Raw Flumazenil prep?

[petey1]

Hi Guys,

This might not be the place for this but I can't think of anywhere with a more knowledgeable group of guys!

My girlfriend suffers from Idiopathic Hypersomnia. It's a sleep disorder in the same family as Narcolepsy characterised in her case as excessive day time sleepiness regardless of long sleeps and naps, brain fog and other debilitating ailments. I'm on a mission to help her.


There is quite a bit of very encouraging research on Flumazenil as a cure. Flumanezil is commonly used to either reverse anaesthesia or prevent benzo overdoses.

It seems to be working great for a lot of people but it has some drawbacks;

The first is cost, best case for branded we're looking at $30-50/mg. At 4mg/day it's not realistic longterm.

Secondly current products are only for IV use. At 1mg/10ml that's a lot of injecting!


In this video you can see an infusion system a guy in Australia is using.



In America and Australia there is are clinics prescribing and trying out different delivery methods. Some have created transdermal creams, some have created sublingual lozenges, others have created implants. These delivery methods have been created in their own labs so aren't available commercially.

There is a patent application for highly concentrated, soluble Flumazenil complexes that will work in a spray for example but commercial products will probably take a good while. http://www.google.com/patents/WO2012114342A1?cl=en



Now the reason I've written this post is generic raw Flumazenil powder is available freely and legally from foreign labs and research companies. It is not terribly expensive.


How realistic would it be to home brew (16mg) Lozenges?

Transdermal Cream?

Is the below invention replicable by a professional chemist given the information provided or is that unrealistic? http://www.google.com/patents/WO2012114342A1?cl=en



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[sekio]

you can be prosecuted for violating a world patent if you formulate drugs according to that (yes even for non-commercial personal usage), but ignoring that, putting flumazenil in a pill is not a difficult thing to do.

 

[petey1]

you can be prosecuted for violating a world patent if you formulate drugs according to that (yes even for non-commercial personal usage), but ignoring that, putting flumazenil in a pill is not a difficult thing to do.

How difficult would it be to create a nasal spray given it's low solubility? is this something a freelance pharmacist could create or will it need a big team/lab?

 

[sekio]

making a nasal spray is easy enough (drug in solvent, solvent in spray bottle), figuring out how efficacious it is needs a little more effort (e.g. you need to be able to conduct blood draws and determine concentration of drug accurately)

you would probably also want to invest in all the quality control shit of a real pharmacy though (reference standards, some sort of analytical equipment like GCMS or LCMS or even TLC, assorted reagents and solvents). it's doable by one individual if he/she is a bored millionaire or otherwise has access to a well equipped lab nobody's using.

there is a little more nuance to drug formulation than "put powder in pills, pills in bottle"

 

[petey1]

Thanks again,

So from the information provided on the patent application a compounding pharmacy should be able to create something similar?

Does the patent application literally explain everything or will there be parts missed out to protect the invention?

Cheers

 

[sekio]

getting a pharmacy to make medication according to that in the patent is a violation of international patent law. i don't know if you missed that part. doing so would open you and anyone you involve in your drug-manufacturing scheme to prosecution by WIPO and friends.

if you read the patent it is very specific in what it covers, there are recipes and suggested formulations detailed. there's tox tests and all that shit too. if you can't make head or tails of it you should probably hand the problem off to someone who does drug formulations for a living, or start hitting the books. otherwise it would be analogous to someone who could not understand a cookbook and did not own flour, salt, eggs or an oven trying to bake cakes

or you can wait some ungodly amount of time, 25 or 30 years i think, before the patent expires.

a compounding pharmacy may be able to make you tablets or what-have-you that do not break the patent but there is no guarantee they will be as efficacious as the patented formulation

(welcome to patent law)

 

[serotonin2A]

Any compounding pharmacy should be able to make this for you, either as an intranasal spray or a solution for IM injection. The USP reference standard costs about $1000 for 200 mg, so only $5/mg. I'm sure they can probably find the USP grade powder for even cheaper than that from a distributor.

 

[petey1]

getting a pharmacy to make medication according to that in the patent is a violation of international patent law. i don't know if you missed that part. doing so would open you and anyone you involve in your drug-manufacturing scheme to prosecution by WIPO and friends.

Does the law protect drugs even when a patent hasn't yet been awarded? unless I've read it wrong it still seems to be in the application stage?

I'm not planning on cooking anything up myself but this is a whole new world for me. I'm trying to figure out what is possible.

 

[Zeds(NCO2CH2CH3)2]

You want to use this for in effect narcolepsy. Albeit that this is a decent idea gaba A antagonists may not be the best idea for this. They will also alter the sleep cycle in a way not great for narcoleptics. The synthesis is not hard but I would not even try this, likewise it definitely has multiple drug interactions.. Of course ethanol but many other drugs included

 

[sekio]

Does the law protect drugs even when a patent hasn't yet been awarded? unless I've read it wrong it still seems to be in the application stage?

A patent application can turn into an issued patent at pretty much any time, unless you are confident it will never be issued as a patent then you need to be prepared for the day it issues and you are forced to cease production.