INTRODUCTION TO DIFFERENT
DOSAGE FORMS
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Ms. Shubhangi V. Shekade
M. Pharm (Pharmaceutics)
Drug
Drugmaybedefinedasan
agent or substance,
intendedforuseinthe
diagnosis, mitigation,
treatment, cure or
preventionofdiseasein
humanbeingsoranimals.
Drugs are rarely
administeredintheiroriginal
orcrudeforms.Theyare
administeredindifferent
dosageformsbyconverting
them into suitable
formulations.
Crude Drugs
•Drug ?
•International nonproprietary names (INN, „generic“ names)
•Direct clinical use of the active drug substances is rare: Why??
•API handlingand Accuratedosingcan be difficult or impossible
(e.g., potent drugs: low mg and g doses)
•API administrationcan be impractical/unfeasible because of
size, shape, smell/odour, taste and low activity.
•Some API are chemically unstable in light, moisture, O
2
•API can be degradedat the site of administration (e.g., low pH
in stomach).
•API may cause local irritations or injurywhen they are present
at high concentrations at the site of administration.
•Administration of active substance would mean to have no
chance for modification (improvement) of its PK
(Pharmacokinetic)profile
DRUG/ACTIVEDRUGSUBSTANCES/API
DRUG/ACTIVEDRUGSUBSTANCES/API
Drug:-(active pharmaceutical ingredient -API)
chemical compound intended for used in
diagnosis, treatment or prevention of diseases.
Excipients:-
(inactive pharmaceutical ingredients)
Technological, biopharmaceutical and/or
stability reasons.
Diluents/fillers, binders, lubricants,
disintegrants, coatings, preservants and
stabilizers, colorants and flavourings
dosageform:-
Drug+excipients
1.To provide for the safe and convenient delivery of accurate dosage
Examples: Tablets, Capsules, syrups
2.For the protection of a drug substance from the destructive influence of
atmospheric oxygen or moisture.
Examples: coated tablets, sealed ampules
3.For the protection of a drug substance from the destructive influence of
gastric acid after oral administration.
Example: enteric coated tablets
4.To conceal the bitter taste, salty obnoxious or odor of a drug substance.
Examples: Capsules, coated tablets, flavored syrups
Needofdosageforms:overcomingthe
difficulties
The majority of drug substances are administered in manufacturing amounts,
much too small to be weighed on anything but a sensitive analytical balance.
Example: How can a layman accurately obtain 325 mg or 5 gr of aspirin found
in common aspirin tablets from bulk supply of aspirin?
Examples Of Drugs with Low Usual doses
Ferroussulfate 300mg Hematinic
Cimetidine 300mg Antiulcer
Amoxicillin 250mg Antibacterial
PropoxypheneHCl 65mg Analgesic
Phenobarbital 30mg Sedative
Diphenhydramine HCl 25mg Antihistamine
Morphinesulfate 10mg Narcotic
Analgesic
Cochicine 0.5mg Goutsuppressant
Nitroglycerin 0.4mg Antianginal
Digoxin 0.25mg Cardiotonic
EthinylEstradiol 0.05mg Estrogen
Needofdosageforms:overcomingthe
difficulties
5.To provide liquid preparations of substances that are either
insoluble or unstable in the desired vehicle.
Example: suspension
6.To provide liquid dosage forms of substances soluble in desired
vehicle.
Example: solution
7.To provide extended drug action through controlled release
mechanisms
Examples: controlled release tablets, capsules, suspensions
8.To provide optional drug action from topical
administration sites
Examples: ointments, creams, ophthalmic, ear and nasal preparations
Needofdosageforms:overcomingthe
difficulties
9.To provide for insertion of a drug into one of the body’s
orifices
Examples: rectal and vaginal suppositories
10.Toprovidefor the placement of drugs
withinbody tissues.
Examples: Implants
11.Toprovidefortheoptimaldrugactionthrough
inhalationtherapy.
Examples: inhalants andinhalations
12.Inaddition,manydosageformspermiteaseofdrug
identificationthroughdistinctivenessofcolor,shape,or
identifyingmarkings
Needofdosageforms:overcomingthe
difficulties
They are classified accordingto:
2.Physical form
Solid
Semisolid
Liquid
Gases
1.Route of administration
Oral
Topical
Transdermal
Parenteral
Inhalation
Buccal & sublingual
Ophthalmic
Otic
Rectal
Vaginal
TYPES OF DOSAGEFORMS
Classification acc.to physical
form
Solid dosage
forms
Unit dosage
forms
Tablets
Capsule
Pills
Bulk
Internal
Fine powders &
granules
External
Dusting powders
Insufflations
Dentifrice
Snuffs
Ear powders
Liquid dosage
forms
Biphasic
Emulsion
Suspension
Monophasic
Internal
External
Syrups
Elixirs
Linctus
Drops
Liniments
Lotions
Gargles
Throat paints
Mouth washes
Sprays
Eye lotions
Eye drops
Nasal drops
Semi solid dosage
forms
Internal
External
Suppositories
Pessaries
Ointment
Creams
pastes
Jellies
Gaseous
dosage
form
Inhaler
aerosols
I) Oral dosage
forms:
1-Tablet:
A tablet is a hard, compressed medication in round, oval or square
shape.
