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Biomimetic Dissolution: A Tool to Predict Amorphous Solid Dispersion Performance.
AAPS PharmSciTech. 2017 Nov; 18(8):2841-2853.AP

Abstract

The presented study describes the development of a membrane permeation non-sink dissolution method that can provide analysis of complete drug speciation and emulate the in vivo performance of poorly water-soluble Biopharmaceutical Classification System class II compounds. The designed membrane permeation methodology permits evaluation of free/dissolved/unbound drug from amorphous solid dispersion formulations with the use of a two-cell apparatus, biorelevant dissolution media, and a biomimetic polymer membrane. It offers insight into oral drug dissolution, permeation, and absorption. Amorphous solid dispersions of felodipine were prepared by hot melt extrusion and spray drying techniques and evaluated for in vitro performance. Prior to ranking performance of extruded and spray-dried felodipine solid dispersions, optimization of the dissolution methodology was performed for parameters such as agitation rate, membrane type, and membrane pore size. The particle size and zeta potential were analyzed during dissolution experiments to understand drug/polymer speciation and supersaturation sustainment of felodipine solid dispersions. Bland-Altman analysis was performed to measure the agreement or equivalence between dissolution profiles acquired using polymer membranes and porcine intestines and to establish the biomimetic nature of the treated polymer membranes. The utility of the membrane permeation dissolution methodology is seen during the evaluation of felodipine solid dispersions produced by spray drying and hot melt extrusion. The membrane permeation dissolution methodology can suggest formulation performance and be employed as a screening tool for selection of candidates to move forward to pharmacokinetic studies. Furthermore, the presented model is a cost-effective technique.

Authors+Show Affiliations

Hovione LLC, 40 Lake Drive, East Windsor, New Jersey, 08520, USA. michael.puppolo@temple.edu. Department of Chemistry, Temple University, 1901 North 13th Street, Philadelphia, Pennsylvania, 19122, USA. michael.puppolo@temple.edu.Banner Life Sciences, 4215 Premier Drive, High Point, North Carolina, 27265, USA.Hovione LLC, 40 Lake Drive, East Windsor, New Jersey, 08520, USA.Hovione LLC, 40 Lake Drive, East Windsor, New Jersey, 08520, USA.Department of Chemistry, Temple University, 1901 North 13th Street, Philadelphia, Pennsylvania, 19122, USA.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

28560506

Citation

Puppolo, Michael M., et al. "Biomimetic Dissolution: a Tool to Predict Amorphous Solid Dispersion Performance." AAPS PharmSciTech, vol. 18, no. 8, 2017, pp. 2841-2853.
Puppolo MM, Hughey JR, Dillon T, et al. Biomimetic Dissolution: A Tool to Predict Amorphous Solid Dispersion Performance. AAPS PharmSciTech. 2017;18(8):2841-2853.
Puppolo, M. M., Hughey, J. R., Dillon, T., Storey, D., & Jansen-Varnum, S. (2017). Biomimetic Dissolution: A Tool to Predict Amorphous Solid Dispersion Performance. AAPS PharmSciTech, 18(8), 2841-2853. https://doi.org/10.1208/s12249-017-0783-4
Puppolo MM, et al. Biomimetic Dissolution: a Tool to Predict Amorphous Solid Dispersion Performance. AAPS PharmSciTech. 2017;18(8):2841-2853. PubMed PMID: 28560506.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Biomimetic Dissolution: A Tool to Predict Amorphous Solid Dispersion Performance. AU - Puppolo,Michael M, AU - Hughey,Justin R, AU - Dillon,Traciann, AU - Storey,David, AU - Jansen-Varnum,Susan, Y1 - 2017/05/30/ PY - 2017/01/15/received PY - 2017/04/13/accepted PY - 2017/6/1/pubmed PY - 2018/5/10/medline PY - 2017/6/1/entrez KW - amorphous solid dispersion KW - bioavailability KW - free drug KW - membrane permeation dissolution KW - poorly water soluble SP - 2841 EP - 2853 JF - AAPS PharmSciTech JO - AAPS PharmSciTech VL - 18 IS - 8 N2 - The presented study describes the development of a membrane permeation non-sink dissolution method that can provide analysis of complete drug speciation and emulate the in vivo performance of poorly water-soluble Biopharmaceutical Classification System class II compounds. The designed membrane permeation methodology permits evaluation of free/dissolved/unbound drug from amorphous solid dispersion formulations with the use of a two-cell apparatus, biorelevant dissolution media, and a biomimetic polymer membrane. It offers insight into oral drug dissolution, permeation, and absorption. Amorphous solid dispersions of felodipine were prepared by hot melt extrusion and spray drying techniques and evaluated for in vitro performance. Prior to ranking performance of extruded and spray-dried felodipine solid dispersions, optimization of the dissolution methodology was performed for parameters such as agitation rate, membrane type, and membrane pore size. The particle size and zeta potential were analyzed during dissolution experiments to understand drug/polymer speciation and supersaturation sustainment of felodipine solid dispersions. Bland-Altman analysis was performed to measure the agreement or equivalence between dissolution profiles acquired using polymer membranes and porcine intestines and to establish the biomimetic nature of the treated polymer membranes. The utility of the membrane permeation dissolution methodology is seen during the evaluation of felodipine solid dispersions produced by spray drying and hot melt extrusion. The membrane permeation dissolution methodology can suggest formulation performance and be employed as a screening tool for selection of candidates to move forward to pharmacokinetic studies. Furthermore, the presented model is a cost-effective technique. SN - 1530-9932 UR - https://www.unboundmedicine.com/medline/citation/28560506/Biomimetic_Dissolution:_A_Tool_to_Predict_Amorphous_Solid_Dispersion_Performance_ L2 - https://dx.doi.org/10.1208/s12249-017-0783-4 DB - PRIME DP - Unbound Medicine ER -