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Optimizing the ability of PVP/PEG mixtures to be used as appropriate carriers for the preparation of drug solid dispersions by melt mixing technique using artificial neural networks: I.
Eur J Pharm Biopharm. 2012 Sep; 82(1):175-86.EJ

Abstract

In the present study, the efficiency of PVP/PEG200 mixtures as appropriate carries for the preparation of solid dispersions by melt mixing was evaluated. Felodipine (FELO) was used as a poorly water soluble model drug. The effect of several melt mixing parameters, (PVP/PEG ratio, time and temperature of melt mixing, and drug content), on the physical state of FELO and the dissolution characteristics of the dispersions were investigated. DSC, XRD, and SEM analysis revealed that in all cases, amorphous drug nanodispersions were prepared. This was attributed to the increased miscibility of the PVP-FELO system, induced by the presence of PEG200, which acted as plasticizer. FT-IR analysis showed hydrogen bonding between FELO (NH) and the PVP carrier (CO). The release rate of the drug depends mainly on the drug content and is higher in solid dispersions with low drug content and ratio of carrier to plasticizer (PVP/PEG200). The melt mixing variations (time and temperature of mixing) had lower impact on FELO release rate. Finally, artificial neural networks, used to correlate the examined formulation and process variables of hot melt mixing with dissolution parameters, showed good prediction ability.

Authors+Show Affiliations

Laboratory of Polymer Chemistry and Technology, Department of Chemistry, Aristotle University of Thessaloniki, Thessaloniki, Greece.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22732266

Citation

Papadimitriou, Sofia A., et al. "Optimizing the Ability of PVP/PEG Mixtures to Be Used as Appropriate Carriers for the Preparation of Drug Solid Dispersions By Melt Mixing Technique Using Artificial Neural Networks: I." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 82, no. 1, 2012, pp. 175-86.
Papadimitriou SA, Barmpalexis P, Karavas E, et al. Optimizing the ability of PVP/PEG mixtures to be used as appropriate carriers for the preparation of drug solid dispersions by melt mixing technique using artificial neural networks: I. Eur J Pharm Biopharm. 2012;82(1):175-86.
Papadimitriou, S. A., Barmpalexis, P., Karavas, E., & Bikiaris, D. N. (2012). Optimizing the ability of PVP/PEG mixtures to be used as appropriate carriers for the preparation of drug solid dispersions by melt mixing technique using artificial neural networks: I. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 82(1), 175-86. https://doi.org/10.1016/j.ejpb.2012.06.003
Papadimitriou SA, et al. Optimizing the Ability of PVP/PEG Mixtures to Be Used as Appropriate Carriers for the Preparation of Drug Solid Dispersions By Melt Mixing Technique Using Artificial Neural Networks: I. Eur J Pharm Biopharm. 2012;82(1):175-86. PubMed PMID: 22732266.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Optimizing the ability of PVP/PEG mixtures to be used as appropriate carriers for the preparation of drug solid dispersions by melt mixing technique using artificial neural networks: I. AU - Papadimitriou,Sofia A, AU - Barmpalexis,Panagiotis, AU - Karavas,Evangelos, AU - Bikiaris,Dimitrios N, Y1 - 2012/06/23/ PY - 2012/03/06/received PY - 2012/05/12/revised PY - 2012/06/04/accepted PY - 2012/6/27/entrez PY - 2012/6/27/pubmed PY - 2013/2/6/medline SP - 175 EP - 86 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 82 IS - 1 N2 - In the present study, the efficiency of PVP/PEG200 mixtures as appropriate carries for the preparation of solid dispersions by melt mixing was evaluated. Felodipine (FELO) was used as a poorly water soluble model drug. The effect of several melt mixing parameters, (PVP/PEG ratio, time and temperature of melt mixing, and drug content), on the physical state of FELO and the dissolution characteristics of the dispersions were investigated. DSC, XRD, and SEM analysis revealed that in all cases, amorphous drug nanodispersions were prepared. This was attributed to the increased miscibility of the PVP-FELO system, induced by the presence of PEG200, which acted as plasticizer. FT-IR analysis showed hydrogen bonding between FELO (NH) and the PVP carrier (CO). The release rate of the drug depends mainly on the drug content and is higher in solid dispersions with low drug content and ratio of carrier to plasticizer (PVP/PEG200). The melt mixing variations (time and temperature of mixing) had lower impact on FELO release rate. Finally, artificial neural networks, used to correlate the examined formulation and process variables of hot melt mixing with dissolution parameters, showed good prediction ability. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/22732266/Optimizing_the_ability_of_PVP/PEG_mixtures_to_be_used_as_appropriate_carriers_for_the_preparation_of_drug_solid_dispersions_by_melt_mixing_technique_using_artificial_neural_networks:_I_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(12)00190-7 DB - PRIME DP - Unbound Medicine ER -