DRUG DELIVERY SYSTEM

BY: Ruth Kristabelle Tizon RPh

Mylene June T. Perez, RPh
What is a DRUG?
DRUG DEFINED…
⚫An agent intended for use in
the diagnosis, mitigation,
treatment, cure or prevention of
disease in humans and in
animals
What is drug in
Filipino?
GAMOT
GAMOT AY…
▪Ginhawa (mitigation)
▪Alisin ang sanhi (cure)
▪Maibalik sa normal (treatment)
▪O(u)miwas sa sakit (prevention)
▪Tukuyin ang dahilan (diagnosis)
 ACTIONS AND EFFECTS OF DRUGS
▪ Stimulant (heart, CNS, ▪ Diuretic
GIT) or depressant ▪ Cathartic and laxative
▪ Mydriatic and miotic ▪ Diaphoretic
▪ Coagulant and ▪ Analgesic
anticoagulant ▪ Antipyretic
▪ Hematinic ▪ sedative – hypnotic
▪ Hypolipidemic ▪ Antacid
▪ Emetic and antiemetic ▪ Antihypertensive
▪ Antidepressant
CLASSIFICATION OF DRUGS
1. Functional modifiers
2. Replenishers
3. Diagnostic agents
4. Chemotherapeutic
agents
FUNCTIONAL MODIFIERS

▪Drugs that alter or change

abnormal physiologic functions
▪Examples:
▪ Fever, give antipyretic drugs
▪ Tachycardia and palpitations,
give Beta-blockers
REPLENISHERS
▪Drugs that are given to supplement
endogenous substances that are
missing or lacking in the body
▪ Examples:
▪ Diabetes is due to lack of insulin, give insulin
SC.
▪ Pernicious anemia causes Vitamin B12
deficiency, give Vitamin B12 IM.
▪ Diarrhea causes loss of electrolytes, give
ORS.
DIAGNOSTIC AGENTS
▪Drugs used to diagnose or determine
a disease by assaying the percentage
of antibodies present.
▪Examples:
▪ Edrophonium in Tensilon test is given
to diagnose myasthenia gravis.
▪ Radiopharmaceuticals are usually
given for the diagnosis of diseases.
CHEMOTHERAPEUTIC
AGENTS
▪Drugs that are used to inhibit the
growth or kill microorganisms/cells.
▪Examples:
▪ Antibacterial
▪ Antifungal
▪ Antiviral
▪ Antineoplastic
 What is a
dosage form?
DOSAGE FORMS
▪ Are preparations designed to contain a specified
quantity of medication for ease and accuracy of dosage
administration
PHARMACEUTICAL DOSAGE FORM
Preparations
containing the
active
ingredient
PHARMACEUTICAL FORMULATION
▪ ACTIVE INGREDIENTS
▪ Pharmacologically active; therapeutic
ingredients
▪ INACTIVE INGREDIENTS
▪ Phamaceutically active; nontherapeutic
ingredients
▪ Give the formulation its unique composition
and characteristic physical appearance
REASONS FOR FORMULATING DOSAGE
FORM
Stability
Improved solubility
Improved appearance
Ease of administration
Palatability
 ROUTES OF DRUG ADMINISTRATION
TERM SITE TERM SITE
ORAL PARENTERAL
SUBLINGUAL INTRAVENOUS
EPICUTANEOUS INTRA-ARTERIAL
TRANSDERMAL INTRACARDIAC
CONJUNCTIVAL INTRATHECAL
INTRAOCULAR INTRAOSSEOUS
INTRANASAL INTRA-ARTICULAR
AURAL INTRASYNOVIAL
INTRARESPIRATORY INTRADERMAL
RECTAL SUBCUTANEOUS
VAGINAL INTRAMUSCULAR
GENERAL CONSIDERATIONS IN DOSAGE
FORM DESIGN
1. PHYSICAL AND CHEMICAL
PROPERTIES OF DRUG SUBSTANCES
a) Physical description
b) Particle size
c) Partition coefficient and dissociation constant
d) Polymorphysim
e) Solubility
 PHYSICAL
DESCRIPTION

■ Drugs can be used therapeutically

as solids, liquids or gases
■ Solids >>> liquids >>> gases
 PARTICLE SIZE
■ Microscopic examination is an important
step in preformulation works that gives
an indication of particle size and size
range of the raw material along with the
crystal structure

■ Particle size affects other factors such as

dissolution, absorption and bioavailability
 PARTITION
COEFFICIENT
■ Lipid/water partition coefficient

■ It is a ratio of the concentration of drug

dissolved in lipid and the concentration
of the drug dissolved in water
■ P = lipid solubility = octanol
water solubility water
 PKA/DISSOCIATION
CONSTANTS
■ It refers to the extent of dissociation or ionization
of drug substances
■ The Ka [dissociation constant] is the ratio of the
ionized to the nonionized portion of the drugs.
■ pKa = -log Ka ; Ka = [H+][A+]
[HA]
■ Most drugs are weak acids or weak bases.
■ The ka/pKa affects the absorption and distribution
of the drug; nonionize form is favored
 POLYMORPHISM
■ Chemical variation

■ The ability of some chemicals to exist in

the crystalline or amorphous form
■ An amorphous form of a compound is
always more soluble than the
corresponding crystal form
 SOLUBILITY
■ Solubility is an indication of the maximum
concentration to which a solution maybe
prepared with a solute and solvent

■ A drug must possess some aqueous

solubility for therapeutic efficacy

■ It is important to determine a drug’s

solubility because it affects the dissolution
rate, the absorption and bioavailability of
the drug from the dosage form
 DESCRIPTIVE TERMS OF
SOLUBILITY
■ Descriptive Parts of Solvent
Terms Required
Very soluble <1
Freely soluble 1 to 10
Soluble 10 to 30
Sparingly soluble 30 to 100
Slightly soluble 100 to 1000
Very slightly soluble 1000 to 10 000
Practically insoluble > 10 000
GENERAL CONSIDERATIONS IN DOSAGE
FORM DESIGN

