Film Coating Equipment - Continuous Coating

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Film Coating Equipment - Continuous Coating Barry Friend Technical Manager

Agenda Batch Manufacture Machine types Scale up problems Continuous Coaters Advantages Recent developments Operation Test Cases

Film coater types Fully perforated pans Partially perforated pans Non-perforated (conventional) pans Modified conventional pans Fluid bed coaters Continuous coaters

Insect screen Pre-heater Dehumidifier Typical Air Handling Requirements HEPA filter 99.99% Pre-filter 96% 5µ Exhaust fan Thermostat Secondary Filter 96% 5µ HEPA Filter 99.99% Humidifier Prefilter 86% 5µ DP DP DP DP DP Inlet fan Main heater Airflow gauge Bypass damper Airflow gauge Exhaust damper Inlet damper DP = Differential Pressure Monitor

Fully Perforated Pans Scale Up Pan Diameter (in/cm) Capacity (Litres) Airflow Volume (cu.m/hr) 12"/30 1 100 15" /40 3 200 19"/50 10 400 24" /60 12 500 30" /75 40 800 36" /90 105 2050 48 /120 150 2300 60 /150 350 6500 30" /75m Continuous 2000L/hr 17000

Pan Diameter - Bed Depth Comparison 75 cm (30 ) Pan Pan Load ~45-55 kg 150cm (60 ) Pan Pan Load ~250-350 kg <30cm Bed Depth >60 cm Bed Depth

Continuous Coating - Advantages Variable output capability depending on machine size Shorter product dwell times in the coating pan (i.e.10-20 min) More uniform distribution of coating material due to: Shallow bed depth More frequent presentation of product to the spray zone Potential for less tablet attrition Simpler scale up Potential for PAT application and QbD One continuous coater could replace several batch coaters

Continuous Coating - Advantages Scale up from 30 batch pan to 30 continuous pan Batch Continuous Common parameters Atomizing air (Bar) 2.0 2.0 Pattern air (Bar) 2.5 2.5 Inlet temp. ( C) 75 75 Exhaust temp. ( C) 47 47 Gun to bed distance (in) 8 8 Gun to Gun distance (in) 6 6.1 Nozzle qty 2 28 Pan speed (RPM) 20* 12 Scalable parameters Pan load (kg) 13 130 Airflow (CFM) 750 7500 Solution flow (L/min) 0.220 2.20 Coating time (mins) 15.5 N/A Residence time (mins) N/A 15.5 Weight gain (%) 3.1 3.0

Continuous Coating - Advantages Capacities and throughputs Models FC C250 FC C500 FC C1200 Process rate @ 3% kg/h 125 250 250 500 600 1200 Air volume m 3 /h 1800 3500 3500 8500 8500 20400 Temperature range C 45 85 45 85 45 85 Type of spray nozzles Anti-bearding Anti-bearding Anti-bearding Spray rate g/min 220 750 450 1500 1500 3600 Pan diameter mm (inches) 380 (15) 480 (19) 760 (30) Width mm (inches) 815 (32) 915 (36) 1350 (53) Depth mm (inches) 2500 (100) 3050 (120) 5260 (207) Height mm (inches) 1850 (72) 2135 (84) 2590 (102)

Continuous Coating - Recent Developments Spray gun design improvements Software controlled spray gun and process sequencing Continuous processing with minimal losses More flexibility for different product volumes Coating options Batch coating Batch/continuous coating

Spray gun design - Gun "Bearding" Turbulent Airstream Around Air Cap Inlet Airstream

Spray gun design - ABC Principle Smooth Flow Airstream Around Air Cap Inlet Airstream

ABC spray gun setup

Operation of the Continuous Coater Extended, small diameter, cylindrical, perforated coating pan

Operation of the Continuous Coater Discharge into dryer/cooler Product Container Controlled feeder Coating Pan

FC C- Rotary Drum Coater

Loading and Discharge Equipment Spiral cooling elevator (not shown) can be integrated for rapid cooling of tablets at discharge of coater Tablet feeding and discharge conveying systems to reduce or eliminate manual tablet handling

Continuous Coating - Original Process LOAD "Click" to start loading Only suitable for large volume products Weight gains limited to approximately 3-4% w/w of core weight Product waste at start up and shutdown Restricted use to high volume single product situations No ethical pharma use due to validation complexity and high volume restrictions Spray gun control and blockage

Continuous Coating - Original Process COAT "Click" to stop coating Partly Fully coated product to for reject sale

Continuous Coating - Original Process PROCESS END Partly coated/uncoated Fully Process end product to for reject sale

Batch/Continuous Coating - New Process LOAD "Click" to start loading "Click" to start coating In batch mode, the pan exit is sealed and the machine filled with tablets. Tablets are spraying to end point. At this point, tablets can either be discharged just as in a normal batch coating or the process can be converted to a continuous process by opening the pan exit and feeding more uncoated tablets.

