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Determination of drug-polymer solubility from supersaturated spray-dried amorphous solid dispersions: A case study with Efavirenz and Soluplus®.
Eur J Pharm Biopharm. 2019 Sep; 142:300-306.EJ

Abstract

Amorphous solid dispersions (ASDs) are found to be a well-established strategy for overcoming limited aqueous solubility and poor oral bioavailability of active pharmaceutical ingredients (APIs). One of the main parameters affecting ASDs physical stability is the API solubility in the carrier, because this value determines the maximal API load without a risk of phase separation and recrystallization. Phase-diagrams can be experimentally obtained by following the recrystallization of the API from a supersaturated homogeneous API-polymer solid solution, commonly produced by processes as solvent casting or comilling, which are very time-consuming (hours). The work deals with the construction of a temperature-composition EFV-Soluplus® phase diagram, from a thermal study of recrystallization of a supersaturated solid solution (85 wt% in EFV) generated by spray drying. This supersaturated solution is kept at a given annealing temperature to reach the equilibrium state and the amount that still remains dispersed in the polymer carrier at this equilibrium temperature is determined by means of the new glass transition temperature of the binary mixture. From our knowledge, this is the first study employing a fast process (spray drying) to prepare a supersaturated solid solution of an API in a polymer aiming to determine a temperature-composition phase diagram. The EFV solubility in Soluplus ranges from 20 wt% at 25 °C to 30 wt% at 40 °C. It can be a very useful preformulation tool for researchers studying amorphous solid dispersions of Efavirenz in Soluplus, to assist for predicting the stability of EFV-Soluplus ASDs at different EFV loadings and under different thermal conditions.

Authors+Show Affiliations

Université de Toulouse, Ecole des Mines d'Albi, UMR CNRS 5302, Centre RAPSODEE, F-81013 Albi, France. Electronic address: bhianca.lins_de_azevedo_costa@mines-albi.fr.Université de Toulouse, Ecole des Mines d'Albi, UMR CNRS 5302, Centre RAPSODEE, F-81013 Albi, France.Université de Toulouse, Ecole des Mines d'Albi, UMR CNRS 5302, Centre RAPSODEE, F-81013 Albi, France.Université de Toulouse, Ecole des Mines d'Albi, UMR CNRS 5302, Centre RAPSODEE, F-81013 Albi, France.Université de Toulouse, Ecole des Mines d'Albi, UMR CNRS 5302, Centre RAPSODEE, F-81013 Albi, France.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

31247317

Citation

Costa, B L A., et al. "Determination of Drug-polymer Solubility From Supersaturated Spray-dried Amorphous Solid Dispersions: a Case Study With Efavirenz and Soluplus®." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 142, 2019, pp. 300-306.
Costa BLA, Sauceau M, Del Confetto S, et al. Determination of drug-polymer solubility from supersaturated spray-dried amorphous solid dispersions: A case study with Efavirenz and Soluplus®. Eur J Pharm Biopharm. 2019;142:300-306.
Costa, B. L. A., Sauceau, M., Del Confetto, S., Sescousse, R., & Ré, M. I. (2019). Determination of drug-polymer solubility from supersaturated spray-dried amorphous solid dispersions: A case study with Efavirenz and Soluplus®. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 142, 300-306. https://doi.org/10.1016/j.ejpb.2019.06.028
Costa BLA, et al. Determination of Drug-polymer Solubility From Supersaturated Spray-dried Amorphous Solid Dispersions: a Case Study With Efavirenz and Soluplus®. Eur J Pharm Biopharm. 2019;142:300-306. PubMed PMID: 31247317.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Determination of drug-polymer solubility from supersaturated spray-dried amorphous solid dispersions: A case study with Efavirenz and Soluplus®. AU - Costa,B L A, AU - Sauceau,M, AU - Del Confetto,S, AU - Sescousse,R, AU - Ré,M I, Y1 - 2019/06/24/ PY - 2018/07/27/received PY - 2019/04/17/revised PY - 2019/06/23/accepted PY - 2019/6/28/pubmed PY - 2019/11/26/medline PY - 2019/6/28/entrez KW - Amorphous solid dispersions KW - Efavirenz KW - Phase diagram KW - Recrystallization method KW - Solubility KW - Soluplus® KW - Spray drying SP - 300 EP - 306 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 142 N2 - Amorphous solid dispersions (ASDs) are found to be a well-established strategy for overcoming limited aqueous solubility and poor oral bioavailability of active pharmaceutical ingredients (APIs). One of the main parameters affecting ASDs physical stability is the API solubility in the carrier, because this value determines the maximal API load without a risk of phase separation and recrystallization. Phase-diagrams can be experimentally obtained by following the recrystallization of the API from a supersaturated homogeneous API-polymer solid solution, commonly produced by processes as solvent casting or comilling, which are very time-consuming (hours). The work deals with the construction of a temperature-composition EFV-Soluplus® phase diagram, from a thermal study of recrystallization of a supersaturated solid solution (85 wt% in EFV) generated by spray drying. This supersaturated solution is kept at a given annealing temperature to reach the equilibrium state and the amount that still remains dispersed in the polymer carrier at this equilibrium temperature is determined by means of the new glass transition temperature of the binary mixture. From our knowledge, this is the first study employing a fast process (spray drying) to prepare a supersaturated solid solution of an API in a polymer aiming to determine a temperature-composition phase diagram. The EFV solubility in Soluplus ranges from 20 wt% at 25 °C to 30 wt% at 40 °C. It can be a very useful preformulation tool for researchers studying amorphous solid dispersions of Efavirenz in Soluplus, to assist for predicting the stability of EFV-Soluplus ASDs at different EFV loadings and under different thermal conditions. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/31247317/Determination_of_drug_polymer_solubility_from_supersaturated_spray_dried_amorphous_solid_dispersions:_A_case_study_with_Efavirenz_and_Soluplus®_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(18)30911-1 DB - PRIME DP - Unbound Medicine ER -