Analyzing the impact of different excipients on drug release behavior in hot-melt extrusion formulations using FTIR spectroscopic imaging

2015 ◽  
Vol 67 ◽  
pp. 21-31 ◽  
Author(s):  
Marieke Pudlas ◽  
Samuel O. Kyeremateng ◽  
Leonardo A.M. Williams ◽  
James A. Kimber ◽  
Holger van Lishaut ◽  
...  
Keyword(s):  
Drug Release ◽  
Spectroscopic Imaging ◽  
Hot Melt Extrusion ◽  
Release Behavior ◽  
Melt Extrusion ◽  
Drug Release Behavior ◽  
The Impact ◽  
Hot Melt

scholarly journals Development and Characterization of Sustained-Released Donepezil Hydrochloride Solid Dispersions Using Hot Melt Extrusion Technology

Pharmaceutics ◽  
2021 ◽  
Vol 13 (2) ◽  
pp. 213
Author(s):  
Abdullah Alshetaili ◽  
Bjad K. Almutairy ◽  
Sultan M. Alshehri ◽  
Michael A. Repka
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Solid Dispersion ◽  
Hot Melt Extrusion ◽  
Release Profile ◽  
Release Behavior ◽  
Melt Extrusion ◽  
Sustained Release Formulation ◽  
Donepezil Hydrochloride ◽  
Hot Melt

The aim of this work was to develop the sustained release formulation of donepezil hydrochloride (DH) using the hot-melt extruded solid dispersion technique via the rational screening of hydrophobic carriers. Hydrophobic carriers with different physicochemical properties such as pH-independent swellability, low-permeability (Eudragit® RS PO (E-RS)), pH-independent non-swellability (ethyl cellulose N7 (EC-N7)), and the presence of lipids (Compritol® 888 ATO (C-888)) with or without pore-forming agents were used to achieve the sustained release profile of DH. Mannitol (MNT) was chosen as the temporary pore-forming agent. The thermal analysis showed that both the drug and C-888 preserved their crystallinity within a solid dispersion. During a dissolution test, MNT could generate pores, and the drug release rate was proportionally correlated to the MNT content. Tailoring of the ratio of C-888 and MNT in the formulations along with an appropriate extrusion temperature profile resulted in the modified release of DH, and a preferable release pattern was obtained under these conditions. C-888 was chosen for the further investigations to obtain tablets with a high integrity. The optimized tablets were compared to the marketed formulation of Aricept® in terms of drug release profiles. The optimized formulation showed the stable and sustained release behavior of extended release profile, which was close to the release behavior of Aricept® with good tablet characteristics. It was concluded that the hot-melt extrusion technique can be utilized for the manufacturing of DH sustained release tablets with improved tablet integrity and characteristics by co-processing the tablet excipient with DH/C-888.

scholarly journals Heat Treatment Induced Specified Aggregation Morphology of Metoprolol Tartrate in Poly(ε-caprolactone) Matrix and the Drug Release Variation

Polymers ◽  
2021 ◽  
Vol 13 (18) ◽  
pp. 3076
Author(s):  
Zhiyu Liu ◽  
Hangling Song ◽  
Xia Chen ◽  
Aichun Han ◽  
Guiting Liu ◽  
...  
Keyword(s):  
Heat Treatment ◽  
Drug Release ◽  
Controlled Drug Release ◽  
Treatment Method ◽  
Melt Processing ◽  
Metoprolol Tartrate ◽  
Release Behavior ◽  
Drug Release Behavior ◽  
Phosphate Buffered Saline ◽  
Hot Melt

Hot-melt blending has been widely used in the pharmaceutical industry to produce drug delivery systems, however, realizing the controlled drug release behavior of a hot-melt blended medicament it is still a tough challenge. In this study, we developed a simple and effective heat treatment method to adjust the drug release behavior, without the addition of any release modifiers. Thin metoprolol tartrate (MPT)/poly(ε-caprolactone) (PCL) tablets were prepared through hot-melt processing, and different morphologies of MPT were obtained by altering processing temperatures and the following heat treatment. MPT particles with different particle sizes were obtained under different processing temperatures, and fibrous crystals of MPT were fabricated during the following heat treatment. Different morphological structures of MPT adjusted the drug diffusion channel when immersed in phosphate-buffered saline (PBS), and various drug release behaviors were approached. After being immersed for 24 h, 7% of the MPT was released from the blend processed at 130 °C, while more than 95% of the MPT were released after the following heat treatment of the same sample. Thus, flexible drug release behaviors were achieved using this simple and effective processing manufacture, which is demonstrated to be of profound importance for biomedical applications.

scholarly journals Influence of Carbamazepine Dihydrate on the Preparation of Amorphous Solid Dispersions by Hot Melt Extrusion

