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The world leader in serving science Kate Comstock Senior Marketing specialist Small molecule and E&L analysis Pharma/Biopharma Marketing, CMD Solution for Extractables & Leachables Analysis - Instruments, Software, Database/Spectral Library

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Page 1: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

The world leader in serving science

Kate Comstock Senior Marketing specialist Small molecule and E&L analysis Pharma/Biopharma Marketing, CMD

Solution for Extractables & Leachables Analysis - Instruments, Software, Database/Spectral Library

Page 2: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

2

• Introduction • Definitions • Industries need Extractable & Leachable (E&L) analysis • Regulatory and industry groups

• Thermo Fisher Scientific solution for extractable & leachable analysis • Multi instrumentations and technologies • Data Analysis software for ID, structure elucidation, and quantitation • Database and spectral library

Outline

Page 3: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

3

Plastics – A Complex Process

Courtesy of Doug Kiehl, Eli Lilly

Page 4: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

4

The Broad Market of Extractable & Leachable Analysis

Medicine container/packaging, implant and diagnostic devices

Single-use systems for bioproduction and storage

Food package Wearable Consumer Electronic Products Printing ink and adhesives

Page 5: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

5

Food Contact Material Migration Test is Mandatory! This image cannot currently be displayed.

Page 6: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

6

Wearable Consumer Electronic Products

The overall market for wearable technology is expected to reach USD 31.27 Billion by 2020, at a CAGR of 17.8% between 2015 and 2020.

Page 7: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

7

• Extractable (E) • Compounds that migrate from the surface under more aggressive conditions

of exposure (solvent, time, and temperature). Controlled extraction study

• Leachable (L) • Compounds that migrate from the contact surface to drug formulation under

normal conditions of exposure. Formulated drug or simulants

Definitions

Extractables

Leachables

Additives Impurities Polymer Components Degradation Products Solvent-material Interactions

Known extractables Extractable – drug formulation interactions Extractable modified by process conditions

Material Safety Product Quality

Some leachables are subset of extractable, but not always the case.

Safety/risk assessment Submission to regulatory agency Market

Page 8: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

8

Safety • Extractables and Leachables are Chemical Impurities, they could contaminate medicine, food,

and drink, affect product quality, and cause adverse effects for consumers.

Regulations • E&L analyses are highly regulated and required for market approval of new products. • More regulations have been made along the way and will continue into the future.

E&L analyses are challenging and complex • It requires multiple instruments, expertise, data processing software, and database. • It needs both identification and quantitation. Unknown structure elucidation is challenging. • It must start at early stage to be ready for product launch.

The Importance and Challenges of E&L Analyses

Page 9: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

9

E&L Regulatory and Method landscape

Industry Groups

National Regulators

Methods & Advisory Bodies

USP 1663 & 1664 665&1665 (drift)

Standardized Extractables Testing Protocol. Pharmaceutical Engineering 34 (2014)

Page 10: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

10

• FDA guidance • Container Closure Systems for Packaging Human Drugs and Biologics (May 1999) • 21 CFR 211.94

• EMA guideline • Guideline on plastic media packaging, EMEA/205/04

• ICH guidelines • Test procedures and acceptance criteria for new drug substances and drug products (Q6A,B) • Pharmaceutical development (ICH Q8)

• PQRI leachables and extractables working group (recommendations to the FDA) Safety thresholds and best practices for extractables & leachables in orally inhaled and nasal drugs

• USP Chapters • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter 661 (Containers – Plastics) • Chapter 1663 Extractables Associated with Pharmaceutical Packaging/Delivery Systems • Chapter 1664 Drug Product Leachables Associated with Pharmaceutical Packaging Delivery Systems • Chapter 1665_draft Plastic Components and Systems Used to Manufacture Pharmaceutical Drug Products.

• ISO 10993 parts (medical devices) • Japan, China, and other countries healthy authorities...

