Lec.

1 Industrial Pharmacy

References:
• The Theory and Practice of Industrial Pharmacy by L. Lachman
• The Science of Dosage Form Design by M. Aulton

Objectives:
This course enables the student to formulate different dosage forms and the
principles needed for the large scale production of them. The syllabus includes
different dosage forms like tablets, capsules, aerosols, emulsion, etc, besides some
advanced techniques.

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 Tablets
The tablet is a unit dosage form containing one or more constituents prepared by
compression to suitable shape.
The oral route is the most important method of administering drugs for systemic
effect. It is estimated that at least 90% of all drugs used to produce systemic effect are
administered by the oral route.
Of drugs that are administered orally, solid oral dosage forms (tablet and capsule)
represent the preferred products.
Tablets and capsules are more preferred than liquid dosed forms (syrup, suspension,
emulsion and elixir) because the latter suffer from the following disadvantages:
1. The patient is asked to measure his medication by a spoon. Such dose
measurements are in error by a factor may reaches up to 50%.
2. Liquid dosed forms are more expensive.
3. They are susceptible to breakage and leakage.
4. Taste-masking is more difficult in liquid dosed forms.
5. They are less stable physically, chemically and biologically.
Now, tablets are more preferred than capsules for the following reasons:
1. Tablets have greater dose accuracy.
2. Lowest cost of all dosage forms.
3. Tablets are the easiest in term of packaging and shipping.
4. Tablets are easer in swallowing than capsules.
5. They may be used for special release profile such as delayed-release and enteric
coated products.
6. Large-scale production is easier.
7. They have better chemical, physical and biological stability than capsules.
8. Flexibility of doses since the tablets can be divided (scored tablets).
On the other hand, tablets possess the following disadvantages:
1. Some drugs resist compression (poor compressibility) resulting in friable tablets
owing to their amorphous nature or low density.
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 2. Drugs with poor wettability, slow dissolution rate and large doses are difficult to
be formulated as tablets.
3. Drugs with very bitter taste (intolerable), objectionable odor or sensitive to air or
moisture are better to be formulated as capsule
Types of Tablets
1. Uncoated tablet: this type refers to the standard conventional tablets made by
compression. It is formulated to provide the usual disintegration and release rates.

MSC

% Released

MEC

Time (hr)

2. Multiple compressed tablets: they are also called bilayer or repeat-action tablets.
They are made by more than one compression cycle and composed of two layers each
containing either different or the same active ingredient. The reasons behind the
formulation of such dosage forms are:
• To separate incompatible drugs.
• To repeat the drug action.

MSC
1st tab.
% Released
2nd tab.

MEC

Time (hr)