The excipients include:
(flowaids)andlubricantstoensureefficient-Binders,glidants
-Disintegrants to ensure that the tablet breaks up in the digestive tract.
-Sweetenersor flavoursto maskthe tasteof
bad-tastingactive ingredients.
-Pigments to make uncoated tablets visually attractive.
.
8
1-Tablet(Cont.)
A coating may be applied to:
1-hide the taste of the tablet's components.
2-make the tablet smoother and easier to
swallow .
3-make it more resistant to the environment.
4-extending its shelf life.
9
2-Buccal and
sublingual tablet:
-Sublingualandbuccalmedicationsareadministeredbyplacing
theminthemouth,eitherunderthetongue(sublingual)or
betweenthegumandthecheek(buccal).
-Themedicationsdissolverapidlyandareabsorbedthroughthe
mucousmembranesofthemouth,wheretheyenterintothe
bloodstream.
-Avoid the acid and enzymatic environment of the stomach and
the drug metabolizing enzymes of the liver.
-Examples of drugs administered by this route: e.g. vasodilators,
steroidal hormones.
4-Chewable
tablet:
-
-
They are tablets that chewed prior to swallowing.
They are designed for administration to children e.g.
vitamin products.
vinaygupta
Dosage forms (Tablet) for oral
administration
Generations of
dosage forms
–1
st gen.
conventional
(unmodified)
release of API
–2
nd gen.
controlled
release of API
(CR)
Conventional vs. controlled
release forms
I. Gen.–disintegration of the dosage form and
dissolution of API is spontaneous process;
– drug absorption and distribution is based only on
physico-chemical properties of API
II. Gen. The release of API is under control of the
drug delivery system (temporal control)
–
–
–Advantages:
Avoids fluctuations of plasma drug concentration better
safety and efficacy
Decreased frequency of drug administration (often once daily
admin) better compliance
Sustained release (SR) –release of the initial API dose
& further prolonged release
Controlled release (CR) –properly controlled (Zero
order) release ofAPI
15
16
5-Capsule:
A capsule is a medication in a gelatin container.
-Advantage: mask the unpleasant taste of its contents.
-The two main types of capsules are:
1.hard-shelledcapsules, whichare
normally used for dry, powdered ingredients,
2.soft-shelled capsules, primarily used for oils and for
active ingredients that are dissolved or suspended in
oil.
Soft gelatincapsule
Hard gelatincapsule
Spansules
17
8-Dental Cones:
- A tabletformintendedtobe
placed inthe empty socket
following a tooth local, formultiplicationof
bacteriaassociatedwithtoothpathogenic
extractions.
maycontainanantibioticor-Thecones
antiseptic.
9-Pills:
-Pillsareoraldosageformswhichconsistofspherical
moremedicaments
-
massespreparedfromoneor
incorporated with inert excipients.
Pills are now rarely used.
11-Powder
(Oral):
There are two kinds of powder intended for internal use.
1-BulkPowdersaremultidosepreparationsconsistingofsolid,
loose,dryparticlesofvaryingdegreesoffineness.Theycontain
oneormoreactiveingredients,withorwithoutexcipientsand,if
necessary,coloringmatterandflavoringsubstances.
-usuallycontainnon-potentmedicamentssuchasantacidssince
thepatientmeasuresadosebyvolumeusinga5mlmedicine
spoon.Thepowderisthenusuallydispersedinwateror,inthe
caseofeffervescentpowders,dissolvedbeforetaking.
2-Divided Powders are single-dose presentations of powder ( for
example, a small sachet) that are intended to be issued to the
patient as such, to be taken in or withwater.
13-Liquidpreparations:
a.Oral solution:
Oral solutions are clear Liquid preparations for oral use containing
one or more active ingredients dissolved in a suitable vehicle.
b.Oral emulsion:
Oralemulsions are stabilized oil-in-water
dispersions,eitheror both phases of which may contain
dissolved solids.
c.Oral suspension:
-Oral suspensions are Liquid preparations for oral use containing
one or more active ingredients suspended in a suitable vehicle.
-Oral suspensions may show a sediment which is readily
dispersed on shaking to give a uniform suspension which
remains sufficiently stable to enable the correct dose to be
delivered.
13-Liquid preparations
(Cont.):
d-Syrup:
-
-
It is a concentrated aqueous solution of a sugar, usually
sucrose.
Flavored syrups are a convenient form of masking
disagreeable tastes.
e-Elixir:
-It is pleasantly flavored clear liquid oral preparation of potent or
nauseous drugs.
-The vehicle may contain a high proportion of ethanol or sucrose
together with antimicrobial preservatives which confers the
stability of the preparation.
13-Liquid preparations
(Cont.):
f-Linctuses:
-Linctuses are viscous, liquid oral preparations that are usually prescribed for
the relief of cough.
-They usually contain a high proportion of syrup and glycerol which have a
demulcent effect on the membranes of the throat.