Regulations & Guidelines

Page 11: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

11

Industry Group: BioPhorum Operations Group (BPOG) The Global Community

http://www.biophorum.com/

BPOG members are leading biopharmaceutical companies around the world to create an environment where the global biopharmaceutical industry can collaborate and accelerate their rate of progress, for the benefit of all. Many Technical Resources on their website http://www.biophorum.com/

Page 12: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

12

Industry Group: Bio-Process Systems Alliance BPSA Published Technical Guides

http://bpsalliance.org/

BPSA members are industry-led corporate member of single use manufactures. BPSA is encouraging and accelerating the adoption technologies used in the production of biopharmaceuticals and vaccines. Many Technical Guides on their website http://bpsalliance.org/

Page 13: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

13

Extractable & Leachable Analysis

Page 14: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

14

• ICP-MS • ICP-OES

• ESI & APCI • LC-UV or CAD • LC-MS/MS • LC-HRMS • Library

• GC-MS • GC-HRMS • EI & CI • Library

• GC-MS • GC-HRMS • Headspace • EI & CI • Library

Volatile Impurities

Semi-Volatile Impurities

Elemental Impurities

Non-Volatile

Impurities

Analysis of Extractables & Leachables

Page 15: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

15

Thermo Scientific Instruments and Software for Impurity ID and E&L Analysis

ASE

ICPMS

Benchtop HRMS Q Exactive

Charged Aerosol Detector

GCMS-Triple Quad GCMS -Single Quad

Software & Database

FTIR

IC

Hybrid HRMS

U3000 UHPLC

Orbitrap Fusion Tribrid MS

Q Exactive GC-MS/MS

Vanquish UHPLC

Triple Quad

Page 16: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

16

GC-MS – Volatile and Semi-Volatile

Thermo Scientific™ TSQ™ 8000 Evo Triple Quadrupole GC-MS/MS

Thermo Scientific™ Q Exactive™ GC Orbitrap GC-MS/MS and Thermo Scientific™ TRACE™ 1310 GC

Thermo Scientific™ ISQ™ Single Quadrupole GC-MS/MS

Solid Phase Microextraction (SPME)

Page 17: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

17

Thermo Scientific Q Exactive MS Models for E&L Analysis

Thermo Scientific™ Q Exactive Plus MS

Thermo Scientific™ Q Exactive™ MS

Thermo Scientific™ Q Exactive™ Focus

Resolving Power: up to 280K @ m/z 200 Scan Range: 50-6,000

Resolving Power: 70K @ m/z 200 Scan Range: m/z50-2,000

Resolving Power: 140K @ m/z 200 Scan Range: 50-6,000

Page 18: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

18

Elemental Analysis

Thermo Scientific™ iCAP™ RQ ICP-MS Series

Thermo Scientific™ iCAP™ 7000 Plus Series ICP-OES

Thermo Scientific™ iCAP Q™ ICP-MS

Page 19: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

19

Thermo Scientific iCAP RQ ICP-MS and Thermo Scientific Qtegra Software

Extract Automated dilution and standard preparation

ICP-MS Compliant data processing

Fully compliant Thermo Scientific™ Qtegra™ ISDS software Full USP 233 & ICH Q3D method capabilities The current compliance deadline for USP 232 and 233 is January 1, 2018

USP <232>/<233>: Be Prepared for the Changes to Come

Thermo Scientific™ iCAP™ RQ ICP-MS Series

Page 20: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

20

Data Analysis Software, Database and Spectral Library for E&L Analysis

Thermo Scientific™ Compound Discoverer™ 2.1

Thermo Scientific™ TraceFinderTM targeted screening and Quan

Thermo Scientific™ mzVault 2.0 Library Search and Manager

TM

HighChem LLC E&L Compound Database

Thermo Scientific™Mass Frontier™ spectral interpretation software

Page 21: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

21

High Resolution Mass Spectrometer for E&L Analysis

Page 22: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

22

The Power of High Resolution

222.1 222.2

222.1253

222.1463

222.1838

Carbofuran

17.5 K

222.1 222.2

222.1124

222.1467

222.1843

222.1 222.20 0

222.1129

222.1465

222.1854

70 K 35 K

222.1237

222.1 222.20

222.1126

222.1466

140 K

Name Molecular Formula [M+H]+

Carbofuran C12H15NO3 222.1125

Formetanate C11H15N3O2 222.1237

O NHNHN

O

O

O O

NH

222.1238 222.1238

Carbofuran

Formetanate

Formetanate

not able to separate baseline separated partially separated completely baseline separated

