By Melt Granulation." European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, vol. 15, no. 1, 2002, pp. 71-8.
Passerini N, Albertini B, González-Rodríguez ML, et al. Preparation and characterisation of ibuprofen-poloxamer 188 granules obtained by melt granulation. Eur J Pharm Sci. 2002;15(1):71-8.
Passerini, N., Albertini, B., González-Rodríguez, M. L., Cavallari, C., & Rodriguez, L. (2002). Preparation and characterisation of ibuprofen-poloxamer 188 granules obtained by melt granulation. European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences, 15(1), 71-8.
Passerini N, et al. Preparation and Characterisation of Ibuprofen-poloxamer 188 Granules Obtained By Melt Granulation. Eur J Pharm Sci. 2002;15(1):71-8. PubMed PMID: 11803133.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and characterisation of ibuprofen-poloxamer 188 granules obtained by melt granulation. AU - Passerini,Nadia, AU - Albertini,Beatrice, AU - González-Rodríguez,Marisa L, AU - Cavallari,Cristina, AU - Rodriguez,Lorenzo, PY - 2002/1/23/pubmed PY - 2002/5/1/medline PY - 2002/1/23/entrez SP - 71 EP - 8 JF - European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences JO - Eur J Pharm Sci VL - 15 IS - 1 N2 - The aim of this study was to prepare, by melt granulation, granules containing ibuprofen as a poorly water soluble model drug in order to improve its dissolution rate and its availability; lactose as a diluent and poloxamer 188 (Lutrol F68), as a new meltable hydrophilic binder, were used. The granules were prepared in a laboratory-scale high-shear mixer, using a jacket temperature of 50 degrees C and an impeller speed of 500 rpm. The particle size analysis shows that the main fraction was between 200 and 500 microm, while the determination of drug content indicated that ibuprofen was quite uniformly distributed in all the fractions. Scanning Electron Microscopy (SEM), image and fractal analysis revealed that the granules did not have a perfect spherical shape and a rugged surface (D(s)=2.6475). The in vitro dissolution tests showed an increase in the dissolution rate of granules compared to pure drug and physical mixture. The characterisation of the samples, performed by Differential Scanning Calorimetry (DSC) and X-ray powder diffraction (XRD), suggests that the improvement of dissolution rate could be correlated to the formation of a eutectic mixture between the drug and the binder. Stability studies indicated that the granule properties do not change, at least after 1 year of storage at 25 degrees C. In conclusion, the results of this work suggest that the melt granulation technique is an easy and fast method to improve the dissolution rate of ibuprofen, using poloxamer 188 as a new hydrophilic meltable binder. SN - 0928-0987 UR - https://www.unboundmedicine.com/medline/citation/11803133/Preparation_and_characterisation_of_ibuprofen_poloxamer_188_granules_obtained_by_melt_granulation_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S092809870100210X DB - PRIME DP - Unbound Medicine ER -