CHAP 14: DISPERSE SYSTEMS
while permitting liquid therapy
DISPERSE SYSTEM
- Types of liquid preparations containing
undissolved or immiscible drug
distributed throughout a vehicle
A. Dispersed phase
- substance distributed
- Usually insoluble materials
Emulsions dispersed phase is
liquid
o Emulsification results in
dispersion of liquid drug as
fine droplets
Aerosol dispersed phase may be
small air bubbles throughout
solution or emulsion
B. Dispersing phase/Dispersing
medium vehicle
Coarse dispersions
- Containing coarse particles
- Ex: Emulsions, suspensions
Fine dispersions
- Containing particles of smaller size
- Ex: Magmas and gels
Colloidal dispersions
- Particles in colloidal range
SUSPENSIONS
- Contain finely divided drug particles or
suspensoid distributed somewhat
uniformly throughout a vehicle
- Drug exhibits a minimum degree of
solubility
For Oral Suspension
- Drugs that are unstable if maintained
for long periods of time in presence of
an aqueous vehicle
- Supplied as dry powder mixtures for
reconstitution
Oral Suspension
- Not requiring reconstitution
Reasons for Suspensions:
Cortez, J.| 2FPH
Suspension ensures chemical stability
Ease of swallowing liquids
- advantageous for infants, children,
and elderly
Disagreeable taste is overcome
o Erythromycin estolate
- less water soluble ester of
erythromycin
-used to prepare a palatable
liquid dosage form of
erythromycin
- Erythromycin Estolate Oral
Suspension, USP
Use of insoluble forms of
drugs in suspension
greatly reduces difficult
taste-masking problems
Features Desired in a Pharmaceutical
Suspension:
1. Should settle slowly and should be
readily dispersed upon gentle
shaking
2. Particle size of suspensoid should
remain fairly constant throughout
long periods of standing
3. Should pour readily and evenly
Stokes equation
- Uniform, perfectly spherical particles
settle without producing
turbulence, without collision,
without affinity to dispersing
medium
- Reducing particle size produces
slower rate of descent
- Ideal feature density of particles is
greater than vehicle
greater particle density, greater rate
of descent
velocity of fall greater for larger
particles
o Viscometer
- determines viscosity of
pharmaceutical prep.
1
 o Brookfield viscometer - Intentional formation of less rigid or
- measures viscosity by loose aggregation of particles
force required to rotate a - Forms a lattice that resists complete
spindle in the fluid settling
- Less prone to compaction
Physical Features of the Dispersed o Clays
Phase of a Suspension: - commonly employed as
flocculating agent
Dry milling
- help support the floc once formed
- Generally used for particle size
-ex: diluted bentonite magma
reduction
Micropulverization For parenteral suspensions:
- Most rapid, most convenient, - floc can be produced by
inexpensive method of producing fine alteration in pH of
drug powders preparation
o Micropulverizers
- high-speed attrition or impact o Electrolytes
mills - can also be used flocculating
Fluid energy grinding agents
- For finer particles - reduce electrical barrier bet.
