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Innovations in Oral Solid Drug Delivery

経口固形製剤デリバリーの革新

レポート概要

このレポートは経口固形製剤のデリバリーシステムにおける革新を中心に、スタートアップ企業と大学の連携に重点を置いています。景気後退の影響、資金調達の制約、提携の機会について分析を行います。市場動態を把握し、さまざまな動向を分析します。例えば、2007-2012年にピークを迎えるブロックバスター医薬品の特許失効、過去数年間における第一世代経口固形製剤の特許消滅、パイプラインから生まれる新規化学物質の不足、などについて解説し、一部の疾患分野ではその市場規模が縮小していますが、こういった市場の現状に関連した新たな動きを分析します。新しい経口固形製剤デリバリーシステムの推進要因とそれを取り巻く課題を明らかにします。

主なテーマは、ペプチドやタンパク質の、静注から経口デリバリーへの移行です。売上、市場動向に言及し、競争環境について考察します。先発品の欠点として、例えば溶解性、バイオアベイラビリティ、効果の持続性などが低い、副作用が多い、安定性がない、経口投与後の吸収性が低い、苦味や不快な味、消化器吸収領域が狭い、患者間、患者内で吸収性にばらつきがある、といった問題を克服するために第一世代の経口固形製剤の組成変更というテーマが度々発生します。

高齢者人口の増大、長寿化に伴ない、経口固形製剤の開発は、アルツハイマー病、パーキンソン病、2型糖尿病と肥満、骨粗しょう症、がん、関節リウマチなどの高齢者の疾患の治療効果を高めることに重点が置かれています。これらの治療薬の多くは副作用があり、その投与条件や効果の持続性の問題、また注射剤しかないといった問題がその受容性を低下させる要因となっています。