2. PRESERVATION AGAINST MICROBIAL

CONTAMINATION
-chlorobutanol, benzalkonium chloride,
phenyl mercuric nitrate- used for
ophthalmic preparations
GENERAL CONSIDERATIONS IN DOSAGE
FORM DESIGN
3. PRESERVATIVES
 Like
preserves like, acidic= acidic
media, alkaline=alkaline media
 with
the use of preservatives such as
benzoic acid, sodium benzoate, phenol
and cresol, alcohol, parabens
GENERAL CONSIDERATIONS IN DOSAGE
FORM DESIGN
4. APPEARANCE AND PALATABILITY
 Flavors
 Salty- Cinnamon, raspberry, orange
 Bitter- cocoa
 Sour- citrus, fruit flavors
- Children prefer sweet and candy like, fruit flavors
- Adult prefer tart rtaher than fruit flavor
GENERAL CONSIDERATIONS IN DOSAGE
FORM DESIGN
4. APPEARANCE AND PALATABILITY
 SWEETENING:
 SUCROSE- commonly used sweetener

 GLYCERIN- less sweet than sucrose

 SACCHARIN- 300X sweeter than sucrose

 ASPARTAME- 180-200X sweeter than sucrose

 CYCLAMATE-has carcinogenic potential

 ACESULFAME K- 130X sweeter

 STEVIA POWDER- natural, 30X

GENERAL CONSIDERATIONS IN DOSAGE
FORM DESIGN
FD and C color additives
Used in foods, drugs and cosmetics
D and C color additives
Some are approved for use in drugs, some
in cosmetics and some in medical devices
External D and C color additives
Use of which is restricted to external parts
of the body
GENERAL CONSIDERATIONS IN DOSAGE
FORM DESIGN
5. PACKAGING
 PLASTIC CONTAINER (PET, PVC, APET, PETG)
 PROBLEMS- Permeability, leaching, sorption,
transmission, alteration
 GLASS CONTAINER- type 1, type 2, type 3, type 4
GENERAL CONSIDERATIONS IN DOSAGE
FORM DESIGN
5. LABELING
 PRESCRIPTION DRUG LABEL
 RX symbol, controlled
 OTC
 Pharmacologic category
 STORAGE CONDITIONS
 Cold, room temperature
TYPES OF STABILITY
■ Chemical stability
■ Physical stability
■ Microbiologic stability
■ Therapeutic stability
■ Toxicologic stability
 REACTIONS LEADING TO
INSTABILITY OF DRUGS
■ Hydrolysis
•A solvolysis process in which drug
molecules interact with water molecules to
yield breakdown products.
•Example:
Aspirin + H2O 🡪 salicylic acid and
acetic acid (vinegar odor)
 REACTIONS LEADING TO
INSTABILITY OF DRUGS
■ Oxidation
•Is the loss of electrons from an atom or a
molecule, it is usually accompanied by an
increase in the valence of an element
■ Example: Fe+2 🡪 Fe+3
•In organic chemistry, oxidation is
frequently considered synonymous with
the loss of hydrogen (dehydrogenation)
from a molecule.
 REACTIONS LEADING TO
INSTABILITY OF DRUGS

■ Polymerization
•Is a reaction between two or more
identical molecules that forms a new and
generally larger molecule
•Example: Formaldehyde
REACTIONS LEADING TO
INSTABILITY OF DRUGS

■ Decarboxylation
•It refers to the decomposition of an
organic compound/acid (RCOOH) and
release of carbon dioxide gas
•Example: Citric acid and tartaric acid
in effervescent granules
 REACTIONS LEADING TO
INSTABILITY OF DRUGS

■ Deamination
•Removal of the nitrogen-containing
group from an organic amine
•Example: Insulin deteriorates in acid
solutions
 STABILITY STUDIES

▪ Studies conducted to determine

the stability of drugs and drug
products.
 TYPES OF STABILITY
STUDIES
•Accelerated Stability Studies
■ Short-term or stressed stability studies

■ Conditions used: T=40C, RH=75%,

time= 6 months
Purposes:
■ To determine the most stable of the
proposed formulations for drug product
■ To predict shelf-life and expiration date
 TYPES OF STABILITY
STUDIES
•Non-accelerated Stability Studies
■ Long-term or real-time stability studies

■ Conditions used: T= 25±2C,

RH= 60±5%, time= 12 months

Purposes:
■ More precise determination of drug
product stability
■ Determination of actual shelf-life

■ Possible extension of expiration date

POWDERS AND GRANULES
 POWDERS

As a pharmaceutical preparation, (Pulvis, in

Latin), a POWDER is a mixture of finely
divided drugs and/or chemicals used
internally or externally

TYPES:
 DIVIDED POWDERS
 BULK POWDERS
 ADVANTAGES AND DISADVANTAGES
Adv Dis

Flexibility in Time consuming

compounding
Good chemical Inaccuracy of
stability doses
Rapid dispersion Unsuitability
USP DESCRIPTIVE
TERMS FOR
PARTICLE SIZE OF
DRUGS
 USP DESCRIPTIVE TERMS
■ These descriptive terms regarding the particle size of powders are
related to the proportion of powder that is capable of passing through
the openings of standard sieves of varying fineness in a specific period
while being shaken

■ Sieves for pharmaceutical testing and measurement are generally

made of wire cloth woven from brass, bronze or other suitable wires
VEGETABLE & ANIMAL DRUGS
Descriptive Powder Characteristic
Term Number
Very coarse No. 8 All particles pass through a # 20 sieve and
NMT 20% through a # 60 sieve

Coarse No. 20 All particles pass through a # 20 sieve and

NMT 40% through a # 60 sieve

Moderately No. 40 All particles pass through a # 40 sieve and

coarse NMT 40% through a # 80 sieve

Fine No. 60 All particles pass through a # 60 sieve and

NMT 40% through a # 100 sieve

Very fine No. 80 All particles pass through a # 80 sieve.