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 3. Enteric coated tablets: they are coated with substances that resist disintegration in
gastric acids but disintegrate in intestine. Enteric coating is useful for two things:
• To protect the drug from the stomach.
• To protect the stomach from the drug.
4. Sugar coated tablets: these are tablets surrounded by sugar coat which is useful in
covering up drugs processing objectionable taste or odor and in protecting drugs
sensitive to oxidation.
5. Film coated tablets: they are covered with a thin layer of water soluble polymer.
Film coating imparts the same general characteristics as sugar coating with the added
advantage of reduced total tablet weight and reduced time required for the coating
operation.
6. Chewable tablets: these are intended to be chewed in the mouth prior to their
swallowing. The purpose of chewable tablets is to provide a unit dosage form which
can easily be administered to children and elderly.
7. Buccal and sublingual tablets: these types are intended to be held in the mouth
(not to be ingested) where they release their drug contents for absorption through oral
mucosa directly. The buccal tablets are intended to be held between the cheek and
gum whereas the sublingual tablets held beneath the tongue.
Drugs administered by this route are intended to produce systemic effect directly
from oral mucosa and thus, they must have very good absorption properties.
The advantages of this route are:
• It avoids the 1st pass metabolism in the liver, therefore, increases the
bioavailability.
• Avoids decomposition in the stomach (for acid sensitive drugs).
• More rapid onset of action.
The most famous example of drugs delivered by this route is nitroglycerin.
8. Orodispersible tablets: they are new type of tablets. These tablets disintegrate and/or
dissolve rapidly in the mouth (either on or beneath the tongue or in the buccal cavity)
without water within few seconds to few minutes. Upon placement in the mouth,
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orodispersible tablets absorb saliva rapidly in to the tablet core allowing the
disintegrants (super disintegrants) to swell, rapture the tablet and liberate its
components that form solution or suspension, which in turn can be swallowed easily
without water. On the other hand, orodispersible tablets can be swallowed intact; i.e.,
as if they were conventional tablets by using water to push them down to the stomach.
Orodispersible tablets have many advantages such as increase patient compliance, ease
of swallowing for both children & elderly, fasting onset of action and much more.
9. Effervescent tablets: In addition to the drug, these tablets contain sodium
bicarbonate and an organic acid such as tartaric or citric acid or both. In the presence
of water, these materials react to liberate carbon dioxide that act as a disintegrant and
produce effervesce.
The advantages of effervescent tablets are that they provide a mean of preparing
solutions containing an accurate dose and they mask the unpleasant taste of drugs by
both the blocking effect of CO2 on the tongue receptors and the flavored carbonated
drink.
10. Tablets for solution: they are intended to be added to a given volume of water by
the pharmacist to provide a solution of a given concentration.
Examples:
• Povidone tablet when dissolved in one litter of water gives 10% povidone
solution.
• Buffer tablet when dissolved in one litter of water gives standard buffer
solution.
The solution tablets contain high concentration of the substance to be prepared as
solution. Therefore, they should not be swallowed, otherwise, sever toxicity or
even death may result.
11. Sustained release tablets: they are designed to release the drug slowly over a
prolonged period of time. This type also called controlled release, prolonged
release or modified release tablet.

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12. Vaginal tablets: they are formulated to undergo slow dissolution in the vaginal
cavity. This type is used mostly to treat vaginal infections (locally) although some
of them may be used for systemic absorption.
13. Implantation tablets: implantation (or depot) tablets are inserted subcutaneously
to provide very long release period ranging from one month to one year. They
designed to provide as constant release rate as possible. These tablets are usually
cylindrical, small in size and do not exceed 8 mm in diameter.
Two disadvantages is the cause of the rare use of implantation tablets:
1. The need for surgical operation to apply and discontinue the therapy.
2. Tissue toxicity at the site of implantation.

Advanced oral drug delivery systems

1. Osmotic controlled-release oral delivery systems (OROS):

A rigid tablet with a semi-permeable outer membrane and one or more small laser
drilled holes in it.
As the tablet passes through the body, water is absorbed through
the semipermeable membrane via osmosis, and the resulting osmotic pressure is
used to push the active drug through the opening(s) in the tablet.
• Osmotic release systems have a number of major advantages over other
controlled-release mechanisms:
➢ They are significantly less affected by factors such as pH, food intake, GI
motility, and differing intestinal environments.
➢ Control over drug delivery rates. This allows for much more precise drug
delivery over an extended period of time, which results in much more
predictable pharmacokinetics.
❑ However, osmotic release systems are relatively complicated, somewhat
difficult to manufacture, and may cause irritation or even blockage of the GI
tract due to prolonged release of irritating drugs from the non-deformable tablet
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2. Floating tablets:
➢ Floating Oral Drug Delivery System (FDDS) are retained in the stomach and
are useful for drugs that are poorly soluble or unstable in intestinal fluids.
➢ Floating drug delivery system (FDDS) have a bulk density less than gastric
fluids and so remain floating in the stomach without affecting the gastric
emptying rate for a prolonged period of time.
➢ While the system is floating on the gastric contents, the drug is released slowly
at the desired rate from the system. After release of drug, the residual system is
emptied from the stomach.