Pharmaceutical Dosage forms

Dr. Doa’a Bashir

MSCs in Pharmaceutical Sciences
• Pharmaceutics: is the discipline of pharmacy that deals
with the process of turning a new chemical entity (NCE) or
an old drug to a safe and effective medication, also called
the science of dosage form design.
• Active ingredient (API), Drug: is a pharmacological agent
used for diagnosis, treatment and prophylaxis.
• Excipient: is an inactive pharmaceutical ingredient used for
technological, biopharmaceutical or/and stability reasons.
• Dosage form: is a combination of both API and excipient.
• Route of administration: is the path by which a drug is
brought into contact with the body. It depends on the
dosage form of a given drug.
• Dose: is a specified quantity of therapeutic agent to be
taken once or at stated intervals.
Dosage Forms according to Physical form
 Solid Dosage forms
• Tablets
A solid preparation each containing a single dose of one
or more API in addition to a suitable excipient formed by
compression after granulation of powder.
Types of tablets:
1- Disintegrating (conventional/plain): the most common,
intended to be swallowed. Ex: Revanin
2- Chewable: to be disintegrated in the mouth. Ex: Rennie
3- Effervescent: dropped in water before administration,
composed of acid and base and liberate CO2 with water.
4- Sublingual: placed under the tongue, followed by
systemic uptake without 1st pass metabolism.
Ex: Nitroglycerin
5- Buccal: placed in the side of the cheek, followed by
systemic uptake without 1st pass metabolism.
6- Lozenges (Troches): tablets of hardened base or sugar
and water containing API and flavors, intended to be
dissolved slowly in the mouth by the saliva. Ex: Strepsils
7- Pastilles: solid medications intended to be dissolved slowly
in the mouth by the saliva, they are softer than lozenges and
their bases are either glycerol and gelatin or acacia and sugar,
and like lozenges they are not to be swallowed. Ex: Smint
8- Dental cones: tablet form intended to be placed in the
empty socket following a tooth extraction, for preventing the
local multiplication of pathogenic bacteria associated with
tooth extractions. - The cones may contain an antibiotic or
antiseptic.
9- Vaginal Tablets. 10- Implantation tablets: Under skin.
** Pills:
- Originally are spherical masses or round small tablets, and
these now are rarely used.
- Pills can be used as a term expresses tablets and capsules.
- Pills is now mostly used to express oral contraceptives.
Tablets most common defects:
- Capping, Chipping, Laminating: detachment of a part of
the tablet or more than one part from the rest parts.
- Sticking and Picking: attachment of granules of tablet to
the punch of compressor, picking is more specific.
- Hardness variation: crushing strength, if the tablet is too
hard it may not disintegrate in the required time and fail
dissolution test, and if it is too soft it may not be able to
withstand handling.
- Friability: the % of tablet weight loss during packaging,
handling and shipping. Usually measured by fibrilator or
tumbler test (wt. loss is accepted to be <1%).
- Content uniformity: Content of API in the tablet must be
the same as the manufacturer claim (+ 15% is accepted).
• Capsules:
They are unit solid dosage forms consist of gelatin shell
that breaks after been swallowed and releases the drug.
- Types:
1- Hard shell capsule: manufactured
in 2 pieces (cap and body) that fit
together and hold the drug in powder
or granular forms. Ex: Ultracillin, Eazit.

2- Soft shell capsule: manufactured

in one piece with drug in liquid or
semisolid form inside.
Ex: Fat soluble vitamins.
- There are 8 sizes of capsules, and the minimum weight
needed for capsule filling is 100mg.
- Moisture content in the shell of capsule must be 13-16%, if
>16% the capsule will be sticky and soft, and if <13% it will
be brittle.
Defects of Capsules
• Powders:
They are mixture of finely divided drugs or chemicals in
dry form, meant to be used internally (except dusting
powder), can be bulk or divided.
Their size can range from 10mm (very coarse) to 0.1𝜇m
or less (very fine).
- Types of powders:
1- Dusting powder: very fine powder made of talcum and
starch that is locally (externally) applied and has no systemic
effect, used as lubricant, protective, absorbent, antiseptic,
antipruritic and antiperspirant. Ex: Johnson baby powder
2- Effervescent powder: a mixture of acid and base (mainly
citric acid and Na bicarbonate) intended to be dissolved in
water just before use, used to mask the unpleasant taste of
certain medicines. Ex: Eno
3- Douche powder: completely water soluble powder,
intended to be dissolved in water just before use, used as
antiseptic and cleansing agent for body cavities (mainly
Vagina).
4- Dentifrices: agent used along with a toothbrush to clean
and polish the teeth.
5- Insufflation: finely divided powders introduced into body
cavities in the dry form.
Can be packaged in insufflators or in pressurized aerosols.
* Nasal inhalation powder drugs are called sniffing
(Snorting) powders, and they are considered one type of
insufflating powders.

