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Hot-Melt Extrusion Pharmaceutical Applications

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ISBN-10: 0470711183

ISBN-13: 9780470711187

Edition: 2012

Authors: Dennis Douroumis

List price: $230.00
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Description:

Hot-melt extrusion (HME)  - melting a substance and forcing it through an orifice under controlled conditions to form a new material - is an emerging processing technology in the pharmaceutical industry for the preparation of various dosage forms and drug delivery systems, for example granules and sustained release tablets.Hot-Melt Extrusion: Pharmaceutical Applications covers the main instrumentation, operation principles and theoretical background of HME. It then focuses on HME drug delivery systems, dosage forms and clinical studies (including pharmacokinetics and bioavailability) of HME products. Finally, the book includes some recent and novel HME applications, scale -up considerations and regulatory issues. Topics covered include:                                               • principles and die design of single screw extrusion• twin screw extrusion techniques and practices in the laboratory and on production scale• HME developments for the pharmaceutical industry• solubility parameters for prediction of drug/polymer miscibility in HME formulations• the influence of plasticizers in HME• applications of polymethacrylate polymers in HME• HME of ethylcellulose, hypromellose, and polyethylene oxide• bioadhesion properties of polymeric films produced by HME• taste masking using HME• clinical studies, bioavailability and pharmacokinetics of HME products• injection moulding and HME processing for pharmaceutical materials• laminar dispersive & distributive mixing with dissolution and applications to HME• technological considerations related to scale-up of HME processes• devices and implant systems by HME• an FDA perspective on HME product and process understanding• improved process understanding and control of an HME process with near-infrared spectroscopyHot-Melt Extrusion: Pharmaceutical Applications is an essential multidisciplinary guide to the emerging pharmaceutical uses of this processing technology for researchers in academia and industry working in drug formulation and delivery, pharmaceutical engineering and processing, and polymers and materials science.
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Book details

List price: $230.00
Copyright year: 2012
Publisher: John Wiley & Sons, Incorporated
Publication date: 6/25/2012
Binding: Hardcover
Pages: 382
Size: 6.80" wide x 10.00" long x 1.00" tall
Weight: 1.738
Language: English

