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 Quality Standards and Compedial Requirements:
• USP Weight Variation Test: 10 tablets are individually weighed
tongue for rapid drug effect.
and average weight calculated.
• Lozenges or troches – disc-shaped solid forms containing a • Content Uniformity: Dosage units are assayed individually and
medicinal substance in a hard candy or sugar base. Meant to requires that each dosage unit is 85% - 115% of the label claim
dissolve slowly for localized effect or systemic effect (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.
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 • Tablet thickness is measured by a hand gauge. are withdrawn for chemical analysis. Samples must meet the requirement
stated in the monograph.
• Tablet hardness affects its disintegration & drug absorption. The
greater the pressure, the harder the tablet. It should be hard Pooled dissolution testing – samples coming from different batches placed
enough to resist breaking during the normal handling and yet soft in individual dissolution vessel in the apparatus or multiple dosage units in a
enough to disintegrate properly after swallowing. single vessel. This recognizes the concept of batch characteristics.

• 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 3 methods for compressed tablet:
weight loss of not more than 1% of the weight of the tablets being  Wet Granulation: Weighing and blending of ingredients (A.I. &
tested is acceptable. adjuvants)  + liquid binder  screen the damp mass (Sieve 6-8)
 dry  size the granules (Sieve 12-20)  + lubricant and blend
• Tablet Disintegration Test – uses a basket-rack assembly compress
containing 6 open ended transparent tubes held vertically upon a  Fillers – lactose and microcrystalline cellulose
10-mesh stainless steel wire screen.  Binder – to facilitate adhesion of powder particles.
Starch, povidone, methylcellulose.
The basket is raised and lowered in the immersion fluid (water at  Flavorant and colorant are added to binder.
37oC) at a frequency of 29-32 times per minute. Result: the  Lubricant – to improve the flow of granules from the
residue of the tablet on the screen is a soft mass having no hopper to the die; prevent adhesion to the punches
palpable inner core. Disintegration time ranged from 2 mins. to 4 and die during compression; reduce friction between
hours depending upon the monograph. tablet and die’s wall during tablet ejection and provide
tablet sheen. Calcium and magnesium stearate are
For enteric coated tablets, test is done in a simulated gastric fluid
examples.
for 1 hr. No sign of disintegration must be seen. They are
immersed in a simulated intestinal fluid for the time stated in the
All-In-One Methods:
monograph where they disintegrate completely.
1) Fluid-bed Process – fluid-bed granulator
which performs the blending, granulating,
• Tablet dissolution test - Uses:
drying into 1 continuous process
2) Microwave Vacuum Process – powder mix
a. guides formulation and product development
is mixed, wetted, agglomerated and dried
b. performance of manufacturing process can be
using microwave
monitored by it (quality assurance)
c. Consistent results assure bioequivalence from batch
 Dry Granulation – the powder mixture is compacted to large
to batch
pieces and broken down or sized into granules
d. As a requirement for regulatory approval
 Active ingredient or diluent must have cohesive
– Its goal to provide a reasonable prediction or correlation with
properties.
the product’s in vivo bioavailability.
 Advantages: For materials that are degraded by
a) High Solubility and High Permeability – IVIVC moisture or by elevated temperature during drying
b) Low Solubility and High Permeability – IVIVC  Steps in Dry Granulation: Weighing & blending powder
c) High Solubility and Low Permeability – limited IVIVC mix  slugging  sizing + lubricant  compression
d) Low Solubility and Low Permeability – none  Tableting machine – compress tablet formulation
within a steel die cavity by the pressure exerted by the
In (a) IVIVC is expected if the dissolution time is slower then movement of the two steel punches (upper and
gastric emptying time (limiting factor). lower).
 Imperfections of tablets:
• Dissolution Test Apparatus consists of: a) a)Laminations – horizontal striations
b) Tablet capping – the top of tablet
1. variable stirrer motor separates from the whole
2. stainless basket on a stirrer shaft (Apparatus I) or a c) Tablet splitting
paddle as stirrer (Apparatus II)  Reasons:
3. 1-L vessel glass with a cover having the shaft of the a) particles has no time to bond due to
stirrer fitted at the center port, with 3 ports for fast high speed production
samples and 1 port for the thermometer b) air is entrapped during direct
4. Water bath to maintain the temp. of the medium in compression
the vessel c) punches not clean
d) aging
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

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 Direct Compression – appropriate for chemicals with flowing and b) more uniform coating
cohesive properties c) uses less coating material resulting to
 Tablet Deduster – to remove traces of loose powder lighter, smaller and easy to swallow
adhering to the tablets following compression. tablets
 Tablets are coated: d) less expensive to package and ship
 Packaging and Storage:
1) to protect from air and/or humidity
2) mask the taste a) Use tight, light resistant (amber) containers,
3) provide characteristics of drug release if adversely affected by light
4) to provide aesthetics or distinction to the product b) Store in places of low humidity and protected
 Sugarcoating – tedious, time-consuming and needs from extreme temperature
expertise of qualified technician and the product c) Use desiccant pellet is affected by moisture
doubles the size and wt.
Oral administration of solid dosage forms
 Film coating – provides a thin, skin-tight coating of a Lozenges – by compression or molding. Meant to dissolve slowly in the
plastic material over the compressed tablet. 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 a) active ingredients
acetate phthalate b) excipients
c) their quantities
b) Alloying substance – to provide water solubility/ d) addition of new excipients
permeability for body fluids to penetrate through and
make the drug available. Polyethylene glycol 2. Changes in methods of manufacturing
a) new machineries
c) Plasticizer – to produce elasticity/flexibility to the b) different steps in manufacturing
coating & provide durability. Castor oil c) different in process controls, tests or assay methods
d) production of different batch sizes
 Advantages: Size and wt. almost the same as the e) use of different product reprocessing procedures
tablet, more resistant to destruction by abrasion,
f) suse of different manufacturing sites
markings can be embossed on the coating.

 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

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