• Granules:
They are powders formulated as aggregates by wet
(Using alcohol) or dry methods.
One example is the effervescent granules (Coli-urinal).
-Main problems of powders:
1- Hygroscopicity: Absorb moisture from air. Ex: Halide salts.
Solution: applied in the granular form, packed in
aluminium foil, addition of light MgO, or addition of
adsorbents.
2- Efflorescence: Crystalline substances lose water during
storage and converted into paste. Ex: Citric acid
Solution: using the anhydrous form, and also the same
solutions for hygroscopicity.
3- Eutexia: Powders liquify (melt) when mixed or triturated
together. Ex: Menthol,Camphor.
Solution: using adsorbent (Starch), or dispensing
separately.
4- Potency: Small amount of drug that is highly effective,
leads to limited precision and accuracy in weighing and
handling.
Solution: adding diluents, or geometric dilution.
5- Incompatibility: 2 salts when triturated together produce
discoloration, deterioration or loss of potency.
Solution: minimum pressure, mixing by tumbling in a jar
or by spatulation but not trituration, or dispense
separately.
6- Explosive mixture: trituration of an oxidizing agent with a
reducing agent can cause them to explode.
Solution: separation, or using a minimum pressure.
• Size Reduction: needed in the preparation of powders
and granules followed by sieving (meshing) and drying (if
needed).
1- Cutting: using sharp knife or scissors,
and using cutter miller for large scale.
Used for leaves and roots.

