OPTIRAY 350 - ioversol injection
OPTIRAY 320 - ioversol injection
OPTIRAY 300 - ioversol injection
OPTIRAY 240 - ioversol injection
OPTIRAY 160 - ioversol injection
Mallinckrodt Inc.
Rx only
WARNING
NOT FOR INTRATHECAL USE
DESCRIPTION
OPTIRAY (ioversol injection) formulations are sterile, nonpyrogenic, aqueous solutions intended for intravascular administration as diagnostic radiopaque media. Ioversol is designated chemically as N,N'-Bis (2,3-dihydroxypropyl)-5-[N-(2-hydroxyethyl) -glycolamido] -2,4,6-triiodoisophthalamide and has the following structural formula:
The molecular weight of ioversol is 807.11 and the organically bound iodine content is 47.2%. Ioversol is nonionic and does not dissociate in solution.
Each milliliter of OPTIRAY 350 (ioversol injection 74%) contains 741 mg of ioversol with 3.6 mg of tromethamine as a buffer and 0.2 mg of edetate calcium disodium as a stabilizer. OPTIRAY 350 provides 35% (350 mg/mL) organically bound iodine.
Each milliliter of OPTIRAY 320 (ioversol injection 68%) contains 678 mg of ioversol with 3.6 mg of tromethamine as a buffer and 0.2 mg of edetate calcium disodium as a stabilizer. OPTIRAY 320 provides 32% (320 mg/mL) organically bound iodine.
Each milliliter of OPTIRAY 300 (ioversol injection 64%) contains 636 mg of ioversol with 3.6 mg of tromethamine as a buffer and 0.2 mg of edetate calcium disodium as a stabilizer. OPTIRAY 300 provides 30% (300 mg/mL) organically bound iodine.
Each milliliter of OPTIRAY 240 (ioversol injection 51%) contains 509 mg of ioversol with 3.6 mg of tromethamine as a buffer and 0.2 mg of edetate calcium disodium as a stabilizer. OPTIRAY 240 provides 24% (240 mg/mL) organically bound iodine.
Each milliliter of OPTIRAY 160 (ioversol injection 34%) contains 339 mg of ioversol with 3.6 mg of tromethamine as a buffer and 0.2 mg of edetate calcium disodium as a stabilizer. OPTIRAY 160 provides 16% (160 mg/mL) organically bound iodine.
The pH of the OPTIRAY formulations has been adjusted to 6.0 to 7.4 with hydrochloric acid or sodium hydroxide. All solutions are sterilized by autoclaving and contain no preservatives. Unused portions should be discarded. OPTIRAY solutions are sensitive to light and therefore should be protected from exposure.
Some physical and chemical properties of these formulations are listed below:
|
|
OPTIRAY |
OPTIRAY |
OPTIRAY |
OPTIRAY |
OPTIRAY |
|
|
160 |
240 |
300 |
320 |
350 |
Ioversol content
(mg/mL) |
339 |
509 |
636 |
678 |
741 |
Iodine content
(mg I/mL) |
160 |
240 |
300 |
320 |
350 |
Osmolality
(mOsm/kg
water) |
355 |
502 |
651 |
702 |
792 |
|
Viscosity (cps) |
|
|
|
|
|
|
at 25°C |
2.7 |
4.6 |
8.2 |
9.9 |
14.3 |
|
at 37°C |
1.9 |
3.0 |
5.5 |
5.8 |
9.0 |
Specific Gravity
at 37°C |
1.188 |
1.281 |
1.352 |
1.371 |
1.405 |
The OPTIRAY formulations are clear, colorless to pale yellow solutions containing no undissolved solids. Crystallization does not occur at room temperature. The products are supplied in containers from which the air has been displaced by nitrogen. OPTIRAY solutions have osmolalities 1.2 to 2.8 times that of plasma (285 mOsm/kg water) as shown in the above table and are hypertonic under conditions of use.
CLINICAL PHARMACOLOGY
The pharmacokinetics of ioversol intravascularly administered in normal subjects conform to an open two compartment model with first order elimination (a rapid alpha phase for drug distribution and a slower beta phase for drug elimination). Based on the blood clearance curves for 12 healthy volunteers (6 receiving 50 mL and 6 receiving 150 mL of O