レポート詳細

目次

Table of Contents

Executive summary
Market overview, dynamics and outlook
Advances in nanotechnology
Innovations in transitioning injectables to oral delivery
Advances in delayed & controlled release delivery
Advances in oral prodrug delivery
Advances in taste masking technologies
Innovative companies
Chapter 1 Market overview, dynamics and
outlook
Summary
Market overview
Market dynamics
Key indications
Key trends
Nanomedicine
Transitioning from injectables
Prodrugs
Chrono release
ODT
OSF
Funding issues
Poor patient compliance
Injections
Poor absorbption
Pediatric
Geriatric
Solubility and variable absorption
Reduction of side effect profiles
Non-invasive protein delivery
Transition from injectables to preferred route of oral drug delivery
Directed delivery and delayed delivery to reduce side effect potential
Formulation technologies for poorly soluble compounds
Taste masking for pediatric and geriatric formulations
Competitive landscape
Conclusions and key findings
Chapter 2 Advances in nanotechnology
Summary
Introduction
Nanotechnology platforms with application for oral drug delivery
Self-Emulsifying Controlled Release Tablet system (SECRET)
Technology
Application
Biotransport nanomedicine technology
Technology
Application
Nanobodies
Technology
Application
NanoDel nanoparticles
Technology
Application
P-gpMask
Technology
Application
NanoDRY and NanoCOAT
Technology
Application
Solumer
Technology
Application
Nanocells
Technology
Application
Polymeric Nano-Delivery System (PNDS)
Technology
Application
FluidCrystal NP Oral nanoparticles
Technology
Application
CaP Technology and BioOral
Technology
Application
Nab Technology and Protospheres
Technology
Application
NanoCrystal Technology
Technology
Application
Bioral
Technology
Application
Squalenoyl nanoparticles
NanoMega
NOD Pharmaceutical
Chapter 3 Innovations in transitioning injectables to oral delivery
Summary
Introduction
Drivers
Patient acceptability & compliance
Cost savings
Restraints
Advances in injectable delivery
Challenges of oral drug delivery
Technologies used in oral drug delivery of peptides and proteins
Enzyme inhibitors
Permeation enhancers
Mucoadhesives
Encapsulation technologies
M-cell targeting
Competitive landscape
Osteoporosis and other bone related conditions
Calcitonin
Current therapies & market landscape
Oral products in development
Parathyroid hormone
Current therapies & market landscape
Oral products in development
Combined oral calcitonin and PTH approaches
Bisphosphonates
Current therapies & market landscape
Novel oral products in development
Diabetes and other metabolic diseases
Oral insulin
Oramed Pharmaceuticals
Biocon Ltd
Emisphere Technologies
Diabetology
NOD Pharmaceuticals
Access Pharmaceuticals
NanoMega Medical Corporation
Biodel Inc
Metabolic Pharmaceuticals Ltd
Glucagon-like peptide-1 (GLP-1) and GLP-1 analogs
Oral GLP-1 & GLP-1 analogs
Obesity
Alzheimer's and other CNS conditions
Oligotropin
Endometriosis and prostate cancer
Leuprolide
Cardiovascular
Angiotensin analogs
Innovative approaches to oral vaccine development
Mucosis B.V.
Plug-and-Play Technology
GEM Particles
Mimopath
Ondek Pty Ltd
Helicobacter pylori Platform Technology (HPPT)
Infexion
Kancer
Immune Solutions
Liporale
Chapter 4 Advances in delayed & controlled release delivery
Summary
Introduction
Types of controlled release systems
Sustained release
Pulsatile release
Modified drug delivery
Fast disintegrating technologies
Pediatric formulations - ODT
Schizophrenia and bipolar disorder - ODT
Alzheimer's disease - ODT
Parkinson's disease - ODT
Anxiety and panic disorder - ODT
Major depressive disorder - ODT
Nausea and vomiting - ODT
Migraine - ODT
Autism - ODT
GERD and gastroparesis - ODT
Release control mechanisms
Zero order
Congestive heart failure and hypertension - sustained release
Pain - sustained release
ADHD - sustained release
Multiple sclerosis - sustained release
Muscle relaxant - sustained release
Parkinson's disease - sustained release
Depression - sustained release
Binary
Diabetes type 2 - combination products
Hypertension - combination products
Other
Biphasic release of drugs
Asthma - biphasic release
Pain - biphasic release
ADHD - biphasic release
Hypertension - biphasic release
Positioned
Parkinson's disease - positioned biphasic release
Insomnia - positioned biphasic release
Spasticity - positioned biphasic release
GERD - positioned release
Diabetes type 2 - positioned extended release
Hot flashes - positioned extended release
Pain - positioned extended release
GERD - positioned extended release
Parkinson's disease - positioned extended release
Others
Accelerated
Timed
Multiple pulse
Targeted delivery to the colon
Ulcerative colitis, gastroenteritis - targeted colon release
Nutraceutical - targeted colon release
Polysaccharide colon selective
COLAL technology
Chrono release
Rheumatoid arthritis - chrono release
Severe asthma - chrono release
Polymyalgia rheumatica - chrono release
Insomnia - chrono release
Sublingual formulations
Formulations to counteract opiate or psychostimulant abuse
Trigger-Lock
OraGuard
NanoDRY and NanoCOAT
ORADUR
Aversion Technology
Egalet ADPREM
DETERx
Avert
Strategic alliances
