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Formulation, characterization and in vitro evaluation of theophylline-loaded Eudragit RS 100 microspheres prepared by an emulsion-solvent diffusion/evaporation technique.
Pharm Dev Technol. 2011 Nov-Dec; 16(6):637-44.PD

Abstract

The aim was to prepare theophylline-loaded Eudragit RS 100 microsphere to achieve sustained release pattern with relatively high production yield. To this end, microspheres were prepared by oil/oil solvent evaporation method using an acetone-methanol mixture and liquid paraffin system containing aluminum tristearate. Drug release profiles were determined at pH 1.2 and 7.4. Morphology and solid state of microspheres were examined using SEM, DSC, X-ray powder diffraction (XRPD), and FT-IR. As the ratio of acetone/methanol increased during the preparation of microspheres the size of microsphere was reduced. The highest drug loading efficiency (87.21%) was obtained for the microsphere containing a high ratio of polymer to drug (6:1) and high volume of acetone. SEM studies showed that the microspheres are almost spherical with a few pores and cracks at surfaces. The FT-IR, XRPD and DSC results ruled out any chemical interaction between theophylline and Eudragit. The microspheres prepared with low ratio of polymer to drug (1:2) showed faster dissolution rate than those with high polymer to drug ratio. The ratio of polymer to drug and the volume of polymer solvent were found to be the key factors affecting the release profile which could lead to microspheres with desired release behavior.

Authors+Show Affiliations

Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.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

20722498

Citation

Jelvehgari, Mitra, et al. "Formulation, Characterization and in Vitro Evaluation of Theophylline-loaded Eudragit RS 100 Microspheres Prepared By an Emulsion-solvent Diffusion/evaporation Technique." Pharmaceutical Development and Technology, vol. 16, no. 6, 2011, pp. 637-44.
Jelvehgari M, Barar J, Valizadeh H, et al. Formulation, characterization and in vitro evaluation of theophylline-loaded Eudragit RS 100 microspheres prepared by an emulsion-solvent diffusion/evaporation technique. Pharm Dev Technol. 2011;16(6):637-44.
Jelvehgari, M., Barar, J., Valizadeh, H., Shadrou, S., & Nokhodchi, A. (2011). Formulation, characterization and in vitro evaluation of theophylline-loaded Eudragit RS 100 microspheres prepared by an emulsion-solvent diffusion/evaporation technique. Pharmaceutical Development and Technology, 16(6), 637-44. https://doi.org/10.3109/10837450.2010.508075
Jelvehgari M, et al. Formulation, Characterization and in Vitro Evaluation of Theophylline-loaded Eudragit RS 100 Microspheres Prepared By an Emulsion-solvent Diffusion/evaporation Technique. Pharm Dev Technol. 2011 Nov-Dec;16(6):637-44. PubMed PMID: 20722498.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation, characterization and in vitro evaluation of theophylline-loaded Eudragit RS 100 microspheres prepared by an emulsion-solvent diffusion/evaporation technique. AU - Jelvehgari,Mitra, AU - Barar,Jaleh, AU - Valizadeh,Hadi, AU - Shadrou,Sanam, AU - Nokhodchi,Ali, Y1 - 2010/08/19/ PY - 2010/8/21/entrez PY - 2010/8/21/pubmed PY - 2012/3/6/medline SP - 637 EP - 44 JF - Pharmaceutical development and technology JO - Pharm Dev Technol VL - 16 IS - 6 N2 - The aim was to prepare theophylline-loaded Eudragit RS 100 microsphere to achieve sustained release pattern with relatively high production yield. To this end, microspheres were prepared by oil/oil solvent evaporation method using an acetone-methanol mixture and liquid paraffin system containing aluminum tristearate. Drug release profiles were determined at pH 1.2 and 7.4. Morphology and solid state of microspheres were examined using SEM, DSC, X-ray powder diffraction (XRPD), and FT-IR. As the ratio of acetone/methanol increased during the preparation of microspheres the size of microsphere was reduced. The highest drug loading efficiency (87.21%) was obtained for the microsphere containing a high ratio of polymer to drug (6:1) and high volume of acetone. SEM studies showed that the microspheres are almost spherical with a few pores and cracks at surfaces. The FT-IR, XRPD and DSC results ruled out any chemical interaction between theophylline and Eudragit. The microspheres prepared with low ratio of polymer to drug (1:2) showed faster dissolution rate than those with high polymer to drug ratio. The ratio of polymer to drug and the volume of polymer solvent were found to be the key factors affecting the release profile which could lead to microspheres with desired release behavior. SN - 1097-9867 UR - https://www.unboundmedicine.com/medline/citation/20722498/Formulation_characterization_and_in_vitro_evaluation_of_theophylline_loaded_Eudragit_RS_100_microspheres_prepared_by_an_emulsion_solvent_diffusion/evaporation_technique_ L2 - https://www.tandfonline.com/doi/full/10.3109/10837450.2010.508075 DB - PRIME DP - Unbound Medicine ER -