Batch/Continuous Coating - New Process BATCH COAT "Click" to start continuous coating Colour change indicates the coating build up. Spraying stops at end point

Batch/Continuous Coating - New Process CONTINUOUS COAT "Click" to stop coating Collect fully coated product for sale New tablets are fed in and guns start sequentially

Batch/Continuous Coating - New Process PROCESS END Collect Process fully coated end product for sale At end point guns stop sequentially

Continuous Coating Trials

Trial 1- Comparison Immediate Release coatings Reason for trial: To evaluate the color uniformity and tablet appearance in both batch and continuous modes. To evaluate product loss typically associated with previous continuous coating technology. Opadry II 85F series high performance film coating system polymer system PVA Suspension solids 20% Opadry II 57U series film coating system polymer system HPMC Suspension solids 17% Substrate Calcium/Vitamin D tablets End point 3% weight gain.

Trial 1- Comparison of Immediate Release coatings Target coating process conditions Batch mode process parameters Continuous mode process parameters Inlet temperature ( C) 80-85 80-85 Exhaust temperature ( C) 50-52 47-52 Product temperature ( C) 44-49 44-49 Airflow (CFM) 9500 9500 Pan pressure ( P) -0.01-0.01 Pan speed (rpm) 16 16 Bed depth (in.) 5.5 5.5 Weigh belt feed rate (kg / hr) n/a 1100-1300 Solution flow rate (g/min.) 3000 3000 Coating solids concentration (%) 20 20 Batch size (kg) 250 250 initial fill - continuous thereafter

Trial 1: Color Development and Uniformity Opadry II 57U - O'Hara Batch Mode Total Color Difference from Reference E (n=20) 20 18 16 14 12 10 8 6 4 2 Uncoated core = 43.69 E from target color reference 250 kg Batch size Limit of visual color detection E = 2 0 0 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 Elapsed Coating Time (min)

Trial 1: Color Development and Uniformity Opadry II 57U - O'Hara Batch/Continuous Mode Total Color Difference from Reference E (n=20) 20 18 16 14 12 10 8 6 4 2 Batch mode 1450 kg Batch size Continuous mode Limit of visual color detection E = 2 Discharge mode 0 0 5 10 15 20 25 30 35 40 45 50 55 60 65 70 75 80 85 Elapsed Coating Time (min)

Trial 1: Color Development and Uniformity Opadry II 85F - O'Hara Batch Mode Total Color Difference from Reference E (n=20) 20 18 16 14 12 10 8 6 4 2 Uncoated core = 47.62 DE from target color reference 250 kg Batch size Limit of visual color detection E = 2 0 0 1 2 3 4 5 6 7 8 9 10 11 12 13 14 Elapsed Coating Time (min)

Trial 1: Color Development and Uniformity Opadry II 85F - O'Hara Batch/Continuous Mode Total Color Difference from Reference E (n=20) 20 18 16 14 12 10 8 6 4 2 Batch mode 1450 kg Batch size Continuous mode Limit of visual color detection E = 2 Discharge mode 0 0 5 10 15 20 25 30 35 40 45 50 55 60 65 70 75 80 Elapsed Coating Time (min)

Trial 1 Conclusions No product waste Batch mode operation has immediate use in the pharmaceutical industry Significantly reduced process time and exposure of tablets to the coating environment Potential for reduced coating weight gains compared to traditional batch coaters At high solids concentration, both PVA based and HPMC based Opadry II systems were well suited for continuous coater operations

Trial 2 Delayed Release Coating Reason for trial: To evaluate the delayed release performance in continuous mode. To evaluate product loss typically associated with previous continuous coating technology. Nutrateric, nutritional enteric coating system Polymer system Ethylcellulose, Suspension solids 10% Substrate Mineral oil (placebo) softgel capsules End point 3.5% weight gain Throughput 200 kg/hr Samples taken for testing directly from discharge point.