∆M= 0.0109 Da

0.9 ppm

0.1 ppm

Page 23: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

23

292.0 292.5 293.0 293.5 294.0 294.5 295.0 295.5 296.0 296.5m/z

0

20

40

60

80

1000

20

40

60

80

1000

20

40

60

80

1000

20

40

60

80

1000

20

40

60

80

100292.04031

293.04327 294.03862 295.04121 296.04098292.04031

293.04327294.03622 295.03952 296.04098

292.04031

293.04327 294.03612 295.03958 296.04127292.04031

293.04368 294.03610 295.03948 296.04035292.04031

293.04368 294.03610 295.03947 296.04035

Very High Resolution Shows Isotope Fine Structure

A1 A2 A0 A1 A2

Parathion C10H15O5NPS

[M+H]+ = 292.04031

35K

75K

140K

240K

500K

15N13C

34S 18O

213C

13C33S

2H

13C

33S 15N 2H13C

OPO

NO

O

S

O

Page 24: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

24

• Mass Accuracy

• Isotopic Pattern Fidelity

• MSn Capabilities

MS Requirements for Characterization of Unknowns

Orbitrap MS High Resolution Accurate Mass (HRAM) data enable confident Component identification Elemental composition determination Structure characterization HR Quantitation

Instrument of Choice: Thermo Scientific™ Orbitrap™ MS

Page 25: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

25

Thermo Scientific Q Exactive MS - First Benchtop Orbitrap Mass Spectrometer

• Bench top • Tune Wizard • Method templates • Drag and drop • Robust • Plug and play

• Resolving power • Sensitivity • Acquisition speed • Mass accuracy • Dynamic range • Rapid polarity switching • Multiple ionization modes

Easy to use High Performance

Page 26: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

26

Thermo Scientific Q Exactive MS Schematics

Hyperbolic Quadrupole Mass filter

HCD Cell

Orbitrap Mass Analyzer

C-Trap

RF-Lens

Page 27: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

27

Thermo Scientific Orbitrap MS – Principle of Operation

1. Ions are injected through the source 2. …and trapped in the C-trap and squeezed into a smaller cloud 3. …then a voltage pulse across C-trap ejects ions towards the Orbitrap 4. …where they are trapped and detected

Collision cell C-Trap Octapole Split Lens

Flatapole

Skimmer

Tubelens

Capillary Orbitrap

Page 28: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

28

Thermo Scientific Q Exactive MS Specifications

• Max Resolution • 140,000 at m/z 200

• Max Scan Speed • Up to 12 Hz (at 17,500)

• Mass Accuracy • < 3 ppm external • < 1 ppm internal

• Mass Range: m/z 50 – 6,000 • Intra-scan Dynamic Range: > 5000:1 • Sensitivity

• Full MS: 500 fg Buspirone on column S/N 100:1 • SIM: 50 fg Buspirone on column S/N 100:1

• Polarity Switching • One full cycle in < 1 sec (one full scan positive mode and one full scan

negative mode at resolution setting of 35,000)

Resolution at m/z 200

Max. Scan Speed (Hz)

17,500 12 35,000 7 70,000 3 140,000 1.5

Page 29: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

29

Scan-to-Scan Mass Accuracy | Carbaryl, C12H11NO2

RMS = 0.62 ppm or 620 ppb across the peak

Resolution @ 70k 5 sec base peak

18 Pos scans

2.00 2.02 2.04 2.06 2.08 2.10 2.12 2.14 Time (min)

0

5

10

15

20

25

30

35

40

45

50

55

60

65

70

75

80

85

90

95

100

Rel

ativ

e A

bund

ance

0.84 ppm

0.62 ppm 0.62 ppm

0.69 ppm

0.84 ppm

0.62 ppm

0.47 ppm

0.77 ppm

0.54 ppm

0.32 ppm

0.24 ppm 0.16 ppm

0.54 ppm

0.69 ppm

0.69 ppm

0.69 ppm

0.24 ppm

0.84 ppm

Scan-to-Scan Mass Accuracy

Page 30: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

30

BPOG is Recommending Accurate MS for E&L Studies

Page 31: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

31

Additives and Their Unknown Degradants are Common Extractables

O

O

O

O

O

O

O

O

O

O

O

O

OO

O

O

OH

OH

OH

OH

O

OH O

OS

O

O O

OH OH

N2H

O

N

NN

OH

O

O O

O

O

O

OO

OH

OH

OH

OH

OH

N

N

N

O

O

O

OH

OH

OH

O

OH

O

O

OH

OP

O

O

Antioxidant, plasticizer, slipping agent, light stabilizer… also monomer, oligomer.