- Also called jet milling or particles of suspensoid
micronizing o Nonionic & surface active
- Shearing action of high velocity agents (surfactants)
compressed airstreams - also induce flocculation of
Spray drying particles
- Produce particles of extremely small
Dispersion Medium:
dimensions
o Spray dryer Suspending agents
- cone-shaped - Added to dispersion medium to lend it
- solution of drug is sprayed and structure
rapidly dried - Employed to thicken the dispersion
medium
Carboxymethylcellulose
Fine particles tend to form a cake upon Methylcellulose
settling Microcrystalline cellulose
- resists breakup with shaking Polyvinylpyrrolidone
- particle shape of suspensoid Xanthan gum
affects caking Bentonite
Symmetrical barrel-shaped
particles of calcium Polymeric and hydrophilic colloids
carbonate - Can bind certain medicinal agents
- produce more stable - When used as suspending agents,
suspensions tests should be done
Asymmetrical needle-shaped Rheology
particles of calcium - Study of flow characteristics
carbonate
- form tenacious sediment cake
Factors that affect support of
suspensoid:
Floc or floccules 1. Density of the suspensoid
2. Whether it is flocculated
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 3. Amount of material requiring support
Preparation of Suspension:
Wetting agents
- When drugs float on top of vehicle
- Employed when aqueous vehicle is to
be used
- Function by: displacing air in crevices
of particles, dispersing particles,
allowing penetration of dispersion
medium
Alcohol
Glycerin
Propylene Glycol
other hygroscopic liquid
Colloid mill
- For large-scale mixing of wetting
agents
Mortar and pestle
- For small-scale
Hand-homogenizer, homomixer,
colloid mill
- Suspension is homogenized
Sustained-release suspensions:
Pennkinetic system
- Combination of ion-exchange resin
complex and particle coating
- Ionic drugs are complexed with ion
exchange resins, and the drug-resin
complex is coated with
ethylcellulose
- Ex: hydrocodone polistirex
(Tussionex Pennkinetic Extended-
Release Suspension)
Extemporaneous Compounding of
Suspensions:
Difficulty/Problem: lack of ready
information on stability of a drug in a vehicle
- Drugs in liquid form have faster
decomposition rates than solid form
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o Leucovorin calcium
- most stable in milk or antacid
- unstable in acidic solutions
International Journal of
Pharmaceutical Compounding
- Contains hundreds of compounded
liquid formulations
Compounding suspensions for neonates
- Should not include preservatives,
colourings, flavourings, alcohol
Alcohol
Alter liver function
Cause gastric irritation
Effect neurologic depression
This is the same for elderly
patients and patients who
are taking medications that
depresses CNS
(metrodinazole [Flagyl],
disulfiram [Antabuse])
Preservatives
- Adverse effects on infants
Benzyl alcohol
- cause gasping syndrome
(deterioration of multiple organ
systems)
Propylene glycol
- seizures and stupors
should be stored in airtight, light
resistant bottle
shake well
Examples of Oral Suspensions:
- antacid and antibacterial suspensions
- Kaolin mixture w/ pectin
treatment for diarrhea
Antacid Oral Suspensions
Antacids
- Intended to counteract effects of
gastric hyperacidity
- Employed by persons who must
reduce the level of acidity in
stomach (peptic ulcer patients)
3
 - OTC patients with acid ingestion
and heartburn
- Mostly composed water-insoluble
materials: water insoluble salts of
aluminum, calcium, magnesium
Sodium carbonate, calcium
carbonate, magnesium
hydroxide
- neutralize acid effectively
Magnesium trisilicate,
Aluminum hydroxide
- less effectively and much more
slowly
Sodium carbonate
- Cause sodium overload and systemic
alkalosis
- Hazard to patients on sodium-
restricted diets
Magnesium preparations
- Diarrhea
- Dangerous to patients w/ diminished
renal function
Calcium carbonate
- Hypercalcemia
- Acid rebound stimulation of gastric
secretion and acid production
Excessive use of Aluminum
Hydroxide
- Constipation
- Phosphate depletion
- Muscle weakness, bone resorption,
hypercalciuria
Heartburn and gastric distress
- Single dose of sodium bicarbonate or