Trial 2 Delayed Release Coating Target coating process conditions Continuous mode process parameters Batch size (Kg) 100 Weigh belt feed rate (kg / hr) Coating solids concentration (%) Suspension Quantity (Kg) Suspension flow rate (g/min.) Suspension flow rate (g/min/gun.) 200 10 35 1200 50

Trial 2: Delayed Release Testing Mineral oil (placebo) softgel capsules Uncoated - 5 minutes in SGF* Nutrateric coated - 60 minutes in SGF* *Simulated Gastric Fluid

Trial 2: Delayed Release Testing Samples taken when product discharge begins, then every 5 minutes for 30 minutes Immersed in simulated gastric fluid (SGF) for 60 minutes. Then selected samples immersed in simulated intestinal fluid (SIF) until disintegrated. Sample time from 1st exit from coater (min) 0 5 10 15 20 25 30 Disintegration time in SGF (n=6), (min) > 60 > 60 > 60 > 60 > 60 > 60 > 60 Disintegration time in SIF (n=6), (min) 27.0 Not tested 37.0 Not tested 31.5

Trial 2: Conclusions No product waste at start-up or shut-down Consistent enteric performance was achieved from start-to-finish The Nutrateric coating provided acid resistance at 3.5% weight gain with a throughput of 200 kg/hr Process was trouble-free

Continuous Coating - Overall Conclusions Recent advances in continuous coating control allow for batch and continuous operation with consistency from start-to-finish and no product waste Opadry II systems (PVA and HPMC) and Nutrateric delayed release coating system well suited for continuous coater applications High speed production Immediate applications for OTC and nutritional products Potential applications for continuous coating of pharma products dependant on GMP/validation issues Batch mode possibilities for large volume pharma products immediately available.

Trial 3 Tablet Migration DoE Reason for trial: To evaluate tablet migration through the Ohara FCC1200 pan without the use of directional mixing baffles to determine an optimal material flow range. Substrate Placebo caplets Marker placebo Coated cores were fed through the system at various rates. During each feed rate, 100 marker tablets were introduced and timed through the machine.

Trial 3 Tablet Migration DoE Measuring Methods: Multiple web cameras with multi-pc interface and custom software for analysis of video with marker tablets. 100 colored marker tablets with white tablet bed background started just ahead of spray zone for each set of conditions. 8 cameras running at 5 frames/second in the first half of the drum. Large quantities of raw data (200+ GB) Custom analysis software to look at pixel counts in each frame (post processed). Individual frame analysis to get information to improve exit data. (accurate start times and process lengths) 1 Time recorder tracking time that the marker tablets exit in relation to the test start time with use of Excel macro. DOE to see main effects Monte Carlo simulation model to tease out relationships

Trial 3 Tablet Migration DoE Images showing recognition (in green) of red marker tablets

Trial 3 Tablet Migration DoE Design-Expert Software SD/Rev 0.2137 0.0492 X1 = A: Feed Rate X2 = C: Bed Depth POOR Uniformity 0.18 0.15 Actual Factors B: Tilt = 1.50 D: Atomazation = 0.50 SD/Rev 0.12 0.09 0.06 BETTER Uniformity 6 5.625 C: Bed Depth 5.25 4.875 4.5 600 750 900 1050 A: Feed Rate 1200

Trial 3 Tablet Migration DoE Conclusion The relationship of bed depth and feed rate (axial transport speed) is the major driver for tablet diffusion/distribution growth rate and the resulting coating uniformity performance at a particular drum speed. Impact of atomization and pattern air is a visible but minor impact on uniformity performance. The variation of time in coating zone is what affects the tablet to tablet uniformity, not total residence time. (Allows mixing at ends for Batch mode start up). Bed tilt has an indirect effect on diffusion, it is needed to maintain flat/uniform depth at specified feed rate. Bed tilt needs to change From batch to continuous.

The information contained herein, to the best of Colorcon, Inc. s knowledge, is true and accurate. Any recommendations or suggestions of Colorcon, Inc. with regard to the products provided by Colorcon, Inc. are made without warranty, either implied or expressed, because of the variations in methods, conditions and equipment which may be used in commercially processing the products, and no such warranties are made for the suitability of the products for any applications that you may have disclosed. Colorcon, Inc. shall not be liable for loss of profit or for incidental, special or consequential loss or damages. Colorcon, Inc. makes no warranty, either expressed or implied, that the use of the products provided by Colorcon, Inc., will not infringe any trademark, trade name, copyright, patent or other rights held by any third person or entity when used in the customer s application. All trademarks, except where noted, are property of BPSI Holdings LLC. BPSI Holdings LLC, 2010