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The Formulation of low dose medicine

powders101

AnaSCI VET
Sep 21, 2007
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The LAB
The Formulation of Low Dose Medicine

By Mr.Rose, dedicated to big_ron.



The formulation of low dose drugs can be very challenging and problems related to content uniformity and physical stability will more than often arise. Many drugs that we often use pose such challenges, for example; Anavar , Dianabol , Anadrol , Cialis , Methyl tren ,etc.

There are many factors that have to be considered in the development of a homogeneous and segregation-free low dose formulation. Factors such as Atmospheric humidity, chosen binders, fillers, excipients, lubricants and disintegrates play a large role in creating acceptable homogeneity. For many of use the use of more complex formulations is mind-boggling, not to mention that most materials mentioned will be hard to come by. This is why many stick with just the active drug and basic filler.

The filler used will play a large role in the homogeneity of the product. For example, take these two common fillers:

Lactose Anhydrous (SEE ATTACHED IMAGE)

Microcrystalline Cellulose (SEE ATTACHED IMAGE)

1500 Starch (SEE ATTACHED IMAGE)


-Lactose Anhydrous had a mean value of 92.43 ± 1.42 % drug content per tablet.
-Starch (1500) had a mean value 96.00 ± 1.25 % drug content per tablet.
-Avicel (cellulose powder) had a mean value 99.59 ± 3.19 % drug content per tablet.

As you can see, one filler, the lactose Anydrous, had a much larger range than the Microcrystalline Cellulose. Over the tablets analyzed Cellulose had the best homogeneity, which an active drug content per tablet (from a batch off 200,000) of 99.59%.

The best and most commonly available fillers, in no particular order, are Lactose Anhydrous, Microcrystalline Cellulose, starch and Acidophilus.

I just wanted to give you guys a short introduction to fillers before I went into a decent method for mixing low dose formulations.

One of the best methods to bet mixtures of up to 99.5%+ is to mill both the filler and active drug to a uniformed consistency using a FitzMill through # 000 plate at a medium pace in order to create a consistent pre-mix. This pre-mix would then be loaded onto segregation cells and vibrated at 4Hz in order to create a uniformed distribution.

HOWEVER, most of you want to kill me already because you think I post too many complex methods, so let’s take it down a notch. Most of us want to mix low dose drugs for personal use, and most of us would be happy with 85%+ distribution rates. So here is a SIMPLE method that will do just that.

METHOD

Equipment/materials

-Filler
-a smooth NON-POROUS Mortar and pestle
-0.001g scale
-Powdered food coloring
-Capsules (any size)

1. Obtain a filler, and I HIGHLY recommend Microcrystalline Cellulose, aka powdered cellulose (the finer the better).
2. Obtain some powdered food coloring (mostly used to color eggs).
3. Grab a capsule (size 4, 3, 2, 1, 0, 00, 000, whichever), weigh it on a 0.001g scale (if you don’t have one, then why the hell are you trying to weight powders in the mg’s?), record its weight and/or zero it off on the scale.
4. Now fill the capsule you just weighed with the filler and cap it. Then weight it and record its weight. This will tell us how much filler can fit into the capsule. As a GENERAL guide,

SIZE..................Actual Volume (mL)................................. Amount of M-Cellulose
000.............................1.37.............. ................................................. 2055 mg
00...............................0.95............. .................................................. 1425 mg
0.................................0.68............ .................................................. . 1002 mg
1.................................0.50............ .................................................. . 750 mg
2.................................0.37............ .................................................. . 555mg
3.................................0.30............ .................................................. . 450 mg
4.................................0.21............ .................................................. . 315 mg
5.................................0.13............ .................................................. . 195mg

5. Empty out the capsule (or toss it), now that you have the total mg that can fit in your capsule with your particular filler, subtract the amount of active drug in mg from the total weight. For example, you’re capsule held 1000mg of filler, and you want 50mg of dianabol in each capsule, therefore you need 950mg of filler per capsule.
6. Now calculate the total amount of filler needed. So using the above example, you have 2g of dianabol powder (2000mg) and you want to make 40x50mg capsules. So that means: 950mg of filler per capsule, 40 capsules, so 0.95*40 = 38 grams of filler.
7. Ok now comes the fun bit. Remove 5 grams of filler and replace it with 5 grams of the powdered food color and mix it until it is uniform in color. What this will do is give color to the filler and let us know when we have a achieved a decently homogenous mixture.
8. Now add all your steroid powder to the smooth mortar and pestle and then add a EQUAL amount of your now colored filler.
9. Mix and grind this mixture with the mortar for a good 5-10 min or until it is uniform in color. (do this in a well lit room).
10. Now you have a 1:1 powder:filler ratio. What we want to do is AGAIN add an equal amount of filler to the amount of powder in the pestle. So using the dianabol example, we should have 4g in there, (2g dbol , 2g filler) so lets add another 4 g of filler. Now again mix and grind this until uniform in color.
11. Now you keep repeating this, doubling the amount of filler added until you have added the whole amount of filler.
12. Each time make sure you mix it WELL for at least 5-10min. The more the better.
13. Once you have completed this you can now begin capping.
14. Enjoy!

*Make sure it's a none-porous mortar and pestle!
 

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