Sublingual ativan in water only... good idea?

Hello.

 

I'd like to try avoiding the vodka in my liquid ativan mixture. Since the sublingual dissolve readily, would you say that a 10 ml water solution would be a homogeneous dissolved solution? Also, does the medicine degrade over time in the water?

As many folks do, you are confusing the deconstruction/disintegration of the carrier (tablet/strip, etc) with dissolving.  Some of the tablet  components  will always be water-soluble, and that's why the tablet falls apart.

 

But the active ingredient, lorazepam, is NOT water soluble, will NOT go into solution, and will NOT be uniformly distributed.

Thank you Builder. Much appreciated. Is a 1 ml vodka to 9 ml water ratio okay?

Thank you Builder. Much appreciated. Is a 1 ml vodka to 9 ml water ratio okay?

 

You really need 2mls vodka for each 1mg of benzo.  A good ratio is 1mg:2ml vodka:8ml water.  That makes a .1mg per ml solution.

I created a water / ativan suspension and divided into 3 smaller doses daily. Worked fine for me.

Hello.

 

I'd like to try avoiding the vodka in my liquid ativan mixture. Since the sublingual dissolve readily, would you say that a 10 ml water solution would be a homogeneous dissolved solution? Also, does the medicine degrade over time in the water?

 

I also wanted to avoid the vodka and am actually doing it with no problems without vodka.

I am using ordinary 1mg lorazepam tablets, from a generic brand, but ativan is also composed of lorazepam.

 

In my opinion lorazepam is sufficiently water soluble. See this thread:

http://www.benzobuddies.org/forum/index.php?topic=210792.0

 

I am using water at room temperature, because maybe the solubility in colder water is less.

I have a 1 mg tablet, put it into a glass jar, and let it fall apart in 100 ml of water, this goes very fast with my brand of lorazepam.

I close the jar with a plastic lid and wait for about 30 minutes.

To stimulate the dissolution I then shake the jar thoroughly for 10 or 15 seconds.

After another 30 minutes I pull the desired volume out with a 50 ml syringe, with rubber piston.

 

There is some fine sediment at the bottom when I do this but this is not the lorazepam but consists of insoluble tablet substances.

I know this because I can see whether or not I pull out this sediment and when I carefully take care not to pull it out it works just fine.

 

I can switch between this method and dry cutting without any problems.

 

I have never kept my solution for more than 24 hours because the tablet mainly contains sugar and I am afraid that this would go bad because sugar is a food for bacteria.

 

https://www.researchgate.net/publication/234954262_The_Improvement_of_Lorazepam_Solubility_by_Cosolvency_Micellization_and_Complexation

 

 

Lorazepam is an almost water insoluble substance. This study investigated the solubilization of lorazepam depending on media pH, cosolvents (ethanol, propylene glycol, polyethylene glycol 200 and 400), surfactants (Tween 80, Tween 20, Brij 35, sodium-cholate, sodium-deoxycholate, sodium-taurocholate) and cyclodextrins (α-cyclodextrin, -cyclodextrin and 2-hydroxypropyl-β-cyclodextrin). The main objective was to find the most suitable method for providing good solubility of this drug and thus its formulation in a liquid dosage form. Based on the results, the changes in the pH value of the media do not lead to a greater solubility of lorazepam . Of the cosolvents used, the greatest increase in solubility of lorazepam in water was achieved with ethanol. Of the bile salts used, sodium taurocholate showed the best solubilization ability, while Brij 35 was the best of the non-ionic surfactants. The solubility of lorazepam with the cyclodextrin derivative, 2-hydroxypropyl-β-cyclodextrin was better than natural cyclodextrin. Surfactants have the highest ability of solubilization of lorazepam in water.

 

 

I agree that lorazepam is not soluble in water. I was able to make a suspension that I divided up quickly before the suspension settled. Im sure my doses were not exactly equal. But, over the course of my liquid taper, I think the suspension was much more accurate than dry cuts. It was much easier and a much smoother taper using this method. I believe some people are so sensitive to minute changes in doses that a vodka solution may be necessary, but in my case it was not. Im now 3 months post taper and feeling so much better after a 9 month taper - the last 4 months using a water/ ativan suspension taper. Good luck to all.

Fp

Y'all need to actually read the data at that Merck reference!

 

"Water Solubility   0.0176 mg/mL"

 

https://www.drugbank.ca/drugs/DB00186

 

So it would take 55ml of lab pure water at standard conditions (neutral Ph, 70F) to dissolve 1mg of lorazepam!

 

Realistically, lorazepam (like other common benzos) is NOT water-soluble.

 

 

 

Pure lorazepam is an almost white powder that is nearly insoluble in water and oil. In medicinal form, it is mainly available as tablets and a solution for injection,

 

 

https://en.wikipedia.org/wiki/Lorazepam

 

For those of you that are averse to alcohol, propylene glycol works just as well (probably better )

 

The Rx liquid lorazepam uses a PG solvent.

Y'all need to actually read the data at that Merck reference!

 

"Water Solubility   0.0176 mg/mL"

 

https://www.drugbank.ca/drugs/DB00186

 

So it would take 55ml of lab pure water at standard conditions (neutral Ph, 70F) to dissolve 1mg of lorazepam!

 

Realistically, lorazepam (like other common benzos) is NOT water-soluble.

 

 

 

 

0.0176 mg/mL is not the Merck index, Builder.

