Alright gents. This may very well be like elementary school for you, but here it goes. The basics of compounding I already understand.

Well here is the reason I am asking. My sons prescription for Captopril is 1mg/ml. It just went from $10 a month to $45 a month! For 100mg of Captopril for goodness sakes! Just because of the compounding fees. I really just need to be able to find the liquids to perform the compound. I would assume that the compound ingredients are freely available without a license but I am not sure.

Any help would be appreciated, after all $120 a year to $540 a year is just a tad steep! I can get enough pills for the year for $70. The rest is gravy....

Alright gents. This may very well be like elementary school for you, but here it goes. The basics of compounding I already understand.

Well here is the reason I am asking. My sons prescription for Captopril is 1mg/ml. It just went from $10 a month to $45 a month! For 100mg of Captopril for goodness sakes! Just because of the compounding fees. I really just need to be able to find the liquids to perform the compound. I would assume that the compound ingredients are freely available without a license but I am not sure.

Any help would be appreciated, after all $120 a year to $540 a year is just a tad steep! I can get enough pills for the year for $70. The rest is gravy....

So hang on, you can get a years worth of pills for $70, and the pharmacist dissolves them for you for $50? I may have misunderstood you...

I have no knowledge of "compounding" whatsoever, in fact I had to go and look it up to find out wtf you're talking about! However, I would assume that you could dissolve it at a level of 1g/Litre to provide you with a liquid form. Looking at the structure, I'm guessing that you have a sporting chance of it being water soluble, but you should probably check that out for yourself.

Assuming that it is indeed sufficiently soluble in water, then you could crush finely 10mg worth of medication (or less/more, provding you stick to the 1mg/mL ratio), and take it up in 10mL of water (use a syringe). I guess that would be then fine to use.

I'm assuming it's for oral use, if you're injecting it you're gonna need to use sterile water/equipment and should be very careful about getting the precise details...

Like I said though, I have no background in this sort of thing, so use any advice at your own risk (In fact, use any advice from this site with a LARGE pinch of salt!, though Lab Tips is probably the best from that point of view)

Alright gents. This may very well be like elementary school for you, but here it goes. The basics of compounding I already understand.

Well here is the reason I am asking. My sons prescription for Captopril is 1mg/ml. It just went from $10 a month to $45 a month! For 100mg of Captopril for goodness sakes! Just because of the compounding fees. I really just need to be able to find the liquids to perform the compound. I would assume that the compound ingredients are freely available without a license but I am not sure.

Any help would be appreciated, after all $120 a year to $540 a year is just a tad steep! I can get enough pills for the year for $70. The rest is gravy....

You want to synthesis it or know why the price went up?

Alright, first I can get a YEARS worth of pills for $70. The compounded prescription costs $45 a MONTH.

The pill is NOT water soluble. The compounding liquid is rather gel/syrup like. It is a type of suspension for oral use.

The actual act of pulverizing 4X25mg. pill via mortar and pestle and then adding enough liquid to the pills to establish a 100ml 1 month supply is fairly simple.

I just need to be able to find the compounding syrup/gel/liquid.

I do not want to synth the meds. The price went up because the insurance company didn't want to spend the money on the compounding and took the prescription from the generic copay to the "Non formulary" copay. Yet another reason to hate the insurance companies.

a) find the brand name -> find the company -> ring company and request MSDS -> discover what is in said compounding liquid -> attempt to recreate.

b) buy a mg accurate scale, weigh out 1mg worth, place in water, swirl into a suspension, and down it. I'd think your son could do that, even at 1. The swallowing bit at least, not the grinding up and weighing out :)

It seems possible to me that the fact that it is syrupy is all that its going to do is sort of... trap the drug in suspension. And therefore something like honey could work, if you just mixed it very well.

I sympathise with your situation, it really does sound pathetic the way that the cost has to shoot up just for that tiny reason.

Edit ; infact, from the way you were describing it, I wouldn't be surprised if it was merely medical grade glycerine or something. It's not extremely sweet?

You may already be planning on this, but for the sake of your child please administer the drug to yourself a few times before even thinking about giving it to him.

Also why can't your son just take the pills? If it must be in liquid form can't you just powder up a 1mg dosage and make a mixture of it with water to swallow?