-The dose volume is small (5ml) and, to prolong the demulcent action, they
should be taken undiluted.
g-Oral drops:
OraldropsareLiquidpreparationsfororalusethatareintendedtobe
administeredinsmallvolumeswiththeaidofasuitablemeasuringdevice.
Theymaybesolutions,suspensionsoremulsions.
13-Liquidpreparations:
h-Gargles:
-
-They are aqueous solutions used in the
prevention or treatment of throat infections.
Usually they are prepared in a concentrated
solution with directions for the patientto
dilute with warm water before use.
i-Mouthwashes:
These are similar to gargles but are used for
oral hygiene and to treat infections of the
mouth.
II) Topical dosageforms:
1-Ointments:
-Ointmentsaresemi-solid,greasy
preparationsfor application to the skin, rectum or
nasal mucosa.
-The base is usually anhydrous and immiscible with skin
secretions.
-Ointments may be used as emollients or to apply
suspended or dissolved medicaments to the skin.
Topical dosage forms
(Cont.):
2-Creams:
-
-
Creams are semi-solid emulsions, that is mixtures of oil and water.
They are divided into two types:
A-oil-in-water(O/W)creams:whicharecomposedofsmalldropletsof
oildispersedinacontinuousaqueousphase.
Oil-in-watercreamsaremorecomfortableandcosmeticallyacceptableas
theyarelessgreasyandmoreeasilywashedoffusingwater.
B-water-in-oil(W/O)creams:whicharecomposedofsmalldropletsof
waterdispersedinacontinuousoilyphase.
Water-in-oilcreamsaremoredifficulttohandlebutmanydrugswhichare
incorporatedintocreamsarehydrophobicandwillbereleasedmore
readilyfromawater-in-oilcreamthananoil-in-watercream.
Water-in-oilcreamsarealsomoremoisturisingastheyprovideanoily
barrierwhichreduceswaterlossfromthestratumcorneum,the
outermostlayeroftheskin.
30
Topical dosage forms
(Cont.):
3-Gels (Jellies):
-Gelsaresemisolidsysteminwhichaliquidphaseisconstrainedwithina3-
Dpolymericmatrix(consistingofnaturalorsyntheticgum)havingahigh
degreeofphysicalorchemicalcross-linking.
-They are used for medication, lubrication and some miscellaneous
applications like carrier for spermicidal agents to be used intra vaginally .
4-Poultice:
Itissoft,viscous,pastypreparationforexternaluse.Theyareappliedtoskin
whiletheyarehot.Poulticemustretainheatforaconsiderabletimebecause
theyareintendedtosupplywarmthtoinflamedpartsofbody.
E.g.Kaolinpoultice(B.P.C.)
Topical dosage forms(Cont.):
5-Pastes:
-Pastes are basically ointments into which a high percentage of insoluble solid
has been added
-The extraordinary amount of particulate matter stiffens the system.
-Pastesare less penetrating and less macerating
and less heatingthan ointment.
-Pastes make particularly good protective barrier when placed on the skin, the
solid they contain can absorb and thereby neutralize certain noxious chemicals
before they ever reach the skin.
-Likeointments,pasteformsanunbrokenrelativelywater–impermeablefilm
unlikeointmentsthefilmisopaqueandthereforecanbeusedasaneffective
sunblockaccordingly.
-Pastes are less greasy because of the absorption of the fluid hydrocarbon
fraction to the particulates.
Topical dosage forms
(Cont.):
There are two types ofpaste:
a)Fatty pastes (e.g: leaser's paste).
b)Non greasy pastes (e g: -bassorinpaste).
6-Dustingpowders:
-These are free flowing very fine powders for external
use.
-Not for use on open wounds unless the powders
are sterilized.
40
Topical dosage forms
(Cont.):
7-Transdermal patch:
-A transdermal patch or skin patch is a medicated adhesive patch
that is placed on the skin to deliver a specific dose of medication
through the skin and into the bloodstream.
-Anadvantageofatransdermaldrugdeliveryrouteoverothertypes
suchasoral,topical,etcisthatitprovidesacontrolledreleaseof
themedicamentintothepatient.
-The first commercially available patch was scopolamine for motion
sickness.
41
Topical dosage forms(Cont.):
8-Plasters:
-Plastersaresolidorsemisolidmassesadheretothe
skinwhenspreaduponcottonfeltlineormuslinasa
backingmaterialandtheyaremainlyusedto,
A-Afford protection and mechanical support.
B-Furnish an occlusive and macerating action.
C-Bring medication into close contact with the surface
of the skin.
42
Topical dosage forms(Cont.):
9-Liniments:
-Liniments are fluid, semi-fluid or, occasionally, semi-
solid preparations intended for application to the skin.
-They may be alcoholic or oily solutions or emulsions.
-Most are massaged into the skin (e.g. counter-
irritant).
-Liniments should not be applied to broken skin.
43
Topical dosage forms(Cont.):
10-Lotions:
Thesearefluidpreparations(aqueous)
forexternal application without friction.
They are either dabbed on the skin or applied
on a suitable dressing and covered with a
waterproof dressing to reduce evaporation.