There is no limit to greater fineness.
CHEMICALS/SYNTHETIC
Descriptive Powder Characteristic
Term Number
Coarse No. 20 All particles pass through a # 20
sieve and NMT 60% through a # 40
sieve
Moderately No. 40 All particles pass through a # 40
coarse sieve and NMT 60% through a # 60
sieve
Fine No. 80 All particles pass through a # 80
sieve. There is no limit to greater
fineness.
Very fine No. 120 All particles pass through a # 120
sieve. There is no limit to greater
fineness.
 PREPARATION OF POWDERS
I. COMMINUTION
- the process of reducing
particle size
Techniques employed:
a. Trituration
b. Pulverization by
intervention
c. Levigation
 PREPARATION OF POWDERS
II. MIXING OF POWDERS
 Geometric dilution is used when potent
substances are to be mixed with large
amount of diluent
 Techniques employed:
a. Spatulation c. Sifting
b. Trituration d. Tumbling
 PREPARATION OF POWDERS
III. PACKAGING OF POWDERS
 BULK POWDERS are packed in wide-
mouthed glass, perforated, or sifter can, or
in aerosol container
 Single unit dosage as sachets or packets
 Divided powders are wrapped in papers
 BULK POWDERS
ORAL POWDERS
Antacid or laxative powders, taken by mixing with
water
DOUCHE POWDERS
dissolved in warm water for vaginal use
DUSTING POWDERS
medicated or non-medicated powders for
external application to the skin
DENTRIFICES
generally containing a soap or detergent, mild
abrasive, and anticariogenic agent
 DIVIDED POWDER
 Chartulae
 Methods of dividing powders
a. By individual weighing
b. Block and divide method
 Dispensed in individual doses, usually
in folded papers
 Powder papers can be vegetable
parchment, white bond, glassine, or
waxed paper
 INSUFFLATIONS
 Are finely divided powders introduced into
the body cavities such as ears, nose, throat,
tooth sockets and vagina.
 An insufflator, or powders blower is used to
administer the product.
 Examples: Norisodrine Sulfate Aerohaler
Cartridge (Abbott)
 TRITURATION
 Are dilutions of potent powdered
drugs prepared by intimately mixing
them with a suitable diluent in a
definite proportion by weight.
 They were once official as 1:10
dilutions
 GRANULES
 Prepared agglomerates of smaller particles of
powder
 Irregularly shaped, usually 4 to 12-sieve size range
 Prepared by wet or dry granulation methods
 Free-flowing, thus are used in tablet making
 More stable to the effects of atmospheric humidity
 Less likely to cake or harden upon standing
 More easily wetted
 EFFERVESCENT GRANULATED SALTS
 Are granules or coarse to very coarse powders containing a
soluble medicinal agent in a dry mixture usually composed of
sodium bicarbonate, citric acid, and tartaric acid.

 When mixed with water, acids and base react to liberate carbon
dioxide resulting in effervescence.

 The resulting carbonated solution masks undesirable taste of

any medicinal agent
SPECIAL PROBLEMS
WITH DIVIDED POWDERS
● Hygroscopic and deliquescent substances that
become moist because of an affinity for
moisture in the air
■ Can be prepared as divided powders by adding
inert diluents

■ Double wrapping is desirable for further protection

GRANULES…
■ These are prepared agglomerates of
smaller particles of powders
■ They are commonly used in the
preparation of tablets
ADVANTAGES
OF GRANULES

● Free-flowing
● Stable
● Less tendency to form cake
● Easily wetted by liquids
EFFERVESCENT
GRANULES
■ Are granules or coarse to very coarse
powders containing medicinal agent in a dry
mixture of sodium bicarbonate, citric acid and
tartaric acid
■ Both acids should be used to avoid any
difficulties
■ When added to water, they liberate carbon
dioxide resulting in effervescence
METHODS OF PREPARING
EFFERVESCENT GRANULES

● Dry Method
■ Dry fusion method
■ The water present in citric acid acts as the
binding agent to form granules
■ The product should be dispensed in tightly
closed glass container to protect it against
humidity and air
METHODS OF PREPARING
EFFERVESCENT GRANULES

● Wet Method
■ Wet fusion method
■ It involves the addition of small amounts of
water-alcohol mixture to the dry salts to
obtain a workable or pliable mass which is
then dried and ground to yield the powder or
granule
METHODS OF PREPARING
EFFERVESCENT GRANULES

● Fluidized-bed Procedure
■ Powders are blended and then suspended in
a stream of air in a “Wurster chamber”.
■ Water is sprayed into the chamber, resulting in
a slight reaction and an expansion of the
particles to form granules (10-30 mesh size).
CAPSULES TABLET AND OTHER
DOSAGE FORMS
CAPSULES

Are solid dosage forms in which

the medicinal agents and/or inert
substances are enclosed in a small
gelatin shell.
TYPES OF CAPSULES
1. HARD GELATIN CAPSULES
2. SOFT GELATIN CAPSULES
HARD GELATIN CAPSULES
Used by community pharmacist in
extemporaneous compounding of
prescriptions
Commonly employed in clinical
drug trials to compare
investigational drug to another
drug or a placebo.
May be made opaque by adding
agents such as titanium dioxide
 CAPSULE SHELLS

Made of gelatin, sugar and water

Clear, colorless and essentially tasteless
May be colored with various FD & C and
D & C dyes
May be made opaque by adding
titanium dioxide
 SELECTION OF CAPSULE
SIZE
• The cap is meant to enclose the powder,
not to retain additional powder.
• Typically, HGC are used to encapsulate
between 65mg and 1 gram of powdered
material, including the drug and any
diluents needed.
 CAPSULE SIZE
Capsule Size Approximate Fill [in grains]
000 10-28
00 6-20
0 5-14
1 3.5-10
2 3-8
3 2-6
4 1.5-4
5 1.5-2
 CAPSULE FORMULATION CONTAINS
Active ingredient
Diluents or Fillers – produce the proper
capsule fill volume
Examples: Lactose, microcrystalline cellulose
and starch
Disintegrants – assist break-up and
distribution of the capsule contents in the
stomach
Examples: pregelatinized starch,
croscarmellose, sodium starch glycolate
 CAPSULE FORMULATION CONTAINS
Lubricants or glidants – improve flow
properties of powder mixture
Examples: Fumed silicon dioxide,
magnesium stearate, calcium stearate,
stearic acid or talc