Von Bass has it correct, look up the solubility and pick the substance that has the highest... and is non toxic of course.

I have done pharmaceutical compounding in the past, at a mail order pharmacy. It was so easy a monkey could do it.

Most of the compounds I mixed were either testosterone, estrogen, triamcinolone, or hydrocortisone. The two solvents I used the most were propylene glycol and everclear. Sometimes IPA as well.

My guess is the drug will be fairly soluble in propylene glycol, find some filler that tastes good, and you have a suspension of the drug.

Also search online, you may be able to find a common used recipe for the compound you were getting at the pharmacy... as a last resort you could call a pharmacy and ask them what is in it.

Just some ideas...

According to

http://msds.chem.ox.ac.uk/CA/captopril.html

it is soluble in water.


I'd do a little more research, though.

According to

http://msds.chem.ox.ac.uk/CA/captopril.html

it is soluble in water.


I'd do a little more research, though.

Yeah, i found that it was soluble - I'm assuming though that the rest of the binders/fillers etc are not.

This may mean that you can simply dissolve the drug in water and leave the crap behind, or it may mean that the gak will prevent it from dissolving efficiently. I doubt this would be an intentional consequence of the binders, but may be an accidental one...

This may mean that you can simply dissolve the drug in water and leave the crap behind, or it may mean that the gak will prevent it from dissolving efficiently.

...or, it means that thiols readily oxidize in the presence of -OH radicals, degrading the molecule, during long-term storage. ;)

i lern'd that from wikipedia. about 15 minutes ago. 'cause I wanted to double-check thiochemistry for the 2cts. Dumb luck. ;)

OP : its solubility in ethanol is 17mg/ml (http://www.sigmaaldrich.com/sigma-aldrich/product_information_sheet/c4042pis.pdf). Straight from the elitist snobs at sigma-aldrich.

Get everclear and an insulin syringe. Chuck a 100mg pill in 10ml of everclear. Filter out anything that doesn't dissolve. Give your kid 0.1ml doses so they don't get flat-out drizzunk on their meds. Chuck a bit of epsom salts in the bottom to keep it dry; it won't dissolve.

Ethanolic solution will be far more dose-accurate than suspension, no matter what you use. 'n in the fridge (5c), it's also pretty stable. Seeing as the solubility in ethanol is given @ 22c, you might want to bring it to room temperature before serving, even though you should have ample leeway.

If you insist on suspension... it doesn't matter what you suspend it in, so long as it's evenly suspended and not harmful to the molecule. I think glycerin is common and OTC.

P.S. While captopril is probably not the usual meaning of the "no sources" rule, I'm not linking...

...but the first link I clicked at random off scroogle for "captopril 100mg buy" suggests that you can effortlessly go from ~$50/month with your insurance, to less than $0.50/month without your insurance, just by liquid measure and DIY.

You... might wanna mention the insurance company's name when giving media interviews about that fact, lol. I hear universal healthcare has an advocacy PR campaign in some parts of the world, which might be happy to sponsor your media exposure to, umm, ream these guys up the ass.

Hard. 'cause that's 100x less expensive without your insurance.

...or, it means that thiols readily oxidize in the presence of -OH radicals, degrading the molecule, during long-term storage. ;)

would water be a sufficient source of OH radicals...?

In fact, thinking about it, first pass metabolism would oxidise it up straight away (at least, I assume it would - my knowledge of pharmacology is close to nil...!) so perhaps it would't matter even if it did oxidise in water...

would water be a sufficient source of OH radicals...?

Water is about 95% OH- by weight.

Of course, the fact that captopril has a huge, unoccupied acidic side chain would change the percentage, by lowering the percent H+ in solution, wouldn't it?

so perhaps it would't matter even if it did oxidise in water...

Well, one is explicitly directed to store the pills free of moisture due to the apparent belief of the medical community that water-mediated oxidization of the thiol completely inactivates it.

'sides, when it cuts your medical care costs by 99% without sacrificing quality, 10ml of ethanol is cheap. ;)

Water is about 95% OH- by weight.

But OH- and OH radicals are very different things...

Incidentally, I'm not having a go or saying that you're wrong in any of this - just interested!


Of course, the fact that captopril has a huge, unoccupied acidic side chain would change the percentage, by lowering the percent H+ in solution, wouldn't it?


