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Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances.
Pharmaceutics. 2020 Jun 12; 12(6)P

Abstract

Delivery of poorly water soluble active pharmaceutical ingredients (APIs) by semi-crystalline solid dispersions prepared by spray congealing in form of microparticles (MPs) is an emerging method to increase their oral bioavailability. In this study, solid dispersions based on hydrophilic Gelucires® (Gelucire® 50/13 and Gelucire® 48/16 in different ratio) of three BCS class II model compounds (carbamazepine, CBZ, tolbutamide, TBM, and cinnarizine, CIN) having different physicochemical properties (logP, pKa, Tm) were produced by spray congealing process. The obtained MPs were investigated in terms of morphology, particles size, drug content, solid state properties, drug-carrier interactions, solubility, and dissolution performances. The solid-state characterization showed that the properties of the incorporated drug had a profound influence on the structure of the obtained solid dispersion: CBZ recrystallized in a different polymorphic form, TBM crystallinity was significantly reduced as a result of specific interactions with the carrier, while smaller crystals were observed in case of CIN. The in vitro tests suggested that the drug solubility was mainly influenced by carrier composition, while the drug dissolution behavior was affected by the API solid state in the MPs after the spray congealing process. Among the tested APIs, TBM-Gelucire dispersions showed the highest enhancement in drug dissolution as a result of the reduced drug crystallinity.

Authors+Show Affiliations

Department of Pharmacy and BioTechnology, Alma Mater Studiorum-University of Bologna, Via S. Donato 19/2, 40127 Bologna, Italy.Department of Pharmacy and BioTechnology, Alma Mater Studiorum-University of Bologna, Via S. Donato 19/2, 40127 Bologna, Italy.Department of Pharmacy and BioTechnology, Alma Mater Studiorum-University of Bologna, Via S. Donato 19/2, 40127 Bologna, Italy.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32545643

Citation

Bertoni, Serena, et al. "Different BCS Class II Drug-Gelucire Solid Dispersions Prepared By Spray Congealing: Evaluation of Solid State Properties and in Vitro Performances." Pharmaceutics, vol. 12, no. 6, 2020.
Bertoni S, Albertini B, Passerini N. Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances. Pharmaceutics. 2020;12(6).
Bertoni, S., Albertini, B., & Passerini, N. (2020). Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances. Pharmaceutics, 12(6). https://doi.org/10.3390/pharmaceutics12060548
Bertoni S, Albertini B, Passerini N. Different BCS Class II Drug-Gelucire Solid Dispersions Prepared By Spray Congealing: Evaluation of Solid State Properties and in Vitro Performances. Pharmaceutics. 2020 Jun 12;12(6) PubMed PMID: 32545643.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances. AU - Bertoni,Serena, AU - Albertini,Beatrice, AU - Passerini,Nadia, Y1 - 2020/06/12/ PY - 2020/04/28/received PY - 2020/06/05/revised PY - 2020/06/10/accepted PY - 2020/6/18/entrez PY - 2020/6/18/pubmed PY - 2020/6/18/medline KW - Gelucire KW - carbamazepine KW - cinnarizine KW - microparticles KW - semicrystalline solid dispersions KW - spray chilling KW - spray cooling KW - tolbutamide JF - Pharmaceutics JO - Pharmaceutics VL - 12 IS - 6 N2 - Delivery of poorly water soluble active pharmaceutical ingredients (APIs) by semi-crystalline solid dispersions prepared by spray congealing in form of microparticles (MPs) is an emerging method to increase their oral bioavailability. In this study, solid dispersions based on hydrophilic Gelucires® (Gelucire® 50/13 and Gelucire® 48/16 in different ratio) of three BCS class II model compounds (carbamazepine, CBZ, tolbutamide, TBM, and cinnarizine, CIN) having different physicochemical properties (logP, pKa, Tm) were produced by spray congealing process. The obtained MPs were investigated in terms of morphology, particles size, drug content, solid state properties, drug-carrier interactions, solubility, and dissolution performances. The solid-state characterization showed that the properties of the incorporated drug had a profound influence on the structure of the obtained solid dispersion: CBZ recrystallized in a different polymorphic form, TBM crystallinity was significantly reduced as a result of specific interactions with the carrier, while smaller crystals were observed in case of CIN. The in vitro tests suggested that the drug solubility was mainly influenced by carrier composition, while the drug dissolution behavior was affected by the API solid state in the MPs after the spray congealing process. Among the tested APIs, TBM-Gelucire dispersions showed the highest enhancement in drug dissolution as a result of the reduced drug crystallinity. SN - 1999-4923 UR - https://www.unboundmedicine.com/medline/citation/32545643/Different_BCS_Class_II_Drug-Gelucire_Solid_Dispersions_Prepared_by_Spray_Congealing:_Evaluation_of_Solid_State_Properties_and_In_Vitro_Performances L2 - https://www.mdpi.com/resolver?pii=pharmaceutics12060548 DB - PRIME DP - Unbound Medicine ER -
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