Thermal Processing of PVP- and HPMC-Based Amorphous Solid Dispersions
Journal Title: AAPS PharmSciTech - Year 2016, Vol 17, Issue 1
Abstract
Thermal processing technologies continue to gain interest in pharmaceutical manufacturing. However, the types and grades of polymers that can be utilized in common thermal processing technologies, such as hot-melt extrusion (HME), are often limited by thermal or rheological factors. The objectives of the present study were to compare and contrast two thermal processing methods, HME and KinetiSol® Dispersing (KSD), and investigate the influence of polymer type, polymer molecular weight, and drug loading on the ability to produce amorphous solid dispersions (ASDs) containing the model compound griseofulvin (GRIS). Dispersions were analyzed by a variety of imaging, solid-state, thermal, and solution-state techniques. Dispersions were prepared by both HME and KSD using polyvinylpyrrolidone (PVP) K17 or hydroxypropyl methylcellulose (HPMC) E5. Dispersions were only prepared by KSD using higher molecular weight grades of HPMC and PVP, as these could not be extruded under the conditions selected. Powder X-ray diffraction (PXRD) analysis showed that dispersions prepared by HME were amorphous at 10% and 20% drug load; however, it showed significant crystallinity at 40% drug load. PXRD analysis of KSD samples showed all formulations and drug loads to be amorphous with the exception of trace crystallinity seen in PVP K17 and PVP K30 samples at 40% drug load. These results were further supported by other analytical techniques. KSD produced amorphous dispersions at higher drug loads than could be prepared by HME, as well as with higher molecular weight polymers that were not processable by HME, due to its higher rate of shear and torque output.
Authors and Affiliations
Justin S. LaFountaine, Leena Kumari Prasad, Chris Brough, Dave A. Miller, James W. McGinity, Robert O. Williams, III
Keywords
Related Articles
- EP ID EP682144
- DOI 10.1208/s12249-015-0417-7
- Views 93
- Downloads 0
Wetting Kinetics: an Alternative Approach Towards Understanding the Enhanced Dissolution Rate for Amorphous Solid Dispersion of a Poorly Soluble Drug
Developing amorphous solid dispersions of water-insoluble molecules using polymeric materials is a well-defined approach to improve the dissolution rate and bioavailability. While the selected polymer plays a vital role...
Efficacy, Pharmacokinetics, and Biodistribution of Thermosensitive Chitosan/β-Glycerophosphate Hydrogel Loaded with Docetaxel
Docetaxel (DTX) is a widely used anticancer drug for various solid tumors. However, its poor solubility in water and lack of specification are two limitations for clinical use. The aim of the study was to develop a therm...
Evaluation of Tadalafil Nanosuspensions and Their PEG Solid Dispersion Matrices for Enhancing Its Dissolution Properties
The aim of this work was to prepare and evaluate Tadalafil nanosuspensions and their PEG 4000 solid dispersion matrices to enhance its dissolution rate. Nanosuspensions were prepared by precipitation/ultrasonication tech...
Development and Characterization of Sorbitan Monostearate and Sesame Oil-Based Organogels for Topical Delivery of Antimicrobials
The online version of this article (doi:10.1208/s12249-014-0223-7) contains supplementary material, which is available to authorized users.
Preparation of Polyamide Nanocapsules of Aloe vera L. Delivery with In Vivo Studies
Aloe vera is the oldest medicinal plant ever known and the most applied medicinal plant worldwide. The purpose of this study was to prepare polyamide nanocapsules containing A. vera L. by an emulsion diffusion technique...