Surfaceactive agents – facilitates wetting

of powder by the GI fluids
Example: Sodium lauryl sulfate
SOFT GELATIN CAPSULE
Made of gelatin in which glycerin or
sorbitol has been added to render it
elastic or plastic like.
Contains more moisture than hard
gelatin capsules thus contains
preservatives like parabens
Hermetically seal and encapsulate
liquids, suspensions, pasty materials or
dry powders
SOFT GELATIN CAPSULE
 Prepared to contain a variety of liquid,
paste, and dry fills
 Liquids encapsulated into SGC include;
1. Water-immiscible volatile and non
volatile liquids
2. Water-miscible nonvolatile liquids
3. Water-miscible and relatively
nonvolatile compounds
TABLETS
Are solid pharmaceutical dosage forms
containing drug substances usually
prepared with the aid of suitable excipients

Prepared by:
 Wet granulation method
 Dry granulation method
 Direct compression
TABLET EXCIPIENTS
DILUENTS – fillers designed to make up the
desired bulk, flow properties and compression
characteristics.
Examples: Lactose, mannitol, starch, dibasic calcium
phosphate, sorbitol, powdered cellulose
BINDERS – used to cause adhesion of powder
particles in tablet granulations
Examples: Acacia, CMC, gelatin, MC, EthC,
compressible sugar, liquid glucose
 TABLET EXCIPIENTS
COLORANTS – FD&C lakes are used
FLAVORING/SWEETENING AGENTS –
usually limited to chewable and buccal tablets

ADSORBENTS – substances capable of holding

quantities of fluids in an apparently dry state
Examples:
Fumed silica Bentonite
Microcrystalline cellulose Kaolin
Magnesium carbonate
TABLET EXCIPIENTS
DISINTEGRANT
– Promote break-up of the tablets after
administration to smaller particles for ready
drug availability
– Facilitate disintegration when the tablet
contacts water in the GIT, this is made
possible by drawing water into the tablet,
swelling and causing the tablet to burst
TABLET EXCIPIENTS
– Lubricants
• Reduce the friction that occurs between the
walls of the tablet and the walls of the die
cavity when the tablet is ejected
– Antiadherents
• Reduce sticking or adhesion of the tablet
granulation or powder to the faces of the
punches or the die walls
– Glidants
• Promote the flow of the tablet granulation or
powder by reducing friction among particles
TABLET EXCIPIENTS
▪ Sugar-coating agents – liquid glucose,
sucrose
▪ Film-coating agents – MC, EthC,
Hydroxy-ethyl/propyl cellulose
▪ Enteric-coating agents – cellulose
acetate phthalate, shellac (35% in
alcohol, “pharmaceutical glaze”)
 TABLET TYPES AND CLASSES
 Multiple Compressed Tablets –
multilayered or tablet-within-a-tablet
 Sugar-coated tablets – 50% larger and
heavier than the original uncoated tablet
 Film-coated tablets – coated with a thin
layer of polymer capable of forming a
skin-like film over the tablet
 Gelatin-coated tablets (GELCAPS)
TABLET TYPES AND CLASSES
▪ CHEWABLE TABLETS
Θ Mannitol is the common excipient
Θ Xylitol may be used for sugar-free
chewable tablets
▪ ENTERIC-COATED TABLETS – has a delayed
release feature
▪ EXTENDED-RELEASE TABLETS
▪ IMMEDIATE RELEASE TABLETS
▪ INSTANT DISINTEGRATING /DISSOLVING
TABLETS
TABLET TYPES AND CLASSES
TABLETS USED IN THE ORAL CAVITY
Buccal tablets
Sublingual tablets

III. TABLETS USED TO PREPARE SOLUTION

Effervescent tablets
Dispensing tablets
Hypodermic tablets
Tablet triturates
 COMMON TABLET MANUFACTURING PROBLEMS

CAPPING - the partial or complete

separation of the top or bottom of the
tablets from the main body.
LAMINATION- is the separation of the
tablet into two or more layers.
CHIPPING – is the splitting of small parts
from the surface of the tablet.
OTHER SOLID DOSAGE FORMS FOR ORAL
ADMINISTRATION
LOZENGES
Are disc-shaped, solid dosage forms
containing medicinal agent and generally a
flavoring substance in a hard candy or sugar
base.
They are intended to be dissolved slowly in
the oral cavity for localized effects
Made by compression or molding
Compressed lozenges are called TROCHES
in the USP
OTHER SOLID DOSAGE FORMS FOR ORAL
ADMINISTRATION
PILLS
Are small, round, solid dosage forms
containing a medicinal agent intended to be
administered orally.
Classes of pills according to weight
a. Parvules (small pills) – 20 mg
b. Granules – 20 to 60 mg
c. Pills – 60 to 500 mg
d. Boluses (big pills) – 700 to 2000 mg; for
veterinary use
 LOLLIPOP
• A sugar-based lozenge on a stick
containing fentanyl citrate
• Actiq is the first product designed to aid
in controlling breakthrough pain in cancer
patients
 METHODS OF TABLET
PREPARATION
• Wet Granulation
– A widely employed method for production of
compressed tablets
– It includes the following steps:
• Weighing and blending of ingredients
• Preparing a damp mass
• Screening the damp mass into pellets or granules
• Drying the granulation
• Sizing the granulation by dry screening
• Adding a lubricant and blending
• Compression
 METHODS OF TABLET
PREPARATION
• Dry Granulation
– Used for materials that are degraded by moisture or
elevated temperature
– A method where the powder mixture is compacted in
large pieces and subsequently broken down or sized
into granules
– It includes the following steps:
• Weighing and blending the ingredients
• Slugging
• Dry screening
• Lubrication
• Compression
 METHODS OF TABLET
PREPARATION

• Direct Compression
– Used for granular chemicals that
possess free-flowing and cohesive
properties that enable them to be
compressed directly in a tableting
machine without need of granulation
MODIFIED RELEASE DOSAGE
FORM
MODIFIED RELEASE DOSAGE FORM
Delayed-release
Sustained-action
Prolonged-action
Sustained-release
Prolonged-release
Timed-release
Slow-release
Extended-action
Extended-release
CLASSIFICATION OF ORAL CONTROLLED-RELEASE
DRUG DELIVERY SYSTEM