magnesium hydroxide
Ulcerative conditions
- Combination of magnesium hydroxide
+ aluminum hydroxide
Gastroesophageal reflux
- Liquid antacids faster action
FDA requires that antacid tablets not
intended to be chewed must
disintegrate within 10 mins
Aluminum and calcium containing
products interfere with absorption of
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fluoroquinone, tetracycline
antibiotics, iron salts
Antibiotic Oral Suspensions:
Antibiotic substances (erythromycin
and tetracycline)
Sulfonamides (sulfamethoxazole and
sulfisoxazole)
Anti-infective agents (methenamine
mandelate and nitrofurantoin)
Combinations (sulfamethoxazole +
trimethoprim)
- Dry powder for reconstitution
- Dispersing phase is aqueous
- Usually colored, sweetened, flavoured
render liquid more appealing and
palatable
Palmitate form of
chloramphenicol
- water insoluble and flavourless
Rectal Suspensions:
Barium Sulfate Suspension USP
- For diagnostic visualization of GI tract
Mesalamine (5-aminosalicylic
acid)
- Marketed as Rowasa
- Treatment of Crohn disease, distal
ulcerative colitis,
proctosigmoiditis, proctitis
- No longer commercially available
Colocort
- Hydrocortisone rectal suspension
- Adjunctive therapy in treatment of
ulcerative colitis
Dry Powders of Oral Suspension:
Contain:
Antibiotic
Colorants (FD&C dyes)
Flavorants
Sweeteners (sucrose or sodium
saccharin)
Suspending agents (guar gum,
xanthan gum, methylcellulose)
4
 Preserving agents (methylparaben,
sodium benzoate)
Fillmaster/ Fillmaster Plus
- Aid in reconstitution
Erythromycin ethylsuccinate +
acetyl sulfisoxazole
- Treatment of acute middle ear
infection caused by Haemophilus
influenzae
Probenecid + ampicillin
- Treatment of uncomplicated infections
caused by Neisseria gonorrhoea
Cholestyramine (Questran)
- Management of hyperlipidemia
Barium sulfate (Barosperse)
- Radiopaque contrast medium
Barium sulfate
- contrast medium for roentgen
ray examination
- water insoluble; not absorbed
in GI tract
EMULSIONS
- Dispersed phase is composed of small
globules of a liquid distributed
throughout a vehicle in which it is
immiscible
A. Dispersed phase
- internal phase
B. Dispersion medium
- external or continuous phase
C. Emulsifying agent
- third phase; to prepare a stable
emulsion
Purpose of Emulsions and of
Emulsification:
1. Enables RPh to prepare relatively
stable and homogenous mixtures of 2
immiscible liq.
2. Permits administration of liquid drug in
form of minute globules
3. Permits palatable administration of
distasteful oils
Cortez, J.| 2FPH
w/o applied more evenly on
unbroken skin; easily removed
o/w more softening; resists drying
and removal
Theories of Emulsification:
1. Surface Tension theory
- Use of tension-lowering substances as
emulsifiers/stabilizers lowers
interfacial tension of 2 immiscible
liquid
Interfacial tension
- force causing each liquid to
resist breaking up into smaller
particles
2. Oriented wedge theory
- Mono-molecular layers of emulsifying
agents curved around the droplet
- Certain emulsifying agents orient
themselves about and within a liquid
in a manner reflective of their
solubility
- Emulsifying agent which is
hydrophilic will promote o/w
emulsion, Hydrophobic promotes
a w/o emulsion
3. Plastic or interfacial film
- Emulsifying agent surround droplets of
internal phase as a thin layer of film
Preparation of Emulsions:
Emulsifying agents
Must be compatible w/ other
ingredients
Must not interfere with stability or
efficacy
Stable and not deteroriate
Non toxic
Possess little odor, taste, color
1. Carbohydrate materials
a. Naturally-occuring
Acacia
- frequently employed
Pectin
Tragacanth
Agar
Chondrus
b. Synthetic
5
 Microcrystalline HLB 8-18
cellulose - produce o/w emulsions
- viscosity regulator
2. Protein Substances Methods of Emulsion Preparation
Gelatin 1. Dry Gum/Continental
- disadvantage: too fluid - EA + oil then water
Egg yolk - 4:2:1 method 4 parts oil, 2 parts
Casein water, 1 part gum
- Produce o/w emulsions 2. Wet/English
3. High molecular weight alcohols - EA + water then oil
Stearyl alcohol 3. Bottle/Forbes method
Cetyl alcohol - Volatile oils and low viscosities
Glyceryl monostearate - Not suited for viscous oils
