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Loprazolam Solubility in Water

Captain.Heroin

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I have a quick question I hope someone can help me out with. I recently compiled a short list of common benzodiazepines and their solubility in water.

Does the imidazole ring in loprazolam enable it to be water soluble? And if so, to what degree?

The closest information I could find about any water solubility regarding imidazobenzos is through this source, which indicated 25mg/mL solubility of midazolam in water.

I'm not exactly sure if loprazolam is as water soluble as midazolam is, or if it's less so. The best description I have seen online is that it's "slightly water soluble". If that means I can dissolve 1mg/mL that's all I was looking into.

Thank you for the replies in advance.
 
It's not so much the imidazole that enhances solubility but the piperazine, which is able to form salts. To my knowledge, its usually formulated as methylsulfonate-salt (mesylate), which is sufficiently water-soluble; I can't provide a number though, sorry.

- Murphy


Edit: I found some numbers: One part is soluble in 100 parts of water, in 200 parts of ethanol or 500 parts chloroform. That means in other words: 10 mg are soluble is 1 ml water (of the mesylate, not the free base!).
Ref: "Clarke's Isolation and Identification of Drugs", 3rd edition, p.710.
 
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You may want to PM phatass, one of the mods of Basic Drugs Discussions, if he doesn't show up here. He used to inject loprazolam quite often.
 
Anyway if you intent to inject it the standard dose is 1mg so you wont need much water for higher doses.

I used to inject 10ml isopropanol 25mg clonazepam oral drop vials....hehe what a fool.
 
I used to inject 10ml isopropanol 25mg clonazepam oral drop vials....hehe what a fool.

Just for information purpose, are the clonazepam oral drops IV'able? Does one have to filter them specifically? Does it hurt? Again, it's just for information purpose. Thanks ;)
 
Not at all, its just a thick liquid, a bit hard to push in (maybe dilute it with a tiny bit of distilled water) and it has a strong 'minty peach' aroma that 'Incredibly' you can taste it even when IVd.

This counts for Rivotril 2,5/ml drops.

Its just like BOOM AHHH. my old days
 
It's not so much the imidazole that enhances solubility but the piperazine, which is able to form salts. To my knowledge, its usually formulated as methylsulfonate-salt (mesylate), which is sufficiently water-soluble; I can't provide a number though, sorry.

- Murphy


Edit: I found some numbers: One part is soluble in 100 parts of water, in 200 parts of ethanol or 500 parts chloroform. That means in other words: 10 mg are soluble is 1 ml water (of the mesylate, not the free base!).
Ref: "Clarke's Isolation and Identification of Drugs", 3rd edition, p.710.

Cool! That's all I need to know. If you can dissolve 10mg of loprazolam mesylate into 1ml of water, that's good enough for me (that's a really high dose!), so I'm satisfied with this.

Thanks for the reference!

You may want to PM phatass, one of the mods of Basic Drugs Discussions, if he doesn't show up here. He used to inject loprazolam quite often.

Thanks for the suggestion! I'll certainly talk to him if I have any further questions.
 
Not at all, its just a thick liquid, a bit hard to push in (maybe dilute it with a tiny bit of distilled water) and it has a strong 'minty peach' aroma that 'Incredibly' you can taste it even when IVd.

This counts for Rivotril 2,5/ml drops.

Its just like BOOM AHHH. my old days

Ok, thanks. So no need to use a micron filter? (of which I by chance have a sample). I never injected any drugs but I'm very tempted if this doesn't equal vein damage...
edit: I have the Rivotril 2,5ml drops, lots of vials.
 
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^ Thanks, I'll look at what's inside this liquid. But as it is a pharmaceutical liquid, maybe fillers aren't prevalent or of a nature to clog in the syringe? I don't know. Thanks for the links anyway ;)
edit: that was for Captain Heroin's post
 
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Why, or even how, the fuck where you injecting 10ml of isopropyl alcohol?

This does not kill you?

LOL, Ask Hammilton, He's the alcohol guru here on ADD =D.

Anyway it was propylene glycol (quite the same) + sodic saccaride, acetic acid, 'peach aroma' (very minty) and obviously clonazepam. Rivotril 2,5mg/ml

Injected it for almost a year and nothing dangerous (well without considering the foolish dose of clonazepam) happend apart from a vein on my wrist that collapsed cause I was using every time. The liquid is sterile (obsviously from the alcohol content) and sterylize everything you should be just fine.

Just be carefull IVing Clonazepam can be very addicting, the rush is so overwhelming.
 
I will stick to midazolam when it comes to IV:ing benzos. Speaking of "rush", all the other benzos have nothing on midazolam...
 
Hi, I found this page for comparing the oral liquid and injectable liquid forms of clonazepam (Rivotril). It's in french but I'll translate the components for both forms. They are quite the same.

Oral liquid (drops): saccharine sodium, acetic acid, propylene glycol and peach aroma

Injectable liquid (ampoule, per ml): "alcool absolu" -> absolute alcohol? (not the brand!, but maybe 100° alcohol), benzilic alcohol 30mg, propylene glycol, "glacial" acetic acid and sterile water.

So, apart from the saccharose and the aroma, there are two sorts of alcohol in the injectable form and none in the oral form, and acetic acid and propylene glycol are in both forms.

That leaves mainly the saccharose as a possible deterrent factor. So I'm skeptical about the hazard of injecting the oral solution, especially if diluted in 2 parts of sterile water for one part of oral solution (.83mg of clonazepam for .33ml). What do you guys think?
 
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The absolute lcohol is not ethanol cuz it would hurt like CRAP!
The saccarin sodium goes into your bloodstrem anyway when injested and the peach aroma never gave me any problems.
Here in Italy they don't sell the injectable solutions GRRR, so i tried the oral drops after having a look at the ingredients and it worked fine and so it went on.

You dont need to mix it with soo much water, I used to inject it pure but it was pretty thick as a liquid so it was a slow injection, a few drops of distilled water would be fine to make it flow better. The funny thing is that you might 'feel' the minty peach aroma even if injected.

Dunno what else to say, I gave you my deal of the experience and it went fine for months, from here the choice is yours.

Bonne chance mec!
 
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