SOLID DOSAGE FORMS

Mutoya Nicholas
Cert Pharm,Cert Psc,Pgd TM,Pgd M&E,Dip
Ph,Dip pharm,Bpharm,MSc Ip ……
STANDARD AND COMPRESSED TABLETS

•made by direct compression or compression

following wet or dry granulation.
•intended for local action in the
gastrointestinal (GI) tract or for systemic
effects.
STANDARD AND COMPRESSED TABLETS

Ideal tablets should have the following

charcteristics;
•uniformity of drug content.
• stability of the drug candidate and the
formulation.
•optimal dissolution and availability for
absorption (whether immediate or
extended release).
•and patient acceptability in terms of
organoleptic properties and appearance.
STANDARD AND COMPRESSED TABLETS

Advantages
•simplicity and economy of manufacture.
•relative stability.
•convenience in packaging.
•convenience in shipping.
•convenience in storage.
•uniformity of dose.
•blandness of taste.
•ease of administration ensure.
STANDARD AND COMPRESSED TABLETS

Disadvantages
•low - density drugs can be difficult to
compress and formulate into tablets.
•poorly water soluble, poorly permeable
drugs or highly metabolized drugs cannot be
given this way.
•local irritant effects can be harmful to the
mucosa of the GI tract.
EXCIPIENTS IN SOLID DOSE FORMULATIONS

•Excipients are additions to the active

ingredients.
•They ensure that the manufacturing process
is successful and that the quality of the
resultant formulation is guaranteed.
•It is during preformulation studies that the
influence of excipients on stability,
bioavailability, and processability is
determined.
EXCIPIENTS IN SOLID DOSE FORMULATIONS

•Excipients are categorized into groups

according to their main function.
•However, some may be multifunctional.
EXCIPIENTS IN SOLID DOSE FORMULATIONS
Diluents
•inert substance frequently added to increase the
bulk of a tablet for processing and handling.
•Ideal diluent;
•chemically inert
•nonhygroscopic
•hydrophilic.
•acceptable taste.
•Low cost.
•Lactose is a common diluent in tablets, and it
fulfils most of these criteria but is unsuitable for
those who are lactose intolerant.
EXCIPIENTS IN SOLID DOSE FORMULATIONS
Binders
•Binders (or adhesives) are added to formulations
to promote cohesiveness within powders.
•They ensure that the tablet remains intact after
compression as well as improving the flow by
forming granules.
•A binder should impart adequate cohesion
without retarding disintegration or dissolution.
•Examples are Starch, gelatin, sugars, acacia,
sodium alginate, celluloses and polyvinyl
pyrrolidone (PVP).
EXCIPIENTS IN SOLID DOSE FORMULATIONS
Lubricants
•Lubricants can reduce friction between the
tablet and the die wall during compression
and ejection by interposing an intermediate
film of low shear strength at the interface
between the tablet and the die wall.
•Examples are stearic acid and stearic acid
salts, primarily magnesium stearate.
EXCIPIENTS IN SOLID DOSE FORMULATIONS
Glidants and Antiadherents
•glidants are fine powders and may be
required for tablet compression at high
production speeds to improve the flow
properties of the material into the die or
during initial compression stages.
•They are added in the dry state immediately
prior to compression and, by virtue of their
low adhesive potential, reduce the friction
between particles. Examples are colloidal
silica, starches and talc.
EXCIPIENTS IN SOLID DOSE FORMULATIONS
Disintegrants
•Disintegrants are added (5%) to a
formulation to overcome the cohesive
strength imparted during compression, thus
facilitating break up of the formulation in the
body and increasing the surface area for
dissolution.
•On contact, disintegrants can draw water into
the tablet, swelling and forcing the tablet
apart.
•Examples are starch and surfactants such as
sodium lauryl sulfate.
EXCIPIENTS IN SOLID DOSE FORMULATIONS

Superdisintegrants
•Compared with starch these are effective at
much lower levels (2-4%)and comprise three
groups: modified starches, modifi ed
cellulose, and cross - linked povidone.
•They may act by water wicking, swelling,
deformation recovery, repulsion, and heat of
wetting.
EXCIPIENTS IN SOLID DOSE FORMULATIONS

Colorants
•mask color changes in the formulation and
are used to provide uniqueness and identity
to a commercial product.
•Colorants are subject to regulations because
of safety concerns.
•Legislation specifies which colorants may be
used in medicinal products and also provides
for purity specifications.
EXCIPIENTS IN SOLID DOSE FORMULATIONS

Interactions and Safety of Excipients

COATED TABLETS

Advantages
•the drug is protected from the external
environment.
•to mask bitter tastes.
•add mechanical strength.
•to enhance ease of swallowing.
•aesthetic or commercial purposes.
•improved product appearance and identity.
COATED TABLETS