- Thickening agents and stabilizers for 4. Auxiliary methods
o/w emulsions - Hand homogenizer
4. Wetting agents 5. In Situ Soap method
Anionic - Calcium soaps and soft soaps
- lipophilic portion is negatively Calcium soaps
charged - w/o emulsions that contain
- pH range greater than 8 certain vegetable oils in
Triethanolamine oleate combination w/ limewater
Sulfonates - SLS
Ex: Calamine liniment
Cationic
- positively charged 6. Microemulsions
- pH range of 3-7 - Thermodynamically stable
Benzalkonium Cl - Surfactants HLB range 15-18
Nonionic (polysorbate 60 and polysorbate 80)
- pH range of 3-10 Advantages:
Sorbitan esters More rapid and efficient oral
Polyoxyethylene absorption
derivatives Enhanced transdermal drug
5. Finely divided solids delivery
- Form o/w emulsions Unique potential in devt of
Bentonite artificial RBCs
Mg hydroxide
Stability of Emulsions:
Al hydroxide
- Emulsions are generally unstable if:
1) Form aggregates of globules upon
Inversion standing
- Change from o/w w/o and vice versa 2) Globules rise to the top or fall to the
bottom
HLB System 3) Separation and form distinct layer
- Emulsifying agents or surfactants Aggregation and Coalescence
categorized on basis of their chemical
makeup as to their HLB hydrophilic- Creaming
lipophilic balance - Particles rise to the top or fall to
- Highly polar - higher number bottom
HLB 3-6 - Reversible
- greatly lipophilic To increase stability:
Particle size reduced as fine as
- produce w/o emulsions
possible
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 Minimal density difference large organic molecules
High viscosity interpenetrated by liquid
- thickeners: tragacanth, o Semirigid systems
microcrystalline cellulose A. Single phase gels
o Upward creaming - no apparent boundaries exist
- lesser density of internal phase B. Magma or Milk
o Downward creaming - floccules of small, distinct
- higher density of internal phase particles
Breaking - two-phase system
- Separation of internal phase from
Colloidal Dispersions:
emulsion
- Irreversible Sol
- Dispersion of a solid substance in
liquid, solid, or gas
Fungistatic preservative - Hydro- (water)
- Methylparaben, propylparaben - Alco- (alcohol)
Alcohol 12-15% - used as - Aerosol dispersion of solid in
preservative in o/w emulsion gaseous phase

Examples of Oral Emulsions:

1) Mineral Oil Emulsion
- Lubricating cathartic
2) Castor Oil Emulsion
- Laxative
- For preparation of colon for
radiographic and endoscopic exam
- Overuse: excessive loss of water and
electrolyte
3) Simethicone Emulsion
- Water-dispersible form of simethicone
- Defoaming agent for relief of painful
symptoms of excessive gas in GI
Examples of Topical Emulsions:
Lotions
- Applied to outer surface of the body
o Estrasorb (estradiol)
- treatment of hot flashes and night
sweats caused by menopause
o Lotrimin (clotrimazole)
o Diprolene (betamethasone
dipropionate)
Shampoo
- Solution, emulsion, or suspension used
to clean the hair
GELS AND MAGMAS
Gels
o Consists of dispersions made up of
either small inorganic particles or
Differences bet. colloidal dispersions
and true solutions:
1. Larger particle size of disperse phase
2. Optical properties
- Colloidal dispersion scatter light
and appear turbid
Lyophilic
- Solvent-loving; disperse phase
interacts w/ dispersion medium
- Disperse readily upon addition to
dispersion medium
Lyophobic
- Solvent-hating; degree of attraction is
small
- Generally composed of inorganic
particles
- Do not disperse readily
- Does not greatly affect viscosity of the
vehicle
Association or Amphiphilic colloid
- Exhibit both lyophilic and lyophobic
properties
Thixotropy
- Become fluid on agitation and resume
solid/semisolid state after remaining
undisturbed

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 - Reversible gel-sol formation b. Natural and synthetic gums
c. Inorganic hydrogels
Natural colloids
Examples:
- Self-dispersing
Artificial colloids Silica
- Require special means for prompt Bentonite
dispersion Tragacanth
Pectin
Sodium alginate
Terminology Related to Gels: Methylcellulose
Sodium CMC
Imbibition Alumina
- Taking up of liquid without measurable 2. Organogels
increase in volume 3.
