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Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine.
Eur J Pharm Biopharm. 2008 Oct; 70(2):493-9.EJ

Abstract

Amorphous solid dispersions are used as a strategy to improve the bioavailability of poorly water-soluble compounds. When formulating with a polymer, it is important not only for the polymer to stabilize against crystallization in the solid state, but also to improve the dissolution profile through inhibiting crystallization from the supersaturated solution generated by dissolution of the amorphous material. In this study, the dissolution profiles of solid dispersions of felodipine formulated with poly(vinylpyrrolidone) (PVP), hydroxypropyl methylcellulose (HPMC) or hydroxypropyl methylcellulose acetate succinate (HPMCAS) were compared. In addition, concentration versus time profiles were evaluated for the supersaturated solutions of felodipine in the presence and absence of the polymers. HPMCAS was found to maintain the highest level of supersaturation for the greatest length of time for both the dissolution and solution crystallization experiments, whereas PVP was found to be the least effective crystallization inhibitor. All polymers appeared to reduce the crystal growth rates of felodipine at an equivalent supersaturation and this mechanism most likely contributes to the enhanced solution concentration values observed during dissolution of the amorphous solid dispersions.

Authors+Show Affiliations

Pharmaceutical Research and Technology Laboratories, Astellas Pharma Inc., Japan.No affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

18577451

Citation

Konno, Hajime, et al. "Effect of Polymer Type On the Dissolution Profile of Amorphous Solid Dispersions Containing Felodipine." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 70, no. 2, 2008, pp. 493-9.
Konno H, Handa T, Alonzo DE, et al. Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine. Eur J Pharm Biopharm. 2008;70(2):493-9.
Konno, H., Handa, T., Alonzo, D. E., & Taylor, L. S. (2008). Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 70(2), 493-9. https://doi.org/10.1016/j.ejpb.2008.05.023
Konno H, et al. Effect of Polymer Type On the Dissolution Profile of Amorphous Solid Dispersions Containing Felodipine. Eur J Pharm Biopharm. 2008;70(2):493-9. PubMed PMID: 18577451.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effect of polymer type on the dissolution profile of amorphous solid dispersions containing felodipine. AU - Konno,Hajime, AU - Handa,Tetsurou, AU - Alonzo,David E, AU - Taylor,Lynne S, Y1 - 2008/06/06/ PY - 2008/03/25/received PY - 2008/05/14/revised PY - 2008/05/16/accepted PY - 2008/6/26/pubmed PY - 2008/12/17/medline PY - 2008/6/26/entrez SP - 493 EP - 9 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 70 IS - 2 N2 - Amorphous solid dispersions are used as a strategy to improve the bioavailability of poorly water-soluble compounds. When formulating with a polymer, it is important not only for the polymer to stabilize against crystallization in the solid state, but also to improve the dissolution profile through inhibiting crystallization from the supersaturated solution generated by dissolution of the amorphous material. In this study, the dissolution profiles of solid dispersions of felodipine formulated with poly(vinylpyrrolidone) (PVP), hydroxypropyl methylcellulose (HPMC) or hydroxypropyl methylcellulose acetate succinate (HPMCAS) were compared. In addition, concentration versus time profiles were evaluated for the supersaturated solutions of felodipine in the presence and absence of the polymers. HPMCAS was found to maintain the highest level of supersaturation for the greatest length of time for both the dissolution and solution crystallization experiments, whereas PVP was found to be the least effective crystallization inhibitor. All polymers appeared to reduce the crystal growth rates of felodipine at an equivalent supersaturation and this mechanism most likely contributes to the enhanced solution concentration values observed during dissolution of the amorphous solid dispersions. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/18577451/Effect_of_polymer_type_on_the_dissolution_profile_of_amorphous_solid_dispersions_containing_felodipine_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(08)00209-9 DB - PRIME DP - Unbound Medicine ER -