Uy, Alyssa V.

2BPh • Effervescent Tablets – prepared by compressing granular

CHAPTER 8 – Tablets effervescent salts that release gas when in contact with water.
This tablet contains medicinal substance which dissolves rapidly
when in contact with water.
Tablets - solid dosage forms usually prepared with the aid of suitable
pharmaceutical excipients
• Molded Tablet Triturate (M.T.T.) – small & cylindrical, very soft,
soluble & designed to dissolve rapidly.
Majority are administered orally, while others sublingually, buccally or
vaginally contain features most applicable to their routes of administration.
• Compressed Tablet Triturate (CTT) – prepared by compression
(limited pressure) usually containing potent substance. Sucrose
Types of Tablets:
and lactose are used for diluent.
• Compressed Tablets (C.T.) - manufactured with tablet machine
capable of exerting great pressure or compacting the powdered
• Hypodermal Tablet (H.T.) – used by physicians for
or granulated tableting material. DILUENTS, BINDERS, DISINTEGRANTS,
extemporaneous preparations of parenterals. It is meant to be
ANTIADHERENTS/ GLIDANTS/LUBRICANT, COLORANTS/FLAVORANTS
dissolved in suitable vehicle, sterility attained, and the injection
performed. The advent of prefabricated injectable products and
• Multiple Compressed Tablets (MCT) – prepared by subjecting the
fill material to more than a single compression, the core (inner) disposable syringes declined its use.
and shell (outer)
• Dispensing Tablets (D.T.) or compounding tablets – used by
pharmacists when compounding prescriptions and not dispensed
• Sugar-Coated Tablet (S.C.T.) – the coating maybe colored or
uncolored sugar layer, water soluble and quickly dissolved after to patients. It contains large amount of potent subs. enabling the
pharmacist to obtain pre-measured amounts. For compounding
swallowing. Purposes: to protect the enclosed drug from the
multiple dosage units.
environment and to provide a barrier to objectionable taste and
smell of the drug. Disadvantages: time and expertise needed in
• Immediate Release Tablets (I.R.) – designed to disintegrate and
the coating process and increased shipping costs
release their medication and therefore are devoid of special rate
controlling features like coating and other ways.
• Film-Coated Tablets (F.C.T.) – coating is made of thin layer of a
polymer capable of forming a skin-like usually colored film over
• Instant Disintegrating/Dissolving Tablets – characterized to
the tablet. Polymer is cellulose acetate phthalate. Advantages of
dissolve within 10 seconds to 1 minute. This is possible with the
film coating over sugar coating: more durable, less bulky and less
use of lyophilization techniques, soft direct compression, or the
time consuming to apply.
use of water-soluble excipients designed to “wick” water into the
tablet for rapid disintegration.
• Gelatin Coated Tablet – capsule-shaped compressed tablet with
1/3 the size of capsule with the same amount of fill, more ease in
• Extended Release Tablet (E.R.) /Controlled Release (C.R.) –
swallowing & more tamper evident. (GelCaps)
designed to release their medication in a predetermined manner
over an extended period of time.
• Enteric-Coated Tablets (E.C.T.) – have delayed release features,
designed to pass the stomach to the intestines where the tablet
• Vaginal Tablet/Inserts – uncoated and bullet- or ovoid- shaped
will disintegrate allowing drug dissolution & absorption. Needed
tablets for localized effect. Prepared by compression and shaped
when drug substance:
to fit smugly into plastic inserter devices. They contain
antibacterials (against Hemophilia vaginitis) and antifungals
a) is destroyed by gastric acid
b) is irritating to the gastric mucosa (against Candida albicans)
c) by-passed the stomach enhances the drug
The physical features of compressed tablets are varied; its
absorption in the intestines
diameter and shapes are determined by the die and punches used
• Buccal tablets – flat, oval tablets intended to be dissolved slowly in the compression. The less concave the punch, the more flat the
resulting tablets. Punches with raised impressions will have
in the buccal pouch. It is for oral absorption of drugs destroyed by
recessed impressions on the tablets.
gastric acid or poorly absorbed in the GI tract.

