دورية أكاديمية

Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances

التفاصيل البيبلوغرافية
العنوان: Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances
المؤلفون: Serena Bertoni, Beatrice Albertini, Nadia Passerini
المصدر: Pharmaceutics, Vol 12, Iss 6, p 548 (2020)
بيانات النشر: MDPI AG, 2020.
سنة النشر: 2020
المجموعة: LCC:Pharmacy and materia medica
مصطلحات موضوعية: microparticles, spray chilling, spray cooling, Gelucire, semicrystalline solid dispersions, carbamazepine, Pharmacy and materia medica, RS1-441
الوصف: 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.
نوع الوثيقة: article
وصف الملف: electronic resource
اللغة: English
تدمد: 1999-4923
Relation: https://www.mdpi.com/1999-4923/12/6/548; https://doaj.org/toc/1999-4923
DOI: 10.3390/pharmaceutics12060548
URL الوصول: https://doaj.org/article/66f2a014f17f4a91995814f06bcdfef1
رقم الأكسشن: edsdoj.66f2a014f17f4a91995814f06bcdfef1
قاعدة البيانات: Directory of Open Access Journals
الوصف
تدمد:19994923
DOI:10.3390/pharmaceutics12060548