Page 32: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

32

RESTEK-STD-500ppb-APCI-MeOH-1 02/02/16 19:09:40APCI Accucore C18 2.1X100 2.6 um A: H2O/0.05% HAc/5mMNH4Ac B: MeOHRT: 8.4 - 35.6

10 12 14 16 18 20 22 24 26 28 30 32 34Time (min)

0

50

1000

50

1000

50

10027.1

27.1

27.022.7 27.325.3 28.326.5 29.5 30.724.321.48.5 34.69.5 16.69.8 10.4 16.111.2 22.712.0 17.712.9 13.5 14.5 30.820.4 33.719.0 32.9

27.1

27.1

27.3 28.3 29.5 30.724.321.4 26.122.716.616.1 17.7 24.620.4 33.713.8 31.115.2 19.0 34.623.8 32.98.6 13.010.6 12.411.810.222.7 27.2

25.3 26.5

8.5 34.68.7 9.4 10.3 11.2 12.1 30.713.4 14.0 25.614.8 23.921.916.1 29.524.416.5 17.3 21.418.0 19.0 29.328.019.6 33.731.7 32.3 35.2

NL: 3.49E8Base Peak MS RESTEK-STD-500ppb-APCI-MeOH-1

NL: 3.49E8Base Peak F: FTMS + p APCI corona Full ms [120.00-1600.00] MS RESTEK-STD-500ppb-APCI-MeOH-1

NL: 3.59E7Base Peak F: FTMS - p APCI corona Full ms [120.00-1600.00] MS RESTEK-STD-500ppb-APCI-MeOH-1

RESTEK-STD-500ppb-APCI-MeOH-1 #5755 RT: 30.68 AV: 1 NL: 1.52E7T: FTMS + p APCI corona Full ms [120.00-1600.00]

540 560 580 600 620 640 660 680 700 720 740 760 780m/z

0

10

20

30

40

50

60

70

80

90

100

Rel

ativ

e Ab

unda

nce

663.4532C 42 H64 O 4 P-0.6426 ppm

664.4565

665.4599607.3909608.3942533.5290 551.5036 666.4629575.5032

Irgafos 168 (Oxidation Product )

OP

O

O OP

O

O

O

(M+H)+

C42H63O3P (M+H)+ 647.45876

C42H63O4P (M+H)+ 663.4537

MS BP (+)

MS BP (-)

Page 33: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

33

Irgafos 168 Degradant ID by Full Scan (+/-) and MS/MS Spectra

200 250 300 350 400 450 500 550 600 650 700 750 m/z

0 20 40

80 100

475.2969

519.2610 497.2787

540.5350 359.3151

200 250 300 350 400 450 500 550 600 650 700 750 m/z

0 20 40 60 80

100 473.2826

541.2703 609.2575

60 80 100 120 140 160 180 200 220 240 260 280 300 320 340 360 380 400 420 440 460 480 500 m/z

0 20 40 60 80

100 363.1713

251.0465

307.1089

57.0708 419.2344 95.0497 153.0697 233.0371 175.0153 73.0284

50 63 75 88 100 113 125 138 150 163 175 188 200 213 225 238 250 263 275 288 300 313 325 338 350 363 375 388 400 413 425 438 450 463 475

0

10

20

30

40

50

60

70

80

90

100363.1712

251.0463

307.1088

419.2340

57.0708

364.1755

308.1128252.0505153.0698

475.2978420.2371175.015695.0496 233.0350 337.5264282.2958

OPOH

OO

H

OHPOOH

O

O P OOH

O H

O P OOH

O H

OPOH

O

O H

OPOOH

O

C28H43O4P (M+H)+ 475.2971 (M-H)- 473.2826

FISh and auto annotation for structure elucidation of Irgafos 168 Degradant

Full Scan (+)

Full Scan (-)

MS/MS (+)

