PHARMACEUTICAL SPRAY DRYING. A Method of Choice to address Low API Solubility, Poor Bioavailability and Drug Formulation Challenges

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1 PHARMACEUTICAL SPRAY DRYING A Methd f Chice t address Lw API Slubility, Pr Biavailability and Drug Frmulatin Challenges

2 POOR API SOLUBILITY PRESENTS A GROWING CHALLENGE FOR DRUG PRODUCT FORMULATION AND DRUG DELIVERY Lw aqueus API slubility and related pr biavailability pse a significant hurdle fr an efficient drug frmulatin, in particular fr ral delivery The number f APIs insluble in water has reached very high levels amng NCEs due t increasing drug lipphilicity fr better targeting enzymes and membrane prteins r because f increasing mlecular cmplexity APIs within BCS Classes II and IV (Bipharmaceutical Classificatin System) having pr slubility and permeability are especially prblematic and frequently fund amng pipeline develpments 100% 50% POORLY SOLUBLE APIs, 90% POORLY SOLUBLE APIs, 40% 0% Marketed Drugs Pipeline Drugs BCS II BCS IV BCS I BCS III POORLY SOLUBLE APIs INCREASINGLY FOUND AMONG NEW DRUG DEVELOPMENTS

3 SPRAY DRYING IS A POWERFUL TECHNOLOGY TO ADDRESS API SOLUBILITY CHALLENGES PARTICULAR BENEFITS OF SPRAY DRYING High applicability cmbined with advantage f reduced frmulatin cmplexity Increasingly utilized t imprve slubility prperties and biavailability f APIs via an amrphus slid API dispersin in a suitable matrix Cnvenient ne-step prcess cnverting an API frm a liquid frm (e.g. slutin, suspensin) directly int a pwder under mild cnditins and very shrt residence time suitable fr thermally unstable and sheer sensitive cmpunds Established, rbust technlgy perated at industrial cmmercial scale fr decades Highly versatile, reprducible prcess that can be scaled up t nearly any prductin size (batch r cntinuus mde) with lwer cst (equipment, utilities, cycle time) and better flexibility than lyphilizatin Mdifies varius particle prperties f API pwders with gd unifrmity, such as size distributin, dispersibility, flwability; increased surface area achievable withut a subsequent milling step Very useful fr inhalatin prducts fr particle size cntrl Applicable fr a large variety f bipharmaceuticals frm small mlecules t prteins Cnvenient t cnvert ily cmpunds int pwders via additin f suitable adjuvants during the prcess Utilized fr imprving direct cmpressibility, mdified release and taste masking frmulatins, particle cating and micrencapsulatin Imprvement f dse variability and lwering required dse leading t less API cnsumptin and cst savings during clinical studies

4 SANOFI CEPiA OFFERS PHARMACEUTICAL SPRAY DRYING FROM CLINICAL TO COMMERCIAL SCALE Extensive experience in pharmaceutical spray drying at Haverhill/UK site Site perates under cgmp standards in cntrlled envirnment and has regularly been inspected by regulatry authrities including FDA, EMEA and MHRA Capacity t supprt prduct requirements frm clinical trials t large cmmercial scale Feedstck (e.g. slutin, suspensin) can be prepared n site r received in liquid frm; USP grade purified water available Crystalline slutins can be re-disslved and spray dried Stirred feed systems Clean-In-Place (CIP) system available Envirnmental cntrls Supplemental drying capabilities available, e.g. fluid bed LABORATORY SPRAY DRYER 1.5 liters/hur water evapratin rate at 250 C inlet temperature Sample feed up t 65 ml/hur Inlet temperature C Drying air thrughput m3/hur Autmatic jet de-blcking INTERMEDIATE SCALE SPRAY DRYER Spray dried prduct vlumes >100 mt/year (prduct dependent) High pressure r tw fluid atmizatin 100 liters/hur liquid flwrate Temperature range: 200 C inlet, 140 C utlet Bag filter Nitrgen inertin fr flammable pwders LARGE SCALE SPRAY DRYER Spray dried prduct vlumes between 200 and >1,000 mt/year (prduct dependent) High pressure atmizatin 1,500 liters/hur liquid flwrate Online cntrl systems fr measuring gas and feed flwrate Internal cameras t mnitr spray patterns and prduct recvery perfrmance Temperature range: 250 C inlet, 140 C utlet Bag filter Pneumatic hammers and air sweep system fr enhanced prduct recvery Explsin suppressin system with fire detectin and deluge system t handle flammable pwders

5 SANOFI CEPiA OFFERS PHARMACEUTICAL SPRAY DRYING FROM CLINICAL TO COMMERCIAL SCALE ANALYTICAL CAPABILITIES Prtfli f nline and ffline analytical testing: Prcess Analytical Technlgy (PAT) NIR, Raman, Mid-IR, UV Particle Size Distributin (Mastersizer) Particle Mrphlgy Feed Density & Feed Cncentratin Dynamic Vapr Srptin (DVS) Misture Analysis X-Ray Flurescence (XRF) GC, GC-MS, HS-GC, Pyrlysis-GC-MS HPLC MS, LC-MS Differential Scanning Calmetry (DSC) Thermgravimetric Analysis (TGA), TGA-MS Size Exclusin Chrmatgraphy In Chrmatgraphy Rhemetry NMR Inductively Cupled Plasma - Optical Emissin Spectrmetry (ICP-OES) Gel Electrphresis Titrimetry Cnductivity Bulk/Tap Density

6 CONTACT INFORMATION CONTACT INFORMATION April pht credits: SANOFI