2- Impaction: using mortar and pestle,

or a roller miller for large scale.
Used for solid materials.
3- Attrition: usually after cutting or impaction.
a) Levigation: wet grinding, using mortar and pestle.
b) Rasping (grating): for wood, using saw mill.
c) Crushing: using pressure, for oily materials.
d) Trituration: using mortar and pestle, or ball mill.
 Semisolid Dosage forms
• Suppositories
Semisolid dosage forms that can be rectal (suppositories) with
size of 2g (adults) & 1g (children) mainly (except glycero-gelatin supp.),
Urethral or Vaginal (pessaries) with size of 5g, and melts at body
temp., They can exert a local (anti-hemorrhoid) or a systemic
effect (NSAIDs).
Consist of a base (vehicle) which can be fatty or water soluble in
addition to one or more API.
* Ideal Base:
- Melts at body temp. - Miscible with API
- Solidifies quickly after melting outside the body.
- Bland (non toxic, non irritant) - stable on storage.
- Withstands handling.
- Easily molded and removed from mold without adhering to its
walls.
1- Fatty Bases:
can be naturally occurring (theobroma oil) or synthetic.
A) Natural, Ex: Theobroma oil (cocoa butter).
Was used for many years, as it was considered as ideal base
for many reasons (advantages):
- Has melting point range of 30-36C, solid at normal room temp.
- Readily liquefies when heated and rapidly solidifies when
cooled.
- Miscible with many active ingredients.
- Bland (non irritant and non toxic).
But recently, this base was replaced by synthetic bases as it
has disadvantages:
- Polymorphic, has 3 polymorphs 𝛼, 𝛽, and 𝛾, only one
polymorph (𝛽) is stable at room temp.
- Need lubricant (soap spirit) as it can adhere to mold walls.
- Relatively low melting point (m.p) and reduced when API is
added (can be solved by adding beeswax).
- Theobroma oil deteriorates on storage by oxidation.
- Can’t be used water-soluble API.
- Expensive.
B) Synthetic fat bases, Ex: Witepsol, Suppocire.
Prepared by hydrogenating suitable vegetable oil.
Advantages of witepsol:
- Have all the advantages but not the disadvantages of
theobroma oil.
- Don’t need lubricant.
Disadvantages:- - Viscosity is less than that of theobroma oil.
- Becomes brittle when cooled too rapidly or refrigerated.
- Has different degrees of hardness, and release in the body may
vary.
2- Water-soluble bases:
A) Glycero-gelatin bases: *size is 4g (adult), 2g (child) & 1g
(infant), composed of glycerin, water and gelatin.
2 types of gelatin can be used, Type A which is cationic and
compatible with acid API, and Type B which is anionic and compatible
with basic API.
It can be used alone for its laxative effect, or as a base.
Disadvantages that cause fatty bases to be used more
frequently:
- Have physiological effect (laxative) and that’s not always
desirable.
- Difficult to prepare and handle.
- Depends on the type of used gelatin.
- Hygroscopic, may cause irritation.
- Microbial growth, so preservatives are needed.
- Need lubricant (almond or arachis oil).
B) Macrogols
They are PEG.
Advantages:
- Have no physiological effect compared to glycero-gelatin.
- Not prone to microbial growth.
- Have high m.p, so can be used for API that can lower the m.p
of other bases.
- High viscosity, so less possibility of leakage from the body.
- Don’t need lubricant.
Disadvantages:
- Hygroscopic, and can cause irritation.
- Incompatible with several drugs and even plastic, so problems
while choosing the correct package could happen.
- Crystallization.
• Creams
They are opaque external (topical) semisolid preparations
containing one or more API dissolved in emulsions that
can be aqueous (oil in water) or oily (water in oil), with
being oil in water is the most common type, and thus
preservatives are needed.
- O/W creams: contain mainly hydrophilic emulsifying agent,
non-greasy, easily washed off by water, rapidly absorbed by
skin, Ex: Vanishing Cream (main component is stearic acid).
- W/O cream: contain mainly lipophilic emulsifying agent,
greasy, difficult to handle, but more moisturizing than o/w
creams as they can stay in contact with skin for longer time
and provides a barrier to prevent water loss from skin (mainly
used as emollient), Ex: Cold Cream.
Creams are cosmetically accepted by users.
- Examples of creams:
Cold Cream (Night cream), Massage cream (applied by rubbing),
Vanishing cream (disappears rapidly), Foundation cream (used to
hold make up above it), Hand and body creams, Whitening creams,
Sun protection creams and Anti-aging creams.
- Ideal Cream:
- Non-toxic - Non-harmful - Non-irritant - Non-allergic -
Easy to apply - Non-staining - Has no side effects.
- Incapable for microbial growth
- Contents of creams:
- API.
- Emulsifying agents, Ex: waxes, borax
- Humectants, Ex: Glycerin, PEG
- Preservatives, Ex: Benzoic acid
- Permeation enhancers, Thickening agents, Fragrances (perfuming
agents), Antioxidants, Chelating agents, UV absorbers, and Buffers.
- General steps to prepare a cream:
- Preparation of the oil phase: by mixing all the oil soluble
agents with a suitable oil (mineral or silicon oil), and melting
may be needed.
- Preparation of the aqueous phase: by mixing all the water
soluble agents with water, and heat may be needed.
- Forming of the emulsion: the two phases are mixed together
under vigorous agitation to form the emulsion.
- Dispersion of the active ingredient.
- Instability:
- Cracking - Discoloration
- Oxidation - Precipitation
- Hydrolysis
• Ointments:
Semi-solid viscous and greasy preparation, usually
immiscible with skin secretions, intended to be applied
topically on skin with or without rubbing.
* Types of ointments:
- Un-medicated: Contains no API, used as emollient and
protectant. Ex: Petroleum jelly (Vaseline).
- Medicated: Contain API that can be dissolved, emulsified or
suspended in the ointment base.
Their use can be dermatological, ophthalmic, nasal, or rectal.
1- Dermatological Ointments: According to their ability to
penetrate the skin, they are
a) epidermic that acts on the epidermis, Ex: Ketoconazole
b) endodermic that has a deeper action, Ex: Antibiotics
c) diadermic which can exert even a systemic effect.
2- Ophthalmic ointments and gels:
Sterile preparations applied to the lower lid of the
eye, and only anhydrous bases are used to prepare
them.
Ex: Demodex ointments which are antibiotic
ointments such as Tobradex eye ointment.
The base of eye ointment is usually composed of yellow soft
paraffin (not white, white can cause irritation), liquid paraffin
and wool fat.
3- Rectal ointments:
ointments to be applied to the peri-anal or into the anal canal.
Ex: Benzocaine ointment.
4- Nasal ointments:
used in topical treatment of nasal mucosa, *can get adsorbed in
the circulation through the rich blood supply to the nasal lining.
- Bases of ointments:
- Oleaginous: Emollients (Not to be applied on infected
skin),Ex: White petroleum,
- o/w emulsion: they are water soluble and water washable,
used as drug vehicles, Ex: PEG oint. And Polybase.
- w/o emulsion: non water removable, used as emollient, Ex:
Hydrous lanolin.
- Absorption ointment base: composed of oleaginous+ w/o
bases, they are not washable, used as emollient, Ex:
anhydrous lanolin.

