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I know that some of you make your own spironolactone topicals (either solutions or creams), so the following should be very relevant and comforting for you do-it-yourselfers!
Even though I also make some of my own topical concoctions, I've always felt slightly uneasy about the general technique of crushing-up spironolactone tablets and mixing them in with Rogaine or other topical vehicles. Does the spironolactone REALLY get dissolved into the alcohol, or does it just stay behind in all that sediment which falls to the bottom of the bottle? I finally decided to put that to the test, and the results appear to be an unequivocal and SPECTACULAR success! :lol: Here's a brief outline of what I did, and afterwards I'll even go into a little more detail by posting the actual numbers I got:
I've previously posted that I use generic spironolactone tablets ("Spirotone" brand) which contain 100 mg of spironolactone each. The tablets themselves weigh 500 mg, so that means that they must contain 100 mg of the active drug and 400 mg of inert tablet fillers and excipients (that's what _apparently_ forms that messy sludge which refuses to dissolve in alcohol!). I took one Spirotone tablet and finely powdered it in a mortar and pestle, just to make sure that every bit of the spironolactone in it would dissolve (assuming it was going to dissolve, of course) in the next step. I dumped the tablet powder into a small glass vial of known weight. Measuring the weight of the vial + powder, I verified the exact mass of the powder sitting at the bottom.
Next I added about 12 mL of pure Everclear, enough to be sure that it could completely dissolve all the spironolactone in that powdered tablet (assuming that it was in fact going to dissolve, of course...I pre-calculated that the concentration of spironolactone in the Everclear would be around the 1% level, which I figured it should easily be able to hold). I capped the vial and THOROUGHLY shook it over an extended period of time to be CERTAIN that the alcohol in the Everclear would completely dissolve whatever it was going to dissolve. Then I set the vial down in a cool, dark place to let the undissolved sediment slowly settle to the bottom of the vial.
24 hours later, it had settled-out nicely, leaving a pale yellow liquid (Everclear and whatever solute it contained) sitting over a milky-looking sediment. Next came the tricky and tedious part: I sat down with a long, slender glass eyedropper with a narrow tip at the end and SLOWLY and CAREFULLY removed as much of that Everclear above the sediment as I could. I did it without moving or jostling the vial, so that the sediment wouldn't get stirred-up and withdrawn by accident, along with the liquid. It took me about 45 minutes of tedious effort to do that (with beads of sweat popping out on my forehead), but I got rid of just about every last bit of liquid that I safely could (about 96% of the liquid, as I was able to calculate later). This left only the sediment lying in the bottom of the vial, which was still wet with a little remaining Everclear. I set the vial out to air-dry the rest of the way by itself.
Two days later it was completely bone-dry, with just the sediment remaining in the vial. And here came the CRITICAL STEP: I weighed the vial and its contents for one last time, and it was EXACTLY 400 mg higher than the empty starting weight of the vial!! It was "dead nuts", to use the technical term! :lol: That proved beyond any reasonable doubt that the Everclear did in fact dissolve all 100 mg of the spironolactone in the crushed-up tablet, and left behind all 400 mg of the fillers and excipients (BTW, this also demonstrates a simple way to remove all that sediment: just remove the good spironolactone-containing liquid with an eyedropper, and discard the remaining junk). I was _thrilled_ to be able to satisfy for myself that the fundamental process that we've been using with spironolactone tablets is sound. Further experiments I'll be doing (Part 2) will try to determine the maximum concentration of spironolactone that can be achieved with Everclear and Everclear/PPG mixtures. Stay tuned.
