Question
Posted on: April 8 2014Formula + stability data for rapamycin (Rapamune) 0.2% ointment
Answer
Finding a formula for a topical application of sirolimus is not obvious. I read that you should go out of tablets which is not conducive to an ointment or cream. According to the literature, sirolimus would be well soluble in chloroform and consequently you could extract the tablets, rinse the undissolved affiltrate and the rest on the filter twice with chloroform.. To date, I could find the following possibilities for a topical product
A. This chloroform solution in various portions mix with a quantity of starch powder and let the chloroform evaporate ; This adsorption mix with petroleum jelly to the appropriate concentration
B. In analogy with tacrolimus, you could also try the following.
1. The extraction with chloroform remains the same
2. Let all chloroform evaporate and mix the evaporative residue with cetiol or isopropyl palmitate (10% of total mass ointment?) ; I suspect that sirolimus dissolves in this solvent
3. Dilute with petroleum jelly to final weight.
EITHER
Extract in chloroform evaporate by evaporation of chloroform at room temperature; Once cloudy, the chloroform extract will be mixed with PLO gel (supplied by Bassron)
I cannot findstability data;
Literature Sirolimus-Vaselin 0.1%:
Document 1 Document 2 Document 3 Document 4