• Sublingual Tablets – designed to erode promptly underneath the
tongue for rapid drug effect.
• Lozenges or troches – disc-shaped solid forms containing a
medicinal substance in a hard candy or sugar base. Meant to
dissolve slowly for localized effect or systemic effect
Quality Standards and Compedial Requirements:
• USP Weight Variation Test: 10 tablets are individually weighed
and average weight calculated.
• Content Uniformity: Dosage units are assayed individually and
requires that each dosage unit is 85% - 115% of the label claim
(S.D. is less than 6%)

• Chewable Tablets – have rapid disintegration when chewed or • Tablet thickness is determined by
allowed to dissolve in the mouth, have a creamy base usually
specially flavored and colored mannitol. Meant for large-sized a. the diameter of the die
b. the amount of fill
tablets given to children and adults with difficulty in swallowing
solid dosage forms c. the compactibility of the fill material
d. the force of pressure applied during compression.
Page 1 of 3
 • Tablet thickness is measured by a hand gauge.
• Tablet hardness affects its disintegration & drug absorption. The
greater the pressure, the harder the tablet. It should be hard
enough to resist breaking during the normal handling and yet soft
enough to disintegrate properly after swallowing.
• A force of 4 kilograms as determined by hardness tester is
minimum requirement for a satisfactory tablet.
• Tablet friability – the tendency to crumble by allowing it to roll
and fall within the rotating machine (friabilator). A maximum
weight loss of not more than 1% of the weight of the tablets being
tested is acceptable.
• Tablet Disintegration Test – uses a basket-rack assembly
containing 6 open ended transparent tubes held vertically upon a
10-mesh stainless steel wire screen.
The basket is raised and lowered in the immersion fluid (water at
37oC) at a frequency of 29-32 times per minute. Result: the
residue of the tablet on the screen is a soft mass having no
palpable inner core. Disintegration time ranged from 2 mins. to 4
hours depending upon the monograph.
For enteric coated tablets, test is done in a simulated gastric fluid
for 1 hr. No sign of disintegration must be seen. They are
immersed in a simulated intestinal fluid for the time stated in the
monograph where they disintegrate completely.
• Tablet dissolution test - Uses:
a. guides formulation and product development
b. performance of manufacturing process can be
monitored by it (quality assurance)
c. Consistent results assure bioequivalence from batch
to batch
d. As a requirement for regulatory approval
– Its goal to provide a reasonable prediction or correlation with
the product’s in vivo bioavailability.
a) High Solubility and High Permeability – IVIVC
b) Low Solubility and High Permeability – IVIVC
c) High Solubility and Low Permeability – limited IVIVC
d) Low Solubility and Low Permeability – none
In (a) IVIVC is expected if the dissolution time is slower then
gastric emptying time (limiting factor).
• Dissolution Test Apparatus consists of:
1. variable stirrer motor
2. stainless basket on a stirrer shaft (Apparatus I) or a
paddle as stirrer (Apparatus II)
3. 1-L vessel glass with a cover having the shaft of the
stirrer fitted at the center port, with 3 ports for
samples and 1 port for the thermometer
4. Water bath to maintain the temp. of the medium in
the vessel
Dissolution medium is placed in the vessel at 37oC + 0.5o C. The stirrer is
rotated at speed specified and at stated intervals; samples of the medium
are withdrawn for chemical analysis. Samples must meet the requirement
stated in the monograph.
Pooled dissolution testing – samples coming from different batches placed
in individual dissolution vessel in the apparatus or multiple dosage units in a
single vessel. This recognizes the concept of batch characteristics.
3 methods for compressed tablet:
 Wet Granulation: Weighing and blending of ingredients (A.I. &
adjuvants)  + liquid binder  screen the damp mass (Sieve 6-8)
 dry  size the granules (Sieve 12-20)  + lubricant and blend
compress
 Fillers – lactose and microcrystalline cellulose
 Binder – to facilitate adhesion of powder particles.
Starch, povidone, methylcellulose.
 Flavorant and colorant are added to binder.
 Lubricant – to improve the flow of granules from the
hopper to the die; prevent adhesion to the punches
and die during compression; reduce friction between
tablet and die’s wall during tablet ejection and provide
tablet sheen. Calcium and magnesium stearate are
examples.
All-In-One Methods:
1) Fluid-bed Process – fluid-bed granulator
which performs the blending, granulating,
drying into 1 continuous process
2) Microwave Vacuum Process – powder mix
is mixed, wetted, agglomerated and dried
using microwave
 Dry Granulation – the powder mixture is compacted to large
pieces and broken down or sized into granules
 Active ingredient or diluent must have cohesive
properties.
 Advantages: For materials that are degraded by
moisture or by elevated temperature during drying
 Steps in Dry Granulation: Weighing & blending powder
mix  slugging  sizing + lubricant  compression
 Tableting machine – compress tablet formulation
within a steel die cavity by the pressure exerted by the
movement of the two steel punches (upper and
lower).
 Imperfections of tablets:
a) a)Laminations – horizontal striations
b) Tablet capping – the top of tablet
separates from the whole
c) Tablet splitting
 Reasons:
a) particles has no time to bond due to
fast high speed production
b) air is entrapped during direct
compression
c) punches not clean
d) aging
Page 2 of 3
 Direct Compression – appropriate for chemicals with flowing and
cohesive properties
 Tablet Deduster – to remove traces of loose powder
adhering to the tablets following compression.
 Tablets are coated:
1) to protect from air and/or humidity
2) mask the taste
3) provide characteristics of drug release
4) to provide aesthetics or distinction to the product
 Sugarcoating – tedious, time-consuming and needs
expertise of qualified technician and the product
doubles the size and wt.
 Film coating – provides a thin, skin-tight coating of a
plastic material over the compressed tablet.
b) more uniform coating
c) uses less coating material resulting to
lighter, smaller and easy to swallow
tablets
d) less expensive to package and ship
 Packaging and Storage:
a) Use tight, light resistant (amber) containers,
if adversely affected by light
b) Store in places of low humidity and protected
from extreme temperature
c) Use desiccant pellet is affected by moisture
Oral administration of solid dosage forms
Lozenges – by compression or molding. Meant to dissolve slowly in the
mouth for localized effect.