- Selection of the appropriate base according to:

Desired release rate, Patient’s skin (dry or weeping),
Short or long term stability, Compatibility of base with API.
- Ideal Ointment base:
- Non-irritant. - Elegance - Non-greasy.
- Neutral - Non-dehydrating. - Stable
- Doesn’t cause sensitivity - Doesn’t retard wound healing.
- Compatible with common API - Washable
- Ease of compounding.
- Examples of ointments:
Sulfur ointment (acne and scabies), Whitefield ointment
(keratolytic), Boric acid ointment (eczema), Zinc oxide
ointment (anti-itching) and Icthanol ointment (antimold).
- Preparation:
- Spatulation (Spatula and tile).
- Fusion (melting).
- Trituration (mortar and pestle).
• Pastes:
They are basically ointments into which a high
percentage (>20%) of insoluble solid has been added, and
that stiffens the paste.
Pastes are less penetrating than ointment.
Can be used as sunblock.
They are two types:
Fatty pastes, Ex: Leaser’s paste, and Nongreasy pastes, Ex:
Bassorin paste.
• Poultices:
Soft, viscous, pasty preparations for external use, usually
applied to the skin while hot.
They are called counter-irritants.
• Gels (Jellies):
Semisolid system in which a liquid phase is constrained
with 3D polymeric matrix (Gum).
Consist of dispersing large molecules in an aq. Liquid, and
became jally-like because of the addition of gelling agent
(gelatin, agar, pectin, tragacanth, CMC, PG alginate).
Used for medication, lubrication or like a carrier for
spermicidal agents to be used intra-vaginally.
Can be oral, intranasal, topical, vaginal or rectal.
They are 2 types: One phase (usually contains organics)
and two phase (usually contains inorganics).
Examples of jellies:
Hydrogels, Carbomer gels, Lidocaine jelly, Aloe vera gel,
Mycoheal oral gel, Vibrocil nasal gel.
• Liniments (Embrocations):
Liquid or semisolid alcoholic or oleaginous (oily) solution
or emulsion of medical substances intended for external
use only.
They are applied to the skin by rubbing, and should not
be applied to a broken skin.
They can be alcoholic (rubefacient), oily (to be used in
massage), and emulsion liniments.
Examples: White liniment.
• Cerates:
Semisolid preparations containing a relatively high wax
content.
• Transdermal drug delivery system (TDDS):
aims to overcome the problems of oral delivery by
providing continuous drug release over a period of time
(1-7days).
The principle of this dosage form is that the drug is
absorbed through the skin into the systemic circulation.
The drug is incorporated into an adhesive patch applied
to the surface of the skin. The patch releases a known
dose of drug over a specific time.
- Examples:
Nitroglycerin patches
Estradiol patches
Nicotine patches.
- Types:
1- The membrane (reservoir) type.

2- The matrix type.

3- Water-based pressure-sensitive type.

 Gas Dosage Forms
• Aerosols
Consist of solutions, suspensions or emulsions of drugs mixed
with inert propellants normally contained under pressure in a
metal canister with a valve.
There are 2 types of valves: Metered dose valve (precise
volume with known dose) and Continuous valve (delivers the
drug as long it is depressed).
Can give local or systemic effect.
The most common use is for asthma via the inhalation route.
The drug is inhaled through the mouth and delivered directly
into the site of action (lungs), and so the dose needed is
much lower than the oral dose.
Drugs can be prophylactic (Na-cromoglycate and steroids) or
bronchodilators used in attacks (Salbutamol and terbutaline)
• There are 3 types of devices used to treat Respiratory
Diseases Patients in addition to nasal sprays:
1- Metered Dose Inhalations (MDI):
The simplest type, composed of
pressurized aerosol fitted with a valve.
- Problems:
Inability of synchronization, Cold Freon effect, Difficulty in
firing the devise (arthritic pt., elderly), Inhaled dose may
deposit in mouth and pharynx, Only 10% of drug reaches the
lung even with perfect technique.
- Devices used to overcome the problems:
a) Haleraid: Instead of firing the aerosol
by pressing down on the canister with
the forefinger, the haleraid is gently
squeezed using the whole hand.
b) Spacer: a standard pressurized inhaler with
an elongated mouthpiece, benefit is that the
delivered dose is more diffused when arrived
to the mouth, and “cold Freon effect” is reduced.
c) Large volume inhaler: spacer attachment
for use with MDI.
Beneficial for use with prophylactic
drugs because it can deliver higher
doses of drug.
d) Autohaler: A pressurized aerosol which
incorporates a self-firing mechanism, the
device fires when pt. inhales.
Approx. 21% of the dose reaches the lung
2- Dry powder “breath-actuated” Inhalers (DPI):
In these devices, the drug is presented in finely divided
form removed from the device by the action of the patient
breathing in rather than being propelled from the container.
- Problems:
May cause reflex coughing in the patient, Bioavailability is less
than MDI, Some devices such as rotahaler can’t be kept
preloaded and not suitable for severe attacks.
- Types:
1- Diskhaler: drug is presented in
small blisters in a circular foil container.

