Increased dissolution rates of tranilast solid dispersions extruded with inorganic excipients

The purpose of this study was to evaluate the performance of Neusilin® (NEU) a synthetic magnesium aluminometasilicate as an inorganic drug carrier co-processed with the hydrophilic surfactants Labrasol and Labrafil to develop Tranilast (TLT)-based solid dispersions using continuous melt extrusion (...

Full description

Saved in:
Bibliographic Details
Published in:Drug development and industrial pharmacy 2017-06, Vol.43 (6), p.947-957
Main Authors: Maniruzzaman, Mohammed, Ross, Steven A., Islam, Muhammad Tariqul, Scoutaris, Nikolaos, Nair, Arun, Douroumis, Dennis
Format: Article
Language:English
Subjects:
Aluminum Compounds
Capsules
Crystallization
Drug Carriers
Drug Compounding
drug-excipient interactions dissolution
Excipients - chemistry
Extrusion
Histamine H1 Antagonists - administration & dosage
Histamine H1 Antagonists - chemistry
inorganic excipients
Kinetics
Magnesium Compounds
ortho-Aminobenzoates - administration & dosage
ortho-Aminobenzoates - chemistry
Particle Size
Silicates
solid dispersions
Solubility
Spectroscopy, Near-Infrared
Surface-Active Agents
X-Ray Diffraction
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:The purpose of this study was to evaluate the performance of Neusilin® (NEU) a synthetic magnesium aluminometasilicate as an inorganic drug carrier co-processed with the hydrophilic surfactants Labrasol and Labrafil to develop Tranilast (TLT)-based solid dispersions using continuous melt extrusion (HME) processing. Twin-screw extrusion was optimized to develop various TLT/excipient/surfactant formulations followed by continuous capsule filling in the absence of any downstream equipment. Physicochemical characterization showed the existence of TLT in partially crystalline state in the porous network of inorganic NEU for all extruded formulations. Furthermore, in-line NIR studies revealed a possible intermolecular H-bonding formation between the drug and the carrier resulting in the increase of TLT dissolution rates. The capsules containing TLT-extruded solid dispersions showed enhanced dissolution rates and compared with the marketed Rizaben ® product.
ISSN:0363-9045
1520-5762
DOI:10.1080/03639045.2017.1287716