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        New Message Board Archives >> Jul-Sep 2003 >> Topical Imitrex Gel! 
        
(Message started by: Mark C on Aug 13^th, 2003, 8:20am)

Title: Topical Imitrex Gel!
Post by Mark C on Aug 13^th, 2003, 8:20am

Wade through this (http://appft1.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=7&f=G&l=50&co1=AND&d=PG01&s1=%22Triticum+vulgare%22&OS=%22Triticum+vulgare%22&RS=%22Triticum+vulgare%22l), it's from the patent application for Imitrex. I wonder if you could do this. Not an easy task but seems possible. A gel you rub on your neck, homebrew!

[0225] Typically the first relief symptom expressed by patients using transdermal sumatriptan is the relaxation of cervical musculature, followed by decreased nausea and photophobia and the eventual relief of throbbing head pain. It is believed that with the local application of transdermal sumatriptan, the brainstem and surrounding tissue are concentrated with the drug accounting for its rapid and prolonged clinical effect. The relative paucity of side effects, particularly the typical "triptan effects" may be explained on the basis of minimal system absorption, with much of the drug remaining concentrated near the site of application. In view of the above, the data suggests that the transdermal route is as effective as injection, but without the usual side effects.

[0226] As can been seen from the above examples, the percentage of patients experiencing migraine or cluster headache pain relief may be significantly improved using an aqueous based topical formulation. Additionally, the percentage of patients experiencing migraine or cluster headache pain relief may be significantly improved without a significant increase in side effects using an increased dose as demonstrated by the above examples.

EXAMPLE 7

[0227] A sumatriptan formulation having a final strength of 12.5 mg/0.1 ml was prepared according to the following procedure:

[0228] 1. Triturate the requisite amount of sumatriptan succinate tablets in a mortar and pestle to a small particle size.

[0229] 2. Wet the powder with 95% ethyl alcohol and triturate. Add pure water and triturate again.

[0230] 3. Filter and rinse the residue twice with enough water to bring the volume of the filtrate to that of the final product. For example, if preparing 100 ml of the transdermal migraine formulation, filter until the total volume of the filtrate reaches 100 ml.

[0231] 4. Concentrate the filtrate using low pressure vacuum to 25% of the original volume (e.g., to 25 ml in the example).

[0232] 5. Mix the condensed filtrate and Lipoderm.RTM. in mixing syringes to the desired volume (e.g., 100 ml in step 3). The final strength is 12.5 mg of sumatriptan succinate per 0.1 ml. "

Anyone got some old pills they want to try? Rub it in Rub it in!

PFDAN's
Mark

Title: Re: Topical Imitrex Gel!
Post by vig on Aug 13^th, 2003, 9:12am

It sounds good, but won't it take too long to get through the skin? Even snorting the stuff takes too long.

This sounds great for migrainers.

Title: Re: Topical Imitrex Gel!
Post by klp on Aug 13^th, 2003, 10:54am

in my line of work we use a ton of transdermal gels. everything from morphine, ativan, haldol, decadron, etc... the abosorption time is approximately 10-15 minutes for most and the effects can last hours. the problem is transdermals are considered compound medications and the cost is usually very high. krista

Title: Re: Topical Imitrex Gel!
Post by eyes_afire on Aug 13^th, 2003, 5:07pm

Didn't really read every detail of that.

I don't know... maybe I'm becoming a cynical bastard in my old age...
It sure sounds to me like an attempt to extend the imitrex patent.
Do we really want to wait another 17 years?

--- Steve, old cynical bastard...

Title: Re: Topical Imitrex Gel!
Post by Drk^Angel on Aug 13^th, 2003, 8:31pm

The patent application isn't by GSK... It's by a neurologist in Sarasota, FL. If anyone knows has a doctor willing to write a script for this treatment, any compounding pharmacy should be able to prepare the gel. After reading the application, it does sound interesting.

PFDAN.................................. Drk^Angel

Title: Re: Topical Imitrex Gel!
Post by andy on Aug 13^th, 2003, 11:12pm

Mark C, transdermal sumatriptan? Hmmmmm, sounds good to me. An Imitrex patch, what a great idea, lets hope it works ...............andy

Title: Re: Topical Imitrex Gel!
Post by Drk^Angel on Aug 14^th, 2003, 3:44am

Here's (http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=/netahtml/srchnum.htm&r=1&f=G&l=50&s1=5807571.WKU.&OS=PN/5807571&RS=PN/5807571) the patent for a controlled release patch for sumatriptan and other tiptans.

PFDAN............................... Drk^Angel