Page 34: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

34

Quantitation of Octabenzone on Thermo Scientific Q Exactive Focus MS

327Y = -32228.1+812672*X R^2 = 0.9992 W: 1/X

0 200 400 600 800 1000ppb

0

100000000

200000000

300000000

400000000

500000000

600000000

700000000

800000000A

rea

327Y = -32228.1+812672*X R^2 = 0.9992 W: 1/X

0.2 0.4 0.6 0.8 1.0 1.2 1.4 1.6ppb

0

200000

400000

600000

800000

1000000

1200000

Are

a

O O

OH

Octabenzone Cas# 1843-05-6 C21H26O3 (M+H)+ 327.18092

Page 35: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

35

Quantitation of Tinuvin 328 on Thermo Scientific Q Exactive Focus MS

352 Y = 59802.9+851108*X R^2 = 0.9999 W: Equal

0 200 400 600 800 1000 ppb

0

100000000

200000000

300000000

400000000

500000000

600000000

700000000

800000000

900000000 A

rea

352Y = 59802.9+851108*X R^2 = 0.9999 W: Equal

0 2 4 6 8 10 12ppb

0

1000000

2000000

3000000

4000000

5000000

6000000

7000000

8000000

9000000

10000000

Are

a

N

NN

OH

Tinuvin 328 Cas# 21615-49-6 C22H29N3O (M+H)+ 352.23834

Page 36: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

36

LC-HRMS Analysis for IV Bag Extractables

UHPLC-HRMS Thermo Scientific™

Compound Discoverer™ 2.1

Software

Result

Thermo Scientific™ Q Exactive™ Plus MS and Thermo Scientific™ Vanquish UHPLC

Extractables Identified . _________ . _________ . _________ . _________

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20Time (min)

0

10

20

30

40

50

60

70

80

90

100

Re

lativ

e A

bu

nd

an

ce

9.2

6.18.1

6.1

10.1 12.113.211.010.5 13.8 15.88.4

12.96.58.87.3 10.0 11.53.5 14.47.86.9

Urine-8-12hr-1 #4384 RT: 8.74 AV: 1 NL: 8.12E6F: FTMS + p ESI Full ms [120.0000-1200.0000]

150 200 250 300 350 400 450 500 550 600 650 700 750 800 850m/z

0

10

20

30

40

50

60

70

80

90

100

Re

lativ

e A

bu

nd

an

ce

595.3498

310.2016

591.3188596.3531

311.2049267.1746219.0477 597.3562198.1280

E&L Mass List

HRAM data

Page 37: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

37

General Workflow for Small Molecule Impurity ID and E&L Analysis

UHPLC-HRMS

Thermo Scientific™ Compound

Discoverer ™2.1 Software

Result

Impurities Identified . _________ . _________ . _________ . _________

1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20Time (min)

0

10

20

30

40

50

60

70

80

90

100

Re

lativ

e A

bu

nd

an

ce

9.2

6.18.1

6.1

10.1 12.113.211.010.5 13.8 15.88.4

12.96.58.87.3 10.0 11.53.5 14.47.86.9

Urine-8-12hr-1 #4384 RT: 8.74 AV: 1 NL: 8.12E6F: FTMS + p ESI Full ms [120.0000-1200.0000]

150 200 250 300 350 400 450 500 550 600 650 700 750 800 850m/z

0

10

20

30

40

50

60

70

80

90

100

Re

lativ

e A

bu

nd

an

ce

595.3498

310.2016

591.3188596.3531

311.2049267.1746219.0477 597.3562198.1280

Custom Database Library

HRAM data

General Workflow for API Impurity and Extractable & Leachable Analysis

Page 38: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

38

• HRAM untargeted screening with polarity switching • ESI/APCI full scan MS and data-dependent top 3 MS/MS data with polarity switching

using 70K &17.5K resolution for FMS and HCD MS2 respectively. Stepped NCE: 30, 45, 60.

MS Method: High Resolution Accurate Mass Untargeted Screening

Positive Negative

Page 39: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

39

IV Bag IPA-H2O Extract - MS Base Peak Chromatogram and UV

D:\SGS-E&L\SGS-IVBag\IPA_H2O_Extract_2 Accucore C18 2.1x100 2.6 um A: H2O/0.05% HAc/5 mM NH4AC B:ACN/0.05% HAc/5mM NH4Ac

2 4 6 8 10 12 14 16 18 20 22 24 26 28 30 32 34 36 Time (min)

