Author Topic: Anatomy of a patent....BodyPart 1  (Read 1786 times)

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wareami

  • Guest
Anatomy of a patent....BodyPart 1
« on: June 20, 2004, 03:28:00 AM »
I'd like to start disecting this patent that Uncle Fester stumbled on and posted in another thread.

Post 512491 (missing)

(UncleFester: "the goo may not spread!", Stimulants)

There are some points I feel need to be addressed in order to alleviate some common misconceptions about the Controlled Released formulations.
Too many to list in one setting, so with the help of AWEBees here, I'm hoping we can arrive at some more exacting info in regards to what bees are faced with concerning extraction when dealing with inactives and their removal.

This dissemination of information would not be complete if the other patents weren't included that directly affect the "Layering" of technology being employed to combat this international problem as seen through the eyes of the lawmakers.
However, for the sake of conciseness here, we'll just list the links to them for reference instead of breaking them down.

Patent US6359011

  Denaturants for sympathomimetic amine salts

Patent US6136864

  Denaturants for sympathomimetic amine salts
A fuller understanding of all the relevant patents is in order, as they relate to one another, and I'm under qualified to break it all down alone.
I'm willing to share what I know and have learned based on what's been uncovered so far.
Several conclusions have been reached based on what is understood and it's thse areas that I intend to highlight and focus on.
Don't everyone fall out of your chairs at once if any of what's about to follow is displayed in a way that closely ressembles anything remotely organized :P .
The act of every bee falling out of their chairs at once might create a moment of silence, and we'll have none of that hear! ;D
I'd like to comment on the following statement:

In post

Post 512491 (missing)

(UncleFester: "the goo may not spread!", Stimulants)
Uncle Fester wrote I did some patent checking, and in particular

Patent US6699502

. The blue goo wasn't invented to frustrate extraction, rather it is the system used to time delay the release of the sudo once it has been swallowed. If it was put into the 30 mg red hot, then the cold sufferer would get no relief from the pill he had taken. That would lead to bad sales to cold sufferers, and so wouldn't be tolerated at corporate HQ. So long as the 30 mg red hot can be cracked by this method..."the spice will flow"...




First I'd like to state that non Sustained Release and/or Extended Released formulation strength OTC pills(30mg and 60mg pseudo) also contain Controlled Release technology and/or Modified delivery systems comprised of Modified components to alter the chemical behavior within the system.
The way I see these shifts in the way the active drug is delivered, while it doesn't point directly toward frustrating extraction, it does frustrate extraction.

These Modified Release systems have been extended beyond a simple definition.
They are employing two different patents that I'm going to highlight and attempt to summerize and will be at the heart of what brought this post into being.
Those two patents of main importance and focus here are:

Patent US6699502

Pharmaceutical compositions for controlled release of active substances

Patent US6419954

Tablets and methods for modified release of hydrophilic and other active agents

Now we'll start to unravel some new terminology such as "delayed and/or pulsatile release.
It's important to zero in on what makes these delivery systems perform the functions they were created for if any success is going to be made toward a reverse engineering technique to enable extraction.
In this first part(see below), I'm going to post the mechanics behind these two patents of interest.
During part two, I'll finish posting what was started toward disecting the individual parts that makeup the patents complexities and how they seem to relate to one another when combined in the same formulation.
The pills strengths, 30mg, 60mg, 120mg, or 240mg, are not an identifiable means of reliably determining the presense of a Delivery System as defined by these patents.
It can be assumed that all pills will be manufactured with the newest technologies that target the most reliable and effective areas that will maximize the effect for which the drug was intended.
Putting everything in the right order is key to understanding and the way the claims read "AS IS" in the patent, it would appear as if they worded things in such a way to discourage the average person from reaching a better understanding.
Those skilled in the art would have no problem!
I'm posting another patent of relevance that has been stumbled upon in the process of this research.
*NEW*2004-05-20

Patent US2004097536

Extended release oral dosage composition


Patent US6419954

  Tablets and methods for modified release of hydrophilic and other active agents

Abstract


The invention provides a tablet and methods for making the tablet comprising a gel-forming material and at least one particle comprising an active agent in contact with a coating material to modify release of the active agent
BACKGROUND OF THE INVENTION