Pharmaceutics ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 379 ◽  
Author(s):  
Xiangyu Ma ◽  
Felix Müller ◽  
Siyuan Huang ◽  
Michael Lowinger ◽  
Xu Liu ◽  
...  
Keyword(s):  
Energy State ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Water Soluble ◽  
Melt Extrusion ◽  
Amorphous Solid Dispersions ◽  
Water Soluble Drugs ◽  
The Impact ◽  
Hot Melt

Amorphous solid dispersions (ASDs) are commonly used in the pharmaceutical industry to improve the dissolution and bioavailability of poorly water-soluble drugs. Hot melt extrusion (HME) has been employed to prepare ASD based products. However, due to the narrow processing window of HME, ASDs are normally obtained with high processing temperatures and mechanical stress. Interestingly, one-third of pharmaceutical compounds reportedly exist in hydrate forms. In this study, we selected carbamazepine (CBZ) dihydrate to investigate its solid-state changes during the dehydration process and the impact of the dehydration on the preparation of CBZ ASDs using a Leistritz micro-18 extruder. Various characterization techniques were used to study the dehydration kinetics of CBZ dihydrate under different conditions. We designed the extrusion runs and demonstrated that: 1) the dehydration of CBZ dihydrate resulted in a disordered state of the drug molecule; 2) the resulted higher energy state CBZ facilitated the drug solubilization and mixing with the polymer matrix during the HME process, which significantly decreased the required extrusion temperature from 140 to 60 °C for CBZ ASDs manufacturing compared to directly processing anhydrous crystalline CBZ. This work illustrated that the proper utilization of drug hydrates can significantly improve the processability of HME for preparing ASDs.

Mechanism of drug release from polymethacrylate-based extrudates and milled strands prepared by hot-melt extrusion

2009 ◽  
Vol 71 (2) ◽  
pp. 387-394 ◽  
Author(s):  
Jessica Albers ◽  
Rainer Alles ◽  
Karin Matthée ◽  
Klaus Knop ◽  
Julia Schulze Nahrup ◽  
...  
Keyword(s):  
Drug Release ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
Hot Melt

scholarly journals The impact of hot-melt extrusion on the tableting behaviour of polyvinyl alcohol

2016 ◽  
Vol 498 (1-2) ◽  
pp. 254-262 ◽  
Author(s):  
W. Grymonpré ◽  
W. De Jaeghere ◽  
E. Peeters ◽  
P. Adriaensens ◽  
J.P. Remon ◽  
...  
Keyword(s):  
Polyvinyl Alcohol ◽  
Hot Melt Extrusion ◽  
Melt Extrusion ◽  
The Impact ◽  
Hot Melt

scholarly journals Impact of Drug Loading Method on Drug Release from 3D-Printed Tablets Made from Filaments Fabricated by Hot-Melt Extrusion and Impregnation Processes

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1607
Author(s):  
Kasitpong Thanawuth ◽  
Lalinthip Sutthapitaksakul ◽  
Srisuda Konthong ◽  
Supakij Suttiruengwong ◽  
Kampanart Huanbutta ◽  
...  
Keyword(s):  
Drug Release ◽  
Drug Loading ◽  
Hot Melt Extrusion ◽  
Water Soluble ◽  
Melt Extrusion ◽  
Drug Content ◽  
Loading Method ◽  
Lower Drug ◽  
3D Printed ◽  
Hot Melt

The purpose of this study was to investigate the impact of the drug loading method on drug release from 3D-printed tablets. Filaments comprising a poorly water-soluble model drug, indomethacin (IND), and a polymer, polyvinyl alcohol (PVA), were prepared by hot-melt extrusion (HME) and compared with IND-loaded filaments prepared with an impregnation (IMP) process. The 3D-printed tablets were fabricated using a fused deposition modeling 3D printer. The filaments and 3D printed tablets were evaluated for their physicochemical properties, swelling and matrix erosion behaviors, drug content, and drug release. Physicochemical investigations revealed no drug–excipient interaction or degradation. IND-loaded PVA filaments produced by IMP had a low drug content and a rapid drug release. Filaments produced by HME with a lower drug content released the drug faster than those with a higher drug content. The drug content and drug release of 3D-printed tablets containing IND were similar to those of the filament results. Particularly, drug release was faster in 3D-printed tablets produced with filaments with lower drug content (both by IMP and HME). The drug release of 3D-printed tablets produced from HME filaments with higher drug content was extended to 24 h due to a swelling-erosion process. This study confirmed that the drug loading method has a substantial influence on drug content, which in turn has a significant effect on drug release. The results suggest that increasing the drug content in filaments might delay drug release from 3D-printed tablets, which may be used for developing dosage forms suited for personalized medicine.

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