Sugar - Coated Tablets

Compression Coating and Layered Tablets
Film - Coated Tablets
Tablet Wrapping or Enrobing
Buccal and sublingual tablet
•Sublingual and buccal medications are
administered by placing them in the mouth,
either under the tongue (sublingual) or
between the gum and the cheek (buccal).
•The medications dissolve rapidly and are
absorbed through the mucous membranes of
the mouth, where they enter into the
bloodstream.
•Avoid the acid and enzymatic environment of
the stomach and the drug metabolizing
enzymes of the liver.
Effervescent tablet
•Effervescent tablets are uncoated tablets that
generally contain acid substances (citric and
tartaric acids) and carbonates or
bicarbonates and which react rapidly in the
presence of water by releasing carbon
dioxide.
•They are intended to be dissolved or
dispersed in water before use providing:
A- Very rapid tablet dispersion and
dissolution.
B- pleasant tasting carbonated drink.
Chewable tablet

•They are tablets that are chewed prior to

swallowing.
•They are designed for administration to
children e.g. vitamin products.
 Compressed tablet manufacturing

•The classification of manufacturing methods

wet granulation: suitable for drugs that are stable to moisture and
granulation heat
dry granulation: suitable for drugs that are sensitive to moisture
and heat
powder compression : suitable for drugs that are sensitive to
moisture and heat, fill material possessing, good flowability and
direct compressibility
compression
crystal compression：suitable for drugs with proper
crystal form and good flowability
 The classification of tablet presses
• Tablet presses:

a. single-punch presses

b. multi-station rotary presses

The main components of single-punch
tablet presses

Core components:
die
lower punch
upper punch
The compression cycle of a rotary tablet press
 Tablet coating
The reasons for tablet coating
1) to protect the medicinal agent against
destructive exposure to air and/or humidity;
2) to mask the taste of the drug;
3) to provide special characteristics of drug release;
4) to provide aesthetics or distinction to the
product;
5) to prevent inadvertent contact by nonpatients
with the drug substance
 Tablet coating

The general methods involved in coating tablets

are as follows
1) sugarcoating tablets
2) film-coating tablets
3) fluid-bed or air suspension coating
4) compression coating
Manufacturing Defects of Tablets

•Capping •Blistering
•Lamination •Cratering
•Chipping
•Picking
•Cracking
•Sticking •Pitting
•Picking •Blooming
•Binding •Blushing
•Mottling •Infilling
•Double impression •Roughness
•Bridging
 Standards of Quality for Tablets
The apparent physical features of compressed tablets:
1) shape: round, oblong, unique
2) thickness: thick or thin
3) diameter: large or small
4) flat or convex
5) unscored or scored in halves, thirds and quadrants
6) engraved or imprinted with an identifying symbol
and/or code number
7) coated or uncoated
8)colored or uncolored
9) number of layers.
Standards of Quality for Tablets
Other physical specifications and quality standards:
tablet weight weight variation
content uniformity tablet thickness
tablet hardness tablet disintegration
drug dissolution
in-process controls
verification after the production
Standards of Quality for Tablets
Tablet hardness
1)The greater the pressure applied, the harder
the tablets.
2) The hardness required by different tablets
a) lozenges and buccal tablets: hard
(dissolve slowly)
b) the tablets for immediate drug release:
3) Measurement
a) special dedicated hardness testers
b) multifunctional equipment
Standards of Quality for Tablets

Friability
1) It is used to determine a tablet’s durability
2) Method: allowing the tablets to roll and
fall within the rotating apparatus
(friabilator); determine the loss in weight;
3) requirement: weight loss ≤1%
Standards of Quality for Tablets— tablet
dissolution
1) The importance of in vitro dissolution test
a) to guide the formulation and product
development process toward product optimization
b) to monitor the performance of manufacturing
process
c) to assure bioequivalence from batch to batch
d) as a requirement for regulatory approval for
product marketing for products registered with the
FDA and regulatory agencies of other countries.
2) The goal of in vitro dissolution is to provide a
reasonable prediction of the product’s in vivo
bioavailability.

Basis: The combinations of a drug’s solubility and its

intestinal permeability are supposed as a basis for
predicting the likelihood of achieving a successful in
vivo – in vitro correlation (IVIVC).
3) The formulation and manufacturing factors affecting
the dissolution of a tablet
a) the particle size of the drug substance
b) the solubility and hygroscopicity of the formulation
c) the type and concentration of the disintegrant,
binder, and lubricant used
d) the manufacturing method, particularly, the
compactness of the granulation and the compression
force
e) the in-process variables
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