List of Contributors
Preface
Single-screw Extrusion: Principles
Introduction
Ideal Compounding
Basics of the Single-screw Extruder
Screw Feed Section
Screw Compressor Section
Screw Metering Section
Mixers
Limitations of Conventional Single-screw Mixers
SSE Elongational Mixers
Summary
References
Twin-screw Extruders for Pharmaceutical Hot-melt Extrusion: Technology, Techniques and Practices
Introduction
Extruder Types and Working Principle
Individual Parts of a TSE
Drive Unit
Screws
Screw Elements
Distributive Flow Elements
Discharge Feed Screw
Barrel
Downstreaming
Individual Processing Sections of the TSE
Feeding Section
Conveying/Melting Section
Mixing Section
Venting Section
Extrusion Section
Feeding of Solids
TSE Operating Parameters
Filling Level
Screw Speed
Feed Rate
Residence Time Distribution
Effect of Screw Speed and Feed Rate on Melt Temperature
Setting up an HME Process using QbD Principles
Understanding Knowledge Space
Denning Design Space
Determining Control Space
Summary
References
Hot-melt Extrusion Developments in the Pharmaceutical Industry
Introduction
Advantages of HME as Drug Delivery Technology
Formulations used for HME Applications
Active Pharmaceutical Ingredient
Solid Dispersions
Bioavailability Improvement
Controlled Delivery Systems
Plasticizers
Characterization of Extrudates
Thermal Analysis
Atomic Force Microscopy
Residence Time
Spectroscopic Techniques
X-ray Diffraction (XRD)
Microscopy
Drug Release
Hot-melt Extruded Dosage Forms
Oral Drag Delivery
Films
Vaginal Rings and Implants
A View to the Future
References
Solubility Parameters for Prediction of Drug/Polymer Miscibility in Hot-melt Extruded Formulations
Introduction
Solid Dispersions
Basic Assumptions for the Drug-polymer Miscibility Prediction
Solubility and the Flory-Huggins Theory
Miscibility Estimation of Drug and Monomers
Summary
References
The Influence of Plasticizers in Hot-melt Extrusion
Introduction
Traditional Plasticizers
Non-traditional Plasticizers
Specialty Plasticizers
Conclusions
References
Applications of Poly(meth)acrylate Polymers in Melt Extrusion
Introduction
Polymer Characteristics
Chemical Structure and Molecular Weight
Glass Transition Temperature
Plasticizers
Thermostability
Viscosity
Specific Heat Capacity
Hygroscopicity
Melt Extrusion of Poly(methacrylates) to Design Pharmaceutical Oral Dosage Forms
Solubility Enhancement
Bioavailability Enhancement of BCS Class IV Drugs
Controlled Release
Time-controlled-release Dosage Forms
pH-dependent Release
Taste Masking
Summary
References
Hot-melt Extrusion of Ethylcellulose, Hypromellose and Polyethylene Oxide
Introduction
Background
Thermal Properties
Processing Aids/Additives
Unconventional Processing Aids: Drags, Blends
Case Studies
Ethylcellulose
Combinations of Excipients
Solubilization
Film
Unique Dosage Forms
Abuse Resistance
Controlled Release
Solubility Parameters
Milling of EC, HPMC and PEO Extrudate
References
Bioadhesion Properties of Polymeric Films Produced by Hot-melt Extrusion
Introduction
Anatomy of the Oral Cavity and Modes of Drug Transport
Structure
Modes of Drug Transport and Kinetics
Factors Affecting Drug Absorption
Mucoadhesive Mechanisms
Factors Affecting Mucoadhesion in the Oral Cavity
Determination of Mucoadhesion and Mechanical Properties of Films
Bioadhesive Films Prepared by HME
Summary
References
Taste Masking Using Hot-melt Extrusion
The Need and Challenges for Masking Bitter APIs
Organization of the Taste System
Taste Perception in Humans and Organization of Peripheral System
Transduction of Taste Signals
Taste Sensing Systems (Electronic Tongues) for Pharmaceutical Dosage Forms
Alpha MOS Electronic Tongue: Instrumentation and Operational Principles
Taste Analysis
Taste Masking Efficiency Testing
Advantages of E-tongue Taste Analysis
Hot-melt Extrusion: An Effective Means of Taste Masking
Taste Masking via Polymer Extrusion
Taste Masking via Solid Lipid Extrusion
Summary
References
Clinical and Preclinical Studies, Bioavailability and Pharmacokinetics of Hot-melt Extruded Products
Introduction to Oral Absorption
In Vivo Evaluation of Hot-melt Extruded Solid Dispersions
Oral Immediate Release
Oral Controlled Release
Implants
Conclusion
References
Injection Molding and Hot-melt Extrusion Processing for Pharmaceutical Materials
Introduction
Hot-melt Extrusion in Brief
Injection Molding
Critical Parameters
Melt Temperature
Barrel Temperature
Cooling Temperature
Holding Pressure
Holding Time
Back Pressure
Injection Speed
Cooling Time/Cycle Time
Example: Comparison of Extruded and Injection-molded Material
Development of Products for Injection Molding
Excipients
Stability
Process Development
Properties of Injection-molded Materials
Egalet� Technology
Controlling Physical State by Means of Hot-melt Extrusion and Injection Molding
Anti-tamper Properties of Injection-molded Tablets
Concluding Remarks
References
Laminar Dispersive and Distributive Mixing with Dissolution and Applications to Hot-melt Extrusion
Introduction
Elementary Steps in HME
Paniculate Solids Handling (PSH)
Melting
Devolatilization
Pumping and Pressurization
Dispersive and Distributive Mixing
HME Processes: Cases I and II
Case I
Case II
Dissolution of Drug Particulates in Polymeric Melt
Process Variables
Equipment Variables
Material Variables
Case Study: Acetaminophen and Poly(ethylene oxide)
Determination of Solubility of APAP in PEO
References
Technological Considerations Related to Scale-up of Hot-melt Extrusion Processes
Introduction
Scale-up Terminology
Scale-up: Batch Size
Scale-up: Feed Rate
Scale-up: Extruder Diameter
Volumetric Scale-up
Volumetric Scale-up: Length/Diameter (L/D)
Volumetric Scale-up: Diameter Ratio
Volumetric Scale-up: Screw Design
Power Scale-up
Heat Transfer Scale-up
Die Scale-up
Conclusion
References
Devices and Implant Systems by Hot-melt Extrusion
Introduction
HME in Device Development
Hot-melt Extruder Types
Comparison of HME Devices and Oral Dosage Forms
HME Processes for Device Fabrication
Issues with HME in preparing Drug-eluting Devices
Devices and Implants
Anatomical Device Locations
Simple Devices
Non-medicated Prolonged Tissue Contact Devices
Medicated (Drug-eluting) Prolonged Tissue Contact Devices
Release Kinetics
Mechanisms of API Release
Example In Vitro Drug Elution Profiles
Conclusions
References
Hot-melt Extrusion: An FDA Perspective on Product and Process Understanding
Introduction
Quality by Design
Utilizing QbD for HME Process Understanding
References
Improved Process Understanding and Control of a Hot-melt Extrusion Process with Near-Infrared Spectroscopy
Vibrational Spectroscopy Introduction
Near-infrared Method Development
Near-infrared Probes and Fiber Optics
NTR for Monitoring the Start-up of a HME Process
NIR for Improved Process Understanding and Control
References
Index