Solubility Enhancement of Poorly Water-Soluble Drugs by Hot-Melt Extrusion Technology and Effects of Surfactant on Dissolution Test

Yakhak Hoeji ◽  
2019 ◽  
Vol 63 (6) ◽  
pp. 384-389
Author(s):  
Sung-min Choi ◽  
Yong-Koo Jeon ◽  
Ju-Hyun Lee ◽  
Chin-Yang Kang ◽  
Jun-Bom Park
Keyword(s):  
Hot Melt Extrusion ◽  
Solubility Enhancement ◽  
Water Soluble ◽  
Dissolution Test ◽  
Melt Extrusion ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Extrusion Technology ◽  
Hot Melt

scholarly journals Innovations in Thermal Processing: Hot-Melt Extrusion and KinetiSol® Dispersing

2020 ◽  
Vol 21 (8) ◽  
Author(s):  
Deck Khong Tan ◽  
Daniel A. Davis ◽  
Dave A. Miller ◽  
Robert O. Williams ◽  
Ali Nokhodchi
Keyword(s):  
Thermal Processing ◽  
Solid Dispersions ◽  
Amorphous Solid ◽  
Hot Melt Extrusion ◽  
Solubility Enhancement ◽  
Water Soluble ◽  
Melt Extrusion ◽  
Amorphous Solid Dispersions ◽  
Poorly Water Soluble ◽  
Hot Melt

AbstractThermal processing has gained much interest in the pharmaceutical industry, particularly for the enhancement of solubility, bioavailability, and dissolution of active pharmaceutical ingredients (APIs) with poor aqueous solubility. Formulation scientists have developed various techniques which may include physical and chemical modifications to achieve solubility enhancement. One of the most commonly used methods for solubility enhancement is through the use of amorphous solid dispersions (ASDs). Examples of commercialized ASDs include Kaletra®, Kalydeco®, and Onmel®. Various technologies produce ASDs; some of the approaches, such as spray-drying, solvent evaporation, and lyophilization, involve the use of solvents, whereas thermal approaches often do not require solvents. Processes that do not require solvents are usually preferred, as some solvents may induce toxicity due to residual solvents and are often considered to be damaging to the environment. The purpose of this review is to provide an update on recent innovations reported for using hot-melt extrusion and KinetiSol® Dispersing technologies to formulate poorly water-soluble APIs in amorphous solid dispersions. We will address development challenges for poorly water-soluble APIs and how these two processes meet these challenges.

Tailor-made release triggering from hot-melt extruded complexes of basic polyelectrolyte and poorly water-soluble drugs

2011 ◽  
Vol 79 (2) ◽  
pp. 372-381 ◽  
Author(s):  
Christoph Kindermann ◽  
Karin Matthée ◽  
Jutta Strohmeyer ◽  
Frank Sievert ◽  
Jörg Breitkreutz
Keyword(s):  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Hot Melt

A review on solubility enhancement methods for poorly water-soluble drugs

2021 ◽  
Vol 10 (1) ◽  
pp. 137
Author(s):  
Ahmad Ainurofiq ◽  
DavidSarono Putro ◽  
DheaAqila Ramadhani ◽  
GemalaMahendra Putra ◽  
LauraDa Costa Do Espirito Santo
Keyword(s):  
Solubility Enhancement ◽  
Water Soluble ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble

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.

Effects of dissolved state of aminoalkyl methacrylate copolymer E/HCl on solubility enhancement effect for poorly water-soluble drugs

2012 ◽  
Vol 291 (5) ◽  
pp. 1191-1199 ◽  
Author(s):  
Takatsune Yoshida ◽  
Ippei Kurimoto ◽  
Hiroyuki Umejima ◽  
Shunsuke Watanabe ◽  
Kazuhiro Sako ◽  
...  
Keyword(s):  
Solubility Enhancement ◽  
Water Soluble ◽  
Enhancement Effect ◽  
Poorly Water Soluble Drugs ◽  
Water Soluble Drugs ◽  
Poorly Water Soluble ◽  
Methacrylate Copolymer
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