2- Rotahaler: drug is presented as capsule.

3- Nebulizers (Atomizers, Nebulizing humidifiers,
Aerosol generators):
Produce and disperse liquid (water) in the form of aerosol
mist.
Used to produce humidification and to deliver drugs as
bronchodilators, mucolytics, steroids and decongestants.
Particle size of water droplet is 0.5-5𝜇m
- Types:
1- Large volume jet nebulizers: works by pushing a jet of high
pressure gas into a liquid, which breaks the liquid into particles.
2- Ultrasonic nebulizers: produce a fine mist by subjecting the
liquid to a high frequency radio wave due to electric current.
3- Mesh Nebulizer: a vibrating mesh creates
the drops and determines their size.
-Problems of Nebulizers:
Can cause over hydration, hypothermia, infection
transmission, bronchospasm, bronchoconstriction, edema.
They are also very expensive, and those which need electric
supply can cause electric shock.
- When nebulizer is used to deliver a drug such as ventolin
solution (bronchodilator) or pulmicort (steroid), a liquid can
be mixed with these drugs.
Best liquid to be used in nebulizers is normal saline as it is
similar to body fluids.
Purified water can also be used.
Large Volume Jet Nebulizer
Ultrasonic Nebulizer
 Liquid Dosage Forms
• Solutions
They are stable homogeneous mixtures contain one or more
solutes dissolved in one or more solvent, and some
excipients can be also added.
Solid in liquid solutions, and aqueous solutions are the most
used pharmaceutically.
- To increase solubility of solutes in the solvents: Co-solvent
(Ethanol, glycerol, propylene glycol, sorbitol) and Solubilizing
agents (Surfactants such as polysorbates and soaps) can be
used.
- Solvents:
*Alcohol (Ethanol): rarely used, good for external prep.
*Glycerol: Stabilizer and sweetener (internal), external,
preservative (conc. >20%).
*Propylene glycol: less viscous and better than glycerol.
*Oils: used for fat soluble compounds.
*Acetone: co-solvent (external prep.)
*Ether: co-solvent (external).
* Syrup: Unsuitable for diabetics & can cause dental carries.
*Water: Widely available, non-toxic, non-irritant, palatable
and relatively inexpensive.
Types of water used in pharmaceutical preparations:
- Potable water: drinking water, safe, contains impurities.
- Purified water: prepared from potable water, and became
impurity-free by distillation or ion exchange.
- Distilled water: purified water prepared by distillation.
- Water for preparation: potable or freshly boiled & cooled
purified water.
- Water for injection: sterile and pyrogen-free distilled water.
- Excipients used in solutions:
1) Preservatives: used to prevent microbial growth.
Ex: Chloroform 0.25% (oral and external) , Benzoic acid 0.1%
(internal), Ethanol, Sorbic acid, Hydroxybenzote esters (can be
used internally) and Chlorocresol 0.1%, chlorobutol 0.5%,
parabens (for external use only).
2) Flavoring agents: used to enhance flavor and make the
solution more palatable, can be synthetic or natural, Ex:
Cinnamon, lemon, Orange, Berries and Liquorice.
3) Coloring agents: to enhance appearance, usually match the
flavor, can be natural, mineral or synthetic.
4) Sweetening agents: glucose and sucrose used to enhance
viscosity and palatability (not suitable for diabetic pt., and can
cause dental carries), and alternatives (Mannitol, sorbitol,
saccharine and aspartame).
5) Viscosity enhancers: Ex: syrups.
6) Stabilizers: used where ingredients are liable to degradation
by oxidation, like oils. They are odorless, tasteless and non-toxic.
Ex: Ascorbic acid, citric acid, Sodium sulphite.
7) Co-solvents: to enhance solubility of sparingly soluble drugs.
Ex: Glycerol, Propylene glycol, Ethanol (minimum due to its
pharmacological effect, cost and burning taste).
8) Diluents: If the medicine must be diluted, then a suitable
diluent must be selected from compendia.
- Solutions can be: Oral solutions
Enemas Tinctures
Nasal solutions Paints
Mouthwashes and gargles Collodions
Ophthalmic solutions Otic solutions
Douche solutions Parenteral solutions
Some lotions and liniments Glycerites
• Oral Solutions:
Solutions to be taken by mouth, usually administered in
multiple of 5mL volume (oral syringe can be used).
They are readily absorbed into GIT, much easier to use than
solid dosage forms specially for children, and there’s no need
to shake the bottle compared to suspensions.
On the other hand, they are hard to carry, and less stable
than solids.
Types:
Elixirs: Clear, flavored, sweetened liquids contain high proportion
of a polyhydric alcohol or ethanol. Used for potent or nauseous
drugs. Ex: Chloral hydrate Elixir (for insomnia)
Linctuses: Viscous liquids used in treatment of cough. Usually
contain high proportion of sugars or alcohols. Should be
swallowed slowly. Ex: Diamorphine Linctus (For cough)
Mixtures: Solution and suspension. Ex: Ammonium and
Ipecacuanha Mixture (Expectorant).
 Mixtures: Solution and suspension. Ex: Ammonium and
Ipecacuanha Mixture (Expectorant).
Oral drops: Solutions or suspensions. Administered in small
volumes using a suitable device.
Syrups: Aqueous solutions contain sugar, usually sucrose.
They can be medicated (Epilim syrup), non-medicated or flavored.
Example of non-medicated syrup is simple syrup (85% wt/vol