Topical dosage forms(Cont.):
11-Collodion:
inetheroracetone,Collodionisasolutionofnitrocellulose
sometimes with the addition of alcohols.
-Its generic name is pyroxylinsolution.
-It is highlyflammable.
-As the solvent evaporates, it dries to a celluloid-likefilm.
-CompoundWartRemoverconsistsofaceticacidandsalicylicacid
inanacetonecollodionbaseusedinTreatmentofwartsby
keratolysis.38
Topical dosage forms(Cont.):
applicationtotheskinor
12-Paints:
- Paintsare
liquidsfor mucous
membranes.
-Skinpaintscontainvolatilesolventthatevaporates
quickly to leave a dry resinous film of medicament.
-Throatpaintsaremoreviscousduetoahighcontent
ofglycerol,designedtoprolongcontactofthe
medicament with the affected site.
39
Topical dosage forms(Cont.):
13-Pressurized dispensers (aerosolsprays):
-Several different types of pharmaceutical product may be
packaged in pressurized dispensers, known as aerosols.
-Surface sprays produce droplets of 100 um diameter or
greater.
-May be used as surface disinfectants, wound or burn dressing,
relieve irritation of bites.
-Spray-on dusting powders are also available from pressurized
containers.
Rectal dosageforms:
2-Enema:
An enema is the procedure of introducing liquids into the rectum
and colon via the anus.
Types of enema:
1-Evacuantenema:usedasabowelstimulanttotreat
constipation. E.g. soft soap enema & Mgso
4enema
-The volumeof evacuantenemas may reach up to 2liters.
before-Theyshouldbewarmedtobodytemperature
administration.
Rectal dosage forms
(Cont.):
2-Retentionenema:
-
-
Their volume does not exceed 100 ml.
No warming needed.
-May exert:
A- Localeffect:e.g.a barium enema is used
as a contrast substance in the radiological imaging of the bowel.
B-Systemic effect:
e.g.theadministrationofsubstancesintothebloodstream.This
maybedoneinsituationswhereitisimpossibletodelivera
medicationbymouth,suchasantiemetics.
e.g.nutrientenemawhichcontains carbohydrates,
vitamins & minerals.
IV) Vaginal dosage
forms:
1-Pessary:
-
-
Pessariesaresolidmedicatedpreparationsdesignedfor
insertion into the vagina where they melt or dissolve.
There are three types:
A-Moulded pessaries: they are cone shaped and prepared in a
similar way to moulded suppositories.
B-Compressed pessaries: made in a variety of shapes and are
prepared by compression in a similar manner to oral tablets.
C-Vaginal capsules: are similar to soft gelatin oral Capsules
differing only in size and shape.
Vaginal dosage
forms:
2-Vaginal ring:
Vaginal ringsare'doughnut-shaped' polymeric
drugdelivery devices
designed to provide controlled release of drugs to the vagina over
extended periods of time.
Several vaginal ring products are currently available, including:
Femring :
a low-dose estradiol-acetate releasing ring, manufactured from
silicone elastomer, for the relief of hot flashes and vaginal atrophy
associated with menopause.
NuvaRing:
a low-dose contraceptive vaginal ring, releasing progesterone and
estrogen.
45
52
Vaginal dosage forms
(Cont.):
3-Douche:
A douche is a device used to introduce a stream
of water into the body cavity for medical or
hygienic reasons.
53
Vaginal dosage forms
(Cont.):
4-Intrauterine device:
-It is a birth control device placed in the uterus, also known as an IUD or a
coil.
-The IUD is the world's most widely used method of reversible birth
control.
-The device has to be fitted inside or removed from the uterus by a doctor .
-It remains in place the entire time pregnancy is not desired. Depending on
the type, a single IUD is approved for 5 to 10 years use.
-There are two broad categories of intrauterine contraceptive devices: A-
inert and copper-based devices.
B-hormonally-based devices that work by releasing a progesterone.
54
V) Parenteral dosage
forms:
Aninjectionisaninfusionmethodofputtingliquidinto
thebody,usuallywithahollowneedleandasyringe
whichispiercedthroughtheskintoasufficientdepth
forthematerialtobeforcedintothebody.
There are several methods of injection, including: 1-An
intravenous injection:
It is a liquid administered directly into the bloodstream
via a vein.
It is advantageous when a rapid onset of action is
needed.
55
Parenteral dosage
forms:
2-Intramuscular injection:
-It is the injection of a substance directly into a muscle.
-Many vaccines are administered intramuscularly.
-Depending on the chemical properties of the drug, the
medication may either be absorbed fairly quickly or more
gradually.
-Intramuscular injections are often given in the deltoid, vastus
lateralis, ventrogluteal and dorsogluteal muscles.
56
Parenteral dosage
forms:
3-Subcutaneous injection:
Subcutaneous injections are given by injecting
a fluid into the sub cutis, thelayer of skin directly
below the dermis and epidermis.
Subcutaneous injections are highly effective in
administering vaccines and such medications as
insulin.
59
Inhaled dosage forms
(Cont.):
2Nebulizer or (atomizer):
A nebulizer is a device used to administer medication to people in forms of
a liquid mist to the airways.
