DESCRIPTION
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WARNING: Increased susceptibility
to infection and the possible development of lymphoma
may result from immunosuppression. Only physicians
experienced in immunosuppressive theray and management
of renal or cardiac transplant patients should use
CellCept. Patients receiving the drug should be
managed in facilities equipped and staffed with
adequate laboratory and supportive medical resources.
The physician responsible for maintenance therapy
should have complete information requisite for the
follow- up of the patient.
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CellCept (mycophenolate mofetil) is the 2-morpholinoethyl
ester of mycophenolic acid (MPA); an immunosuppressive agent;
inosine monophosphate dehydrogenase (IMPDH) inhibitor.
The chemical name for mycophenolate mofetil (MMF) is
2-morpholinoethyl (E)-6-(l,3-dihydro-4-hydroxy-6-methoxy-7-methyl-3-oxo-5-isobenzofuranyl)-4-methyl-4-hexenoate.
It has an empirical formula of C23H31NO7 a molecular weight
of 433.50.
Mycophenolate mofetil is a white to off-white crystalline
powder. It is slightly soluble in water (43 µg/mL
at pH 7.4); the solubility increases in acidic medium
(4.27 mg/mL at pH 3.6). It is freely soluble in acetone,
soluble in methanol, and sparingly soluble in ethanol.
The apparent partition coefficient in 1-octanol/water
(pH 7.4) buffer solution is 238. The pKa values for mycophenolate
mofetil are 5.6 for the morpholino group and 8.5 for the
phenolic group.
Mycophenolate mofetil hydrochloride has a solubility
of 65.8 mg/mL in 5% Dextrose Injection USP (D5W). The
pH of the reconstituted solution is 2.4 to 4.1.
CellCept is available for oral administration as capsules
containing 250 mg of mycophenolate mofetil, tablets containing
500 mg of mycophenolate mofetil, and as a powder for oral
suspension, which when constituted contains 200 mg/mL
mycophenolate mofetil.
Inactive ingredients in CellCept 250 mg capsules include
croscannellose sodium, magnesium stearate, povidone (K-90)
and pregelatinized starch. The capsule shells contain
black iron oxide, FD&C blue #2, gelatin, red iron
oxide, silicon dioxide, sodium lauryl sulfate, titanium
dioxide, and yellow iron oxide.
Inactive ingredients in CellCept 500 mg tablets include
black iron oxide, croscannellose sodium, FD&C blue
#2 aluminum lake, hydroxypropyl cellulose, hydroxypropyl
methylcellulose, magnesium stearate, microcrystalline
cellulose, polyethylene glycol 400, povidone (K-90), red
iron oxide, talc, and titanium dioxide; may also contain
ammonium hydroxide, ethyl alcohol, methyl alcohol, n-butyl
alcohol, propylene glycol, and shellac.
Inactive ingredients in CellCept Oral Suspension include
aspartame, citric acid anhydrous, colloidal silicon dioxide,
methylparaben, mixed fruit flavor, sodium citrate dihydrate,
sorbitol, soybean lecithin, and xanthan gum.
CellCept Intravenous is the hydrochloride salt of mycophenolate
mofetil. The chemical name for the hydrochloride salt
of mycophenolate mofetil is 2-morpholinoethyl (E)-6-(l,3-dihydro-4
hydrochloride. It has an empirical formula ofC23H31NO7
HCl and a molecular weight of 469.96.
CellCept Intravenous is available as a sterile white
to off-white lyophilized powder in vials containing mycophenolate
mofetil hydrochloride for administration by intravenous
infusion only. Each vial of CellCept Intravenous contains
the equivalent of 500 mg mycophenolate mofetil as the
hydrochloride salt. The inactive ingredients are polysorbate
80, 25 mg, and citric acid, 5 mg. Sodium hydroxide may
have been used in the manufacture of CellCept Intravenous
to adjust the pH. Reconstitution and dilution with 5%
Dextrose Injection USP yields a slightly yellow solution
of mycophenolate mofetil, 6 mg/mL (For detailed method
of preparation, see DOSAGE AND ADMINISTRATION.)
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