Chapter 5 Advances in oral prodrug delivery
Summary
Introduction
Classification based on site of conversion to active drug
Classification based on chemical linkages or promoiety/carriers that attach to the active drug
Classification based on the deficiency in the active drug
Classification based on carrier-linked or bioprecursor categories
Applications of prodrug technology
Reducing side effect profile
Introducing site specificity - colon
Taste masking applications
Marketed products and market share
Antiviral prodrugs
Oseltamivir
Valaciclovir
Valganciclovir
Famciclovir
Anticancer prodrugs
TS-1
Cardiovascular prodrugs
ACE inhibitors
Angiotensin II receptor antagonists
HMG Co A reductase inhibitors
Respiratory prodrugs
Bambuterol
CNS prodrugs
Lisdexamfetamine
Late and early stage development product formulations
Improving oral bioavailability/reducing toxicity of older marketed injectable drugs
Antiviral prodrugs
Cidofovir
Vidarabine
Zanamivir
Anticancer prodrugs
Triciribine
Camptothecin
Gemcitabine
Docetaxel
Methotrexate
Aimpila
FAP activated ultra-smart prodrug cytotoxic agent
CNS prodrugs
Gabapentin encarbil
Arbaclofen placarbil
Levodopa
LY2140023
ARX-111 and ARX-211
Antibiotic prodrugs
Sulopenem etzadroxil
Torezolid phosphate
Others
Tranexamic acid
ABS-15 and ABS-16
Chapter 6 Advances in taste masking
technologies
Summary
Introduction
Taste masking strategies
Flavor enhancers
Limiting solubility of the drug
Polymer coating
Complexation with ion exchange resins
Liposomes
Chemical modifications
Multiple emulsions
Mass extrusion method (dispersion coating)
Anesthetic agents
Other agents
Orally disintegrating tablets
ODT technologies
Capricorn Pharma Inc.
RDT (rapidly dispersible tablet)
RMB (Rapid Melt Beads)
DAB (Disperse Beads)
KORCAP
RapidMelt
KORKOAT beads
Egalet
Parvulet
Ethypharm
Flashtab and T-mask
Eurand BV
AdvaTab, Microcaps & Liquitard
Supernus
ForTe BV
FlavoRiTe
NOW
Glycologics
Beta-limit dextrin (BLD)
Alginate-Pectin-Starch (APS)
ADD Technologies Ltd
MicroPx
Cambrex
Camouflage DDT
CIMA
OraSolv
DuraSolv
Lyoc
OTS and OraVescent transmucosal tablet
OraGuard
Alte BioSciences
Oraleze
Oral soluble films
Labtec GmbH
RapidFilm
MonoSol Rx
PharmFilm
PharmFilm and Nanocell
University research into new taste masking technologies
Bharati Vidyapeeth Deemed University
University Institute of Chemical Technology
Prin. K.M. Kundanani College of Pharmacy
Chapter 7 Innovative companies
Summary
Introduction
Proxima Concepts Ltd Laboratory
Overview
Technology platforms
Axcess
Vaxcine
Mozaic
Lexicon
Bone Medical Ltd
Overview
Product development pipeline
Diabetology
Overview
Product development pipeline
Kancer Ltd
Overview
Infexion
Overview
Strategy
Nanolymf Ltd
Overview
Technology platform
P-gpMask
Strategy
Patents portfolio related to technologies
Chimerix
Overview
Technology platform
ProLipTag
Product development pipeline
Strategy
Mucosis B. V.
Overview
Technology platforms
Plug-and-Play Technology
GEM Particles
Mimopath
Product development pipeline
Research and development collaborations
Strategy
Ondek Pty Ltd
Overview
Technology platform
Helicobacter pylori Platform Technology (HPPT)
Product development pipeline
Strategy
Patent portfolio relating to technologies
MBC Pharma Inc
Overview
Technology platforms
Bisphosphonate B6 Technology
Product development pipeline
Research and development collaborations
Strategy
Patents portfolio related to technologies
OraDel Medical Ltd
Overview
Technology platform
CPL - Chitosan-coated proliposome technology
Patent portfolio related to technologies
ImmuPharma plc
Overview
Technology platforms
Peptide-to-Drug Converting Technology (PDCT)
Product development pipeline
Strategy
Access Pharmaceuticals
Overview
Technology platforms
Cobalamin-Mediated Oral Delivery
Product development pipeline
Strategy
ActoGeniX
Technology platforms
TopAct
Product development pipeline
Research and development collaborations
Strategy
Biocon Ltd
Overview
Product development pipeline
Chiasma (Israel) Ltd
Overview
Technology platforms
Transient Permeability Enhancer (TPE)
Product development pipeline
Strategy
Patent portfolio related to technology
Emisphere
Overview
Technology platforms
Eligen Technology
Product development pipeline
Strategy
Kytogenics
Overview
Technology platforms
Tight Junction Opener Technology (TIJO)
Product development pipeline
Strategy
Merrion Pharmaceuticals
Overview
Technology platforms
GIPET
GIRES
Product development pipeline
Research and development collaborations 2006-2009
Strategy
Patent portfolio relating to technologies
NOD Pharmaceuticals, Inc.
Overview
Technology platforms
NOD Technology
Product development pipeline
Strategy
Patents portfolio related to technology
Oramed Pharmaceuticals
Overview
Technology platform
Product development pipeline
Strategy
Patents portfolio related to oral delivery technology
Samyang Corporation
Technology platforms
SY-CSDS
ODT
Patent portfolio relating to technologies
Unigene
Overview
Technology platforms
Enteripep
Product development pipeline
Research and development collaborations 2007-2009
Strategy
Patent portfolio relating to technologies
Chapter 8 Appendix
Primary research methodology
MedTRACK platform identification
IMS data
Glossary
Index

