Pharmaceutical Technology-II

BPM-313

Dr. Nargis Sultana Chowdhury

Associate Professor & Head
Department of Pharmacy
Manarat International University
Dhaka, Bangladesh
Pharmacutics (Dosage form Design)
 Pharmacutics (Dosage form Design)

Pharmaceutics is the discipline of pharmacy that deals with

all facets of the process of turning a new chemical entity
(NCE) into a safe and effective medication. Pharmaceutics is
the science of dosage form design. Pharmaceutics deals with
the formulation of a pure drug substance into a dosage form. In
a simple way-----
Pharmaceutics converts a drug into medicine.
Branches of pharmaceutics include: Pharmaceutical
formulation, Pharmaceutical Manufacturing, Dispensing
Pharmacy, Pharmaceutical Technology, Physical Pharmacy,
Pharmaceutical jurisprudence etc.
Lecture-1
Lecture-1
 Tablet Dosage form (Historical Background)

 Wilium Brockedon an English man in December 1843

patented a single punch tablet machine. The first tablet is
formed by the constituent of compressed Potassium-bi-
carbonate (KHCO3). But the term tablet was not
introduced at the time. The Welcome Company for the
first time in history introduced the term tablet for
compressed dosage form.
 Tablets have in wide spread used since the later part of
19th century and their popularity continues.
7
 Lecture-1 (Definition)
Tablet is a solid pharmaceutical dosage form containing
a single dose of one or more suitably prepared active
ingredient usually with additives and obtained by
compressing or compacting a uniform volume of particles.

Tablets are intended for oral administration, some are

swallowed whole, some after being chewed, some are
dissolved or dispersed in water before administrated and
some are retained in the mouth where the active
ingredient is liberated (e.g. nitroglycerin, antacids etc).
 Lecture-1

Size and shape of tablet: Tablet may be of various shape

and size commonly they are round shape. They may also
exist in the form of oval, oblong, cylindrical or triangular. Their
reasonable diameter is within the range of 3/16 inch to ½ inch.

Objective: The objective of design and manufacturing

tablet is to deliver orally the correct amount of drug in the
proper form, at over the proper time, in the desire location
and have its chemical integrity protected to that point.
 Advantages of Tablet

Tablet is a unit dosage form.

They offer themselves at the greatest dose precision and least content variability.
The cost is lowest over all other dosage form.
They are the highest and most compact than all other oral dosage form.
They are in general the easiest and cheapest to package, shipment than all other
dosage form.
Product identification is potentially is simplest when employing an embossed or
monogram punch face.
They lend themselves to contain special release profile products, such as: enteric
coated tablet, delayed action tablet etc.
They are better suited to large scale production than other unit oral dosage form.
They have the best combined properties of chemical, mechanical and
microbiological stability than other oral dosage form,
Tablet is an essentially tamper proof dosage form,
Self administration is possible,
Long expiry period and minimum microbial spillage owing to lower moisture content.
 Disdvantages of Tablet

Tablets are not suitable for emergency case.

Sometimes they are not recommended for patients have swallowing problem.
Some drugs resist compression into dense compact, owing to their amorphous
nature. flocculent property, or low density character. These types of drugs may not
formulate as a tablet.
Drugs with poor wetting, slow dissolution properties may be difficult to formulate and
manufacture as a tablet.
Bitter testing drug, drug with disagreeable odor may require additional coating.
Coated tablet may increase in weight and also increase in cost accordingly.
Drugs that are sensitive to oxygen and moisture may require encapsulation.
The main disadvantage of tablet as dosage form concern the bioavailability of poorly
water soluble or poorly absorbable drug.
Tablets administered orally experience first pass metabolism, as a result
bioavailability of medicinal substance may be lessen than that administered
parenterally.
Tablet swallowing for pediatric and geriatric patient may be difficult.
For unconscious and vomiting patient tablet swallowing orally is not possible.
 Essential quality of a good tablet
The tablet should include the correct dose of the drug,
A tablet should be elegant product having its own identity,
It should be free from defects like chips, cracks, discoloration, contamination etc.
Tablet should have the strength to withstand the mechanical shock encountered
in its production, packaging, shipping and dispensing,
It should be accurate and uniform in weight,
Size and shape of a tablet should be reasonable for its easy administration,
The tablet should not be too hard or too soft,
There should not any incompatibility among the formulation ingredients,
They should have their physical stability to maintain their physical attribute over
time,
They must be able to release the medicinal agent into the body in a predictable
and reproducible manner,
They must have the suitable chemical stability and not to allow the alteration of
the medicinal agent,
They must be easier and economical in production.
 Types of Tablets

