Improvement of stability and release of (-)-epicatechin by hot melt extrusion

2019 ◽  
Vol 40 (1) ◽  
pp. 75-85 ◽  
Author(s):  
Catalina María Álvarez ◽  
Laura Restrepo-Uribe ◽  
Jorge Andrés López ◽  
Omar Augusto Estrada ◽  
María del Pilar Noriega
Keyword(s):  
High Performance ◽  
Hot Melt Extrusion ◽  
Taste Masking ◽  
Melt Extrusion ◽  
Scanning Calorimetry ◽  
The Stability ◽  
Physical Changes ◽  
Hot Melt ◽  
Shed Light

Abstract Besides its poor dissolution in polymers, the stability, and bitterness of (-)-epicatechin present challenges for additional developments. Polymer formulations rich in flavonoids or other antioxidants can be developed by hot melt extrusion (HME) for enhancement of stability, release, and taste masking. The formulations are extruded at a temperature substantially below the melting point of (-)-epicatechin to avoid its degradation. The corresponding compound consists of about 50% wt. of an active nutraceutical ingredient, in this case (-)-epicatechin, and food grade polymers (GRAS: generally recognized as safe). In order to identify possible chemical or physical changes in the formulations, they were characterized using various techniques, such as differential scanning calorimetry, thermogravimetric analysis, polarized optical microscopy, in vitro release profile, sensory analysis, high-performance liquid chromatography, and Fourier transform infrared spectroscopy. The crystallinity of (-)-epicatechin was reduced after melt extrusion, but its chemical structure remained unchanged. The main contribution of this research is to shed light on the preparation of polymeric formulations based on (-)-epicatechin using HME as an encapsulation technique to improve stability, release, and taste masking, which may be scaled up and commercially launched as nutraceutical products.

Taste masking of paracetamol by hot-melt extrusion: An in vitro and in vivo evaluation

2012 ◽  
Vol 80 (2) ◽  
pp. 433-442 ◽  
Author(s):  
Mohammed Maniruzzaman ◽  
Joshua S. Boateng ◽  
Marion Bonnefille ◽  
Attila Aranyos ◽  
John C. Mitchell ◽  
...  
Keyword(s):  
Hot Melt Extrusion ◽  
Taste Masking ◽  
Melt Extrusion ◽  
In Vivo Evaluation ◽  
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 TASTE ABATEMENT AND CHARACTERIZATION OF DISPERSIBLE TABLETS OF ARTEMETHER PREPARED BY HOT MELT EXTRUSION

2017 ◽  
Vol 9 (6) ◽  
pp. 28
Author(s):  
Yogesh A. Sonar ◽  
Mrudula H. Bele ◽  
Nitin H. Sonar ◽  
Vishal S. Bagul ◽  
Prashik S. Shimpi
Keyword(s):  
Sensory Evaluation ◽  
Solid Dispersion ◽  
In Vitro Release ◽  
Hot Melt Extrusion ◽  
Taste Masking ◽  
Melt Extrusion ◽  
Evaluation Panel ◽  
Dispersible Tablets ◽  
Hot Melt