List of Figures
Figure 1.1: Market share of oral solid dose forms, 2008
Figure 1.2: Prodrugs, nanomedicines & peptides targeting specific indications
Figure 1.3: Formulations targeting specific indications
Figure 2.4: Advantages of nanotechnology for oral solid dose drug delivery
Figure 3.5: Mechanisms of drug transport across the intestinal epithelium
Figure 3.6: Market share of leading calcitonin products, 2008
Figure 4.7: Approaches to targeted colon delivery
Figure 5.8: Influenza antivirals market share (%) in the US, 2008
Figure 6.9: Oral soluble film products in the OTC sector

List of Tables
Table 2.1: US sales for opioid dependence ($m), 2008
Table 2.2: US sales for fenofibrate ($m), 2008
Table 2.3: Oral nanomedicines in development
Table 3.4: Global sales for calcitonin ($m), 2008
Table 3.5: Oral calcitonin products in development
Table 3.6: Major market sales for Forteo and Preotact ($m), 2008
Table 3.7: Oral PTH and analog products in development
Table 3.8: Global sales for bisphosphonates ($bn), 2008
Table 3.9: Oral bisphosphonates products in development
Table 3.10: Oral insulins in development
Table 3.11: Byetta (exenatide) sales in major markets ($m), 2008
Table 3.12: Oral GLP-1 and GLP-1 analogs in development
Table 3.13: Other oral peptide/protein products under development
Table 4.14: US sales for anti-Alzheimer's disease products ($m), 2008
Table 4.15: US sales for leading antidepressant products in N6A9 ($m), 2008
Table 4.16: US sales for SSRI antidepressants ($m), 2008
Table 4.17: US sales for leading beta-blockers plain ($m), 2008
Table 4.18: US sales for leading muscle relaxants ($m), 2008
Table 4.19: US sales for SNRI antidepressant products ($m), 2008
Table 4.20: Formulations to counter opiate/psychostimulant abuse
Table 5.21: Prodrug classification based on site of conversion to active drug
Table 5.22: Major market sales for Valtrex (valaciclovir) ($m), 2008
Table 5.23: Major market sales for Valcyte (valganciclovir) ($m), 2008
Table 5.24: US sales for herpes antivirals ($m), 2008
Table 5.25: Major market sales for Xeloda (capecitabine) ($m), 2008
Table 5.26: Leading antimetabolite anticancer drugs in the US ($m), 2008
Table 5.27: Leading antimetabolite anticancer drugs in Japan ($m), 2008
Table 5.28: US sales for leading psychostimulant drugs ($m), 2008
Table 5.29: Major market sales for Vistide (cidofovir) ($m), 2008
Table 5.30: Major market sales for Hycamtin (topotecan) ($m), 2008
Table 5.31: Major market sales for Gemzar (gemcitabine) ($m), 2008
Table 5.32: US sales of vinca alkaloid cancer agents ($m), 2008
Table 5.33: Major market sales for Taxotere (docetaxel) ($m), 2008
Table 5.34: Major market sales for methotrexate ($m), 2008
Table 5.35: US sales for leading anti-Parkinson's preparations ($m), 2008
Table 5.36: Major market sales for Zyvox (linezolid) ($m), 2008
Table 6.37: US sales for leading antiepileptic products ($m), 2008
Table 6.38: US sales for antismoking products ($m), 2008
Table 7.39: Bone Medical product development pipeline
Table 7.40: Diabetology product development pipeline
Table 7.41: Chimerix product development pipeline
Table 7.42: Ondek product development pipeline
Table 7.43: MBC Pharma product development pipeline
Table 7.44: MBC Pharma R&D collaborations, 2005- 09
Table 7.45: ImmuPharma product development pipeline
Table 7.46: Access product development pipeline
Table 7.47: Access R&D collaborations, 2003-09
Table 7.48: ActoGeniX product development pipeline
Table 7.49: ActoGeniX R&D collaborations, 2005-09
Table 7.50: Biocon Ltd product development pipeline
Table 7.51: Chiasma product development pipeline
Table 7.52: Emisphere product development pipeline
Table 7.53: Emisphere R&D collaborations, 2005-09
Table 7.54: Kytogenics product development pipeline
Table 7.55: Merrion product development pipeline
Table 7.56: Merrion R&D collaborations
Table 7.57: NOD Pharmaceuticals product development pipeline
Table 7.58: Oramed Pharmaceuticals product development pipeline
Table 7.59: Unigene product development pipeline
Table 7.60: Unigene R&D collaborations

発刊日

2010/04/01

体裁

PDF / 369ページ

販売価格

3,835USD

発行

Business Insights Ltd.

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