Fusion Pro QbD-aligned DOE Software

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Fusion Pro QbD-aligned DOE Software Statistical Experimental Design Analysis & Modeling Robustness Simulation Numerical & Graphical Optimization 2D, 3D, & 4D Visualization Graphics 100% aligned with Quality by Design Principles and Guidelines S-Matrix Corporation 1594 Myrtle Avenue Eureka, CA 95501 USA Phone: 707-441-0404 URL: www.smatrix.com

Initial DOE Software Development and Verification Software development began in the mid-1990s in consultation with recognized leaders in the field of Statistical Design of Experiments methodology. DOE Verification by Douglas C. Montgomery, Ph.D. Dr. Montgomery is a well known authority in the field of Industrial Statistics with a special emphasis on Design of Experiments. He is the author of the best selling book Design and Analysis of Experiments (John Wiley and Sons, Inc.). Dr. Montgomery has consulted in the development and verification of all major DOE features, including: Wizard guided experiment design selection Wizard guided data analysis Automated regression modeling capabilities 2

Initial DOE Software Development and Verification DOE Verification by John A. Cornell, Ph.D. Dr. Cornell is considered the foremost authority on mixture experiment design. He is the author of the best selling book Experiments With Mixtures (John Wiley and Sons, Inc.). Dr. Cornell worked closely with S-Matrix on development of our mixture design and analysis capabilities. Among the specific capabilities that he has guided and verified are: Unconstrained and Singly-constrained Mixture Designs Unconstrained and Singly-constrained Mixture-Process Designs Mixture-Process Designs with Multicomponent Constraints Analysis of Mixture and Mixture-Process Experiment Data 3

[ICH Q8(R2) - Guidance for Industry, Pharmaceutical Development, August, 2009] Quality by Design (QbD) A systematic approach to development that begins with predefined objectives and emphasizes product and process understanding and process control, based on sound science and quality risk management.. Formal Experimental Design A structured, organized method for determining the relationship between factors affecting a process and the output of that process. Also known as Design of Experiments. QbD Design Space The multidimensional combination and interaction of input variables (e.g., material attributes) and process parameters that have been demonstrated to provide assurance of quality. 4

QbD Design Space QbD Design Space - The multidimensional combination and interaction of input variables (e.g., material attributes) and process parameters that have been demonstrated to provide assurance of quality. Curves defining the acceptable performing regions are generated by equations (models) IMPORTANT interactions also induce curvature in response surfaces The design space is the un-shaded overlapping region of acceptable performance [ICH Q8(R2) - Page 23] 5

Fusion Pro Critically Differentiating Features Which Support QbD-aligned R&D 1. Automated Design of Experiments (DOE) 2. Response Data Handler 3. Automated Analysis and Modeling 4. Fully Integrated Monte Carlo Robustness Simulation 5. Best Answer Search Wizard 6. Design and Operating Space Characterization 6

Feature 1 Automated DOE Integrated DOE with Automated and User-interactive Design Modes Automated Mode selects the most efficient design for you. 7

Automated DOE Integrated DOE with Automated and User-interactive Design Modes User-interactive Mode you select and tailor the design. 8

Feature 2 Response Data Handler (RDH) Handles Response Data Simply and Easily Single test result per run. Descriptive Statistics multiple test results per run. Time Series results at multiple time points per run. 9

Single Test Result Per Run Responses consisting of only one measurement per run (no test repeats) can be entered directly onto the Experiment Design grid. 10

Descriptive Statistics multiple test results per run 11

Descriptive Statistics multiple test results per run 12

Descriptive Statistics multiple test results per run Can automatically: handle test repeat data handle non-normally distributed data Log-normal Exponential Gamma Weibull compute descriptive statistics based responses compute differences of all statistics from a reference standard map all computed responses to the experimental design for analysis 13

Time Series results at multiple time points per run Can automatically handle: Uniform or variable testing protocols Multiple sample preparation repeats Multiple test repeats at each time point Internal test standard data 14

Time Series results at multiple time points per run Can automatically: handle test repeat data compute average profiles compute f1 & f2 curve fit metrics compute sensitive Weibull curve fit metrics compute additional profile response metrics Map all computed responses to the experimental design for analysis 15