sucrose solution).
Syrups have the advantage of high viscosity and self preservating
property, The optimum concentration of syrups is 65% or more.
Problems:
- Crystallization: When concentration is too high, sorbitol or glycerin
can be added to prevent crystallization.
- Microbial growth: when conc. is too low, preservatives are added.
- Sugar inversion: Sucrose may hydrolyze to its components (glucose
and fructose) when heated.
- Caramellization: when syrup is overheated.
 Spirits, Essences: Alcoholic or hydro-alcoholic solutions of volatile
substances (Alcohol content is 60%), can be medicated or flavored.
Can be taken orally, externally or by inhalation (Ammonia spirit).
Aromatic waters: Saturated aqueous solutions of volatile oils or
substances. Mainly used as vehicle in oral soln.
Usually prepared from conc. ethanolic soln. in a dilution with water.
Ex: Chloroform water.
• Ear, aural, otic solutions:
Used locally for removal of wax (excess cerumen) such as
Dewax, or to treat infections, inflammations, and pain.
Ex: Sodium Bicarbonate Ear Drops (Removal of wax).
• Nasal Solutions:
Isotonic and buffered (usually aqueous) solutions
administered as nose drops or nose spray.
Used as decongestant in common cold (mostly),
and for treatment of allergic rhinitis (local steroids).
*Decongestants must not be used for more than 5 days to
avoid rebound congestion and also overuse can lead to nasal
mucosal edema.
• Eye (Ophthalmic, ocular) Solutions:
They are sterile, saline-containing, buffered, viscous solutions
used as antibiotics, anti-itching (antihistamines) antifungal,
or topical anesthetics.
Sometimes they don’t contain
medications and used only for
lubricating and tears-replacing.
• Enemas, Rectal injections, Clysters:
They are oily or aqueous solutions that are administered
rectally.
Types:
Evacuation enema: bowel stimulant,
Ex: Sodium Phosphate enemas.
Retention enema: can give local or systemic
actions, used for nutritive, medicated or
diagnostic purposes.
Micro enemas: single use and small dose.
• Douches (Irrigation):
Aqueous solutions directed against a part
or into a body cavity for cleansing and
antiseptic agent by the use of bulb syringe.
Used for vagina (mostly), eyes, nose, pharynx.
• Gargles and Mouth washes:
-Gargles: Concentrated aq. solutions used to treat the
pharynx and sore throat. May be diluted or non-diluted with
warm water prior use. Ex: Betadine gargle.
-Mouth washes: Aqueous solutions
used for their deodorizing, refreshing
and antiseptic effect.
Ex: Compound Sodium Chloride M/W
* Both liquids are usually not intended
to be swallowed.
• Glycerites:
Viscous solutions or mixtures contain
not less than 50% glycerin, gelatin and water.
Used as medicinal agent or as co-solvent.
Ex: Starch glycerite (topical protective).
• Collodions:
Ethereal liquid solutions composed
of pyroxillin (nitrocellulose) dissolved in
a mixture of ether and alcohol with or
without added medicine, intended for
external use only, applied to skin with
a brush.
Ex: Collodion USP (useful in holding the edges of an incised wound
together, but not flexible), Flexible collodion (with 3% castor oil
and 2% camphor), Salicylic acid collodion.
• Paints:
Liquids for application to skin or mucous membranes.
Skin paints contain volatile oil that evaporates
quickly, while throat paints contain glycerol and
are more viscous to prolong contact with affected site.
• Tinctures:
Alcoholic or hydro-alcoholic solutions
prepared from non-volatile substances,
alcohol content is 15-80%.
Ex: Iodine tincture, Belladonna tincture
• Lotions:
They are not defined in USP, but they are liquid or semi-liquid
(aqueous) preparations for external application on unbroken
skin without friction (without rubbing), they are either
dabbed on skin or applied with a suitable dressing and
covered to reduce evaporation..
They are mostly suspensions, but some of them
can be solutions or emulsions.
Ex: Benzyl benzoate lotion, Calamine lotion
• Parenteral products:
They are solutions, suspensions or emulsions delivered to
patients by injection, infusion or implantation.
Used when the drug can’t be taken orally.
They are sterile, pyrogen-free, isotonic, packaged in special
hermetic containers, and can never be colored.
- Parenteral routes:
-Subcutaneous (SC): volume is 1-2ml injected under the skin in the
abdomen, upper back, upper arms or the internal upper hips.
-Intramuscular (IM): can be aq. Or oily soln. or emul. Injected in
gluteal muscle (buttock), deltoid muscle (shoulder) when rapid
effect is needed, and vastus lateralis (thigh) in infants. It’s faster
than SC.
-Intravenous (IV): injected or infused in a superficial vein (back of
the hand or in the internal flexure of elbow). Must not be oily.
-Intracardiac: in emergencies in the cardiac muscle.
 -Intradermal: Vol. of 0.1mL is injected into the skin between
epidermis and dermis, usually for diagnostic tests of allergy.
-Intraspinal: aq. Soln. with vol. <20mL given into the spinal column
(epidural) or into the spinal fluid (intrathecal).
-Intra-arterial: directly into an artery, to deliver the drug rapidly to
an organ that is served by the artery.
- Intra-articular (into the joint) and intrasynovial (into the synovial
fluid of the joint): local effect.