{0004}A variety of hydrogel-type preparations have been developed to effect the sustained release of orally ingested drugs. All of these preparations are designed to release a drug continuously while the administered preparation is still retained in the upper digestive tract, typically in the stomach and small intestine. They were not intended to provide for a release of a drug in the lower digestive tract including the colon, where little water is available.
{0005} Hydrophilic gel-forming preparations have been further developed so that they can provide a sustained release of orally ingested drugs throughout the digestive system, including in the lower digestive tract..... a preparation adapted to absorb water into its core to undergo substantially complete gelation during its stay in the upper digestive tract. As the tablet moves down the digestive system in the form of a gel to the lower digestive tract, the preparation swells and the gelled outer surface of the tablet erodes gradually releasing the drug. This type of oral tablet is capable of providing a sustained release of the drug throughout the digestive tract, including in the colon.
{0006} While the gel-forming preparations, such as those described in the EP 0 661 045, have many applications, they may not be suitable for certain types of active agents, particularly when the active agents are unstable in the gel-forming preparations or may be released in a manner that is not desirable. Thus, there exists a continuing need for improved forms of sustained release preparations which can continuously release an active agent throughout the digestive tract, regardless of the physical or chemical properties of the active agent. Moreover, many situations may require that an active agent be delivered to the patient in a non-random or pulsatile manner, or, that the active agent be delivered to a particular anatomic compartment, e.g., the colon. For example, if an easily degradable drug or a drug with a short biological half-life needs to be delivered to the colon, it cannot be released in the upper digestive tract. Thus, there is a need for tablets that are capable of providing delayed and/or pulsatile release of an active agent. The present invention fulfills these and other needs.





Patent US6699502

Pharmaceutical compositions for controlled release of active substances

Abstract


The present invention is directed a pharmaceutical composition which can be administered orally, allowing for the controlled release of at least one active substance. The composition includes at least one active substance, between 5 and 60% by weight, relative to the total weight of the composition, of at least one excipient, selected from inert matrices, hydrophilic matrices, lipid matrices, mixtures of inert matrices and of lipid matrices, and mixtures of hydrophilic matrices and of inert matrices, with the exception of mixtures including a polyacrylic acid and at least one hydrophilic matrix of the cellulose type; and between 5 and 50% by weight, relative to the total weight of the composition, of at least one alkalinizing agent soluble in an aqueous phase under physiological pH conditions, selected from alkali or alkaline-earth metal hydroxides, carbonates, bicarbonates, phosphates, sodium borate and basic salts of organic acids. The invention further includes a process for preparation of the composition, multi-layered pharmaceutical compositions including at least one layer of the inventive composition, and processes for producing same.






BodyPart 2 should follow soon I hope once E-gor makes it back from the cemetary ...




WzKid

  • Guest
Awesome
« Reply #1 on: June 20, 2004, 12:38:00 PM »
Awesome Research Ware!

UncleFester

  • Guest
candelilla wax
« Reply #2 on: June 22, 2004, 03:42:00 AM »
Has anyone noticed on the name brand pills that the favorite wax other than acacia is now candelilla?? There is a reason for that....the wax from my researches is very hard to filter, even when hot...of course...one may wish to heat a soak to dissolve more out...but the wax is gooey stuff.

wareami

  • Guest
Forecast....
« Reply #3 on: June 22, 2004, 04:45:00 AM »
Moldie with a chance of meatier showers ;D
The Kidz are still buried in the translation of these patents but will chime in regarding this observation made by UncleFester.
This wax switch does seem to be a prevelant modification.
It's interesting to note that a waxy precipitate has been isolated with the use of selected solvents.
It will precipitate out along with the pfed in acetone following exposure to japandrier/tetra using white60 actifool knockoffs.
It takes on the coloration of this yellow oily substance.
These waxes seem to be modified in such a way as to appear as part of the pfed xtals and will immwediately go back into solution when dissolving the pfed again.
Because it is one with the pfed in the various solvent solutions, it makes it hard to separate the two.
The only way Ibee's been able to isolate the pfed from this substance is with the use of solvents suitable for dissolving Eudragit.
As much as I've strived to become a spelling bee over the past few years, I'm not at liberty to spell it out step by step for fear it will hurt the collective.
Therefore you'll need to decypher the pdf files posted in other threads that deal with this issue.
The wax is indeed an oil based substance according to whats been revealed through Ibee's testing and it's also been revealed through the patent research that they have modified some components and this wax observation on the part of UncleFester seems to be the likely culprit that is acting as the acrylate carrier.
BodyPart 2 is the toughest undertaking Ibees undertook so bee patient as the disecting continues!
Just wanted to say "Good call uncle fester!"
More will be revealed.