-It is commonly used in treating asthma, and other respiratory diseases.
-It pumps air or oxygen through a liquid medicine to turn it into a vapor,
which is then inhaled by the patient.
-As a general rule, doctors generally prefer to prescribe inhalers for their
patients, because:
1-These are cheaper 2-more portable
3-carry less risk of side effects.
Nebulizers, for that reason, are usually reserved only for serious cases of
respiratory disease, or severe attacks.
60
VII) Ophthalmic dosage
forms:
1-Eye drops:
Eye dropsare saline-containingdropsused as a
vehicleto administer medication in the eye.
maycontainsteroids,
inthemandareonly
Dependingontheconditionbeingtreated,they
antihistamines or topical anesthetics.
Eye dropssometimes do not
havemedications lubricating and
tear-replacing solutions.
2-Ophthalmic ointment & gel:
These are sterile semi-solid
Preparations intended for application
To the conjunctiva or eyelid margin.
61
VIII) Otic dosage
forms:
-Ear drops are solutions, suspensions or emulsions of
drugs that are instilled into the ear with a dropper.
It is used to treat or prevent ear infections,
especially infections of the outer ear and ear
canal.
1-Eardrops:
-
IX) Nasal dosage
forms:
1-Nasal Drops and Sprays:
Drugs in solution may be instilled into the nose from a
dropper or from a plastic squeeze bottle.
The drug may have a local effect, e.g. antihistamine,
decongestant.
Alternatively the drug may be absorbed through the
nasal mucosa to exert a systemic effect.
The use of oily nasal drops should be avoided
because of possible damage to the cilia of the nasal
mucosa.56
Solid dosage forms
Solid dosage forms
Tablets Pills
Dusting Powders
Capsules
Granules
Medical Dusting
Powders
Medical Dusting powders are used to
increase superficial condition of skin.
These are not applied on wounds, burns etc
Medical dusting powders must be free from
dangerous pathogenic micro-organism.
Surgical Dusting Powders
Surgical dusting powders are used in body
cavities and also on major wounds like as
burns etc.
They should be sterilized before use.
They are mainly used for their antiseptic,
absorbent action.
Effervescent Granules
Effervescent granules are meant for internal use.
Theycontainedmedicamentsmixedwithcitricacid,
tartaricacid&sodiumbicarbonates,sometime
saccharinorsucrosemaybeaddedforsweetening
taste.
Before,administrationdesiredquantityofgranulesare
dissolvedinwater,theacid&bicarbonatereactswith
eachothertoproduceeffervescence.
Effervescentgranulesarepreparedbytwomethods,
namelyas,I)Heatmethod,II)Wetmethod
Heat method
A large porcelain or stainless steel evaporating dish is placed over
the boiling water bath.
The dish must be sufficiently hot (generally heating takes place for 1
–5 min.) before transferring the powders into it, to ensure rapid
liberation of water of crystallization from citric acid.
If heating of the dish is delayed then the powder which is added to
it, will heat up slowly & liberated water of crystallization will also be
liberated simultaneously.
As a result, sufficient water will not be available to make a coherent
mass.
This coherent mass will pass through the sieve to obtained suitable
size of granules, dry it in oven at 60
0
c then packed in air tight
container.
Wet method
In this methods all the ingredients are mixed thoroughly
This powders mixture make moistened with non –
aqueous vehicle (e.g. alcohol), to prepare a coherent
mass which is then passed through sieve no 8 to
obtained suitable granules.
Then dried in oven at 60
0
c. The dried granules are again
passed through the sieve to break the lumps which may
be formed during drying.
The dried granules are packed in air tight container.
Tablets
These are solid dosage forms of medicaments which are
prepared by moulding or by compression with or without
Excipients.
The tablets can be prepared by two methods namely as
a
I) Dry granulation, II) Wet Granulation
Capsule
Capsules are solid unit dosage forms in which one or more
medicaments enclosed within a shell.
Capsules mainly divided in to two parts namely as –
I) Body (Longest part of capsule shell), II) Cap(Smallest part
of capsule shell)
The capsule are generally prepared by gelatin.
Depending on their formulation, two types of gelatin are used
namely as –I) Hard gelatin, II) Soft gelatin.
Body
Cap
Pills
These are small, rounded solid dosage forms containing
medicaments intended for oral use.
The medicaments are mixed with excipients to forms a
firms plastic mass.
The mass is rolled to uniform pill pipe, which cut into
numbers of uniform pills. The pills are spherical in
shape & produced by rolling them under wooden pill
rounder.
Sometimes pills are coated with varnish, gold leaf, etc to
improve finish, unpleasant taste & stability.
Now a days pills are outdated preparations because of
number of disadvantages such as -
Disintegration time of pill is uncertain means freshly
prepared pills are disintegrates readily rather than old
dried pills.
It is difficult to prepare pills of uniform size & weight.
Monophasic liquid dosage forms are represent by true or
colloidal solution.
The component of the solution which is present in a large
quantity is known as “SOLVENT” where as the component
present in small quantity is termed as “SOLUTE”.
A solution is homogenous because the solute is an ionic or
molecular forms of subdivision.