Feature 3 Automated Analysis and Modeling 1. Statistical DOE runs information rich data set. 2. Automated modeling generates a highly predictive and diagnostic model for each critical performance characteristic studied. 120.0 Spray Rate 50 55 40.0 10 Atomizing Air 4.0 Gun Distance 10.0 Hardness = 9.3 + 4.2(GD) - 5.4(SR) 2 + 12.7(AA) 2 + 1.3(PA*GD) + 1.6(SR) 2 AA+ Interaction Linear Effects Curvature Effects Complex Effects Effects 16

Automated Analysis and Modeling Automated Modeling Includes: Error Analysis Regression Analysis Transformation Analysis Outlier Analysis Instant Analysis Reports Include: Model Sufficiency Summary Analysis Detail Reports Error Analysis Regression Analysis Residuals Report and Graphs Transformation Analysis Coefficients Table and Model Mean Effects Report and Plot 17

Feature 4 Fully Integrated Robustness Simulation Simultaneously optimize mean performance and robustness during development! NOTE - the value defines the maximum expected setpoint variation for the study factor. 18

Fully Integrated Robustness Simulation Simultaneously optimize mean performance and robustness during development! NOTE - the Tolerance Limit Delta values define the maximum allowable ± limits on response variation. 19

Fully Integrated Robustness Simulation Atomizing Air (psi) Pattern Air (psi) Spray Rate (gm/min) Gun-to-Bed Distance (inches) Critical Quality Attribute (CQA) X Process Flow Simulate 10,000 Runs = variation around setpoint Acceptable Variation Process A - Small Variation Process B - Large Variation 20

Process Capability - Quantified Process Capability (C p ) a direct, quantitative measure of process robustness used routinely in Statistical Process Control (SPC) applications. The classical SPC definition of Inherent Process Capability (C p ) is UTL LTL C p = 6 σ var iation Critical Quality Attribute (CQA) X LTL UTL UTL and LTL 6σ Variation = Tolerance Limits (tolerance width). = ±3σ process output variation. Traditional Goal 1.33 - based on setting the UTL and LTL at ±4σ of process performance variation. - Note: a 6-sigma process would have a C p = 2.00 6σ Variation 21

Process Capability: Example Response = f1 (curve fit metric) 6σ c p = = 1.00 6 σ ±3σ Variation = Tolerance Limit Interval X LTL UTL ±3σ ±3σ 3.0 7.0 API - % released f1 22

Process Capability: Example Response = f1 (curve fit metric) 8σ c p = = 1.33 6 σ ±3σ Variation = 75% of Tolerance Limit Interval X LTL UTL ±4σ ±3σ 3.0 7.0 API - % released f1 23

Process Capability: Example Response = f1 (curve fit metric) 12σ c p = = 6 σ 2.00 ±3σ Variation = 50% of Tolerance Limit Interval X LTL ±6σ UTL ±3σ 3.0 7.0 API - % released f1 24

Fully Integrated Robustness Simulation Simultaneously optimize mean performance and robustness during development! With built in robustness metrics no additional experiments are needed! f1 = 5.00: C p < 1.00: Good Mean Performance Poor Robustness (steep slope) X 3.0 5.0 7.0 API - % Released f1 25

Fully Integrated Robustness Simulation Simultaneously optimize mean performance and robustness during development! With built in robustness metrics no additional experiments are needed! f1 = 5.00: C p 1.33: Good Mean Performance Good Robustness (shallow slope) X 3.0 5.0 7.0 API - % Released f1 26

Feature 5 Best Answer Search Wizard 27

Best Answer Search Wizard 28

Feature 6 Design and Operating Space Characterization Edge of Failure Mean Performance Edges of Failure Robustness 29

Design and Operating Space Characterization Design Space joint region of acceptable mean performance and robustness. Operating Space Joint safe operating ranges of critical study parameters 30

Design and Operating Space Characterization 31

Design and Operating Space Characterization Acceptable Mean Performance all performance characteriastics Acceptable Robustness all performance characteriastics 3 rd Factor = Low 3 rd Factor at 3 rd Factor = High Setpoint 32