- Excipients in parenterals:
Buffers.
Solubilizers.
Anti-oxidants
Preservatives (in multi-dose
parenterals such as vials).
- Sterilization of parenterals:
Steam Sterilization (autoclave): for heat and moisture resistant drugs.
Dry heat (Oven): for heat resistant, moist labile drugs.
Filtration: for heat labile drugs by sieving using a membrane filter.
Gas sterilization: for sterile powder and plastic containers using
ethylene oxide, propylene oxide or betapropiolactone.
Ionizing radiation: gamma, beta or cathode radiation.
- Parenterals can be packaged in glass type 1, 2 or 3 or some
types of plastic like PVC for IV bags and tubes.
- Parenterals according to volume are 2 types:
1- Small volume parenterals:
Single dose ampoules (packaged in type 1 glass)
Multidose vials (powders or solutions in a container with double seal.
2-Large volume parenterals
Bottles and bags for infusion.
• Suspensions:
They contain one or more insoluble medicament in a
vehicle, with other additives.
Most pharmaceutical suspensions are aqueous
suspensions, they can be coarse(particles diameter
>1mm) or Colloidal (particles diameter <1mm).
Suspended solids may slowly separate on standing, but
can be re-dispersed.
Useful for drugs or bulk powders that have very low
solubilities and for drugs with bitter taste.
Their absorption in GI is faster than solids but slower
than solutions.
IM, IV or SC injections are often formulated as
suspensions to prolong the release of the drug.
 Lotions containing insoluble solids are formulated to leave
a thin coating of medicament on the skin. As the vehicle
evaporates, it gives a cooling effect (Ex: Calamine lotion).
- Properties of good suspension:
Pourable, Ready dispersion of any sediment after gentle
shaking, Particles are small and uniform.
- To ensure formulation of a good suspension, 3 steps can
be taken:
Grinding (to control size of particles), Using wetting agent, and
Using thickening agents (to increase viscosity of liquid).
- Insoluble solids can be diffusible or indiffusible:
Diffusible (dispersible) solids: light and easily wetted by water. They
will remain dispersed long enough for dose measuring.
Indiffusible solids: not easily wetted and may form clumps. They will
not remain dispersed long enough for dose measuring.
- Problems of suspensions:
1) Sedimentation:
Factors affecting the sedimentation (settling) rate (velocity) are
particle size (increase sedimentation), particle density (increase
sedimentation), density of liquid (decrease sedimentation) and
viscosity of liquid (decrease sedimentation)

2) Poor wetting (floating):

