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Development of stability-enhanced ternary solid dispersions via combinations of HPMCP and Soluplus® processed by hot melt extrusion.
Int J Pharm. 2017 Oct 30; 532(1):603-611.IJ

Abstract

The aim of this study was to evaluate a novel combination of hydroxypropyl methylcellulose phthalate (HPMCP-HP-50) and Soluplus® polymers for enhanced physicochemical stability and solubility of the produced amorphous solid dispersions (ASDs). This was achieved using hot melt extrusion (HME) to convert the crystalline active pharmaceutical ingredient (API) into a more soluble amorphous form within the ternary systems. Itraconazole (ITZ), a Biopharmaceutics Classification System class II (BCS II) API, was selected as the model drug. The ASDs were characterized by Powder X-Ray diffraction (PXRD), Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), Fourier Transform Infrared (FTIR) spectroscopy, Solid State Nuclear Magnetic Resonance (ssNMR) and dissolution studies. The data showed that the ASDs were physically and chemically stable at 20°C and 50% RH over 12 months. PXRD results indicated that the ITZ in the ASDs was in the amorphous state and no recrystallization occurred. DSC scans confirmed that each formulation exhibited a single intermediate glass transition (Tg), around 96.4°C, indicating that ITZ was completely miscible in the polymeric blends of HPMCP and Soluplus® at up to 30% (w/w) drug loading and that the two polymers were miscible with each other in the presence of ITZ. The FTIR analysis indicated the formation of strong hydrogen bonding between ITZ, HPMCP and Soluplus®. The dissolution end-point of the ASDs was determined to be approximately 10 times greater than that of the crystalline ITZ.

Authors+Show Affiliations

Synthesis and Solid State Pharmaceutical Cluster (SSPC), Bernal Institute, University of Limerick, Limerick, Ireland. Electronic address: Ahmad.B.Albadarin@ul.ie.Synthesis and Solid State Pharmaceutical Cluster (SSPC), Bernal Institute, University of Limerick, Limerick, Ireland.Synthesis and Solid State Pharmaceutical Cluster (SSPC), Bernal Institute, University of Limerick, Limerick, Ireland.Synthesis and Solid State Pharmaceutical Cluster (SSPC), Bernal Institute, University of Limerick, Limerick, Ireland.Centre for Pharmaceutical Engineering Science, University of Bradford, Bradford, BD7 1DP, United Kingdom.Centre for Pharmaceutical Engineering Science, University of Bradford, Bradford, BD7 1DP, United Kingdom.Centre for Pharmaceutical Engineering Science, University of Bradford, Bradford, BD7 1DP, United Kingdom.Synthesis and Solid State Pharmaceutical Cluster (SSPC), Bernal Institute, University of Limerick, Limerick, Ireland.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28923766

Citation

Albadarin, Ahmad B., et al. "Development of Stability-enhanced Ternary Solid Dispersions Via Combinations of HPMCP and Soluplus® Processed By Hot Melt Extrusion." International Journal of Pharmaceutics, vol. 532, no. 1, 2017, pp. 603-611.
Albadarin AB, Potter CB, Davis MT, et al. Development of stability-enhanced ternary solid dispersions via combinations of HPMCP and Soluplus® processed by hot melt extrusion. Int J Pharm. 2017;532(1):603-611.
Albadarin, A. B., Potter, C. B., Davis, M. T., Iqbal, J., Korde, S., Pagire, S., Paradkar, A., & Walker, G. (2017). Development of stability-enhanced ternary solid dispersions via combinations of HPMCP and Soluplus® processed by hot melt extrusion. International Journal of Pharmaceutics, 532(1), 603-611. https://doi.org/10.1016/j.ijpharm.2017.09.035
Albadarin AB, et al. Development of Stability-enhanced Ternary Solid Dispersions Via Combinations of HPMCP and Soluplus® Processed By Hot Melt Extrusion. Int J Pharm. 2017 Oct 30;532(1):603-611. PubMed PMID: 28923766.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of stability-enhanced ternary solid dispersions via combinations of HPMCP and Soluplus® processed by hot melt extrusion. AU - Albadarin,Ahmad B, AU - Potter,Catherine B, AU - Davis,Mark T, AU - Iqbal,Javed, AU - Korde,Sachin, AU - Pagire,Sudhir, AU - Paradkar,Anant, AU - Walker,Gavin, Y1 - 2017/09/18/ PY - 2017/07/09/received PY - 2017/09/13/revised PY - 2017/09/14/accepted PY - 2017/9/20/pubmed PY - 2018/1/11/medline PY - 2017/9/20/entrez KW - Analytical techniques KW - Dissolution studies KW - Enhanced solubility KW - Itraconazole KW - Physical stability SP - 603 EP - 611 JF - International journal of pharmaceutics JO - Int J Pharm VL - 532 IS - 1 N2 - The aim of this study was to evaluate a novel combination of hydroxypropyl methylcellulose phthalate (HPMCP-HP-50) and Soluplus® polymers for enhanced physicochemical stability and solubility of the produced amorphous solid dispersions (ASDs). This was achieved using hot melt extrusion (HME) to convert the crystalline active pharmaceutical ingredient (API) into a more soluble amorphous form within the ternary systems. Itraconazole (ITZ), a Biopharmaceutics Classification System class II (BCS II) API, was selected as the model drug. The ASDs were characterized by Powder X-Ray diffraction (PXRD), Differential Scanning Calorimetry (DSC), Thermogravimetric Analysis (TGA), Fourier Transform Infrared (FTIR) spectroscopy, Solid State Nuclear Magnetic Resonance (ssNMR) and dissolution studies. The data showed that the ASDs were physically and chemically stable at 20°C and 50% RH over 12 months. PXRD results indicated that the ITZ in the ASDs was in the amorphous state and no recrystallization occurred. DSC scans confirmed that each formulation exhibited a single intermediate glass transition (Tg), around 96.4°C, indicating that ITZ was completely miscible in the polymeric blends of HPMCP and Soluplus® at up to 30% (w/w) drug loading and that the two polymers were miscible with each other in the presence of ITZ. The FTIR analysis indicated the formation of strong hydrogen bonding between ITZ, HPMCP and Soluplus®. The dissolution end-point of the ASDs was determined to be approximately 10 times greater than that of the crystalline ITZ. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/28923766/Development_of_stability_enhanced_ternary_solid_dispersions_via_combinations_of_HPMCP_and_Soluplus®_processed_by_hot_melt_extrusion_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(17)30901-8 DB - PRIME DP - Unbound Medicine ER -