Mespiperone C11Injection
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»Mespiperone C11Injection is a sterile,isotonic solution,suitable for intravenous administration,of 3–N-[11C]methylspiperone in which a portion of the molecules are labeled with radioactive 11C.It contains not less than 90.0percent and not more than 110.0percent of the labeled amount of 11Cexpressed in GBq (or mCi)at the time indicated in the labeling.Its specific activity is not less than 18.5GBq (500mCi)per µmol.
Specific activity—
Chromatographic system—
Proceed as directed in the test for Chemical purity.
Procedure—
Calculate the specific activity,in MBq (or mCi)per µmol,of Mespiperone C11Injection by the formula:
3.11(CrPr)/C,
in which Cris the radioactivity content,in MBq (or mCi)per mL,as determined in the Assay for radioactivity,Pris the radiochemical purity (in %),as determined in the test for Radiochemical purity,and Cis the concentration (in µg per mL)of 3-methylspiperone in the Injection,as determined in the test for Chemical purity.
Packaging and storage—
Preserve in single-dose or in multiple-dose containers that are adequately shielded.
Labeling—
Label it to include the following:the time and date of calibration;the amount of 11Cas methylspiperone expressed as total GBq (or mCi)at time of calibration;the expiration time and date;the lot or batch number;and the statements,“Caution—Radioactive Material”and “Do not use if cloudy or if it contains particulate matter.”The labeling indicates that in making dosage calculations correction is to be made for radioactive decay,and states that the radioactive half-life of 11Cis 20minutes.
Radionuclide identification (see Radioactivity á821ñ)—
Its gamma-ray spectrum is identical to that of a specimen of 11Cin that it exhibits a positron annihilation peak at 0.511MeVand possibly a sum peak of 1.022MeV,dependent on geometry and detector efficiency.
Bacterial endotoxins á85ñ—
It contains not more than 175/VUSP Endotoxin Unit per mLof the Injection,in which Vis the maximum recommended total dose,in mL,at the expiration time.
pHá791ñ:
between 4.5and 7.
Radionuclidic purity á821ñ—
Using a multichannel analyzer,count all radioactivity from 40to 2500KeVto determine the absence of radiation,other than at 0.511MeVand 1.022MeV,over a period of 4hours.Determine the half-life (20minutes)by a suitable detector system.
Chemical purity—
Mobile phase—
Prepare a filtered and degassed mixture of acetonitrile and 0.05Mmonobasic potassium phosphate (70:30).Make adjustments if necessary (see System Suitabilityunder Chromatography á621ñ).
Standard solution—
Dissolve an accurately weighed quantity of 3-methylspiperone hydrochloride in Mobile phase,and dilute quantitatively,and stepwise if necessary,with Mobile phaseto obtain a solution having a known concentration of about 0.1mg per mL.
Test solution—
Pipet an accurately measured volume of Injection into a suitable container,and dilute with Mobile phaseto obtain a solution containing about 0.1mg per mL.
Chromatographic system
(see Chromatography á621ñ).The liquid chromatograph is equipped with a 254-nm detector and a 3.9-mm ×30-cm column that contains packing L1.The flow rate is about 0.8mLper minute.For simultaneous analysis of radiochemical purity,a suitable radioactivity detector (see Radioactivity á821ñ)is coupled to the system.Chromatograph the Standard solution,and record the peak responses as directed for Procedure:the column efficiency determined from the analyte peak is not less than 100theoretical plates,the tailing factor for the analyte peak is not more than 1.1,and the relative standard deviation for replicate injections is not more than 3.2%.
Procedure—
Inject about 20µLof the Test into the chromatograph,record the chromatogram,and measure the peak responses.Separately calculate the percentage of each impurity in the portion of Injection taken by the formula:
100(ri/rs),
in which riis the peak response obtained for each impurity,and rsis the sum of the responses of all of the peaks:not more than 0.2%of any individual impurity is found,and the sum of all impurities is not more than 0.9%.
Radiochemical purity á821ñ—
Proceed as directed in the test for Chemical purity,except that the liquid chromatograph is also equipped with a suitable collimated radioactivity detector.The radioactivity under the main peak is not less than 98%of the total radioactivity measured.
Other requirements—
It meets the requirements under Injections á1ñ,except that the Injection may be distributed or dispensed prior to completion of the test for Sterility,the latter test being started on the day following final manufacture,and except that it is not subject to the recommendation on Volume in Container.
Assay for radioactivity á821ñ—
Using a suitable counting assembly (see Selection of a Counting Assemply),determine the radioactivity,in GBq (or mCi)per mL,of Injection by use of a calibrated system.
Auxiliary Information—
Staff Liaison:Andrzej Wilk,Ph.D.,Senior Scientific Associate
Expert Committee:(RMI)Radiopharmaceuticals and Medical Imaging Agents
USP28–NF23Page 351
Phone Number:1-301-816-8305