2.Tablets used in the oral cavity Tablets for oral ingestion.1

• Buccal tablets.
• Sublingual tablets. • Compressed tablets.
• Multiple compressed tablets
• Lozenges, Troches and
- Layered tablets.
dental cones.
- Compression-coated
Tablets used to prepare .3 tablets
solutions • Repeat-action tablets.
• Effervescent tablets. • Delayed-action and enteric-
• Dispensing tablets. coated tablets.
• Hypodermic tablets. • Sugar and chocolate-coated
• Tablet triturates. tablets.
4.Tablets administered by other • Film-coated tablets.
route Implantation tablets • Chewable tablets.
 1. Oral Tablets for ingestion

Over 90% of the tablets manufactured today are ingested orally. Orally ingested
tablets are designed to be swallowed intact, with the exception of chewable tablet.
This category refers to standard uncoated tablets made by compression. Most
compressed tablets containing drugs intended to exert local or systemic effects.
Example: Paracetamol, Aspirin, Antacid etc.
 Multiple compressed Tablets

These are compressed tablets made by more than one compressed cycle.
The result may be a multiple layered tablet or a tablet within a tablet, the
inner tablet being the core ant outer tablet portion being the shell. Tablets in
this category are usually for one or two reason. These are ---
 
To separate physically or chemically incompatible ingredients.
To produce repeat-action or prolonged action product.
 
This process is best used when separation of active ingredients is needed
for stability purposes, or if the mixing process is inadequate to guarantee
uniform distribution of two or more active ingredients.

There are two classes of multiple compressed tablets. These are ---
Layered tablets
Compression coated tablets.
 Layered Tablets and Compression Coated Tablets

Layered tablets: Such tablets are prepared by compressing additional tablet granulation on
a previously compressed granulation. The operation may be repeated to produce
multilayered tablets of two or three or more layers. Special tablet presses are required to
produce multi layered tablet.
Example: cetrizine(rhynis) + pseudoephedrine (nasal congestion) + naproxen
(headache)

Compression coated tablet: Such tablets are referred to as dry-coated, are prepared by
feeding previously compressed tablets into a special tableting machine and compressing
another granulation layer around the preformed tablet. This process applies a thinner, more
uniform coating than sugar-coating, and it can be used safely with drugs that are sensitive to
moisture.
This process can be used to:
• Separate incompatible materials.
• Produce repeat action or prolonged-action products.
Example: Amoxicillin + Potassium clavulanate
 Repeat Action Tablets

Repeat-action
  tablets usually contain two single doses of a
medication, one for immediate release and one
for delayed release. The mode of operation of repeat-action
tablets is
• The core tablet is usually coated with shellac or an enteric
coated polymer so that it will not release its drug load in
the stomach.
• The second dose of drug is then added in the sugar
coating, either in solution in the sugar syrup or as a part of
the dusting powder added for rapid coat builds up.

Examples: Dexchlorpheniramine Maleate (Antihistamine),

Drotaverin (antispasmodic) etc.
 Delayed action Tablets

Delayed Action tablets delay the release of a drug from a dosage

form. This delay is intended to:
Prevent destruction of the drug by gastric juices.
To prevent irritation of the stomach lining by the drug.
To promote absorption, this is better in the intestine than in
the stomach.
Agents used to coat these tablets include fats, fatty acids,
waxes, shellac, and cellulose acetate phthalate.
Example: Omeprazole, Ciprofloxacin, Cephradin, Contine (Theophylline)
etc. Gliclazide, Indomethacine, Neomycin, Diclofenal, Aspirin and
most of the pain killer drugs and strong electrolytes e.g. NH 4Cl.
 Enteric coated tablets