It is the predicted solubility instead.

 

The Merck index is an experimental value and is 0.08 mg/ml.

So only 12,5 ml of water would be needed to dissolve 1 mg of lorazepam, and 100 ml would be more than enough.

 

This number says nothing about the time which is needed to dissolve this 1 mg, which might be long.

For this reason I thoroughly shake the jar for a long time, to stimulate the dissolution, and wait 30 minutes after this, like I already described.

 

It cannot be a suspension like you suggest because when I wait many hours after shaking, and as a result there is a fine sediment at the bottom, and I take care to not pull the sediment out, the medicine I get this way works very well, in fact the same as when I would have done a dry cut, which could not be so if I would have created a suspension, because everything would have sunk to the bottom as a sediment after so many hours, and I did not pull this out.

 

 

[

 

It cannot be a suspension like you suggest because when I wait many hours after shaking, and as a result there is a fine sediment at the bottom, and I take care to not pull the sediment out, the medicine I get this way works very well, in fact the same as when I would have done a dry cut, which could not be so if I would have created a suspension, because everything would have sunk to the bottom as a sediment after so many hours, and I did not pull this out.

 

 

I have never suggested that benzos mixed in water will make a suspension.  A suspension agent must have sufficient viscosity to hold the particles suspended.  Water has very poor viscosity, as evidenced by the particles sinking to the bottom.

Y'all need to actually read the data at that Merck reference!

 

"Water Solubility   0.0176 mg/mL"

 

https://www.drugbank.ca/drugs/DB00186

 

So it would take 55ml of lab pure water at standard conditions (neutral Ph, 70F) to dissolve 1mg of lorazepam!

 

Realistically, lorazepam (like other common benzos) is NOT water-soluble.

 

 

 

 

0.0176 mg/mL is not the Merck index, Builder.

It is the predicted solubility instead.

 

The Merck index is an experimental value and is 0.08 mg/ml.

So only 12,5 ml of water would be needed to dissolve 1 mg of lorazepam, and 100 ml would be more than enough.

 

This number says nothing about the time which is needed to dissolve this 1 mg, which might be long.

For this reason I thoroughly shake the jar for a long time, to stimulate the dissolution, and wait 30 minutes after this, like I already described.

 

It cannot be a suspension like you suggest because when I wait many hours after shaking, and as a result there is a fine sediment at the bottom, and I take care to not pull the sediment out, the medicine I get this way works very well, in fact the same as when I would have done a dry cut, which could not be so if I would have created a suspension, because everything would have sunk to the bottom as a sediment after so many hours, and I did not pull this out.

 

John-

 

I have posted here many times that folks should choose a taper protocol they feel comfortable with.

 

If you believe your method will give you good results, then I only wish you a smooth, successful taper.

It cannot be a suspension like you suggest because when I wait many hours after shaking, and as a result there is a fine sediment at the bottom, and I take care to not pull the sediment out, the medicine I get this way works very well, in fact the same as when I would have done a dry cut, which could not be so if I would have created a suspension, because everything would have sunk to the bottom as a sediment after so many hours, and I did not pull this out.

 

Forgive my confusion, why do you take care not to pull the sediment out? isn't the sediment filler?

 

It cannot be a suspension like you suggest because when I wait many hours after shaking, and as a result there is a fine sediment at the bottom, and I take care to not pull the sediment out, the medicine I get this way works very well, in fact the same as when I would have done a dry cut, which could not be so if I would have created a suspension, because everything would have sunk to the bottom as a sediment after so many hours, and I did not pull this out.

 

Forgive my confusion, why do you take care not to pull the sediment out? isn't the sediment filler?

 

Yes, when you do it the way I described, the sediment is filler.

You can pull it out without problems.

 

The reason I took care not to pull it out was because it was an experiment.

I wanted to be sure that there was no lorazepam in the sediment and because it worked as well when I did not pull out any sediment, I was sure that there was no lorazepam in it.

 

If it would have contained lorazepam I would have noticed it, because when I do a dry cut I notice very well changes of approximately 10 percent.

It cannot be a suspension like you suggest because when I wait many hours after shaking, and as a result there is a fine sediment at the bottom, and I take care to not pull the sediment out, the medicine I get this way works very well, in fact the same as when I would have done a dry cut, which could not be so if I would have created a suspension, because everything would have sunk to the bottom as a sediment after so many hours, and I did not pull this out.

 

Forgive my confusion, why do you take care not to pull the sediment out? isn't the sediment filler?

 

Yes, when you do it the way I described, the sediment is filler.

You can pull it out without problems.

 

The reason I took care not to pull it out was because it was an experiment.

I wanted to be sure that there was no lorazepam in the sediment and because it worked as well when I did not pull out any sediment, I was sure that there was no lorazepam in it.

 

If it would have contained lorazepam I would have noticed it, because when I do a dry cut I notice very well changes of approximately 10 percent.

 

john17, thank you for clarifying! 

For what it is worth I do up my dosage for the day and shake to have as much in suspension as possible [although I have also started using vodka to dissolve as per builder suggestion I think] and split into the two daily amounts. I also shake each vigorously prior to drinking and rinse the glass/jar out with water and drink to get anything whether filler/solution taken. Seems to work

 

John-

 

I have posted here many times that folks should choose a taper protocol they feel comfortable with.

 

If you believe your method will give you good results, then I only wish you a smooth, successful taper.

Thank you Builder.