Author Topic: Beating orange gakk, chapter two  (Read 7415 times)

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wareami

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Just In....patent # 6,649,186
« Reply #20 on: November 26, 2003, 11:24:00 PM »
This Just In...Hot Off The Press
A quick peek into this patent

Patent US6649186

with the date November 18th 2003 might add some validation toward what Ibee's been saying in regards to inactives making up separate compounds as well as granulation issues and the processes used...
The fact that it includes many other drugs just gives credence to the fact that their aim is that no medicine should be easily extractable from it's formulation as a way of guarding against uses other than intended purpose.
While Ibee doesn't think that the pfed tablet will come in this effervescent form....the inactives are what Ibee is concerned with here.
What is claimed is:

1. An effervescent granule having a controllable rate of effervescence comprising:

a mixture consisting essentially of an acidic agent, pharmacologically active agent, a hot-melt extrudable binder and optionally a plasticizer; and an alkaline agent;
the effervescent granule made by an essentially water free and essentially solvent free thermal heat process comprising:
dry blending said mixture; and hot-melt extruding said blended mixture to form an effervescent granule.

The Kicker:
Claim 24 where the effervescent granule of claim 1 wherein the effervescent granule is formulated into a tablet.
How Broad and encompassing (and convenient)since all the other claims specify a target drug or compound???

EXAMPLE 14

Preparation of Tablets Containing Effervescent Granules

The following general procedure can be used to prepare a wide variety of tablet dosage forms containing the effervescent granules of the invention. It should be understood that the ingredients listed below are merely representative and can be replaced by many other equivalent compounds. Any of the effervescent granules detailed here as granules A through S may be employed where effervescent granule (EG) is indicated in the following tablet formulations.
        A.    Ingredients                     Amount (% Wt.)
              Effervescent Granule (EG)             40
              Dicalcium Phosphate                   10
              Microcrystalline Cellulose (MCC)          5
              Calcium Stearate                      2.5
              Silicon Dioxide                       1.0
              APAP                                 41.5
          B.        Ingredients             Amount (% Wt.)
                    EG                            50
                    Pseudoephedrine HCI            20
                    Mannitol                      29
                    Magnesium Stearate            0.5
                    Silicon Dioxide               0.5
          C.        Ingredients             Amount (% Wt.)
                    EG                            25
                    MCC                           15
                    Diltiazem                     10
                    Lactose                       47
                    Magnesium Stearate             0.5
                    Silicon Dioxide               0.5
                    Aspartame                     1
                    Grape Flavor                  1
          D.        Ingredients             Amount (% Wt.)
                    APAP                          60
                    EG (C)                        8
                    Mannitol                      30
                    Aspartame                     1.5
                    Magnesium Stearate             0.5


EXAMPLE 16

Drug-containing hot Melt Extrudable Effervescent Granulations

The following examples are presented to demonstrate the utility of the present invention in the preparation of drug-containing granules. The drugs identified in Table 4 are for representative purposes only, as many other pharmacologically agents may be similarly included alone or in combination in the granulation process employing techniques known to those of ordinary skill in the art.


                             TABLE 4
    Drug-Containing Hot-Melt Extruded Effervescent Formulations
        Ibuprofen         50    50     0       0       0    30
        Chlorphesinamine   0     0     5       5       0     5
        Maleate
        Pseudoephridine    0     0     0      25      20
        HCl
        AcDiSol            5     5     0       0       5     5
        Microcrystalline  20    10    32      20             5
        Cellulose
        Na Bicarbonate    13    13    15      18      20    15
        Citric Acid       12    12    14      15      18    13
        PEG 3350           0    10    14      12      10    12
        Crosslinked PVP    0     0     5       3       3     3
        Explotab           0     0     0       2             2
        Mannitol           0     0     5               9
        Xylitol            0     0    10              15    10


SHORTY

  • Guest
I don't want to get off topic here but....
« Reply #21 on: November 27, 2003, 01:05:00 AM »
I don't doubt one bit the abilities or experience that the Pharmaceutical chemists possess.  As a matter of fact i think that if they truly wanted to stop us from getting the pseudo then they would do it.

What I am finding hard to beleive is how the government is even involved in gaaking pills.  It sounds good and even likely when broadly mentioned as if the government were one man with the ability to keep his mouth shut.  However, we are talking about hundreds if not thousands of government officials keeping a huge secret from the rest of the public when it would bee more effective to do the opposite.  How would it hamper their efforts if they were to announce that they are working with the pharmaceutical companies in an effort to prevent the unlawful use of otc medications?  I mean surely that would stop alot of would be cooks from even trying to do it.

I would just like to understand how this all got started and how it could bee able to bee kept secret for so long.  Surely the government isn't getting this done for free so where is the budget allocation. If it were true then basically it would mean that the government was somehow strongarming the entire pharmaceutical industry and those involved are so scared that they not dare speak to anyone.  In this day and age we are informed of everything from the soap operas the Queen of England is fond of to the daily activities of the people of some tribe of people in the most remote places of the planet.

Can't anyone just give a possible scenario as to how these various meetings take place and how they are conducted.