0

10000

20000

30000

40000

50000

uAU

Rel

ativ

e A

bund

ance

22.7

20.9 22.9 13.1 22.7

24.0 25.3 30.9 22.1 17.6 27.2

19.4 28.3 17.4 15.4 18.7 15.1 9.9 10.8 28.5 32.5 33.7 9.8 16.4 34.0 4.8 9.0 6.0 4.1 3.2 1.6

21.0 18.0

25.3

15.4 28.1 22.4 19.7 15.1 31.8 36.2 33.6 30.9 10.4 17.7 10.9 9.8 8.6 7.1 1.1 6.1 4.5 3.8

13.1 31.5 24.0 30.9 34.7 33.5 30.0 25.3 22.9 20.8 19.7 19.3 17.9 16.6 12.6 11.4 8.8 8.0 2.0 6.9 3.8 5.7

NL: 1.00E9 Base Peak F: FTMS + p ESI Full ms MS IPA_H2O_Extrac t_2

NL: 1.00E9 Base Peak F: FTMS - p ESI Full ms MS IPA_H2O_Extrac t_2

NL: 5.00E4 Total Scan PDA IPA_H2O_Extrac t_2

X = present in the blank

X X

MS Base Peak (+)

MS Base Peak (-)

UV 200-400 nm

Zoom-in View

Page 40: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

40

Full Scan and HCD MS/MS Data for Component ID and Structure Elucidation

G:\Old Passport\...\IPA_H2O_Extract_1 01/18/16 07:08:13Accucore C18 2.1x100 2.6 um A: H2O/0.05% HAc/5 mM NH4AC B:ACN/0.05% HAc/5mM NH4Ac C24 H39 O6: C24 H39 O6 pa Chrg 1

200 300 400 500 600 700 800m/z

0

10

20

30

40

50

60

70

80

90

100

Rel

ativ

e A

bund

ance

422.2899

405.2634

427.2451

149.0233

463.3162321.2057279.1589

343.1877

C24 H39 O6: C24 H39 O6 pa Chrg 1

200 300 400 500 600 700 800m/z

0

10

20

30

40

50

60

70

80

90

100

Rel

ativ

e A

bund

ance

405.2634

149.0234

427.2452

463.3163

389.2683335.2213

O

OO

O

O

50 63 75 88 100 113 125 138 150 163 175 188 200 213 225 238 250 263 275 288 300 313 325 338 350 363 375 388 400

0

13

25

38

50

63

75

88

100149.02341

57.0708371.08633 109.10157

83.08629 167.03340 276.19998202.07068

O

OH

O

OH

O

OH

O

OH

O

O

50 63 75 88 100 113 125 138 150 163 175 188 200 213 225 238 250 263 275 288 300 313 325 338 350 363 375 388 400

0

13

25

38

50

63

75

88

100149.02348

109.10166

127.11199

71.08636

83.08618

180.52640 256.29141

OH

O

OH

O

O

OHO

OHO

O

OO

O

O

O

(M+H)+

(M+H)+

422.2898

(M+NH4)+

(M+NH4)+

(M+Na)+

(M+Na)+

Full Scan Full Scan

HCD MS/MS HCD MS/MS

Page 41: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

41

Pos/Neg Switching Maintain High Mass Accurate Mass and Fine Isotope Pattern

200 210 220 230 240 250 260 270 280 290 300 310 320 330 340 350 m/z

0

50

100

Rel

ativ

e Ab

unda

nce

251.1214 C 13 H 19 O N 2 S 0.7336 ppm

253.1169 233.1108

200 210 220 230 240 250 260 270 280 290 300 310 320 330 340 350 m/z

0

50

100

Rel

ativ

e Ab

unda

nce

249.1066 C 13 H 17 O N 2 S -0.3776 ppm

304.9139 251.1023

253.11 253.12 253.13 m/z

253.1171

253.1272

253.1169

253.1272

Experimental

Theoretical

A+2 isotope pattern show separation of 34S and 213C at 70K

A+2

S

NNH

OH

Proposed Structure From O-Ring WFI Extract

Page 42: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

42

Ultra High Resolution MS Reveals Fine Isotope Structure

Accurate Mass

High Isotope Fidelity

MS/MS Spectrum

Fine Isotope Structure

HRAM Data

Structure Elucidation ------------ ------------ ------------ ------------

mzCloud

ChemSpider

Thermo E&L DB

CD 2.1 Result - Predicted Compositions for a unknown component in cosmetic product IPA/H2O extract