For those of you who want to see the actual numbers I got in my little test to double-check my method, here they are, straight out of my notes:
Mass of empty glass vial: 11.88 grams
Mass of vial + crushed spironolactone tab: 12.39 grams (my scale is accurate to +/- 0.01 grams)
Mass of vial + tab + Everclear: 21.94 grams
(After removing liquid and drying for two days)
Mass of vial + sediment: 12.28 grams
There ya have it: 12.28 - 11.88 = exactly 0.4 grams (400 mg) of sediment. Yes, I was as astonished as the rest of you to see it work out EXACTLY like that, to within the accuracy of the scale itself. I almost fell off the chair when I saw that! :lol:
Bryan
Even though I also make some of my own topical concoctions, I've always felt slightly uneasy about the general technique of crushing-up spironolactone tablets and mixing them in with Rogaine or other topical vehicles. Does the spironolactone REALLY get dissolved into the alcohol, or does it just stay behind in all that sediment which falls to the bottom of the bottle? I finally decided to put that to the test, and the results appear to be an unequivocal and SPECTACULAR success! :lol: Here's a brief outline of what I did, and afterwards I'll even go into a little more detail by posting the actual numbers I got:
I've previously posted that I use generic spironolactone tablets ("Spirotone" brand) which contain 100 mg of spironolactone each. The tablets themselves weigh 500 mg, so that means that they must contain 100 mg of the active drug and 400 mg of inert tablet fillers and excipients (that's what _apparently_ forms that messy sludge which refuses to dissolve in alcohol!). I took one Spirotone tablet and finely powdered it in a mortar and pestle, just to make sure that every bit of the spironolactone in it would dissolve (assuming it was going to dissolve, of course) in the next step. I dumped the tablet powder into a small glass vial of known weight. Measuring the weight of the vial + powder, I verified the exact mass of the powder sitting at the bottom.
Next I added about 12 mL of pure Everclear, enough to be sure that it could completely dissolve all the spironolactone in that powdered tablet (assuming that it was in fact going to dissolve, of course...I pre-calculated that the concentration of spironolactone in the Everclear would be around the 1% level, which I figured it should easily be able to hold). I capped the vial and THOROUGHLY shook it over an extended period of time to be CERTAIN that the alcohol in the Everclear would completely dissolve whatever it was going to dissolve. Then I set the vial down in a cool, dark place to let the undissolved sediment slowly settle to the bottom of the vial.
24 hours later, it had settled-out nicely, leaving a pale yellow liquid (Everclear and whatever solute it contained) sitting over a milky-looking sediment. Next came the tricky and tedious part: I sat down with a long, slender glass eyedropper with a narrow tip at the end and SLOWLY and CAREFULLY removed as much of that Everclear above the sediment as I could. I did it without moving or jostling the vial, so that the sediment wouldn't get stirred-up and withdrawn by accident, along with the liquid. It took me about 45 minutes of tedious effort to do that (with beads of sweat popping out on my forehead), but I got rid of just about every last bit of liquid that I safely could (about 96% of the liquid, as I was able to calculate later). This left only the sediment lying in the bottom of the vial, which was still wet with a little remaining Everclear. I set the vial out to air-dry the rest of the way by itself.
Two days later it was completely bone-dry, with just the sediment remaining in the vial. And here came the CRITICAL STEP: I weighed the vial and its contents for one last time, and it was EXACTLY 400 mg higher than the empty starting weight of the vial!! It was "dead nuts", to use the technical term! :lol: That proved beyond any reasonable doubt that the Everclear did in fact dissolve all 100 mg of the spironolactone in the crushed-up tablet, and left behind all 400 mg of the fillers and excipients (BTW, this also demonstrates a simple way to remove all that sediment: just remove the good spironolactone-containing liquid with an eyedropper, and discard the remaining junk). I was _thrilled_ to be able to satisfy for myself that the fundamental process that we've been using with spironolactone tablets is sound. Further experiments I'll be doing (Part 2) will try to determine the maximum concentration of spironolactone that can be achieved with Everclear and Everclear/PPG mixtures. Stay tuned.
For those of you who want to see the actual numbers I got in my little test to double-check my method, here they are, straight out of my notes:
Mass of empty glass vial: 11.88 grams
Mass of vial + crushed spironolactone tab: 12.39 grams (my scale is accurate to +/- 0.01 grams)
Mass of vial + tab + Everclear: 21.94 grams
(After removing liquid and drying for two days)
Mass of vial + sediment: 12.28 grams
There ya have it: 12.28 - 11.88 = exactly 0.4 grams (400 mg) of sediment. Yes, I was as astonished as the rest of you to see it work out EXACTLY like that, to within the accuracy of the scale itself. I almost fell off the chair when I saw that! :lol:
Bryan