I. DIFFUSION CONTROLLED
SYSTEMS
1. COATED BEADS or PELLETS
➢ The drug is distributed into beads,
pellets, granules or other particulate
system
➢ The granule mixture: Uncoated and
Coated pellets may be filled into
capsules or compressed lightly into
tablets
EXAMPLES:

Product Component Form

Ornade Phenylpropanolamine Coated pellets

Spansule and chlorpheniramine in capsule
maleate
Theo-Dur Theophylline Pellets in tablet
Toprol XL Metoprolol Pellets in tablet
Indocin SR Indomethacin Coated pellets
in capsule
Compazine Prochlorperazine Coated pellets
spansule in capsule
2. MICROENCAPSULATION
▪ Solids, liquids, or even gases may be
encapsulated into microscopic size
particles through the formation of thin
coatings of “wall” materials around the
substance being encapsulated.
▪ Gelatin, polyvinyl alcohol, ethylcellulose,
polyvinyl chloride are examples of wall-
forming materials
▪ Examples: Micro-K Extencaps, Bayer
Timed-release Aspirin
 3. MATRIX TABLETS
▪ Embedding drug in an inert plastic
matrix such as polyethylene,
polyvinyl acetate, or
polymethacrylate
▪ Examples: Gradumet (Abbott),
Lontabs (Geigy),Slow-K (Ciba), and
Dospan (Merill Dow)
II. OSMOTICALLY CONTROLLED SYSTEMS
▪ OROS SYSTEM – pioneer oral osmotic
pump delivery system
▪ Composed of a core tablet surrounded by
a semipermeable membrane coating having
a hole
▪ Core tablet:
(1) “Active” layer – containing the drug
(2) “Push” layer – containing the
polymeric osmotic agent
OSMOTIC SYSTEMS

• GITS (Gastrointestinal Therapeutic System)

Examples: Glucotrol XL(Glipizide),
Procardia XL (Nifedipine), Minidiab OD,
Adalat GITS
• COER (Controller-Onset Extended Release)
Example: Covera-HS Tablet
 OTHER OSMOTICALLY CONTROLLED
ORAL PRODUCTS
Products Active Drug
Calan SR Verapamil
Volmax Albuterol
Minipress XL Prazosin
Teczem Enalapril and
Diltiazem
Tiamate Diltiazem
 III. ION-EXCHANGE RESINS
A complex of resin-drug is formed; tableted,
encapsulated or suspended in an aqueous
vehicle
The release of the drug is dependent upon
the pH and the electrolyte concentration in
the GIT
Examples: Hydrocodone polisterix and
chlorpheniramine polisterix suspension
(Tussionex pennkinetic Extended Release
Suspension); Phentermine Resin Capsules
(Duromine)
IV. DISSOLUTION CONTROLLED SYSTEMS

1. HYDROCOLLOID SYSTEM
The drug is embedded in a slowly eroding
or hydrophilic matrix system
Examples:
1. Valrelease (Roche) – slow release form of
diazepam
2. Oramorph SR tablets (Roxane) – contains
morphine sulfate in HPMC
3. Trilafon tablets (Perphenazine)
2. COMPLEX FORMATION
Drug substances are combined
with other chemical agent to form
complexes that may be only slowly
soluble in body fluids
The slow dissolution provides the
extended release of the drug
Example: Rynatan (Wallace)
3. ENCAPSULATED DISSOLUTION
CONTROLLED SYSTEM
Involves microencapsulation technique or
multiparticulate formulation consisting
beads of varying coating thickness
The coat is made of slowly dissolving
polymeric materials

Products Components
Cardizem CD Diltiazem HCl
Diamox Sequels Acetazolamide
Dexedrine Spansule Dextroamphetamine
Thorazine Spansule Chlorpromazine
NON-ORAL MODIFIED-RELEASE SYSTEMS

1. OCULAR INSERTS
 Ocusert – Ocular Pilocarpine therapeutic
system which releases medication over a
7-day period in the treatment of glaucoma
 Lacrisert – for the treatment of dry eyes
2. PARENTERAL SYSTEMS
 Depo-Provera Contraceptive Injection
 Penadur LA injection
 Decadron LA injection
 NON-ORAL MODIFIED-RELEASE SYSTEMS
3. VAGINAL INSERTS
▪ Cervidil Vaginal insert – contains dinoprostone for
the induction of labor
▪ Crinone Gel – contains progesterone used to assist
reproduction
▪ Estring – vaginal ring containing estradiol for the
treatment of urogenital symptoms associated with
postmenopausal atrophy of the vagina
 NON-ORAL MODIFIED-RELEASE SYSTEMS

4. SUBDERMAL IMPLANT
▪ Solid dosage form designed to be inserted under
the skin by special injectors or by surgical
incisions
▪ Zoladex Implant (Zeneca) – contains goserelin
acetate for the treatment of advanced prostatic
cancer
▪ Norplant System (Wyeth-Ayerst) – conatins
levonorgestrel that provides up to 5 years
contraception
 TRANSDERMAL DRUG DELIVERY SYTEMS
(TDDS)
▪ Transdermal patches
▪ Controlled release devices
containing the drug for systemic
absorption after topical application
to the skin surface
 TYPES OF TDDS
▪ Monolithic System
▪ A TDDS that incorporates a drug matrix between backing
and frontal layers
▪ Examples
▪ Salonpas
▪ Band-aid

▪ Membrane-Controlled System
▪ A TTDS designed to contain a drug reservoir [or a pouch
usually in liquid or gel form], a rate-controlling membrane
and backing, adhesive and protective layer
 TDDS DESIGNS
Backing Layer
Liquid Drug Reservoir

Protective Peel Strip Semipermeable membrane

Adhesive + Drug

Backing layer Peripheral adhesive

Drug in semisolid matrix

Reservoir Type design Protective peel strip

(Transderm-Nitro and Estraderm)