In case of colloidal solutions, the solutes are present as
aggregates although they cannot be seen by necked eye or
ordinarymicroscope.
It is sub classified as –
I) Internal Use, II) External use
Monophasic Liquid Dosage
forms
Internal Use
External Use
Syrup
Elixirs
Linctuses
Drops
Liniments
Lotions
Gargles
Mouth Wash
Throat paints
sprays
Inhalations
Nasal drops
Eye drops
Eye lotions
Ear drops
Monophasic liquid dosage forms
for Internal Use
Syru
p
Itisaconcentratedorsaturatedsolutionsofsucrosein
purifiedwater.
Theconcentrationofsucroseis66.7%w/w&duetothat
itisaviscouspreparations.
Thesyrupwhichcontainsmedicalsubstancecalledasa
medicatedsyrup&thosecontainingaromaticorflavored
substanceknownasaflavoredsyrup.
Importance of syrup
Itretardsoxidationbecauseitspartlyhydrolyzedinto
reducingsugar.
Itpreventsdecompositionofmanyvegetablesubstance
becauseitshavehighosmoticpressurewhichprevent
thegrowthofbacteria.
Theyarepalatableduesweettaste.
Linctuse
s
Theseareviscousliquidpreparations
that’sareusedforthetreatmentof
cough.
Theycontainmedicamentswhich
have demulcent, sedative,
expectorantaction.
Theyaretakeninsmalldoseswithout
dilutingwithwatertohaveprolonged
effectofmedicines.
Simplesyrupisusedasavehiclefor
mostofthelinctuses.
Tolusyrupispreferredincertain
casesbecauseofitsaromaticodour&
flavour.Moreoverithaveamild
Drop
s
These are liquid preparations meant for oral
administration.
The oil soluble vitamins, such as vitamin A & D
concentrates in fish –liver oil are presented as drops for
administration.
Since these preparations contain potent medicaments,
the dose must be measured accurately
The following two methods are commonly used for this
purpose.
Use of a dropper which is accurately graduated in
fractions of a milliliters.
Use of a pre –calibrated dropper.
Monophasic liquid dosage
forms for External use
Liniments
Liniments are liquid or semi-liquid
preparations meant for external application to
the skin.
They are usually applied to the skin with
friction & rubbing of the skin.
Are usually alcoholic and oily liquid
preparations (monophasic) or emulsion
(biphasic).
Alcoholic liniments are used generally for
their rubefacient and counterirritant effects.
Such liniments penetrate the skin more
readily than do those with an oil base.
The oily liniments are milder in their action
and may function solely as protective
coatings
Liniments should not be applied to skin that
Throat paints
Throat paints are viscous liquid
preparations used for mouth
and throat infections
Glycerin is commonly used as a
base because being viscous it
adheres to mucous membrane
for long period and it possess a
sweet taste.
Nasal drops
Drugs in solution may be instilled into the nose from a dropper or
from a plastic squeeze bottle.
The drug may have a local effect, e.g. antihistamine, decongestant.
Alternatively the drug may be absorbed through the nasal mucosa
to exert a systemic effect.
The use of oily nasal drops should be avoided because of possible
damage to the cilia of the nasal mucosa & if it is used for long
period may reach the lungs & cause lipoid pneumonia.
To avoid that Nasal drops are prepared so that they are similar in
many respects to nasal secretions, so that normal ciliary action is
maintained thus aqueous nasal solutions usually are isotonic and
slightly buffered to maintain a pH of 5.5 to 6.5.
Eye drops
Sterile, aqueous/oily solutions or suspensions intended for
instillation in eye sac.
Eye drops may contain buffers, stabilizing agents, dispersing
agents, solubilising agents, anti-oxidants & agents required for
tonicity/ viscosity adjustment
Single dose container should not contain anti-microbial
preservative.
In case of multi dose container a dropper should be supplied with it
for administration. Maximum size of such containers is 10 ml.
Eye lotions
These are the aqueous solutions used for washing the eyes.
These are supplied in concentrated forms & are required to diluted
with warm water immediately before use.
They should be free from foreign particles to avoids irritation to the
eye.
They are required to prepared fresh & should not be stored for
more than two days to avoid microbial contaminations.
Emulsion
Emulsionisabiphasicliquidpreparationscontainingtwo
immiscibleliquid(ContinuousPhase&dispersedphase)made
missicible.
Theliquidwhichisconvertedintominuteglobulesiscalledas
dispersedphase&theliquidinwhichtheglobulesaredispersedis
calledthecontinuousphase
dispersed phase
continuous phase
Two Immiscible Liquids
Dispersed Phase
(Internal
phase)
Continuous Phase
(External phase)
An emulsion is a thermodynamically unstable system consisting of
at least two immiscible liquid phases one of which is dispersed as
globules in the other liquid phase stabilized by a third substance
called emulsifying agent.
The globule size in emulsion varies from 0.25 to 25 µm.
Examples for emulsions:-milk, rubber latex, crude oiletc.
A.: Two immiscible liquids not emulsified
B. An emulsion of phase B dispersed in Phase A
C. Unstable emulsion slowly separates.
D. The emulsifying agent ( black film) places it self on the interface
between phase A and phase B and stabilizes the emulsion.
