| Rapamune (sirolimus) is an immunosuppressive agent. Sirolimus is a macrocyclic lactone produced by Streptomyces hygroscopicus. The chemical name of sirolimus (also known as rapamycin) is (3S,6R,7E,9R,10R,12R,14S,15E,17E,19E,21S,23S,26R,27R,34aS)-9,10,12,13,14,21,22,23,24,25,26,27,32,33,34, 34a-hexadecahydro-9,27-dihydroxy-3-[(1R)-2-[(1S,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethyl]-10,21-dimethoxy-6,8,12,14,20,26-hexamethyl-23,27-epoxy-3H-pyrido[2,1-c][1,4] oxaazacyclohentriacontine-1,5,11,28,29 (4H,6H,31H)-pentone. Its molecular formula is C51H79NO13 and its molecular weight is 914.2. The structural formula of sirolimus is illustrated as follows.
Sirolimus is a white to off-white powder and is insoluble in water, but freely soluble in benzyl alcohol, chloroform, acetone, and acetonitrile.
Rapamune is available for administration as an oral solution containing 1 mg/mL sirolimus. Rapamune is also available as a white, triangular-shaped tablet containing 1 mg sirolimus, and as a yellow-to-beige triangular-shaped tablet containing 2 mg sirolimus.
The inactive ingredients in Rapamune Oral Solution are Phosal 50 PG® (phosphatidylcholine, propylene glycol, mono- and di-glycerides, ethanol, soy fatty acids, and ascorbyl palmitate) and polysorbate 80. Rapamune Oral Solution contains 1.5% - 2.5% ethanol.
The inactive ingredients in Rapamune Tablets include sucrose, lactose, polyethylene glycol 8000, calcium sulfate, microcrystalline cellulose, pharmaceutical glaze, talc, titanium dioxide, magnesium stearate, povidone, poloxamer 188, polyethylene glycol 20,000, glyceryl monooleate, carnauba wax, dl-alpha tocopherol, and other ingredients. The 2 mg dosage strength also contains iron oxide yellow 10 and iron oxide brown 70.
|
Product Name |
Rapamycin(Sirolimus) |
Manufacture Date |
09/10/2009 |
|
Batch No. |
091009 |
Report Date |
13/10/2009 |
|
Quantity |
1710G |
Expiry Date |
08/10/2011 |
|
Test Item |
Specifications |
Results |
|
Appearance |
Odorless , off-white to yellow crystalline powder |
Conforms |
|
Identification 1 |
The IR spectrum of potassium bromide preparation of the sample exhibits maxima at the same wavelengths as that of a similar preparation of in-house reference standard |
Conforms |
|
Identification 2 |
The UV spectrum of 95% Ethanol preparation of the sample exhibits maxima at 267nm, 277nm,288nm, as that of similar preparation of in-house reference standard |
Conforms |
|
Identification 3 |
The retention times of the peaks for the Trans- and cis-stereoisomers in the chromatogram of assay preparation corresponds to that in the chromatogram of the Standard preparation as obtained in the Assay |
Conforms |
|
Loss on dry |
≤ 0.5% |
0.3% |
|
Chromatographic purity Individual Impurity |
≤ 1.0% |
0.2% |
|
Total Impurities |
≤ 2.0% |
0.3% |
|
Heavy Metals |
≤ 0.002% |
＜0.002% |
|
Cis-stereoisomer of sirolimus |
≤ 5.0% |
1.3% |
|
Assay |
98.0%～102.0%(calculated cis-and trans- stereisomers of sirolimus on the anhydrous basis) |
99.4% |
|
Residual Organic Solvents |
|
|
Ethanol |
≤ 5000PPM |
16PPM |
|
Ethyl acetate |
≤ 5000PPM |
Not Detected |
|
Petroleum Ether |
≤ 1000PPM |
Not Detected |
|
Acetone |
≤ 5000PPM |
55PPM |
|
Conclusion：Pass | |
