Download pharmaceutical spray drying - CEPiA

PHARMACEUTICAL SPRAY DRYING
A Method of Choice to address Low API Solubility,
Poor Bioavailability and Drug Formulation Challenges
POOR API SOLUBILITY PRESENTS A GROWING
CHALLENGE FOR DRUG PRODUCT FORMULATION
AND DRUG DELIVERY
• Low aqueous API solubility and related poor bioavailability pose a significant hurdle for an
efficient drug formulation, in particular for oral delivery
• The number of APIs insoluble in water has reached very high levels among NCEs due to increasing drug lipophilicity for better targeting enzymes and membrane proteins or because
of increasing molecular complexity
• APIs within BCS Classes II and IV (Biopharmaceutical Classification System) having poor
solubility and permeability are especially problematic and frequently found among pipeline
developments
100%
50%
POORLY
SOLUBLE
APIs,
90%
POORLY
SOLUBLE
APIs,
40%
0%
Marketed Drugs
BCS II
Pipeline Drugs
BCS IV
BCS I
BCS III
POORLY SOLUBLE APIs INCREASINGLY FOUND AMONG
NEW DRUG DEVELOPMENTS
SPRAY DRYING IS A POWERFUL TECHNOLOGY TO
ADDRESS API SOLUBILITY CHALLENGES
PARTICULAR BENEFITS OF SPRAY DRYING
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High applicability combined with advantage of reduced formulation complexity
Increasingly utilized to improve solubility properties and bioavailability of APIs via an amorphous solid API dispersion in a suitable matrix
Convenient one-step process converting an API from a liquid form (e.g. solution,
suspension) directly into a powder under mild conditions and very short
residence time suitable for thermally unstable and sheer sensitive compounds
Established, robust technology operated at industrial commercial scale
for decades
Highly versatile, reproducible process that can be scaled up to nearly any
production size (batch or continuous mode) with lower cost (equipment,
utilities, cycle time) and better flexibility than lyophilization
Modifies various particle properties of API powders with good uniformity, such
as size distribution, dispersibility, flowability; increased surface area
achievable without a subsequent milling step
Very useful for inhalation products for particle size control
Applicable for a large variety of biopharmaceuticals from small molecules
to proteins
Convenient to convert oily compounds into powders via addition of suitable
adjuvants during the process
Utilized for improving direct compressibility, modified release and taste masking formulations, particle coating and microencapsulation
Improvement of dose variability and lowering required dose leading to less API consumption and cost savings during clinical studies
SANOFI CEPiA OFFERS PHARMACEUTICAL SPRAY
DRYING FROM CLINICAL TO COMMERCIAL
SCALE
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Extensive experience in pharmaceutical spray drying at Haverhill/UK site
Site operates under cGMP standards in controlled environment and has regularly been inspected by regulatory authorities including FDA, EMEA and MHRA
Capacity to support product requirements from clinical trials to large commercial scale
Feedstock (e.g. solution, suspension) can be prepared on site or received in liquid form; USP grade purified water available
Crystalline solutions can be re-dissolved and spray dried
Stirred feed systems
Clean-In-Place (CIP) system available
Environmental controls
Supplemental drying capabilities available, e.g. fluid bed
LABORATORY SPRAY DRYER
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1.5 liters/hour water evaporation rate at 250 oC inlet temperature
Sample feed up to 65 ml/hour
Inlet temperature 40-250 oC
Drying air throughput 38-73 m3/hour
Automatic jet de-blocking
INTERMEDIATE SCALE SPRAY DRYER
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Spray dried product volumes >100 mt/year (product dependent)
High pressure or two fluid atomization
100 liters/hour liquid flowrate
Temperature range: 200 oC inlet, 140 oC outlet
Bag filter
Nitrogen inertion for flammable powders
LARGE SCALE SPRAY DRYER
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Spray dried product volumes between 200 and >1,000 mt/year
(product dependent)
High pressure atomization
1,500 liters/hour liquid flowrate
Online control systems for measuring gas and feed flowrate
Internal cameras to monitor spray patterns and product recovery performance
Temperature range: 250 oC inlet, 140 oC outlet
Bag filter
Pneumatic hammers and air sweep system for enhanced product recovery
Explosion suppression system with fire detection and deluge system to handle
flammable powders
SANOFI CEPiA OFFERS PHARMACEUTICAL SPRAY
DRYING FROM CLINICAL TO COMMERCIAL
SCALE
ANALYTICAL CAPABILITIES
Portfolio of online and offline analytical testing:
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Process Analytical Technology (PAT)
o NIR, Raman, Mid-IR, UV
Particle Size Distribution (Mastersizer)
Particle Morphology
Feed Density & Feed Concentration
Dynamic Vapor Sorption (DVS)
Moisture Analysis
X-Ray Fluorescence (XRF)
GC, GC-MS, HS-GC, Pyrolysis-GC-MS
HPLC
MS, LC-MS
Differential Scanning Calometry (DSC)
Thermogravimetric Analysis (TGA), TGA-MS
Size Exclusion Chromatography
Ion Chromatography
Rheometry
NMR
Inductively Coupled Plasma - Optical Emission Spectrometry (ICP-OES)
Gel Electrophoresis
Titrimetry
Conductivity
Bulk/Tap Density
CONTACT
INFORMATION
CONTACT INFORMATION
www.cepia-sanofi.com
April 2016 - photo credits: SANOFI