Enteric­ coated tablets are tablets with a coating that resists dissolution or
disruption in the stomach but not in the intestines, thereby allowing for tablet
transit through the stomach in favor of tablet disintegration and drug
dissolution and absorption from the intestines.
Examples: Omeprazole, Ciprofloxacin, Cephradin, strong electrolytes
e.g. NH4Cl etc
 Sugar Coated Tablets

These are compressed tablets surrounded by a

sugar coating. Such coating may be colored and
beneficial in covering up drug substances

• possessing objectionable tastes or odors

• and in protecting materials sensitive to
oxidation.
• The coating is water soluble and quickly
dissolves after swallowing.
• Sugar coating also enhances the appearance
of the compressed tablets.

Examples: Ferrus Sulphate, Ibuprofen,

multivitamins etc
 Film Coated Tablets

The tablet is coated with a membrane of polymeric substances that

improves physicochemical stability of the drug and delays the rate of
drug absorption.
The function of the coating may be to improve esthetics, mask taste, or
modify drug release.
Example: Ciprofloxacin, Ranitidine USP, Metronidazole etc.
 Chewable Tablets

Chewable tablets are intended to be chewed in the mouth

prior to swallowing and are not intended to be swallowed
intact. Chewable tablets have a smooth, rapid
disintegration when chewed or allowed to dissolve in the
mouth. The purpose of chewable tablet is to provide a
unit dosage form of medication which can be easily
administered to infants and children or to the elderly, who
may have difficulty swallowing a tablet intact.
Example: Anthalmintic drugs (e.g. Albendazole,
Mabendazole etc), Antacid tablet, Vitamin-C tablet,
coated chewable tablet (e.g. Mg(OH)2, Mg trisilicate,
Magaldrate etc).
 Tablets used in Oral Cavity

Tablets used in the oral cavity are allowed to

dissolve in the mouth.
(1) Sublingual tablets
The tablet is placed under the tongue
Sublingual tablets are absorbed quickly into the
bloodstream
e.g. Nitroglycerin, atropine sulphate, Methyl
testosterone
(2) Buccal tablets
Buccal tablets are placed in the pouch between the
cheek and gum
They are usually small, flat and oval in shape
e.g. Desaminooxitocin, Riboflavin, Progesterone
tablet.
 Troches and Lozenges

Troches (lozenges or pastilles)

The tablets contain a drug substance in flavored
base.
Lozenges are allowed to dissolve in the mouth. They
are commonly used for cold and sore throat.
Example: Strepsil  (Dextromethorphan hydrobromide
5mg, Dichlorobenzyl alchohol 1.2mg,
Amylmetacresol 0.6mg) is used
 Dental Cones

Dental cones are relatively minor tablet forms that are designed to be
placed in the empty socket remaining following a tooth extraction. Their
usual purpose is to
• prevent the multiplication of bacteria in the socket following such
extraction by employing a slow-releasing antibacterial compound,
• reduce bleeding by containing an astringent or coagulant.
 
Example: Pentoxyphylline, amino caproic acid, NaHCO3,NaCl
 
 Tablets used to prepare solution

Effervescent tablets are designed to produce a solution rapidly with

simultaneously release of carbon dioxide (Co2). The tablets are typically
prepared by compressing

• the active ingredients with mixtures of

• organic acids- such as citric acid or tartaric acid and
• sodium bi carbonate.

When such a tablet is dropped into a glass of water a chemical reaction

is initiated between the acid and the sodium bi carbonate to form carbon
dioxide and water. This reaction is quite rapid and usually completed
within one minute or less.
Examples: Supradin(multivitamin, minerals, trace element, Vit C)
Aspirin etc.
 Tablet administered by other route

Implantation tablets or depot tablets are designed for

subcutaneous implantation in animals or man. Their purpose is
to provide prolonged drug effects, ranging from one month to a
year. They are usually designed to provide as constant a drug
delivery release rate as possible. These tablets are usually
small, cylindrical, or rosette shaped forms, and are typically not
more than 8mm in length.
 
Example: Contraceptive tablets.