Types of emulsions
Simple type
Water in oil (w/o)
Oil in water (o/w)
Depending on globule size
Micro emulsion
Fine emulsion
Special type
Multiple emulsion (w/o/w, o/w/o)
Water in oil (w/o)
In this types of emulsion water is dispersed phase& oil is
continuous phase
w/o types of emulsion generally meant for External use.
Examples are butter, lotions, creams etc.
In rare case they are used internally.
Water is dispersed
phase
Oil is continuous phase
Oil in water (o/w)
In this types of emulsion oil is dispersed phase& water is
continuous phase
o/w types of emulsion meant for both Internal use & External use.
Examples for internal use are Vitamin A in corn oil, liquid paraffin in
water etc.
Examples for External use are Benzyl benzonate emulsion.
Oil is dispersed phase
water is continuous phase
Fine emulsion
Normallythesehaveamilkyappearance.
Theglobulesizerangesfrom0.25to25µm.
Multiple emulsion
These are emulsion with in emulsion & designated as w/o/w or
o/w/o.
The drugs that is incorporated in the innermost phase must cross
two phase boundaries before getting absorbed.
It is generally used in oral sustained release or intramuscular
therapy.
Identification tests
Dilution test
Conductivity test
Dye test
Fluorescence test
Cobalt chloride test
Filter paper test
Dilution test
Theemulsionisdilutedwithwater,afterdilutionemulsionremain
stablethenitissaidtobeo/wtypeofemulsionbecausewaterisin
continuousphase.Ifemulsionisbreakafterdilutionwithwaterthen
itissaidtobew/otypeofemulsion.
Add drops of water
Water distribute
Uniformly
Add drops of water
O/W Emulsion W/O Emulsion
Conductivity test
Conductivitytestcanbeperformedbydippingapairofelectrode
connectingwithlowvoltagebulb&passthecurrent.
Ifbulbglowsthenitissaidtobeo/wtypeofemulsionbecause
waterisincontinuousphase&itisgoodconductorofelectricity.
Ifbulbdoesn'tglowthenitissaidtobew/otypeofemulsion
becauseoilisbadconductorfelectricity.
Bulb glows with O/W
Emulsion
Emulsion
Bulb doesn’t glow with W/O
Dye test
Oil soluble Scarlet red dye is mixed with emulsion.
Place a drop of emulsion on microscopic slide cover it with cover
slip & examine under microscope.
If disperse globules appears red & ground is colourless then it said
to be o/w type of emulsion because water is present in continuous
phase.
If reserve condition occurs (If disperse globules appears colourless
& ground is red colour then it said to be w/o type of emulsion
because oil is present in continuous phase.)
Oil is dispersed
phase
Water is
continuous
phase
Water is disperse
phase
Oil is continuous
phase
Fluorescence test
Certainfixedoilpossesthephysicalpropertiesoffluorescinginthe
presenceofultravioletradiations.
Ifexamineundermicroscopegroundisfluorescencethenitsaidto
bew/otypeofemulsionbecauseoilispresentincontinuousphase.
Ifexamineundermicroscopedropletisfluorescencethenitsaidto
beo/wtypeofemulsionbecauseoilispresentindispersephase.
Creaming test
Thedirectionofcreamingidentifiestheemulsiontype,ifthe
densitiesofaqueousandoilphasesareknown.
Water-in-oilemulsionsnormallycreamdownwardasoilisusually
lessdensethanwater.
Oil-in-wateremulsionsnormallycreamupwards.
Cobalt chloride test
Pourtheemulsiononfilterpaperthenitissoakedincobaltchloride
solutions&allowedtodryturnsfrombluetopink.
Thenthisemulsionissaidtobeo/wtypeofemulsion.
Thistestmayfailifemulsionunstableorbreaksinpresenceof
electrolyte.
Filter paper test
Thistestisbasedonthefactthatano/wemulsionwillspreadout
rapidlywhendroppedontofilterpaper.
Incontrast,aw/oemulsionwillmigrateonlyslowly.Thismethod
shouldnotbeusedforhighlyviscouscreams.
Advantage of suspension
Suspension can improve chemical stability of certain drug. E.g.
Procaine penicillin
Drug in suspension exhibits higher rate of bioavailability than other
dosage forms.
Solution > Suspension > Capsule > Compressed Tablet >
Coated tablet
Duration and onset of action can be controlled. E.g. Protamine
Zinc-Insulin suspension.
Suspension can mask the unpleasant/ bitter taste of drug. E.g.
Chloramphenicol
Ideal qualities of good
suspension
It should settle slowly & easily re –dispersed on shaking
It should readily & evenly pour from container.
It should be chemically inert.
It should not forms hard cake.
It should prevent degradation of drug or to improve stability of
drug.
It should mask the taste of bitter of unpleasant drug.
Difference between flocculated & deflocculated
suspension
Flocculated Suspension Deflocculated suspension
Particles form loose aggregates & forms
network likestructure.
Particle exist as separate entities.
Particles experience attractive forces.Particles experience repulsive forces.