 ADVANTAGES OF TDDS

▪ Avoid GI absorption difficulties and incompatibilities

▪ Substitute for oral administration of drug when the
route is unsuitable
▪ Avoid first-pass effect
▪ Avoid the inconvenience of parenteral therapy
▪ Provide extended therapy with single application
▪ Provide extended activity of drugs having short half-
lives
▪ Drug therapy may be terminated rapidly
▪ Rapid identification of medication in emergencies
 DISADVANTAGES OF TDDS
▪ Only potent drugs are suitable for
transdermal drug delivery
▪ Some patients may develop contact
dermatitis due to one or more of the
system components
 EXAMPLES OF TDDS
1. TRANSDERMAL SCOPOLAMINE-
antinauseant
2. TRANSDERMAL NITROGLYCERIN – used in
prophylactic treatment of angina
3. TRANSDERMAL CLONIDINE – for
hypertension
4. TRANSDERMAL NICOTINE – adjuncts in
smoking cessation
5. TRANSDERMAL ESTRADIOL
6. TRANSDERMAL TESTOSTERONE
 OTHER TRANSDERMAL THERAPEUTIC SYSTEMS
▪ Cardiovascular agents: Diltiazem,
Isosorbide dinitrate, Propranolol,
Mepindolol and Verapamil
▪ For hormonal contraception:
Levonorgestrel/Estradiol
▪ For Alzheimer’s disease: Physostigmine
and Xanomeline
▪ For substance addiction: Naltrexone and
Methadone
▪ For anxiety: Buspirone
▪ For smoking cessation: Bupropion
▪ For impotency: Papaverine
SUPPOSITORIES AND
INSERTS
SUPPOSITORIES
✓Are solid dosage forms
intended for insertion into the
body orifices where they melt,
soften, or dissolve and exert
localized or systemic effects
TYPES OF SUPPOSITORIES
Types Rectum Vagina Urethra
Name Rectal Pessaries Bougies
Shape Bullet, Globular, Pencil-
torpedo, little oviform, shaped
finger cone-shaped
Size A – 32 mm M – 140 mm
long long
C – 16 mm F – 70 mm
long long
Weight A – 2 grams 5 grams M – 4 grams
C – 1gram F – 2 grams
 TYPES OF SUPPOSITORIES
RECTAL SUPPOSITORIES
▪ About 32 mm (1 ½ inches) in length,
cylindrical, one or both ends tapered and
some are bullet shaped
▪ Adult rectal suppositories weigh about 2
grams when cocoa butter is used as a base
▪ Intended both for local and systemic action
 RECTAL SUPPOSITORIES
FOR LOCAL EFFECT
✓ Used to relieve constipation

Examples: Glycerin supp., Dulcolax supp.

✓ Used to relieve pain, irritation, itching, and inflammation

associated with hemorrhoids and other anorectal

conditions
Examples: Hydrocortisone supp., Mesalamine supp.
 RECTAL SUPPOSITORIES
FOR SYSTEMIC ACTIONS
✓ For the relief of nausea and vomiting - Ondansetron

supp.
✓ As tranquilizer - Prochlorperazine and

Chlorpromazine supp.
✓ Narcotic analgesic – Oxymorphone supp.

✓ For migraine – Ergotamine tartrate supp.

✓ Analgesic-antipyretic – Opigesic supp.

(Paracetamol)
 EXAMPLES OF RECTAL
SUPPOSITORIES
Generic Name Brand Name Type of Effect Category
Bisacodyl Dulcolax Local Cathartic
Chlorpromazine Thorazine Systemic Antiemetic and
tranquilizer
Hydrocortisone Anusol-HC Local Antiinflam-
matory
Hydromorphone Dilaudid Systemic Analgesic
Mesalamine Canasa Local Antiinflam-
matory
Oxymorphone Numorphan Systemic Analgesic
Prochlorperazine Compazine Systemic Antiemetic
Promethazine Phenergan Systemic Antihistamine
 VAGINAL SUPPOSITORIES
▪ Also called “ PESSARIES”
▪ Globular, oviform, or cone shaped
▪ Weigh about 5 grams when cocoa butter
is used as the base
▪ Employed mainly as contraceptives,
antiseptics in feminine hygiene, and as
specific agents to combat invading
pathogen
▪ Examples: Canesten supp.,Monistat
supp.
 EXAMPLES OF VAGINAL
SUPPOSITORIES AND INSERTS
Generic Name Brand Name Category
Sulfanilamide AVC Antifungal
Suppositories
Miconazole Monistat 7 Antifungal
nitrate Suppositories
Clotrimazole Mycelex – G Antifungal
Vaginal tablets
Nonoxynol-9 Semicid Vaginal Contraceptive
Contraceptiive
Insert
 URETHRAL SUPPOSITORIES
🖉 Also known as “BOUGIES”
🖉 Slender, pencil-shaped
2 types:
1. Male Urethral suppository – 3 to 6 mm in
diameter and approx. 140 mm in length;
weigh about 4 grams when cocoa butter
is used as the base
2. Female Urethral suppository – 70 mm in
length and weigh about 2 grams when
cocoa butter is used as the base
 SUPPOSITORY BASES

I. BASES THAT MELT – FATTY OR OLEAGINOUS BASES

• COCOA BUTTER –Theobroma oil
© Melts at 34-35°C
© Good base for rectal suppositories but less ideal for vaginal
and urethral supp.
© Exhibits polymorphism
© Its melting can be lowered by certain drugs (e.g. chloral
hydrate)
 SUPPOSITORY BASES

I. BASES THAT MELT – FATTY OR OLEAGINOUS

BASES
• WITEPSOL BASES – triglycerides of staurated fatty acids
(lauric acid)
• WECOBEE BASES – triglycerides derived from coconut oil
• FATTIBASE® - triglycerides from palm, palm kernel, and
coconut oils with self emulsifying glyceryl monostearate and
polyoxyl stearate
 SUPPOSITORY BASES
II. BASES THAT DISSOLVE
WATER SOLUBLE AND WATER MISCIBLE
BASES
PEG POLYMERS
✓ Use combination of different MW’s PEG polymers:
PEG 400 –liquid; PEG 1000 – semisolid; PEG 1500 to
1540 – fairly firm semisolids; PEG 4000 to 6000 – wax-
like
✓ Do not “leak” from the orifice
 SUPPOSITORY BASES
II. BASES THAT DISSOLVE
WATER SOLUBLE AND WATER MISCIBLE
BASES
GLYCERINATED GELATIN
✓ Frequently used in vaginal suppositories