Thermo Scientific™ Fusion™ Lumos™ Tribrid™ MS 1 Million Resolution

#6 and #7

Page 43: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

43

A2 Isotope Fine Structure Validates Correct Elemental Composition

549.240 549.245 549.250 549.255 549.260m/z

0

10

20

30

40

50

60

70

80

90

1000

10

20

30

40

50

60

70

80

90

100

Rel

ativ

e A

bund

ance

549.2536549.2429

549.2515

549.2475549.2500

549.2564

549.2536

549.2511549.2473

549.2565549.2409 549.2594

549.240 549.245 549.250 549.255m/z

0

10

20

30

40

50

60

70

80

90

1000

10

20

30

40

50

60

70

80

90

100

Rel

ativ

e Ab

unda

nce

549.2536549.2429

549.2515

549.2475 549.2500 549.2564

549.2430 549.2540

549.2515

549.2500549.2476 549.2569549.2412

Experimental Experimental

Simulation C30H32N3O4P

Simulation C28H35NO7S

The correct formula matches the ana fine isotope structure.

15N13C

18O

33S13C

The incorrect formula doesn’t match the result.

#7 #6

The above results demonstrate that the fine isotope structure made available by ultra high resolution mass spectrometer greatly enhances the ability to confidently determine the correct unknown elemental composition.

Page 44: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

44

mzCloud - HR Mass Spectral Database

https://www.mzcloud.org

mzCloudTM - Advanced high resolution mass spectral database (Free) - Very high quality data: standardized acquisition, highly curated data - Search through spectrum, structure, substructure, m/z, … - Identifying compounds even when they are not present in the library through substructure search

Free and cloud-based

Page 45: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

45

mzCloud Spectral Library

Spectral tree Reference library

Search by different terms

Metadata available for selected library entry

Recalibrated spectra fragment ions annotation

Permanent citable links for entry, tree, and spectra

Breakdown curves

Page 46: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

46

Thermo Scientific mzVault 2.0

Exact Mass-Enabled Library Search and Management - local mzCloud - Creating customer library - Searching library

Page 47: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

47

E&L Compound Database the “E&L Mass List” in CD 2.1

This Excel sheet database contains ~2000 common E&L related compounds. This is a “living document” and new E&L related compounds are added periodically.

This database has been added to Thermo Scientific™ Compound Discoverer™ as “E&L Mass List”.

Page 48: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

48

Thermo Scientific Compound Discoverer 2.1 Software for Compound ID and Structure Elucidation

Component extraction and elemental composition prediction • HRAM data • Isotope pattern • fine isotope structure • MS/MS fragments

Unknown identification through multiple databases searching in parallel Known unknown compound ID

Unknown compound structure elucidation using “Structure Proposals” • Predicted Compositions • MS/MS fragment ions • The similarity search identify the fragment ions or substructures in mzCloud, which facilitated unknown structure elucidation.

De Novo ID Most Challenge Task Need Chemistry knowledge and expertise

Validity check of the proposed structure • using “FISh Scoring” feature by searching the embedded “HighChem Fragmentation Library”.

Differential Analysis for different lots, batch, or type samples analyses.

FISh stands for “Fragment Ion Search”

Page 49: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

49

Thermo Scientific Compound Discoverer 2.1 Software Study and Analysis Wizard

Creating a study and analysis use the guided “New Study and Analysis wizard”

Page 50: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

50

Pharma Label Extractable Study - Nodes-based Processing Workflow

Page 51: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

51

Result View – Data Interpretation

sub-tables

Page 52: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

52

469.32846 472.24991462.14740464.28354

479.31470461.28552460.28329 478.31226 482.26532

477.31000459.27982[M+H]+1481.26184[M+Na]+1

476.30664[M+NH4]+1

460 465 470 475 480 485m/z

0

10

20

30

40

50

Inte

nsity

[cou

nts]

(10^

6)

LF_IPA_Extrac-1-PN-1 (F2) #1230, RT=4.258 min, MS1, FTMS (+) C20 H42 O11 as [M+NH4]+1

Component Detection with Adducts Grouping

Resolution aware Mass accuracy Isotope pattern are color coded.

