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Formulation and characterization of ternary solid dispersions made up of Itraconazole and two excipients, TPGS 1000 and PVPVA 64, that were selected based on a supersaturation screening study.
Eur J Pharm Biopharm. 2008 May; 69(1):158-66.EJ

Abstract

Both d-alpha-tocopheryl polyethylene glycol 1000 (TPGS 1000) and polyvidone-vinylacetate 64 (PVPVA 64) provided an increase in the degree of supersaturation and stability of supersaturated Itraconazole solutions, compared to a blanc without excipient. Therefore, both components were combined as carrier in order to make ternary solid dispersions of Itraconazole by spray drying. This way, TPGS 1000 could be incorporated into a powder. Dissolution experiments on the ternary solid dispersions revealed that during the first hour the release was much higher than for the binary Itraconazole/PVPVA 64 solid dispersions. For some compositions a release of more than 80% was reached after 10min. However, after the first hour the drug started to precipitate. The ternary solid dispersions were all XRD amorphous, but MDSC revealed the coexistence of multiple amorphous phases and a crystalline Itraconazole phase, depending on the composition. Therefore the burst effect during the first hour can be ascribed to an accelerated dissolution of the amorphous Itraconazole fraction in the presence of TPGS 1000. The precipitation after 1h, however, is probably due to the combination of the surfactant properties of TPGS and the small crystalline Itraconazole fraction.

Authors+Show Affiliations

Laboratorium voor Farmacotechnologie en Biofarmacie, Catholic University of Leuven, Leuven, Belgium.No 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

18164929

Citation

Janssens, Sandrien, et al. "Formulation and Characterization of Ternary Solid Dispersions Made Up of Itraconazole and Two Excipients, TPGS 1000 and PVPVA 64, That Were Selected Based On a Supersaturation Screening Study." European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, vol. 69, no. 1, 2008, pp. 158-66.
Janssens S, Nagels S, Armas HN, et al. Formulation and characterization of ternary solid dispersions made up of Itraconazole and two excipients, TPGS 1000 and PVPVA 64, that were selected based on a supersaturation screening study. Eur J Pharm Biopharm. 2008;69(1):158-66.
Janssens, S., Nagels, S., Armas, H. N., D'Autry, W., Van Schepdael, A., & Van den Mooter, G. (2008). Formulation and characterization of ternary solid dispersions made up of Itraconazole and two excipients, TPGS 1000 and PVPVA 64, that were selected based on a supersaturation screening study. European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Fur Pharmazeutische Verfahrenstechnik E.V, 69(1), 158-66. https://doi.org/10.1016/j.ejpb.2007.11.004
Janssens S, et al. Formulation and Characterization of Ternary Solid Dispersions Made Up of Itraconazole and Two Excipients, TPGS 1000 and PVPVA 64, That Were Selected Based On a Supersaturation Screening Study. Eur J Pharm Biopharm. 2008;69(1):158-66. PubMed PMID: 18164929.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Formulation and characterization of ternary solid dispersions made up of Itraconazole and two excipients, TPGS 1000 and PVPVA 64, that were selected based on a supersaturation screening study. AU - Janssens,Sandrien, AU - Nagels,Sophie, AU - Armas,Hector Novoa de, AU - D'Autry,Ward, AU - Van Schepdael,Ann, AU - Van den Mooter,Guy, Y1 - 2007/11/19/ PY - 2007/10/16/received PY - 2007/11/12/accepted PY - 2008/1/1/pubmed PY - 2008/8/12/medline PY - 2008/1/1/entrez SP - 158 EP - 66 JF - European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V JO - Eur J Pharm Biopharm VL - 69 IS - 1 N2 - Both d-alpha-tocopheryl polyethylene glycol 1000 (TPGS 1000) and polyvidone-vinylacetate 64 (PVPVA 64) provided an increase in the degree of supersaturation and stability of supersaturated Itraconazole solutions, compared to a blanc without excipient. Therefore, both components were combined as carrier in order to make ternary solid dispersions of Itraconazole by spray drying. This way, TPGS 1000 could be incorporated into a powder. Dissolution experiments on the ternary solid dispersions revealed that during the first hour the release was much higher than for the binary Itraconazole/PVPVA 64 solid dispersions. For some compositions a release of more than 80% was reached after 10min. However, after the first hour the drug started to precipitate. The ternary solid dispersions were all XRD amorphous, but MDSC revealed the coexistence of multiple amorphous phases and a crystalline Itraconazole phase, depending on the composition. Therefore the burst effect during the first hour can be ascribed to an accelerated dissolution of the amorphous Itraconazole fraction in the presence of TPGS 1000. The precipitation after 1h, however, is probably due to the combination of the surfactant properties of TPGS and the small crystalline Itraconazole fraction. SN - 0939-6411 UR - https://www.unboundmedicine.com/medline/citation/18164929/Formulation_and_characterization_of_ternary_solid_dispersions_made_up_of_Itraconazole_and_two_excipients_TPGS_1000_and_PVPVA_64_that_were_selected_based_on_a_supersaturation_screening_study_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0939-6411(07)00383-9 DB - PRIME DP - Unbound Medicine ER -