Objective: The aim of this study was to formulate and evaluate a taste-masked formulation using hot melt extrusion approach for artemether.Methods: Taste masking of artemether was done by preparing solid dispersion with coating polymer kollicoatsmartseal 30D using hot melt extrusion. The prepared solid dispersion was subjected to taste masking evaluation like sensory evaluation parameters against five levels set for taste evaluation using artemether as control standard along with in vitro release studies in simulated salivery fluid. After taste evaluation of solid dispersion was subjected to the formulation of dispersible tablets by direct compression method. The final taste masking evaluation of dispersible tablets of solid dispersion containing artemether were done by a sensory evaluation panel of nine members along with in vitro release study in simulated salivary and gastric fluid.Results: The percent drug content was found 35.09±0.06 % in solid dispersion. The drug excipients compatibility studies performed with the help of FTIR instrument and DSC that indicates there were no interactions between drug and polymers. Solid dispersions (1:1, 1:2, 1:3 drug polymer ratio) of artemether were evaluated by sensory evaluation panel from which 1:3 drug: polymer solid dispersion was found more palatable. Release rate study in simulated salivary fluid shown no release but shows release of drug in simulated gastric fluids which indicates that the drug was taste masked. The optimized batch of dispersible tablets (F1) were subjected for evaluation parameters like dispersion time (70±1.90), wetting time (63±1.86), etc. Dissolution studies of optimized formulation indicated that the polymer does not allow drug to release in simulated salivery pH 6.8 but shows immediate release in simulated gastric pH which also confirms taste masking efficiency of polymer. Final optimized F1 batch evaluated for taste masking evaluation by sensory evaluation panel using pure drug as control standard found to be palatable.Conclusion: It may be concluded that kollicoatsmartseal 30D could mask the taste of the drug in salivary pH and shows drug release at gastric pH which confirms its efficiency for taste masking.

Hot melt extrusion of ion-exchange resin for taste masking

2018 ◽  
Vol 547 (1-2) ◽  
pp. 385-394 ◽  
Author(s):  
David Cheng Thiam Tan ◽  
Jeremy Jianming Ong ◽  
Rajeev Gokhale ◽  
Paul Wan Sia Heng
Keyword(s):  
Ion Exchange ◽  
Exchange Resin ◽  
Hot Melt Extrusion ◽  
Ion Exchange Resin ◽  
Taste Masking ◽  
Melt Extrusion ◽  
Hot Melt

scholarly journals Vacuum Compression Molding as a Screening Tool to Investigate Carrier Suitability for Hot-Melt Extrusion Formulations

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1019
Author(s):  
Gauri Shadambikar ◽  
Thomas Kipping ◽  
Nicole Di-Gallo ◽  
Alessandro-Giuseppe Elia ◽  
Anja-Nadine Knüttel ◽  
...  
Keyword(s):  
Screening Tool ◽  
Drug Carriers ◽  
Hot Melt Extrusion ◽  
Compression Molding ◽  
Simulated Gastric Fluid ◽  
Formulation Development ◽  
Melt Extrusion ◽  
Scanning Calorimetry ◽  
Production Scale ◽  
Hot Melt

Hot-melt extrusion (HME) is the most preferred and effective method for manufacturing amorphous solid dispersions at production scale, but it consumes large amounts of samples when used for formulation development. Herein, we show a novel approach to screen the polymers by overcoming the disadvantage of conventional HME screening by using a minimum quantity of active pharmaceutical ingredient (API). Vacuum Compression Molding (VCM) is a fusion-based method to form solid specimens starting from powders. This study aimed to investigate the processability of VCM for the creation of amorphous formulations and to compare its results with HME-processed formulations. Mixtures of indomethacin (IND) with drug carriers (Parteck® MXP, Soluplus®, Kollidon® VA 64, Eudragit® EPO) were processed using VCM and extrusion technology. Thermal characterization was performed using differential scanning calorimetry, and the solid-state was analyzed via X-ray powder diffraction. Dissolution studies in the simulated gastric fluid were performed to evaluate the drug release. Both technologies showed similar results proving the effectiveness of VCM as a screening tool for HME-based formulations.

scholarly journals A Novel Approach to Optimize Hot Melt Impregnation in Terms of Amorphization Efficiency

2020 ◽  
Vol 21 (11) ◽  
pp. 4032
Author(s):  
Kamil Garbera ◽  
Krzesimir Ciura ◽  
Wiesław Sawicki
Keyword(s):  
High Performance ◽  
Scanning Calorimetry ◽  
Novel Approach ◽  
Innovative Methodology ◽  
Melt Impregnation ◽  
Scanning Electron Micrography ◽  
Critical Process Parameters ◽  
Face Centered ◽  
The Stability ◽  
Hot Melt