Swelling a. Hydrocarbons Jelene or Plastibase,
- Taking up of liquid w/ an increase in Petrolatum
volume b. Animal and vegetable fats
- Liquids that solvate gel cause swelling c. Soap base greases
Syneresis d. Hydrophilic organogels
- Interaction bet. dispersed phase is polyethylene glycol (Carbowax)
great
- Dispersing medium is squeezed out
and gel shrinks Jellies
- A form of instability
- Structural coherent matrix contains a
high proportion of liquid
- Formed by adding thickening agent
Xerogel (tragacanth or
- Liquid is removed from gel and only carboxymethylcellulose) resultant
framework remains product is clear, uniformly semisolid
- Gelatin sheets, tragacanth
ribbons, acacia tears Preparation of Magmas and Gels:

Magmas and gels (inorganic)

- Prepared by freshly precipitating the
Classification and Types of Gels: disperse phase
Primary classification - Some are prepared by directly
hydrating the inorganic chemical
1. Inorganic
- Two-phase systems Examples of Gelling Agents:
- Aluminum hydroxide gel, 1. Alginic acid
bentonite magma
2. Organic - Obtained from seaweed, prepared
- Single-phase system
products is tasteless, odorless,
- Carbomer, tragacanth, Plastibase
yellowish-white colored fibrous powder
- Used as thickening agent in
concentrations of 1 to 5%
2nd classification - Swells in water to about 200 to 300
1. Hydrogels times its own weight without
- Ingredients are dispersible as colloidal dissolving
or soluble in water
a. Organic hydrogels 2. Carbomer (Carbopol)
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 - Resins with high molecular weight 11. PVA
allylpentaerythrital-cross-linked acrylic - Used at conc of about 2.5% in the
acid- based polymers modified with preparation of various jellies that dry
C10 to C30alkyl acrylates rapidly when applied to the skin
- Fluffy white powders with large bulk 12. Povidone
density (0.5 and 1% aqueous - about 10% to produce gels
- increase solubility of poorly insoluble
dispersion)
o Carbomer 934 effective in thick drugs
13. Sodium alginate
formulations
- 10% to produce gels
o Carbomer 934P for mucosal and
14. Tragacanth gum
oral applications - Used to prepare gels that are most
o Carbomer 940 forms sparkling
stable at pH 4 to 8
clear water or hydroalcoholic gels;
most efficient Examples of Magmas and Gels:
3. CMC
- concentrations of 4% to 6% of medium
1. Bentonite magma
viscosity can be used to produce gel
- Suspending agent
- glycerin may be added to prevent
- Thixotropic ge
drying 2. Sodium Fluoride and Phosphoric
- incompatible with alcohol
Acid Gel
4. CMC Sodium
- Dental care prophylactic
- Soluble in water
3. Fluocinonide Gel
5. Colloidal silicon dioxide
- Anti-inflammatory corticosteroid
- used with other ingredients of similar
4. Tretinoin Gel
refractive index to prepare transparent - Stimulates epidermal cell turnover
gels - Causes peeling
6. Gelatin - Treatment of acne
- dispersed in hot water and cooled to 5. Milk of Magnesia
form gels - 7-8.5% magnesium hydroxide
7. Magnesium aluminum silicate - Reaction between sodium hydroxide
(Veegum) and magnesium sulfate
- Concentrations of about 10% forms a - Side effect: diarrhea
firm thixotropic gel 6. Starch glycerite
- Material is inert and has few - Topical vehicle and protectant
incompatibilities but is less used 7. Lubricating Jelly
above pH 3.5 - Assist in medical procedures
8. Methylcellulose - Aid in insertion of various devices
- Long-chain substituted cellulose 8. Clear Aqueous Gel w/ Dimethicone
- Concentration up to about 5% o Dimethicone copolyol reduce
9. Plastibase/Jelene sticky feel of gelatin
- Mixture of 5% low molecular weight - Vehicle
polyethylene and 95% mineral oil 9. Poloxamer Gel Base
10. Poloxamer/Pluronic - Absorption-enhancing topical vehicle
- Concentrations ranging from 15% to (w/isopropyl palmitate and lecithin)
50% to form gel
- F = flake form; L = liquid form Examples of topical gels:
o Pluronic F-127 o Erythromycin and benzoyl
- low toxicity peroxide gel (Benzamycin
- good medium for topical drug Topical Gel)
delivery
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 o Clindamycin topical gel
(Cleocin)
o Clindamycin and benzoyl
