scholarly journals Formulation of aripiprazole-loaded pH-modulated solid dispersions via hot-melt extrusion technology: In vitro and in vivo studies

2019 ◽  
Vol 554 ◽  
pp. 302-311 ◽  
Author(s):  
Haley McFall ◽  
Sandeep Sarabu ◽  
Vijaykumar Shankar ◽  
Suresh Bandari ◽  
S. Narasimha Murthy ◽  
...  
Keyword(s):  
Solid Dispersions ◽  
Hot Melt Extrusion ◽  
In Vivo Studies ◽  
Melt Extrusion ◽  
Extrusion Technology ◽  
Hot Melt

scholarly journals Development of taste masked caffeine citrate formulations utilizing hot melt extrusion technology and in vitro–in vivo evaluations

2015 ◽  
Vol 487 (1-2) ◽  
pp. 167-176 ◽  
Author(s):  
Manjeet B. Pimparade ◽  
Joseph T. Morott ◽  
Jun-Bom Park ◽  
Vijay I. Kulkarni ◽  
Soumyajit Majumdar ◽  
...  
Keyword(s):  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Caffeine Citrate ◽  
Extrusion Technology ◽  
Hot Melt

scholarly journals Preparation of Curcumin-Eudragit® E PO Solid Dispersions with Gradient Temperature through Hot-Melt Extrusion

Molecules ◽  
2021 ◽  
Vol 26 (16) ◽  
pp. 4964
Author(s):  
Wenling Fan ◽  
Xiaotong Zhang ◽  
Wenjing Zhu ◽  
Xinyi Zhang ◽  
Liuqing Di
Keyword(s):  
Solid Dispersions ◽  
Hot Melt Extrusion ◽  
Solubility Parameters ◽  
Sprague Dawley ◽  
Melt Extrusion ◽  
Scanning Calorimetry ◽  
In Vivo Experiments ◽  
Hot Melt

Hot-melt extrusion (HME) has great advantages for the preparation of solid dispersion (SD), for instance, it does not require any organic solvents. Nevertheless, its application to high-melting-point and thermosensitive drugs has been rarely reported. In this study, thermally unstable curcumin (Cur) was used as a drug model. The HME process was systematically studied by adjusting the gradient temperature mode and residence time, with the content, crystallinity and dissolution of Cur as the investigated factors. The effects of barrel temperature, screw speed and cooling rate on HME were also examined. Solubility parameters and the Flory–Huggins method were used to evaluate the miscibility between Cur and carriers. Differential scanning calorimetry, X-ray diffraction, Fourier transform infrared spectroscopy, equilibrium solubility and in vitro and in vivo experiments were used to characterize and evaluate the results. An amorphous Cur SD was successfully obtained, increasing the solubility and release of Cur. In the optimal process, the mass ratio of Cur to Eudragit® E PO (EPO) was 1:4 and the barrel temperature was set at a gradient heating mode (130 °C–135 °C–140 °C–145 °C–150 °C–155 °C–160 °C) at 100 rpm. Related pharmacokinetic test results also showed the improved bioavailability of the drug in rats. In a pharmacodynamic analysis of Sprague–Dawley rats, the Cmax and the bioavailability of the Cur-EPO SD were 2.6 and 1.5 times higher than those of Cur, respectively. The preparation of the amorphous SD not only provided more solubility but also improved the bioavailability of Cur, which provides an effective way to improve the bioavailability of BCS II drugs.

scholarly journals Processing Impact on In Vitro and In Vivo Performance of Solid Dispersions—A Comparison between Hot-Melt Extrusion and Spray Drying

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1307
Author(s):  
Yongjun Li ◽  
Amanda K. P. Mann ◽  
Dan Zhang ◽  
Zhen Yang
Keyword(s):  
Spray Drying ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Drug Solubility ◽  
Melt Extrusion ◽  
Amorphous Solid Dispersions ◽  
Hot Melt

Presently, a large number of drug molecules in development are BCS class II or IV compounds with poor aqueous solubility. Various novel solubilization techniques have been used to enhance drug solubility. Among them, amorphous solid dispersions (ASD), which convert a crystalline drug into an amorphous mixture of drug and polymer, have been demonstrated to be an effective tool in enhancing drug solubility and bioavailability. There are multiple ways to produce amorphous solid dispersions. The goal of the present study is to investigate two commonly used processing methods, hot-melt extrusion (HME) and spray drying, and their impact on drug bioperformance. The amorphous solid dispersions of a model compound, posaconazole (25% drug loading) in HPMCAS-MF, were successfully manufactured via the two processing routes, and the physicochemical properties, in vitro and in vivo performance of the resulting ASDs were characterized and compared. It was found that in vitro drug release of the ASDs from two-stage dissolution was significantly different. However, the two ASDs showed similar in vivo performance based on cynomolgus monkey PK studies. A mechanistic understanding of the in vitro and in vivo behaviors of the solid dispersions was discussed.

scholarly journals Coupling Additive Manufacturing with Hot Melt Extrusion Technologies to Validate a Ventilator-Associated Pneumonia Mouse Model

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 772
Author(s):  
Bahaa Shaqour ◽  
Juliana Aizawa ◽  
Clara Guarch-Pérez ◽  
Żaneta Górecka ◽  
Lars Christophersen ◽  
...  
Keyword(s):  
Additive Manufacturing ◽  
Thermoplastic Polyurethane ◽  
Hot Melt Extrusion ◽  
Polymeric Matrix ◽  
Ventilator Associated Pneumonia ◽  
Melt Extrusion ◽  
Good Thermal Stability ◽  
Hot Melt

Additive manufacturing is widely used to produce highly complex structures. Moreover, this technology has proven its superiority in producing tools which can be used in different applications. We designed and produced an extrusion nozzle that allowed us to hot melt extrude drug-loaded tubes. The tubes were an essential part of a new mouse ventilator-associated pneumonia (VAP) model. Ciprofloxacin (CPX) was selected for its expected activity against the pathogen Staphylococcus aureus and ease of incorporation into thermoplastic polyurethane (TPU). TPU was selected as the carrier polymer for its biocompatibility and use in a variety of medical devices such as tubing and catheters. The effect of loading CPX within the TPU polymeric matrix and the physicochemical properties of the produced tubes were investigated. CPX showed good thermal stability and in vitro activity in preventing S. aureus biofilm formation after loading within the tube’s polymeric matrix. Moreover, the produced tubes showed anti-infective efficacy in vivo. The produced tubes, which were extruded via our novel nozzle, were vital for the validation of our mouse VAP model. This model can be adopted to investigate other antibacterial and antibiofilm compounds incorporated in polymeric tubes using hot melt extrusion.

Sign in / Sign up

Export Citation Format

Share Document