Page 53: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

53

Result Filters - Flexible Result Review

Filtering the result based on your need

Page 54: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

54

Multiple Database Searching in Parallel to Identify Known Unknowns

Mirror plot for each mzVault hit: observed MS2 vs. library MS2 • Matches collision energy between raw file MS/MS and reference MS/MS

Sub table show detailed info for compound

Page 55: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

55

Add Chemspider Search Result to “Structure Proposal and Apply FISh” for Unknown ID

FISh stands for “Fragment Ion Search”

Page 56: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

56

FISh Scoring Result: Fragment Ion Matching and Fragment Structure Annotation

95.08617C7 H11 [M-e]+1

225.23193C14 H29 N2 [M-e]+1309.3262

71.08630C5 H11 [M-e]+1

57.07080C4 H9 [M-e]+1

310.31003C20 H40 N O [M-e]+1226.21648C14 H28 N O [M-e]+1

282.27905C18 H36 N O [M-e]+1

254.24771C16 H32 N O [M-e]+1

100 200 300 400 500m/z

0.0

0.5

1.0

1.5

2.0In

tens

ity [c

ount

s] (1

0^6)

IPA_H2O_Extract_2 (F1) #9364, RT=35.375 min, MS2, FTMS (+), (HCD, DDF, 509.5041@(30;45;60), +1) N,N'-1,8-Octanediyldidodecanamide, C32 H64 N2 O2 FISh Co NH

NHO

O

Page 57: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

57

Unknown Structure Elucidation Based on CD 2.1 “Predicted Compositions”

226.18013222.14873224.18520 225.19609

223.00858223.15370

222.12064226.11403225.18463

225.14859223.16905

225.12189

226.12236222.96649 225.11076224.11839

223.11507[M+H]+1

223 224 225 226m/z

0

2

4

6

8

10

Inte

nsity

[cou

nts]

(10^

6) IPA_H2O_Extract_2 (F1) #2428, RT=10.245 min, MS1, FTMS (+) C13 H18 O S as [M+H]+1

225.12189

225.11076

225.09 225.10 225.11 225.12 225.13 225.14m/z

0

100

200

300

400

500

600

700

800

900

Inte

nsity [

co

un

ts]

(10

^3

)

IPA_H2O_Extract_2 (F1) #2428, RT=10.245 min, MS1, FTMS (+) C13 H18 O S as [M+H]+1

Page 58: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

58

Unknown Structure Elucidation Using Compound Annotation Editor and FISh Scoring

Propose structure based on “Predicted Composition” and MS/MS fragments

Apply “FISh Scoring” to search the embedded “HighChem Fragment Library”

Page 59: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

59

FISh Scoring Result: Fragment Ion Matching and Fragment Structure Annotation

224.11726

206.10915139.05728

105.07021107.0858664.97821

161.04135C10 H9 S [M-e]+1175.0573

73.06555C4 H9 O [M-e]+1205.10481C13 H17 S [M-e]+1

151.05766C9 H11 S [M-e]+1

162.04982C10 H10 S [M-e]+1

223.11511C13 H19 O S [

177.07326C11 H13 S [M-e]+1

163.05760C10 H11 S [M-e]+1

50 100 150 200m/z

0

100

200

300

400

500

600

700

800

Inte

nsity

[cou

nts]

(10^

3)

IPA_H2O_Extract_2 (F1) #2429, RT=10.250 min, MS2, FTMS (+), (HCD, DDF, 223.1151@(30;45;60), +1) C13 H18 O S FISh Coverage: 9 D

S

O

Page 60: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

60

Specialized Traces

Page 61: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

61

Specialized Traces Provide Additional Information

DAD Signal Overlay

Page 62: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

62

CD 2.1 Differential Analysis Feature: Volcano Plot

Using the interactive volcano plot to find compounds that are significantly different between two sample groups

Page 63: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

63

Thermo Scientific Compound Discoverer Software Home Page http://mycompounddiscoverer.com

Page 64: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

64

Thank you! www.thermofisher.com/learnleachables

[email protected]

Page 65: Solution for Extractables & Leachables Analysis · • Chapter 87,88 (materials direct or indirect in contact with patients biological reactivity test in vitro, in vivo) • Chapter

65

• Plasticizers • Flame Retardants • Impact Modifiers • Antioxidants • Antimicrobials • UV Stabilizers • Colorants • Lubricants & processing aids

Some of the Common Additives