✓ Suppositories using this base should be moistened

first with water to avoid irritation to the tissue upon
insertion
 PREPARATION OF SUPPOSITORIES

A. HAND ROLLING
B. COMPRESSION
C. FUSION METHOD
- Molding from a melt
OINTMENTS AND OTHER
MEDICATED APPLICATIONS
 OINTMENTS
 Are semisolid preparations intended
for external application of such
consistency that they may be readily
applied to the skin with or without
inunction (rubbing)
 Are typically used as:
🟒 Emollients
🟒 Protective barriers
🟒 Vehicles
TYPES OF OINTMENTS
 MEDICATED
> Those with medicaments for the treatment
of cutaneous infections
> Examples: Sulfur Ointment, Zinc oxide
Ointment, Whitfield Ointment, Compound
Resorcinol Ointment
 NON-MEDICATED
* Also referred to as “Ointment bases”
* Used as protectants, emollients or
lubricants
 FOUR GENERAL GROUPS OF
OINTMENT BASES
(1) HYDROCARBON BASES OR OLEAGINOUS BASE
 Water free and contain petrolatum and/or modified petroleum
waxes or paraffin oil
 Retained on the skin for prolonged periods
 Do not permit the escape of moisture from the skin
 Difficult to wash-off (greasy)
 Used for emollient and occlusive action
 FOUR GENERAL GROUPS OF
OINTMENT BASES
(2) ABSORPTION BASES
 Are not easily removed from the skin
with water washing
 Useful as pharmaceutical adjuncts to
incorporate small volumes of aqueous
solutions into hydrocarbon bases
 FOUR GENERAL GROUPS OF
OINTMENT BASES
(3) WATER-REMOVABLE BASES
 Are Oil-in-Water emulsion resembling creams in appearance
 Are easily washed from the skin and are often called “WATER-
WASHABLE” bases
 May be diluted with water or with aqueous solutions
 They have the ability to absorb serous discharges
 Example: Hydrophilic Ointment, USP
 FOUR GENERAL GROUPS OF
OINTMENT BASES
(4) WATER-SOLUBLE BASES
 Commonly referred to as “greaseless”
ointment bases
 Water-washable, because of the absence of
oleaginous material
 Soften with the addition of large amount of
aqueous solutions
 Example: Polyethylene Glycol Ointment,NF –
contains PEG 3350 (40%) and PEG 400 (60%)
METHODS OF PREPARATION

1. LEVIGATION
2. MECHANICAL INCORPORATION
3. FUSION
 CREAMS
🞛 Are viscous liquids or semisolid
emulsions either the Oil-in-
Water (O/W) or Water-in-Oil
(W/O) type
🞛 Easier to spread and remove
than ointments
🞛 Prepared by fusion method
 TYPES OF CREAMS
❖ O/W CREAMS
Foundation Cream
Shaving Cream
Hand Cream
Vanishing Cream
❖ W/O CREAMS
Cold Cream – Petrolatum Rose Water Ointment
Emollient Cream
 PASTES
• Thicker and stiffer than ointments
• More absorptive and less greasy than ointments
• Effective employed to absorb serous secretions and therefore
preferred for crusting and oozing lesions
• Not generally suited for application to hairy parts of the body
• Example: Zinc oxide Paste –Lassar’s Plain Zinc Paste
 PLASTERS
• Are solid or semisolid adhesive masses
spread upon a suitable backing material and
intended for external application to a part of
the body to provide prolonged contact at that
site
COMPONENTS
• Backing Material
• Adhesive material
• Medicinal Substances
 TYPES OF PLASTERS
 MEDICATED
🟒 Salicylic Acid Plaster (Corn Plaster) –
Keratolytic
🟒 Chili Plaster
🟒 Antiseptic Plaster
🟒 Salonpas
 NON-MEDICATED
🟒 Used to provide protection or mechanical
support
🟒 Examples: Leukoplast, Micropore,
Bandages
 GLYCEROGELATINS
• Are plastic masses intended for topical
application and containing:
✯Gelatin – 15 %
✯Glycerin – 40 %
✯Water – 35 % and
✯An added Medicinal substance as Zinc
Oxide – 10 %
• Melted prior to application, cooled and
applied with a fine brush
• Official glycerogelatin is ZINC GELATIN (Zinc
Gelatin Boot) – used in the treatment of
varicose ulcers
 CATAPLASMS/POULTICES
 Are ointment like preparations
intended for warm, external
application to a body surface for the
purpose of reducing inflammation
and/or allaying pain
 Should be warmed before application
and applied with a piece of cloth
 Example: Numotizine® Cataplasm
 CERATES
Harder than ointments since it contains
higher percentage of wax

