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Elemental Scientific prepfast ICP-MS: USP <232><233> Oral Drugs by Dilution Automated Inline Calibration and Sample Dilution Authors: Kyle Uhlmeyer and Paul Field (field@icpms.com) Brief The prepfast inline autodilution system with ICP-MS fully automates USP <233> sample dilutions and J based calibrations. The prepfast automatically 1) dilutes a single stock standard to build linear calibration curves surpassing all USP<233> validation criteria and 2) dilutes samples to the appropriate Total Dissolved Solids (TDS). Features Autocalibration from a single J stock standard Stability 10x Inline dilution 0.2% TDS USP <233> Definition: Auto Sample Dilution Priority Sample Dilution Daily walk-up and analyze ICP-MS instrument for USP Perfect for laboratories new to ICP-MS Automate labor intensive steps to significantly reduce notebook entries Elemental Scientific Figure 1. Stability is assessed (at 0.8J spike) throughout one analytical day. The long-term stability of the method is illustrated in a 7 1/2 hr run of 14 analytes from 150 analyses of oral medication. A drift of ± 2% RSD surpasses the USP acceptance criteria (± 20%) by a factor of 10. 1

1. Fill Loop V2:P7+ Load V1:P6 Load Sample Standard Waste S2:Carrier Carrier Vacuum 2. Dilute Sample V2:P7+ Inject S3:Diluent V1:P6 Load To ICPMS Sample Standard S2:Carrier Waste Carrier Vacuum To ICPMS 3. Inject Sample Clean V2 V2:P7+ Load S3:Diluent Figure 2. The prepfast system schematic illustrating a two-step process of loading sample into a loop and injecting sample while performing inline dilution. Rinse Standard Waste Abstract S2:Carrier Carrier The target value (J) for USP <233> defined calibration and validation is dependent on a drugs daily To dose. ICPMS Oral drugs have a wide range of daily doses that require drug specific J values and therefore drug specific Vacuum calibrations. The prepfast rapidly and automatically performs inline dilutions to build linear calibration curves from a single stock solution (r 2 > 0.999s) S3:Diluent for any J value. Dilution factors entered into the ICP-MS software 4. Clean are used V1 for precise and V2:P7+ accurate Inject inline dilution. Samples already in the solution V1:P6 Load phase are simply poured into a sample tube eliminating manual sample preparation. The seamlessly integrated prepfast ICP-MS system easily surpasses USP <233> validation criteria of, 1) stability < ± 5% (USP limit ± 20%), 2) repeatability < ± 3% (USP limit ± 20%), 3) ruggedness Standard < ± 4% (USP limit ± 25%) and 4) accuracy < ± 10% (USP limit Sample ± 20%). Automating the full calibration and sample Waste dilution process removes human error and reduces note book entries simplifying compliance S1:Rinse with FDA s 21 CFR Part 11 record integrity regulation. Carrier Vacuum To ICPMS S3:Diluent 5. Tune V2:P7+ Load V1:P6 Load 2 Sample Standard

Introduction All drugs absorbed through the digestive track and mucosal membranes are included in the oral category. The oral route has the greatest Permissible Daily Exposure (PDE) of all pathways outlined by USP <232>. Liquid oral drugs such as syrups and mucosal sprays can simply be diluted and analyzed by ICP-MS. USP <233> outlines specific validation protocols that require standardization, precision and spike recovery to be based on a target (J) value. J values vary as a function of PDE (mg/day), final dilution (dilution factor) and a drugs daily dose (g/day). This work will illustrate how the prepfast ICP-MS system automatically calibrates and dilutes samples, easily exceeding all acceptance criteria outlined by USP <233>. Table 1. The USP Chapter <232> defined PDE (µg/day) values for Oral drugs are used (Figure 3) to calculate target values (J). USP <233> requires a calibration curve and a series of QC validation protocols including repeatability, ruggedness and spike recovery be based on the J value. Table 1. Maximum Permissible Daily Exposure - PDE Element Oral Daily Dose PDE (µg/day) Cadmium 25 Lead 5 Arsenicb (Inorganic) 1.5 Mercuryb (Inorganic) 15 Iridium Osmium Palladium Platinum Rhodium Ruthenium Molybdenum Nickel 500 Vanadium Copper 0 USP <232> <233> Definition: Figure 3. USP <232><233> defined calculation of J using As as an example. PDE from Table 1 is combined with a hypothetical daily dose (20g) and a dilution factor of 500. It is clear from this calculation that J value is inversely proportional to the daily dose. 3

"J" Calibrations - 1g Daily Dose R 2 = 1.000000 2 J 0.5 J "J" Calibrations - 20g Daily Dose R 2 = 0.999999 2 J 0.5 J Figure 4. Fully automated inline dilutions of a single stock standard are used to generate linear calibration curves. The formula from Figure 3 is used to calculate J values for drugs with a wide range of daily doses (1 and 20 g/day are given as examples). Arsenic, the most challenging USP analyte with poor ionization efficiency, ArCl interference and the lowest PDE is easily autocalibrated with prepfast for a wide range of J values. 4

"J" Calibration Coefficients 1.000 0.999 Calibration Coefficient 0.998 0.997 0.996 0.995 1g/day 5g/day 10g/day 20g/day V Ni Cu As Mo Ru Rh Pd Cd Os Ir Pt Hg Pb Figure 5. Fully automated inline dilutions from a single stock standard generates linear (>0.9999) calibration curves over a wide range of J values for all USP elements. Figure 6. Simply pour solution (syrup) into tube and start analysis. Sample is autodiluted inline to appropriate TDS. 5

Repeatability USP <233> Definition: prepfast - ICP-MS RSD < 3.0% Figure 7. Repeatability for all analytes of interest of < ± 3% at 1J spike in over the counter flu remedy (liquid) is significantly below the USP accepted criteria of < ± 20% RSD. Ruggedness USP <233> Definition: prepfast - ICP-MS Average RSD = 4.0% Figure 8. The ruggedness of the method demonstrated on 3 separate days yields accuracy (recoveries) of < ± 10% and reproducibility of < ± 4%. The USP acceptance criteria is defined as < ± 25% RSD for each target analyte. 6

USP <233> Definition: Spike Recovery Figure 9. Excellent recovery for 1J spike in over the counter flu remedy (liquid) indicates the method is very robust; constantly yielding spike recoveries (< ± 10%) that are significantly better than the USP threshold (70-150%). Isotope Table 2. Results PDE (µg/day) 7 OTC Flu Remedy (Liquid) µg/day V 51 1.08 Ni 60 500 - Cu 63 0 - As 75 1.5 0.42 Mo 98 - Ru 102 0.04 Rh 103 - Pd 106 - Cd 111 25 - Os 192 - Ir 193 - Pt 195 - Hg 202 15 - Pb 208 5 - Table 2. Results for OTC liquid flu remedy are significantly lower than USP <232> PDEs.

Benefits prepfast autocalibration - Single multi-element standard for all J values prepfast auto inline dilution - Eliminate final manual dilution step Brings samples to constant total dissolved solids (0.2%) Easy-to-use automated system for USP protocols Pre-developed fully automated methods Exceeds all USP validation criteria: Stability, Repeatability, Ruggedness, and Accuracy Well-suited to the demands of a high throughput pharmaceutical laboratory SC-2 DX prepfast System 7277 World Communications Drive Omaha, NE 68122 USA Phone: 1.402.991.7800 Fax: 1.402.991.7799 Email: prepfast@icpms.com Web: www.prepfast.com www.icpms.com Elemental Scientific 14055