Design and Operating Space Characterization Tablet Coater Optimization Example 33

Design and Operating Space Characterization Tablet Coater Optimization Example 34

Final Report Output file formats include Word and PDF 35

Conclusions The Fusion Pro QbD-based Approach: Greatly accelerates successful R&D through: - Automation - Statistically valid experimentation - Novel data treatments Provides quantitative knowledge of all critical parameter effects Enables establishing Design Space for both: - Mean Performance (setpoint optimization) - Process Robustness (operating space) Required time for the work is dramatically reduced Success promotes further the use of QbD 36

Fusion Pro QbD-aligned R&D Software Case Study 1 Tablet Coating Process

Case Study 1 Tablet Coating Process The experiment was undertaken to optimize a tablet coating process for several critical tablet quality characteristics. The two which will be discussed in this case study are Hardness and Dissolution (% Released profile). The four critical process parameters (CPPs) selected for study are entered into the Experiment Setup template shown below. 38

Automated Experiment Design Generation One Click: Software maps the experimental design to the study factors. 55.0 PAP (psi) Spray Rate 0.0 10.0 AAP 50.0 (psi) 39

Case Generate Study Design 1 Tablet Statistical Coating Efficiency Process 5 levels of Atomizing Air Pressure 5 levels of Pattern Air Pressure 5 levels of Spray Rate 5 levels of Gun-to-Bed Distance 5 x 5 x 5 x 5 = 625 possible combinations Fusion Screening design = 25 runs (excluding replicates) ~ 25x efficiency. 40

Create Case Study Testing 1 Design Tablet Coating Hardness Process Testing. 41

Testing Case Study Design 1 Data Tablet Entry Coating Hardness Process Data 42

Response Data Reductions Hardness Data Software automatically: handles test repeat data handles non-normally distributed data Log-normal Exponential Gamma Weibull computes descriptive statistics based responses computes differences of all statistics from a reference standard Maps all computed responses to the experimental design for analysis 43

Response Data Reductions Hardness Data 44

Create Testing Design Time Series (Dissolution) Testing. Software automatically handles: Uniform or variable sampling plans Multiple sample preparation repeats Multiple test repeats at each time point Internal test standard data 45

Create Testing Design Import Test Results From the CDS. 46

Response Data Reductions Time Series (Disso) Data Software automatically: handles test repeat data computes average profiles compute f1 & f2 curve fit metrics computes sensitive Weibull curve fit metrics computes additional profile response metrics Maps all computed responses to the experimental design for analysis 47

Response Data Reductions Time Series (Disso) Data 48

Analysis Wizard. Automated Mode One Click: Software automatically creates a predicitve and diagnostic equation (model) for each response that characterizes the effects of the study variables on the response. 49

Numerical Answer Search Best Overall Conditions Set goals and Acceptable Performance Limits for each Response 50

Numerical Answer Best Overall Conditions The software automatically identifies and reports the best overall answer the level setting combination which meets your defined performance goals for all responses simultaneously. 51

Graphical Visualization Best Overall Conditions The graphics wizards can generate graphical representations which visualize the linear, interaction, and complex effects of the study variables for each critical response. 52

Graphical Visualization Best Overall Conditions Note: different Critical Quality Attributes have different regions of good performance. X- Axis = Pattern Air Pressure (psi) Y-Axis = Spray Rate (mg/min) Atomizing Air Pressure = 10 psi Gun-to-Bed Distance = 9 inches 53

Graphical Visualization Mean Performance Design Space Fusion Pro Overlay Graph. Each color on the graph corresponds to a response for which goals have been defined. Note: Shaded region indicates the Spray Rate and Gun-to-Bed Distance combinations which do NOT meet performance requirements. A region shaded with a given color shows the study variable level setting combinations that will NOT meet the goals for the corresponding response. Note: the un-shaded region corresponds to level setting combinations that meet all response goals. 54

Graphical Visualization Mean Performance Design Space Unshaded Region With Predicted Best Settings: AAP = 21.0 psi PAP = 55.0 psi Spray Rate = 60.0 gm/min G-to-B Distance = 9.0 inches 55