 Components: Impact of Changes on Solid dosage forms:

1. Changes in formulation
a) Film former – to produce thin smooth film. Cellulose
acetate phthalate
b) Alloying substance – to provide water solubility/
permeability for body fluids to penetrate through and
make the drug available. Polyethylene glycol 2.
c) Plasticizer – to produce elasticity/flexibility to the
coating & provide durability. Castor oil
 Advantages: Size and wt. almost the same as the
tablet, more resistant to destruction by abrasion,
markings can be embossed on the coating.
a) active ingredients
b) excipients
c) their quantities
d) addition of new excipients
Changes in methods of manufacturing
a) new machineries
b) different steps in manufacturing
c) different in process controls, tests or assay methods
d) production of different batch sizes
e) use of different product reprocessing procedures
f) suse of different manufacturing sites

 Enteric coating – maybe accomplished through coating

with enough thickness or coating which allow
dissolution at a pH 4.9 or higher. Example is shellac

 Fluid –Bed or Air Suspension Coating – spray coating of

powder, pellets, granules or tablets held in suspension
by a column of air

 Depending where the coating solution come from:

a) Wurster – the bottom of the cylinder

b) Top spray –sprayed downward
c) Tangential – spray techniques – rotary fluid
bed coater

 Top spray – recommended for taste masking, enteric

release and barrier film on tablets.
Bottom spray – for sustained release and enteric
release
Tangential – layering coating, sustained and enteric
releases
 Compression Coating – the coating material
(granulation or powder form) is compressed into the
tablet core.

 Advantages:

a) It is anhydrous process appropriate for

drugs affected by moisture

Page 3 of 3