دورية أكاديمية

Preparation of Hot-Melt Extruded Dosage Form for Enhancing Drugs Absorption Based on Computational Simulation

التفاصيل البيبلوغرافية
العنوان: Preparation of Hot-Melt Extruded Dosage Form for Enhancing Drugs Absorption Based on Computational Simulation
المؤلفون: Sung-Min Choi, Sung-Hoon Lee, Chin-Yang Kang, Jun-Bom Park
المصدر: Pharmaceutics; Volume 12; Issue 8; Pages: 757
بيانات النشر: Multidisciplinary Digital Publishing Institute
سنة النشر: 2020
المجموعة: MDPI Open Access Publishing
مصطلحات موضوعية: hot-melt extrusion technology, cilostazol, dissolution rate and permeability, PBPK simulation, parameter-sensitive analysis
الوصف: The aim of this study was to control the dissolution rate and permeability of cilostazol. To enhance the dissolution rate of the active pharmaceutical ingredient (API), hot-melt extrusion (HME) technology was applied to prepare a solid dispersion (SD). To control permeability in the gastrointestinal tract regardless of food intake, the HME process was optimized based on physiologically based pharmacokinetic (PBPK) simulation. The extrudates were produced using a laboratory-scale twin-screw hot-melt extruder with co-rotatory screws and a constant feeding rate. Next, for PBPK simulation, parameter-sensitive analysis (PSA) was conducted to determine the optimization approach direction. As demonstrated by the dissolution test, the solubility of extrudate was enhanced comparing cilostazol alone. Based on the PSA analysis, the surfactant induction was a crucial factor in cilostazol absorption; thus, an extrudate with an even distribution of lipids was produced using hot-melt extrusion technology, for inducing the bile salts in the gastrointestinal tract. In vivo experiments with rats demonstrated that the optimized hot-melt extruded formulation was absorbed more rapidly with lower deviation and regardless of the meal consumed when compared to marketed cilostazol formulations.
نوع الوثيقة: text
وصف الملف: application/pdf
اللغة: English
العلاقة: Pharmaceutical Technology, Manufacturing and Devices; https://dx.doi.org/10.3390/pharmaceutics12080757Test
DOI: 10.3390/pharmaceutics12080757
الإتاحة: https://doi.org/10.3390/pharmaceutics12080757Test
حقوق: https://creativecommons.org/licenses/by/4.0Test/
رقم الانضمام: edsbas.8272FEE8
قاعدة البيانات: BASE