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Amorphous-state characterization of efavirenz--polymer hot-melt extrusion systems for dissolution enhancement.
J Pharm Sci. 2012 Sep; 101(9):3456-64.JP

Abstract

The aim of this study was to improve the dissolution rate of efavirenz (EFV) by formulating a physically stable dispersion in polymers. Hot-melt extrusion (HME) was used to prepare solid solutions of EFV with Eudragit EPO (a low-glass transition polymer) or Plasdone S-630 (a high-glass transition polymer). The drug-polymer blends were characterized for their thermal and rheological properties as a function of drug concentration to understand their miscibility and processability by HME. The solid-state stability of extrudates was characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, and dissolution studies. Thermal and rheological studies revealed that the drug is miscible with both polymers, and a decrease in melt viscosity was observed as the drug concentration increased. XRD and DSC studies confirmed the existence of amorphous state of EFV in the extrudates during storage. The dissolution rate of EFV from the extrudates was substantially higher than the crystalline drug. FTIR studies revealed an interaction between the EFV and Plasdone S-630, which reduced the molecular mobility and prevented crystallization upon storage. EFV and Eudragit EPO systems lack specific interactions, but are less susceptible to crystallization due to the antiplasticization effect of the polymer.

Authors+Show Affiliations

Department of Pharmacal Sciences, Auburn University, Auburn, Alabama 36849, USA.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

22437488

Citation

Sathigari, Sateesh Kumar, et al. "Amorphous-state Characterization of Efavirenz--polymer Hot-melt Extrusion Systems for Dissolution Enhancement." Journal of Pharmaceutical Sciences, vol. 101, no. 9, 2012, pp. 3456-64.
Sathigari SK, Radhakrishnan VK, Davis VA, et al. Amorphous-state characterization of efavirenz--polymer hot-melt extrusion systems for dissolution enhancement. J Pharm Sci. 2012;101(9):3456-64.
Sathigari, S. K., Radhakrishnan, V. K., Davis, V. A., Parsons, D. L., & Babu, R. J. (2012). Amorphous-state characterization of efavirenz--polymer hot-melt extrusion systems for dissolution enhancement. Journal of Pharmaceutical Sciences, 101(9), 3456-64. https://doi.org/10.1002/jps.23125
Sathigari SK, et al. Amorphous-state Characterization of Efavirenz--polymer Hot-melt Extrusion Systems for Dissolution Enhancement. J Pharm Sci. 2012;101(9):3456-64. PubMed PMID: 22437488.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Amorphous-state characterization of efavirenz--polymer hot-melt extrusion systems for dissolution enhancement. AU - Sathigari,Sateesh Kumar, AU - Radhakrishnan,Vinod K, AU - Davis,Virginia A, AU - Parsons,Daniel L, AU - Babu,R Jayachandra, Y1 - 2012/03/21/ PY - 2011/11/06/received PY - 2012/02/29/accepted PY - 2012/02/05/revised PY - 2012/3/23/entrez PY - 2012/3/23/pubmed PY - 2012/12/12/medline SP - 3456 EP - 64 JF - Journal of pharmaceutical sciences JO - J Pharm Sci VL - 101 IS - 9 N2 - The aim of this study was to improve the dissolution rate of efavirenz (EFV) by formulating a physically stable dispersion in polymers. Hot-melt extrusion (HME) was used to prepare solid solutions of EFV with Eudragit EPO (a low-glass transition polymer) or Plasdone S-630 (a high-glass transition polymer). The drug-polymer blends were characterized for their thermal and rheological properties as a function of drug concentration to understand their miscibility and processability by HME. The solid-state stability of extrudates was characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier transform infrared (FTIR) spectroscopy, and dissolution studies. Thermal and rheological studies revealed that the drug is miscible with both polymers, and a decrease in melt viscosity was observed as the drug concentration increased. XRD and DSC studies confirmed the existence of amorphous state of EFV in the extrudates during storage. The dissolution rate of EFV from the extrudates was substantially higher than the crystalline drug. FTIR studies revealed an interaction between the EFV and Plasdone S-630, which reduced the molecular mobility and prevented crystallization upon storage. EFV and Eudragit EPO systems lack specific interactions, but are less susceptible to crystallization due to the antiplasticization effect of the polymer. SN - 1520-6017 UR - https://www.unboundmedicine.com/medline/citation/22437488/Amorphous_state_characterization_of_efavirenz__polymer_hot_melt_extrusion_systems_for_dissolution_enhancement_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0022-3549(15)31431-3 DB - PRIME DP - Unbound Medicine ER -