Wetting of the particles can be encouraged by reducing the interfacial
tension between the solid and the liquid, using wetting agents such as
Hydrophilic colloids (acacia),
Polysorbates and sorbitan esters (internally)
and Sodium lauryl sulphate (SLS) externall.
3) Flocculation:
The natural tendency towards aggregation of particles.
In a deflocculated suspension, the dispersed solid particles
remain separate, and settling is very slow, but the sediment
that forms is hard to redisperse and is described as a “cake” or clay.
In a flocculated suspension, individual small particles
aggregate into clumps or floccules, and may cause a more
rapid rate of sedimentation, but the sediment is looser
and easily redispersible.
- Suspending agents:
Natural polysaccharides: Tragacanth, acacia.
Semi-synthetic polysaccharides: derived from cellulose.
Clays: Bentonite
Synthetic thickeners.
Miscellaneous compounds: Gelatin.
- Preservatives like benzoic acid are added as suspensions
contain water, and when natural susp. agent is used.
- Extemporaneously prepared and reconstituted
suspensions will have a relatively short shelf life of 1-4 wks.
- Suspensions can be used for oral administration,
inhalation, topical application (ophthalmic), parenteral
administration and as aerosols.
- Examples:
Calamine lotion BP (contains bentonite) used as cooling lotion
for sunburn or skin irritation.
Menthol and Eucalyptus Inhalation used in nebulizer for relief of
nasal congestion.
• Emulsions:
They consist of 2 immiscible liquids, one is uniformly
dispersed through the other as droplets
(diameter > 0.1μm) with the aid of emulsifying agent.
- Can be oil in water (o/w) or water in oil (w/o).

- Used orally (o/w), externally (o/w or w/o), or

parenterally (o/w usually except for depot preparations).
- Used to deliver oily drugs and enhance their palatability
and absorption in GIT, and also to provide a slow release
(depot) and a greater response for some drugs.
- Examples: Oily calamine lotion (topical), Paraffin lotion (oral)
- Identification tests to determine the type of emulsion
(o/w or w/o):
1) Miscibility test (Dilution test):
An emulsion will mix with a liquid
that is miscible with the continuous
phase.
2) Conductivity test:
o/w systems will conduct electricity,
while w/o systems won’t.
3) Staining test (Cobalt chloride paper test):
Filter paper soaked in cobalt chloride and
dried turns from blue to pink on exposure
to stable o/w emulsions.
4) Dye test: If a water-soluble dye is used,
w/o emulsions are paler in color than o/w
emulsions and vice versa.
- Instability of emulsions:
1) Phase inversion:
The process in which an emulsion changes
from o/w to w/o and vise versa.
It can happen if a substance that alters the
emulsifying agent was added, or if the conc.
Of disperse phase was very high.
The most stable range of disperse phase
conc. is 30-60% (not <20% and not>74%).
2) Creaming:
Used to describe the aggregation of globules
of the dispersed phase on the top or the bottom
of the emulsion (similar to cream on milk). It is
reversible but can cause cracking.
3) Cracking (Braking): Irreversible.
Is the coalescence of dispersed globules and
separation of disperse phase.
- Methods of preparation of emulsions:
Wet method, Dry method, Bottle (Forbes method).
Whatever the method is, a primary emulsion is always a must in
the preparation of oral emulsions (but not in external ones).

*Acacia emulsions containing less than 20% oil tend to cream

readily. A bland inert oil, such as arachis oil, should be added to
increase the amount of oil and so prevent this from happening.
- Emulsion is composed of oil, water, emulsifying agent in addition to
medicaments and excipients.
Emulsifying agents:
1- Naturally occurring: Form barriers and increase viscosity.
- Polysaccharide: Acacia is the best for extemporaneously
prepared oral emulsions, but too sticky for external use.
Form o/w emulsions.
- Semi-synthetic polysaccharides: Methylcellulose
Form o/w emulsions.
- Sterol-containing substances: Beeswax, wool fat.
Form w/o emulsions.
2- Surfactants: Reduce the interfacial tension.
- Ampholytic: Used in detergents and soaps.
- Anionic: Used for external prep., forms o/w emulsions.
Ex: Amine and alkali soaps (o/w),
Soaps of di and trivalent metals, like Ca oleate(w/o)
- Cationic: Quaternary ammonium compounds.
Used in the external prep. of o/w emulsions.
- Non-ionic: Used to produce either w/o or o/w emulsions
for both external and internal use.
3- Finely divided solids: They are adsorbed at the oil-water
interface and form a coherent film around the disperse phase
globules, so prevent the coalescence of the globules.
Particles preferentially wetted by oil form w/o emulsions.
Particles preferentially wetted by water form o/w emulsions.
The type of emulsion formed depends on the balance between
hydrophilic and lipophilic groups which is given by the HLB
number.
High numbers (8-18) produce o/w emulsions and low numbers (3-6)
produce w/o emulsions.
Excipients:
- Anti-oxidants (citric acid or ascorbic acid): w/o emulsions.
- Preservatives (Benzoic acid, chloroform water or cetrimide):
o/w emulsions.
- Colors and flavors.