Source: FDA, National Drug Code (US) Revision Year: 2020
DEFINITY (Perflutren Lipid Microsphere) Injectable Suspension is an ultrasound contrast agent. The DEFINITY vial contains components that upon activation yield perflutren lipid microspheres. The vial contains a clear, colorless, sterile, non-pyrogenic, hypertonic liquid, which upon activation with the aid of a VIALMIX or VIALMIX RFID, provides a homogeneous, opaque, milky white injectable suspension of perflutren lipid microspheres. The suspension of activated DEFINITY is administered by intravenous injection.
The perflutren lipid microspheres are composed of octafluoropropane encapsulated in an outer lipid shell consisting of (R) – hexadecanoic acid, 1-[(phosphonoxy)methyl]-1,2-ethanediyl ester, monosodium salt (abbreviated DPPA); (R) - 4-hydroxy-N,N,N-trimethyl-10-oxo-7-[(1-oxohexadecyl)oxy]-3,4,9-trioxa-4-phosphapentacosan-1-aminium, 4-oxide, inner salt (abbreviated DPPC); and (R) - α-[6-hydroxy-6-oxido-9-[(1-oxohexadecyl)oxy]-5,7,11-trioxa-2-aza-6-phosphahexacos-1-yl]- ω-methoxypoly(ox-1,2-ethanediyl), monosodium salt; commonly called N-(methoxypolyethylene glycol 5000 carbamoyl)-1,2-dipalmitoyl-sn-glycero-3- phosphatidylethanolamine, monosodium salt (abbreviated MPEG5000 DPPE).
Octafluoropropane is chemically characterized as 1,1,1,2,2,3,3,3-octafluoropropane. It has a molecular weight of 188, empirical formula of C3F8 and has the following structural formula:
DPPA has a molecular weight of 670, empirical formula of C35H68O8PNa, and following structural formula:
DPPC has a molecular weight of 734, empirical formula of C40H80NO8P, and following structural formula:
MPEG5000 DPPE has an approximate molecular weight of 5750 represented by empirical formula C265H527NO123PNa, contains <100ppm Ca+2 and Mg+2 and the following structural formula:
Prior to activation, the DEFINITY vial contains 6.52 mg/mL octafluoropropane in the headspace which was required to be confirmed by positive IR spectroscopic testing in every vial. Each mL of the clear liquid contains 0.75 mg lipid blend (consisting of 0.045 mg DPPA, 0.401 mg DPPC, and 0.304 mg MPEG5000 DPPE), 103.5 mg propylene glycol, 126.2 mg glycerin, 2.34 mg sodium phosphate monobasic monohydrate, 2.16 mg sodium phosphate dibasic heptahydrate, and 4.87 mg sodium chloride in Water for Injection. The pH is 6.2-6.8. DEFINITY does not contain bacterial preservative.
After activating the contents of the DEFINITY vial, each mL of the milky white suspension contains a maximum of 1.2 × 1010 perflutren lipid microspheres, and about 150 microL/mL (1.1 mg/mL) octafluoropropane. The microsphere particle size parameters are listed in Table 2 below:
Table 2. Microsphere Size Distribution:
| Microsphere particle size parameters | |
|---|---|
| Mean diameter range | 1.1 µm – 3.3 µm |
| Percent less than 10 µm | 98% |
| Maximum diameter | 20 µm |
| Dosage Forms and Strengths |
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DEFINITY is supplied as a single use 2-mL clear glass vial or RFID-tagged vial containing a clear liquid in packages of four (4) and sixteen (16) single-use vials. Prior to activation, the headspace of each vial contains 6.52 mg/mL octafluoropropane and the clear liquid contains 0.75mg/mL of a lipid blend. After activation, each vial contains a maximum of 1.2 × 10 10 perflutren lipid microspheres, and about 150 microL/mL (1.1 mg/mL) octafluoropropane [see Description (11)]. |
| How Supplied |
|---|
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DEFINITY is supplied as a single use 2 mL clear glass vial or a single use 2 mL clear glass Radio Frequency Identification (RFID)-tagged vial containing clear liquid in packages of four (4) and sixteen (16) single-use vials.
Distributed By: Lantheus Medical Imaging, 331 Treble Cove Road, N. Billerica, Massachusetts 01862 USA |
| Drug | Countries | |
|---|---|---|
| DEFINITY | Canada, New Zealand, United States |
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