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Use of conventional surfactant media as surrogates for FaSSIF in simulating in vivo dissolution of BCS class II drugs.
Eur J Pharm Biopharm. 2011 Aug; 78(3):531-8.EJ

Abstract

The usefulness of selected conventional surfactant media to enhance dissolution of BCS class II drugs similarly to fasted state simulated intestinal fluid (FaSSIF) and to predict the absorption of drugs in vivo was evaluated. Dissolution behavior of danazol (Danol), spironolactone (Spiridon) and N74 (phase I compound) was compared between FaSSIF, containing physiological levels of sodium taurocholate (STC) and lecithin, and dissolution media containing various concentrations of anionic surfactant, sodium lauryl sulfate (SLS) or non-ionic surfactant, polysorbate (Tween) 80. Although these media differed largely in their solubilization ability, micelle size, diffusivity and surface tension, similar dissolution enhancing levels were achieved between FaSSIF and drug-specific concentrations of conventional surfactants. The dissolution enhancement was shown, however, to be important only for danazol and N74, molecules that are characterized by high hydrophobicity. An in vivo pharmacokinetic dog study was carried out with N74. Comparison of observed plasma profiles with simulated profiles obtained using compartmental absorption and transit model (CAT) indicated that 0.1% SLS medium was the best to predict in vivo plasma profiles and pharmacokinetic parameters (C(max) and AUC). This study demonstrates the potential of substituting FaSSIF with more simple and cost-effective conventional surfactant media. Use of in vivo prognostic amounts of synthetic surfactants in dissolution testing could largely assist in industrial drug development as well as in quality control purposes.

Authors+Show Affiliations

Division of Pharmaceutical Technology, University of Helsinki, Helsinki, Finland.No affiliation info availableNo affiliation info availableNo affiliation info availableNo 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

21329757

Citation

Lehto, Paula, et al. "Use of Conventional Surfactant Media as Surrogates for FaSSIF in Simulating in Vivo Dissolution of BCS Class II Drugs." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 78, no. 3, 2011, pp. 531-8.
Lehto P, Kortejärvi H, Liimatainen A, et al. Use of conventional surfactant media as surrogates for FaSSIF in simulating in vivo dissolution of BCS class II drugs. Eur J Pharm Biopharm. 2011;78(3):531-8.
Lehto, P., Kortejärvi, H., Liimatainen, A., Ojala, K., Kangas, H., Hirvonen, J., Tanninen, V. P., & Peltonen, L. (2011). Use of conventional surfactant media as surrogates for FaSSIF in simulating in vivo dissolution of BCS class II drugs. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 78(3), 531-8. https://doi.org/10.1016/j.ejpb.2011.02.007
Lehto P, et al. Use of Conventional Surfactant Media as Surrogates for FaSSIF in Simulating in Vivo Dissolution of BCS Class II Drugs. Eur J Pharm Biopharm. 2011;78(3):531-8. PubMed PMID: 21329757.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Use of conventional surfactant media as surrogates for FaSSIF in simulating in vivo dissolution of BCS class II drugs. AU - Lehto,Paula, AU - Kortejärvi,Hanna, AU - Liimatainen,Anni, AU - Ojala,Krista, AU - Kangas,Heli, AU - Hirvonen,Jouni, AU - Tanninen,Veli Pekka, AU - Peltonen,Leena, Y1 - 2011/02/15/ PY - 2009/12/22/received PY - 2011/01/26/revised PY - 2011/02/09/accepted PY - 2011/2/19/entrez PY - 2011/2/19/pubmed PY - 2012/1/25/medline SP - 531 EP - 8 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 78 IS - 3 N2 - The usefulness of selected conventional surfactant media to enhance dissolution of BCS class II drugs similarly to fasted state simulated intestinal fluid (FaSSIF) and to predict the absorption of drugs in vivo was evaluated. Dissolution behavior of danazol (Danol), spironolactone (Spiridon) and N74 (phase I compound) was compared between FaSSIF, containing physiological levels of sodium taurocholate (STC) and lecithin, and dissolution media containing various concentrations of anionic surfactant, sodium lauryl sulfate (SLS) or non-ionic surfactant, polysorbate (Tween) 80. Although these media differed largely in their solubilization ability, micelle size, diffusivity and surface tension, similar dissolution enhancing levels were achieved between FaSSIF and drug-specific concentrations of conventional surfactants. The dissolution enhancement was shown, however, to be important only for danazol and N74, molecules that are characterized by high hydrophobicity. An in vivo pharmacokinetic dog study was carried out with N74. Comparison of observed plasma profiles with simulated profiles obtained using compartmental absorption and transit model (CAT) indicated that 0.1% SLS medium was the best to predict in vivo plasma profiles and pharmacokinetic parameters (C(max) and AUC). This study demonstrates the potential of substituting FaSSIF with more simple and cost-effective conventional surfactant media. Use of in vivo prognostic amounts of synthetic surfactants in dissolution testing could largely assist in industrial drug development as well as in quality control purposes. SN - 1873-3441 UR - https://www.unboundmedicine.com/medline/citation/21329757/Use_of_conventional_surfactant_media_as_surrogates_for_FaSSIF_in_simulating_in_vivo_dissolution_of_BCS_class_II_drugs_ DB - PRIME DP - Unbound Medicine ER -