peroxide gel (BenzaClin)
o Benzoyl peroxide (Desquam-X
10)
- control and treatment of acne
vulgaris
o Hydroquinone gel (Solaquin
Forte Gel)
- bleach for hyperpigmented skin
o Salicylic acid gel (Compound W
gel)
- keratolytic
o Desoximetasone gel (Topicort)
and augmented
bethamethasone diproprionate
gel (Diprolene)
- antipruritic; anti-inflammatory
Antacids:
o Aluminum phosphate
o Aluminum hydroxide
- treatment of hyperacidity and
peptic ulcers
- disadvantage: constipation
o Dihydroxyaluminum
aminoacetate magma
AEROSOLS
- Pressurized dosage forms
- Emit a fine dispersion of liquid and/or
solid materials
- Dependence upon function of
container, valve assembly, and
propellant
Pressurized package
- Term when referring to the aerosol
container or completed product
Product may be expelled as:
o Mist
o Coarse, wet, or dry spray
o Steady stream
o Stable or fast-breaking foam
Cortez, J.| 2FPH
For inhalation therapy form of fine
liquid or as finely divided solid
particles
Dermatologic spray coarser; may
be powder, wet spray, stream of liquid,
or ointment-like
Vaginal and rectal foams
Space sprays
- used to provide airborne mist
- room disinfectants, deodorizers,
space insecticides
Surface sprays
- Carry active ingredient to a surface
- Dermatologic aerosols
TYPES OF AEROSOLS:
1. Inhalation aerosols
- Metered-dose inhalers (MDIs)
- Produce fine particles for inhalatation
through mouth and deposition in
pulmonary tree
- Release measured quantities
2. Nasal aerosols
- Nasal MDIs
- Delivery through nasal vestibule and
deposition through nasal cavity
- One dose w/ each actuation
3. Topical aerosols
- Application to the skin
- Metered amount or continuous release
Advantages of Aerosol Dosage Forms:
1. Portion of medication easily
withdrawn without contamination
or exposure
2. Aerosol containers protect medicinal
agents from atmosphere, light, and
maintains sterility
3. Topical medication may be applied in a
uniform, thin layer to skin
reducing irritation; rapid
volatilization provides cooling effect
4. Emitted product may be controlled;
dosage is controlled
5. Aerosol application is a clean process
Aerosol Principle:
2 components:
1. Product concentrate
10
 - Contains active ingredient and
adjuncts
2. Propellant
- Liquefied gas (serves as propellant
and vehicle) or compressed gas
(carbon dioxide, nitrous oxide,
nitrogen)
Liquefied gas
o Chlorofluorocarbons (CFC)
- reduce amount of ozone in
stratosphere
- used if:
a) there are no alternatives
b) provides substantial health or
other public benefits
c) does not involve significant
release of CFC
Examples:
dichlorodifluoromethane,
dichlorotetrafluoroethane,
trichloromonofluoromethane
Aerosol Systems:
Pressure can be controlled by:
a) Type and amt of propellant
b) Nature and amt of product
concentrate
Space sprays
- Contain greater proportion of
propellant
- Release with great pressure
Foam aerosols
- Considered to be emulsions liquefied
propellant is partially emulsified
Fluorinated HC
- Relatively low order of toxicity
- Nonirritating
Two Phase Systems
1. Liquid phase liquefied propellant
and product concentrate
2. Vapor phase
Three-Phase Systems
1. Water-immiscible liquid propellant
Cortez, J.| 2FPH
- Greater density than product
concentrate and resides at bottom
2. Highly aqueous product
concentrate
3. Vapor phase
Compressed Gas Systems
- No reservoir of propellant
- Higher gas pressure is required
Advantage of nitrogen as propellant:
Inert
Protective influence
Odorless and tasteless
Other compressed gases: nitrous oxide,
carbon dioxide employed when product
concentrate is desired to achieve foaming
or spraying
Aerosol Container and Valve Assembly:
Effectiveness of aerosol depends on:
1. Formulation
- Must not chemically interact with
container or other components
2. Container Must withstand pressure,
3. valve assembly resist erosion
- must contribute to the form of product
Containers
a) glass, uncoated or plastic coated
- preferred if not for brittleness
Advantages:
fewer problems with chemical
compatibility
not subject to erosion
more adaptive on design
Disadvantage:
must be precisely engineered
for safety
o Plastic coatings