Graphical Visualization Mean Performance Design Space Mean Performance Edges of Failure 56

Robustness Simulation Expected Variation of CPPs NOTE - the value defines the maximum expected setpoint variation for the study factor. 57

Robustness Simulation Acceptable Variation Limits in CQAs NOTE - the Tolerance Limit Delta values define the maximum allowable ± limits on response variation. 58

Final Design and Operating Space Mean Performance + Robustness The software automatically visualizes the final robust design space. 59

Final Design and Operating Space Mean Performance + Robustness You can also graphically represent your safe operating ranges within the region, and the software will define verification runs to demonstrate that all performance goals are met. 60

Fusion Pro QbD-aligned R&D Software Case Study 1 END

Fusion Pro QbD-aligned R&D Software Case Study 2 Tablet Excipient Formulation & Processing

Case Study 2 Tablet Excipient Study The three critical excipient formulation parameters (CPPs) selected for study are entered into the Experiment Setup template shown below. The one critical excipient process parameter (CPPs) selected for study is also entered into the Experiment Setup template shown below. 63

Case Study 2 Tablet Excipient Study The experiment was undertaken to optimize the excipient formulation and the critical process parameter for two critical tablet quality attributes: Friability and Dissolution Profile For the dissolution response, the two critical release goals were: 10% Released at t = 10 minutes 25% Released at t = 60 minutes. 64

Automated Experiment Design Generation One Click: Software maps the experimental design to the study factors. 65

Case Enter Study Test Results 1 Tablet Friability Coating Process Testing Responses consisting of only one measurement per run (no test repeats) can be entered directly onto the Experiment Design grid. 66

Create Testing Design Time Series (Dissolution) Testing Software automatically handles: Uniform or variable sampling plans Multiple sample preparation repeats Multiple test repeats at each time point Internal test standard data 67

Create Testing Design Enter Test Results 68

Response Data Reductions Time Series (Disso) Data Software automatically: handles test repeat data computes average profiles compute f1 & f2 curve fit metrics computes sensitive Weibull curve fit metrics computes additional profile response metrics Maps all computed responses to the experimental design for analysis Two critical release goals: % Released at t = 10 minutes % Released at t = 60 minutes. 69

Analysis Wizard. Automated Mode One Click: Software automatically creates a predicitve and diagnostic equation (model) for each response that characterizes the effects of the study variables on the response. 70

Numerical Answer Search Best Overall Conditions Set goals and Acceptable Performance Limits for each Response 71

Numerical Answer Best Overall Conditions The software automatically identifies and reports the best overall answer the level setting combination which meets your defined performance goals for all responses simultaneously. 72

Graphical Visualization Best Overall Conditions The graphics wizards can generate graphical representations which visualize the linear, interaction, and complex effects of the study variables for each critical response. 73

Graphical Visualization Mean Performance Design Space Fusion Pro Overlay Graph. Each color on the graph corresponds to a response for which goals have been defined. Note: Shaded region in this graph identifies all excipient formulations which do NOT meet performance requirements for % Released at 10 Minutes. A region shaded with a given color shows the study variable level setting combinations that will NOT meet the goals for the corresponding response. Note: the un-shaded region corresponds to level setting combinations that meet all response goals. 74

Graphical Visualization Mean Performance Design Space Edges of Failure Unshaded Region With Predicted Best Settings: Excipient 1 = 20% Excipient 2 = 23% Excipient 3 = 57% Compaction Forve = 20 kn 75

Robustness Simulation Expected Variation of CPPs NOTE Enter the expected variation (±3σ value) around target setpoint for each study variable. 76

Robustness Simulation Acceptable Variation Limits in CQAs NOTE - the Tolerance Limit Delta (± value) defines the maximum acceptable limits on process performance variation. This can be your Process Specification. 77

Final Design and Operating Space Mean Performance + Robustness The software automatically visualizes the final robust design space. 78

Final Design and Operating Space Mean Performance + Robustness You can also zoom in and graphically represent your safe operating ranges, and the software will define verification runs to demonstrate that all performance goals are met. 79

Fusion Pro QbD-aligned R&D Software Case Study 2 END