In this study, an innovative methodology to optimize amorphization during the hot melt impregnation (HMI) process was proposed. The novelty of this report revolves around the use of thermal analysis in combination with design of experiments (DoEs) to reduce residual crystallinity during the HMI process. As a model formulation, a mixture of ibuprofen (IBU) and Neusilin was used. The main aim of the study was to identify the critical process parameters of HMI and determine their optimal values to assure a robust impregnation process and possibly the highest possible amorphization rate of IBU. In order to realize this, a DoE approach was proposed based on a face-centered composite design involving three factors. The IBU/Neusilin ratio, the feeding rate, and the screw speed were considered as variables, while the residual crystallinity level of IBU, determined using differential scanning calorimetry (DSC), was measured as the response. Additionally, the stability of IBU under HMI was analyzed using high-performance liquid chromatography to estimate the extent of potential degradation. In order to verify the correctness of the DoE model, tested extrudates were manufactured by HMI and the obtained extrudates were thoroughly examined using scanning electron micrography, X-ray powder diffraction, and DSC.

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

Application of hot-melt extrusion technology in immediate-release abuse-deterrent formulations

2017 ◽  
Vol 13 (6) ◽  
pp. 473 ◽  
Author(s):  
Klaus Wening, PhD ◽  
Sebastian Schwier, PhD ◽  
Hans-J. Stahlberg, MD ◽  
Eric Galia, PhD
Keyword(s):  
Phase 1 ◽  
White Male ◽  
Immediate Release ◽  
Hot Melt Extrusion ◽  
Pharmacokinetic Parameters ◽  
Mechanical Resistance ◽  
In Vitro Test ◽  
Melt Extrusion ◽  
Hot Melt

Objective: Hot-melt extrusion (HME) technology has been used for manufacturing extended-release abuse-deterrent formulations (ADFs) of opioid-type analgesics with improved tamper-resistant properties. Our objective was to describe application of this technology to immediate-release (IR) ADFs.Design: For development of a sample IR ADF (hydrocodone 10 mg/acetaminophen 325 mg) based on HME, feasibility studies were performed using different excipients. The formulation selected for further development was evaluated via in vitro test battery. Moreover, in vivo performance of IR ADF technologies was investigated in an open-label, randomized, cross-over, phase 1, relative oral bioavailability study with another opioid (model compound).Setting: Single-center bioavailability trial.Participants: Twenty-four healthy white male subjects.Interventions: ADF IR formulation of an opioid and marketed IR formulation.Main Outcome Measure(s): For feasibility and in vitro studies, dissolution profiles, syringeability, particle size distribution after physical manipulation, and extractability were evaluated. For the phase 1 study, pharmacokinetic parameters were evaluated and compared for ADF IR and a marketed IR formulation.Results: After manipulation, the majority of particles from the ADF IR formulation were >500 μm and, thus, not considered suitable for intranasal abuse, while the majority of particles for the reference marketed IR formulation were <500 μm. The ADF IR formulation was resistant to syringing and preparation for potential intravenous injection. In healthy subjects, pharmacokinetics of an ADF and marketed IR formulation of an opioid were nearly identical.Conclusions: Application of HME to IR formulations led to development of products with improved mechanical resistance to manipulation for intranasal or intravenous preparation, but similar bioavailability.

Taste masking of isoniazid by hot melt extrusion and spray drying – A comparative study

2016 ◽  
Vol 511 (2) ◽  
pp. 1142
Author(s):  
Alison Keating ◽  
Duncan Craig ◽  
Catherine Tuleu ◽  
Claire Forbes ◽  
Barry Aldous ◽  
...  
Keyword(s):  
Comparative Study ◽  
Spray Drying ◽  
Hot Melt Extrusion ◽  
Taste Masking ◽  
Melt Extrusion ◽  
Hot Melt
Sign in / Sign up

Export Citation Format

Share Document