Supernatant liquid is clear. Supernatantliquid is cloudy.
The rate of sediment is high. The rate of sediment is slow.
Sediment is rapidly formed. Sediment is slowly formed.
sediment are looselypacked, hence hard
cake is not formed.
Sediments are closely packed, hence
hard cake is formed.
The sediment is easy to redisperseon
shaking.
Sediment is difficult to redisperse on
shaking. (due to formation of hard cake)
Bioavailabilityis comparatively less. Bioavailability is relatively high.
The suspension is not pleasing in
appearance.
The suspension is pleasing in
appearance.
Semisolid dosage forms
Semisolid dosage forms meant for external application
Semisolid dosage forms subcategorized are as-
I) ointment
II) creams
III) paste
IV) Jellies
V) Suppositories
The suppositories are also included in this category but it is a unit
dosage forms.
Semisolid dosage forms
Disadvantages of oleaginous
bases
Theyaregreasy.
Theyaresticky&aredifficulttoremovebothfromskin&clothing.
Theyretainbodyheatwhichmayproduceanuncomfortablefeeling
ofwarmth.
Theydonothelpintheabsorptionofmedicaments.
Absorption bases
These bases are generally anhydrous substance which have the
property of absorbing considerable quantities of water but still
retaining their ointment like consistency.
The absorption bases are of two type namely as
I) Non emulsified bases
II) Water in oil emulsion
Non emulsified bases absorb water & aqueous solutions producing
w/o emulsion. E.g. Wool fat, wool alcohol, beeswax & cholesterol.
Water in oil emulsions are capable of absorbing more water & have
the properties of non-emulsified bases. E.g. hydrous wool fat (
lanoline)
Water soluble bases
Thesearecommonlyknownasgreaselessointmentbases.
Thewatersolublebasesconsistofwatersolubleingredientssuch
ascarbowaxes(polyethyleneglycolpolymer)
Thecarbowaxesarewatersoluble,non–volatile&inertsubstance.
Selectionofappropriatecarbowaxesisdependontheirmolecular
weight.
creams
These are viscous semisolid emulsions which are meant for
external use.
Cream is divided in to two types namely as
I) Aqueous creams
II) Oily creams
In case of aqueous creams the emulsions are o/w type & it is
relatively non greasy. The emulsifying waxes are anionic, cationic
& non –ionic used. Generally polysorbate, triethanolamine soap
are used as emulsifying agent.
In case of oily creams w/o type & it is relatively greasy. The
emulsifying agent such as wool fat, wool alcohols, beeswax &
calcium soap is used.
The cream should be store in collapsible tube & supplied in well
closed container to prevent evaporation & contamination.
jellies
Jellies are transparent or translucent, non greasy, semi solid
preparations mainly used for external application to skin.
These are also used for lubricating catheters, surgical gloves &
rectal thermometer.
The substance like gelatin, starch, tragacanth, sodium alginate &
cellulose derivatives are used for the formulation of jellies.
Jellies are of three types namely as
Medicated jellies
Lubricating jellies
Miscellaneous jellies
New drug delivery system
Introduction
With the advancement of pharmaceutical sciences, a new concept
have evolved various modern dosage forms & methods of their
administration. Some of the modern dosage forms are
Implants
Films & strips
Liposome drug carriers
Controlled drug delivery modules
Erythrocytes
Nanoparticles
prodrugs
Implants
These are hypodermic tablets are placed under the skin by a minor
surgery in order to release drugs over prolonged periods of time.
Now the magnetically controlled implants have been developed
which can be opened or closed at will in order to release or stop the
drug.
These implants are placed at upper thigh at a depth of 5mm.
These implants are useful in hormone therapy.
Films & strips
Thesearemeantfortopicalapplicationforslowreleaseofdrugover
predeterminedperiodoftime.Films&stripsaremorepopularthese
days.Theyaresubcategorizedintofollowingtypesnamelyas
Zero order release films
Buccal strips
Spray bandages
Zero order release films
Thesearecalledaslaminates&meantfortopicalapplication.E.g.
Nitroglycerinelaminatesarepreparedbymixingpropyleneglycol
withabout1%carbopolresin.ThemixtureisneutralizedwithNaoH
solution&then0.1%ofnitroglycerinisadded.Itisthenplacedin
polythenesheet5*5cm&itsedgesaresealedbyheat.Itisthen
placedonpressuresensitiveadhesivesheetof5.5*5.5cmsothat
itcanbeproperlyadhesivetoskin.Suchlaminatesreleasethedrug
slowlyintocirculationforabout12hours.
Applications
Flourescein isothinocyanate (FITC) nanoparticles have been used
to incorporate cytotoxic agent into tumor cell in cancer
chemotherapy.
Nanoparticles along with biological maker like immunoglobulin can
be used to target the drugs to very specific site.
Prodrugs
The compound which undergo biotransformation before showing
desired pharmacological activity are called prodrugs or proagents.
Prodrugs are generally the ester or amides of parent drugs.
These are useful to improving the stability, solubility, bioavailability
of drugs, masking the unpleasant taste & odour of the parent drug &
reducing the toxicity