SQUIDIPPY

  • Guest
don't fool your self
« Reply #22 on: November 27, 2003, 09:25:00 AM »
Don't fool yourself. Lots of folks, government employees in particular, line their wallets, with the profits from pharmaceutical stocks.
Believe this. Those pharmaceutical engineers are told this; Make it very difficult to extract the pfed from these pills.(This increases sales), But, do not make it impossible. (That would decrease sales.)


halfkast

  • Guest
ware & geez, all that information and ...
« Reply #23 on: November 27, 2003, 12:42:00 PM »
ware & geez, all that information and discussion on my questions was and is much appreciated  ;)

I don't think it has to be too strainful catching up with responses, but now isn't the time unfortunetly, but I wanted to say that it was very nice of you to go to all that trouble.

The orange gak is nasty

The dry-mixing of the base is a side-step, a work-around.
But it's limited


See, the task is to provide for the pfed an alternative


What would be ideal, to make the dry-basing a full yielding side-step is to cause a change of polarity with no water present. Just a Non-polar for the newly formed pfed freebase. Bubbles? moist air? some so of mechanical reflux or mixing at some special stage which. talk bout later, very tired.

At this point, the orange gak can be removed with strong basic water washes, safely and quantitatively. See?

I'm not sure that this oil is slightly soluble in non-polar as you theorize...I was leaning more towards the orange formed upon over-basification providing a solvent for transiting a second compound?

But you probably have a better idea because I get the strong impression that you have been described things on a bigger scale where things are more clear.

The haughty chloroform gloater, SPISSHAK, might bee having success removing it in a procedure with no polarity change because the orange isnt dissolved by the chloroform?

Using a liquid-liquid exaction of the over-based orange water would bee spectacular.
But theres uncertainties when you consider this orange, strongly water soluble non-volitile, which


If you concentrate it, it's more dense...ohh it looks like a lot of water is the key to free the free base, as hellman and bos have said.

I want to know if this orange stuff is less efficient at dissolving pfed.fb in hot or cold conditions, as this will allow for a minimum amount of water.

oh (very tired). but as the pfed is released in to the NP, there will be fresh room in it to dissolve more pfed.fb in a given amount of water. dunno

Ware what would bee a pleasurable outcome is a proper liquid-liquid extraction, or to crash out/salt out.

DCM washed out PEG like she's a girl, well she is a girl.
ohh that could help for the basing with little to no water present, as it provides a bottom-layer and a top layer of non-polar for the pfed.fb escapees.

a tetra wash would bee essential in agreiches procedure.

ohh a solvent above and below the basing process would double the escape routes, thus leaving less opportunity to dissolve in this orange.

shaking in this environment might help crack this fun puzzle too? i got no idea, bed.

i know what about the washing machine?


ahgreich

  • Guest
as above, so below?
« Reply #24 on: December 01, 2003, 07:48:00 AM »
isn't the dh20 already the 'middle solvent' of which you postulate to add to the tetra trap, or is it merely a base activator?
If it's a base activator, why not
1.heat the gups/carbonate +h20 to dryness (before addition of tetra)
2. then saturate with tetra
3. then add toluene and proceed as normal.
--think about it: you would begin the tetra trap with pre-based pfed, so no need for dh20 to activate gakks once your solvent-play begins.
Possibility - after dry-mixing with carbonate, oven-heat the gups below mp of pseudo (hcl and fb). also, use an excess of carbonate (by mass) to act as a gakk sponge for anything that escapes the tetra?

spectralshift

  • Guest
nah man. so heating a base with the special...
« Reply #25 on: December 16, 2003, 06:24:00 AM »
nah man.

so heating a base with the special alcohol definetly freebases the alcohol? in part or almost completely?


In the tetra trap, the role of the perc is to dissolve the...? you tell me, the polymers id guess.

What I said was that having twice the interface area, two non-polars, below and above the non-polar, for the pfed to migrate to at the point of activation of the orange acqueous middle layer PEG(?) solvent, the better.


Sorry I havent replied, I PM'd geezmeister, no response, I'm, guessing he is either you or is crying about something else.


Anyway, no one understood.
orange acquous oil dissolves pfed ( dont know and dont care really which polarity)

orange is removed by strongly basic acqueous solutions......obviously.

so after basifaction and greatest migration of the highest propertion of pfed as possible in the NP(S) (chlorinated below & aromatic/regular NP above)


I'm not sure3 of the role of tetra/bottom layer in your writer-up...swihk has seen DCM and absolutely nothing produce identical results when used as bottom layers.


Anyway depending what you say about the base/pfed.hcl heating causing the change.

I was thinking at that time about a ternary azeotrope of DCM, Toluene and methylated spirits completing the job.


Let me tell you...wareami's discovery of the solvent perchlorethylene is the greatest discovery of the era, and when it doiesnt lock up the PEG in a procedure its being used innefectively.
This is perfectly fine, every procedure gets amended doesnt it?
1. tetra rinse/boil n rinse
2. tetra trap, except tetra is used as a second NP (below), a regular NP is used above.
They are combined. (everything is decanted as one layer, including any water)
3. washes of the nonpolar with heavily based water/


Edit: there's probably several ways to do it...already detailed at the Hive.
It's just that some of them are really too busy to make a fuss about it, and definetly too busy to do a write-up.

But the Tetra-trap is a sound foundation, your open to admendments arent you?


There was one bee who stated that he/her concentrated a solution of orange water and prcipitated the pfed out with HCl.

another bee at that time, BenWiffen, claimed to bee washing the Non-polar with water until no orange appears...this is entirely in line with what I've just detailed. In fact i stand corrected, it doesnt require a strongly basic solution once that orange has been activated, just plain water washes.

Scottydog isn't capable of lying, he's adament he's found another solution recently.