how to increase the solubility of the paracetamol ?

[myvow]

is it valid to covert it into the form of ionic salt as shown by picture below?

HC8H8NO2 + NaOH ↔ C8H8NO2-NA+ + H2O

thanks

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[y0ssarian87]

is it valid to covert it into the form of ionic salt as shown by picture below?

HC8H8NO2 + NaOH ↔ C8H8NO2-NA+ + H2O

thanks

I'd be concerned that you'd hydrolyze the amide and/or lead to great conditions for oxidizing the para-aminophenol. Not sure how much that matters for your use...

 

[y0ssarian87]

I'd be concerned that you'd hydrolyze the amide and/or lead to great conditions for oxidizing the para-aminophenol. Not sure how much that matters for your use...

Oh, um, disclaimer: my only chemistry experience is in OChem from undergrad several years ago.

 

[myvow]

I'd be concerned that you'd hydrolyze the amide and/or lead to great conditions for oxidizing the para-aminophenol. Not sure how much that matters for your use...

Thank you for your reply.
Are there any method increasing paracetamol's solubility if this is not work.

 

[Mad Jack]

What are you looking to increase its solubility for? Different methods work for different things. If you're looking to make it more soluble for lab filtration, that's one thing, but if you're looking to make it more soluble for in vivo testing or use, that's another.

 

[myvow]

What are you looking to increase its solubility for? Different methods work for different things. If you're looking to make it more soluble for lab filtration, that's one thing, but if you're looking to make it more soluble for in vivo testing or use, that's another.

i want increase the solubility of the drug in body.....

 

[Mad Jack]

i want increase the solubility of the drug in body.....

Given that I don't know your credentials or why you would want to do this, and the fact that paracetamol has a very narrow therapeutic range, I don't feel comfortable telling you the best way of going about this over the internet.

 

[myvow]

Given that I don't know your credentials or why you would want to do this, and the fact that paracetamol has a very narrow therapeutic range, I don't feel comfortable telling you the best way of going about this over the internet.

In fact, i am doing a project about "how acetaminophen can increase solubility in Panadol’s analgesic."
and the concept and acid and base should be applied in the project.
i found one method to increase the dissolution rate of the drug by mixing paracetamol with citric acid and sodium bicarbonate
But I want to find another method except this.......
i don't know what's your meaning of feeling uncomfortable ........enhancement of drug's solubility don't the pharmaceutical manufacturer most want to do?

 

[myvow]

so..if you don't want to tell me..it's ok
thank you for your reply

 

[Mad Jack]

I'm no expert, so your idea is probably superior to anything I'd come up with. Just be careful with the pH of your final solution, as paracetamol becomes unstable below a pH of 4 or so.

 

[Chriskahn]

There's a bunch of ways to increase solubility of a drug but since you are trying to incorporate acids and bases you can use:
1. Salt form. Better solubility than free acid or free base (which you did)
2. Addition of acidic or basic excipients. pH of the dissolution medium greatly influences the solubility of weak acids and weak bases. A drug will be more soluble in water when its ionized so a basic drug will be more soluble in acidic pH, an acidic drug will be more soluble in basic pH.

An example of this is buffered aspirin that contains sodium bicarb that makes the solution around the dosage form more basic. The aspirin will then dissolve quickly in this favorable pH environment and diffuse out of the basic pH area. Then it will precipitate and will be very fine in size.

Fine particle size = very large surface area = increased solubility.