- render glass containers more
resistant to accidental breakage
- prevents scattering of glass
fragments
b) metal
11
 o Tin-plated steel Gasket rubber or plastic resistant to
- most widely used formulation
- seamed and soldered
o Aluminum Metered-Dose Inhalers
- seamless Metered valves
- greater safety against leakage, - Employed when formulation is potent
incompatibility and corrosion medication
o Stainless steel - Material is regulated by auxiliary
- great deal of chemical resistance valve chamber
is required - Integrity is controlled by dual-valve
- high cost mechanism
c) Plastics
- Problem: being permeated by vapor Factors that affect effectiveness of delivering
within the container medication:
1. Particle size of inhaled drug
Valve Assembly 2. Breathing patterns and depth of
- Permit expulsion of contents of the can respiration
in the desired form, desired rate,
proper amount Areas of research in developing aerosol
- Must be inert production:
Parts: 1. Analysis of dose uniformity
1. Actuator 2. Particle size distribution patterns
- Button the user presses 3. Respirable fractions
- Permits easy opening and closing of
valve Translingual aerosol formulation
- Large orifices for foams and solid
of nitroglycerin (Nitrolingual
streams
Spray)
2. Stems
- Spray droplets onto or under tongue
- Supports actuator
- Acute relief of an attack or prophylaxis
- Delivers formulation in proper form to
of angina pectoris
the chamber
- Not to be inhaled
3. Gasket
- Prevents leakage of formulation
4. Spring Filling Operations:
- Holds gasket in place Cold Filling
- Mechanism by which actuator retracts - Product concentrate and propellant
5. Mounting cup cooled to -34.5-40 deg. Celsius
- Holds valve in place - Cooling system: dry ice and acetone
6. Housing - Aqueous systems cant be filled turn
- Link dip tube, stem and actuator to ice
- Helps determine the delivery rate and
Pressure Filling
form
- Liquefied gas is metered into valve
7. Dip tube
- Brings formulation from container to stem from pressure burette
- Used for most pharmaceutical aerosols
valve
Advantages:
1. Less danger of moisture contamination
Actuator, stem, housing, dip tube
2. Less propellant is lost
made of plastic
Mounting cup, spring metal
Testing Filled Containers

Cortez, J.| 2FPH 12

 - Tested under various environmental Disadvantage:
conditions for leaks or weakness 1. Difficulty in applying in small areas
Valve discharge rate 2. Greater expense
- Determined by discharging a portion Vaginal and Rectal Aerosols
of the contents of a previously Vaginal
weighed aerosol - Contains inserter
- Foams are o/w emulsions water
Other tests: spray patterns, particle size miscible and nongreasy
distribution, accuracy and reproducibility Rectal
o Proctofoam
Packaging, Labeling and Storage - pramoxine hydrochloride
Protective cap - relieve inflammatory anorectal
- Protects the valve against disorders
contamination FOAMS
- Generally made of plastic or metal - Emulsion dosage form containing
dispersed gas bubbles
Must warn patients not to: - Fluffy, semisolid consistency
- Puncture pressurized containers Medicated Foams
- Use or store them near heat or open - Dispersed phase: gas bubbles
flame - Continuous phase: AI
- Incinerate them - Packaged in pressurized containers
- Applied to skin and mucous
Proper Administration and Use of
membranes
Pharmaceutical Aerosols
PREPARATION OF FOAMS
1. Active ingredient/s
Extender devices/Spacers 2. Surfactants
- For patients who could not learn to 3. Aqueous/nonaqueous liquids
coordinate release of medication with 4. Propellants
inhalation o Stable foam propellant is
- Separate activation of aerosol (3-5 internal
secs) o Spray or quick-breaking foam -
- Aerosol velocity is reduced and droplet propellant is external; create
size increased cooling sensations w/ alcohol

Topical administration clean area and

pat dry

Topical Aerosols
Anti-infective agents
- Povidone iodine, tolnaftate, thimerosal
Adrenocortical steroid
- Betamethasone dipropionate and
valerate, dexamethasone,
triamcinolone acetonide
Local anesthetic
- Dibucaine HCl
Advantages:
1. Convenient
2. Less messy

Cortez, J.| 2FPH 13

Cortez, J.| 2FPH 14