It would indeed lower the pH, but this is achieved by increasing the proportional H+ content


Well, one is explicitly directed to store the pills free of moisture due to the apparent belief of the medical community that water-mediated oxidization of the thiol completely inactivates it.

Fair enough! It surpises me though... Possibly the thiol is required for absorption reasons... Dunno really...


'sides, when it cuts your medical care costs by 99% without sacrificing quality, 10ml of ethanol is cheap. ;)

Oh absolutely! Note that, in light of this info, I would certainly not use water to do this job...!

Thanks Gents! Your assistance was most helpful. I happened across this : https://lra.le.ac.uk/bitstream/2381/440/1/hrt.2006.100537v1.pdf in the process and will likely go with the Water/Vitamin C solution. I will also be getting "Flavorit" to make it more appealing. A nice new Mortar and Pestle is in order as well.

Nice to see that there was/is really no "right" way to do this. Plenty of wrong ways to be sure, but no specific right way.

But OH- and OH radicals are very different things...

Not really. That unsupported extra electron the oxygen sucks from the H+ is why the molecule is called a radical.

It would indeed lower the pH, but this is achieved by increasing the proportional H+ content

Decreasing the percent increases the proportion?

k.

Fair enough! It surpises me though... Possibly the thiol is required for absorption reasons... Dunno really...

Could be. Alternately, maybe it's like LSD - unstable, but sticking around barely long enough to work anyways. I dunno...

Incidentally, the thiol's at the part of the molecule which is the ghb analogue... the thiol analogue of gamma-hydroxyisobutric acid. thioGHiB(2,4aminocyclo)butramide, or somesuch. It's really wierd molecular pr0n.

Oh absolutely! Note that, in light of this info, I would certainly not use water to do this job...!

'n ironically... the dox posted by the OP after this suggest that ascorbic acid (plus there's some other random crap in "suspension dilutant A"), is a sufficient antioxidant.

~shrug~ Curiouser and curiouser... but yeah, just-plain-water, it breaks down like asprin or heroin, but quicker, it seems. Fine in short-term solution, poor storage.

Bases also reduce oxidization, according to the pdf I posted above. Possibly by occupying the acidic side-chain.

Nice to see that there was/is really no "right" way to do this. Plenty of wrong ways to be sure, but no specific right way.

:D

Yeah. That's the beautiful thing about DIY tech. It's free, 'n hard to fuck up if you can find what a few of the wrong ways are. Nice 'n freeform.

Not really. That unsupported extra electron the oxygen sucks from the H+ is why the molecule is called a radical.

not quite following you here...

Also, having just read the PDF from sigma, it actually says

"this product undergoes an oxygen facilitated, first order, free radical oxidation at its thiol to yield captopril disulfide"

This, and the fact that oxidation can be minimised by degassing and low headspace volumes suggest that the radicals in question actually originate from molecular oxygen, rather than hydroxide...

Decreasing the percent increases the proportion?

k.

No, increasing the [H+] = increasing the proportional amount = increased acidity = lower pH


Could be. Alternately, maybe it's like LSD - unstable, but sticking around barely long enough to work anyways. I dunno...

I dunno either!

edit: actually - I was thinking about oxidation to the sulfone, but it seems fair enough that the disulfide would be inactive. Course, one might be able to cleave that bridge to "reactivate"...


It's really wierd molecular pr0n.

thexy!


Bases also reduce oxidization, according to the pdf I posted above. Possibly by occupying the acidic side-chain.

That PDF says that low pH (acidic conditions) increases the stability... No idea why really - possibly acidic conditions recued radical formation, or protonation of the carboxylate lowers its nucleophilicity and stops it chewing the fuck out of the rest of the molecule... hmmm....!

Try looking around for a product called 'Simple Syrup.' Check your pharmacy.

Edit: Here you go. (http://www.medkb.com/Uwe/Forum.aspx/pharmacy/1420/Compounding-w-Simple-Syrup)

what says you can't just give him the powder/ ground up pills (proper dose of course) in a emptied jell cap or 2 part pill?

what says you can't just give him the powder/ ground up pills (proper dose of course) in a emptied jell cap or 2 part pill?

Read the thread.