A. DISCUSSION:
Consumers prefer tablets over gel caps. The tablet maker has a responsibility to make a safe product; since, once those tablets are delivered, there is no control over the end use. One's karmic burden would be great, should one be responsible for an innocent's accident or illness. Only pharmaceutical grade ingredients should be used. Dosage must be carefully controlled.
In order to successfully compete against the myriad of products on the market, the tablet must be strong and have a good appearance.
Typical Amsterdam tablets are extremely well-made with creative logos; however, there is no reason a smaller producer cannot achieve similar results.
The active hydrochlorides that are discussed in this forum cannot be compressed by themselves. One must mix the active ingredient with a binder and a lubricant in order to make a pill. Binders, lubricants, coloring agents and any other non-active ingredients of a tablet are called excipients.
B. TABLET INGREDIENTS:
1. Active hydrochloride (your favorite honey) screened through a fine stainless steel screen, such as can be found in the kitchen section of most department stores. The active MUST be screened into a fine powder. 1 kg will make about 10,000 tablets.
2. Microcrystalline cellulose (MCC). This is the best binder. It compresses into a hard tablet. It is insoluble, thus acting as a disintegrant as well as a binder. It is used specifically for tablets. Buy 2 kg for every 1 kg of active you plan to press.
3. Lactose Powder. (USP grade--any other grade will be off-white, almost yellowish, which only matters for esthetics) This is a commonly used binder also known as milk sugar. It has less compressibility than MCC, but provides a sweet taste and imparts a sheen to the tablet. Buy 1 kg of lactose for every 1 kg of active you plan to press.
4. Magnesium Stearate (NF grade). This is a lubricant. It is a fine white powder that looks and feels like corn starch. One kg will be enough for 250,000 tablets.
5. Stearic Acid powder. (NF vegetable origin). This is another lubricant. The stearic acid we want is made from coconuts, not the stearic acid made from rendered cows (you'll thank me for this in ten years, when half the world will be dying of mad cow disease--at least you won't get it from a pill made by this recipe). If you cannot find stearic acid in powder and what you find is granular or in small flakes, you will have to screen it, just as you screened the active. 1 kg will be enough for 125,000 tablets.
C. SOURCES:
MCC can be obtained from the larger supply houses--the kind that supply pharmaceutical manufacturers. Lactose powder can be purchased in a pharmacy without a prescription. Mag stearate and vegetable stearic acid (aka stearin) can be found by calling around in the Yellow Pages to pharmacy supply houses and chemical companies. Manufacturers and distributors can be found on the Web. These excipients are not controlled, yet. However, as in any procurement, it helps to have a legitimate reason for the purchase, to sound knowledgable when talking to suppliers, and to have shipping accounts, fax, e-mail, and other business accoutrements. Please do not call up an industry rep with "Hey Dood! Can you sell me that stuff to make pills?" You'll just fuck it up for us legitimate guys.
D. DOSAGE:
In a nutshell: 25% active. 50% MCC. 22% Lactose. 1% magnesium stearate. 2% stearic acid.
Your goal is to make a 400mg pill that contains 100mg of active ingredient. A 400mg pill is larger than what comes from Europe, but the Europeans' main concern is lowering weight and volume for "transport," whereas your concern is hardness and durability. Also, the Europeans have access to real punch and die sets made by real manufacturers. You will have to make your own. A 400mg punch set is pretty small for a non-expert lathe operator. 400 mg is roughly the size of a Bayer aspirin.
Per 1000 g of active (for 10,000 pills @ 100 mg active each) use the following quantities of excipients:
2000 g MCC
880 g Lactose powder
40 g Magnesium stearate
80 g Stearic acid
(Tip: If you cannot find MCC, it can be substituted with lactose powder. In other words, you can make a passable pill entirely from lactose, lubricants, and active, without any MCC. However the calibration of your press will require more attention, since the lactose has less compressibility.)
Weigh the excipients into a large Tupperware bowl with an airtight cover. Do not add the active ingredient, yet! Mix the excipients by vigorous shaking for at least 15 minutes. Really shake them up, until you are convinced they are thoroughly mixed.
Use 20 grams of this mixture to calibrate your tablet press, until you have a 400 mg pill that is hard and cannot be broken between your fingers without a real effort. By calibration I mean adjusting the fill depth until you have a 400mg tablet and adjusting the top punch for hardness. Bear in mind that you will have to re-adjust everything once you add the active, since it has a higher specific gravity than the excipients.
IMPORTANT NOTE--If after making your test pills, you find that because of the shape or size of your punches and die that the optimum weight of your particular tablet is greater or less than 400mg, then adjust the amount of active that you add in the next step accordingly, so that each tablet has 100 mg of active. Obviously, for higher or lower dosages, you add more or less active, or you adjust the tablet press to make a heavier or lighter pill. Common sense and a calculator will be needed, since there are many factors to juggle when adding active to the excipients.
Add the active ingredient (it must be screened first) to the Tupperware bowl containing the excipients and thoroughly shake for 15 minutes. The mixture must be as homogenous as you can make it. Real pharmaceutical companies use a cone mixer to prepare tablet ingredients. A cone mixer works on the same principle as you shaking a Tupperware bowl. Just shake it up and down over and over and over, until your arms start to ache. Then mix it some more. The ingredients MUST as perfectly mixed as possible: the lives of users depend on your diligence.
E. ADVICE:
Wear disposable plastic gloves during the entire process of weighing, mixing, and tabletting. Wear a dust mask over your mouth and nose (this protects you as much as it protects the quality of the tablets). ALWAYS wash your hands. Once opened, store excipients in airtight containers to avoid contamination--remember, people will be eating this stuff. You might even consider a hair net while tabletting--you don't want your DNA in those pills. Your burden will be great, if you scrape up the dirty powder that has fallen around your machine--powder that contains metal filings and lubrication oil--and press it into pills. Just throw it away and call that the price of doing business.
ALWAYS wear gloves when you put the tablets into plastic bags. You do NOT want your fingerprints on those bags! Experience shows that vacuum bagging the pills keeps everybody honest.
Good luck.
I'll follow up with photos of a tablet press and how to build.
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