CEMENTS
Dental preparations

DRESSINGS
Paraffin Dressing, NF
Surgical Dressing
LIQUID DOSAGE
FORMS
 SOLUTIONS

Are liquid preparations that contain one

or more substances dissolved in water or
co-solvent mixtures
 SOLUBILITY
▪ It indicates the maximum concentration
to which a solution can be prepared
from the solute and the solvent
 DESCRIPTIVE TERMS
OF SOLUBILITY
Descriptive Term Parts of Solvent
Required to Dissolve
1 part of the Solute
Very soluble Less than 1
Freely soluble 1 to 10
Soluble 10 to 30
Sparingly soluble 30 to 100
Slightly soluble 100 to 1000
Very slightly soluble 1000 to 10,000
Practically insoluble More than 10,000
 SOME SOLVENTS FOR LIQUID
PREPARATIONS
▪ ALCOHOL, USP
▪ DILUTED ALCOHOL, NF
▪ RUBBING ALCOHOL
▪ GLYCERIN, USP
▪ ISOPROPYL RUBBING ALCOHOL
▪ PROPYLENE GLYCOL, USP
▪ PURIFIED WATER, USP
 TYPES OF SOLUTIONS
As to its use: As to composition
1. Oral solutions ▪ Aromatic waters
2. Topical solutions ▪ Syrups
3. Ophthalmic solutions ▪ Elixirs
4. Nasal and Otic ▪ Spirits
solution ▪ Tinctures and fluidextracts
▪ Douches, Enemas and
gargles
▪ Liniments, collodions, and
others
 ORAL SOLUTIONS
ADVANTAGES DISADVANTAGES
1. Homogenous 1. Bulky
2. Easier to swallow than 2. Degrade more rapidly
the solid dosage forms 3. More likely to interact
3. Onset of action and with other constituents
bioavailability of drugs
that have slow
dissolution rate are
improved
 ORAL SOLUTIONS…..
▪ DRY POWDER FOR SOLUTION
🟒 Dry powder for reconstitution prior to use
🟒 Examples: Cloxacillin Na, Oxacillin Na and Penicillin V K
for oral solution (antibiotics)
▪ ORAL REHYDRATION SOLUTION
🟒 Available in liquid or powder/packet for reconstitution
🟒 Examples: Pedialyte and Rehydrate solution, Glucolyte,
Oresol
▪ ORAL COLONIC LAVAGE SOLUTION
▪ OTHERS – Magnesium citrate solution
 2. TOPICAL SOLUTIONS
▪ Employ an aqueous vehicle
▪ Should be labeled “FOR EXTERNAL USE ONLY”
Examples:
1. Aluminum Acetate Solution
2. Calcium Hydroxide Topical Solution
3. Hydrogen Peroxide Topical Solution
4. Chlorhexidine Gluconate Solution
5. Povidone Iodine Solution
6. Strong Iodine Solution
 3. OTIC SOLUTIONS
▪ Ear or aural solutions
USES:
▪ For the removal of excessive cerumen
Examples: Cerumenex Ear drop, Debrox
Drops
▪ For the treatment of ear infections,
inflammation, or pain
Examples: Auralgan Otic Solution,
Americaine Otic, Chloromycetin Otic,
Corticosporin Otic, Otobiotic solution, VoSol Otic
Solution
 4. NASAL SOLUTIONS
▪ Administered as nose drops or sprays
EXAMPLES:
1. Afrin Nasal Drops and Nasal Spray, Nasalide and Privine Nasal
Solution - Decongestant
2. Beconase AQ Nasal Spray and Nasalcrom Nasal Spray – for
the prevention and treatment of perrenial allergic rhinitis
3. Salinase and Ocean Mist – to restore moisture and relieve
dry, crusted and inflamed nasal membrane
4. Syntocinon Nasal Spray – employed for initial milk let-down
preparatory to breast feeding
5. Diapid Nasal Spray - antidiuretic
 METHODS OF PREPARING SOLUTIONS
SIMPLE SOLUTION METHOD
Example: Strong Iodine Solution
SOLUTION BY CHEMICAL REACTION
Example: Magnesium Citrate Solution
SOLUTION BY EXTRACTION
 SOLVENTS FOR ORAL LIQUID DOSAGE
FORMS
▪ WATER
▪ ALCOHOL (Ethyl alcohol and Ethanol)
- alcohol limit for children: 0.5% - under 6 years of age; 5% -
6 to 12 years old; 10% - 12 years old and above
▪ GLYCERIN
▪ PROPYLENE GLYCOL
▪ POLYETHYLENE GLYCOL 400
 PHARMACEUTICAL SOLVENT WATERS
PURIFIED WATER, USP
WATER FOR INJECTION, USP
STERILE WATER FOR INJECTION, USP
BACTERIOSTATIC WATER FOR INJECTION, USP
STERILE WATER FOR INHALATION, USP
STERILE WATER FOR IRRIGATION, USP
* WFI, SWFI and BWFI are discussed in Chapter 15
PURIFIED WATER, USP
▪ Obtained by: distillation, reverse osmosis or by ion
exchange treatment
▪ pH 5 to 7
▪ Contains NMT 10 ppm of total solids
▪ Used in preparations and in finished and manufactured
products, except for the preparation of parenterals and
ophthalmic products
 WATER FOR INJECTION, USP
 Conforms with the standards of Purified Water,
USP but is also pyrogen-free
 Intended to be used in the manufacture of
injectable products which are to be sterilized
after their preparation
 Intended to be used for 24-hours after its
collection
 STERILE WATER
FOR INJECTION, USP

▪ WFI that has been sterilized

▪ Packaged in single-dose containers of type I
or type II glass that do not exceed the capacity
of 1 liter
▪ Intended to be used as a solvent, vehicle or
diluent for already-sterilized and packaged
injectable medications
BACTERIOSTATIC WATER FOR INJECTION,
USP
▪ SWFI that contains one or more suitable
bacteriostatic agents
▪ Packaged in pre-filled syringes or in vials
containing NMT 30 mL
▪ Employed as a sterile vehicle in the
preparation of small volumes of injectable
preparations (in multiple-dose vials)
▪ To be labeled “NOT FOR USE IN NEWBORNS”
 STERILE WATER FOR IRRIGATION, USP
▪ Same requirements as SWFI except in
container design, particulate matter and
labeling
▪ Labeling:
▪ “ For Irrigation Only ”
▪ “ Not for Injection ”
 AROMATIC WATERS
▪ Are clear, saturated aqueous solutions of
volatile oils or other aromatic or volatile
substances
▪ A pleasantly flavored vehicle for water soluble
drugs or an aqueous phase in an emulsion or
suspension
▪ Addition of electrolytes may result to “salting-
out” of the volatile ingredient
▪ Stored in a tight, light-resistant containers
 GARGLES
▪ Are solutions used to treat the pharynx
and the nasopharynx by forcing air
through the lungs thru the gargle which
is held in the throat
▪ Must be diluted with water prior to use
▪ Examples: Phenol Gargle, Betadine
Gargle, Bactidol
 MOUTHWASHES
▪ Are aqueous solutions most often used
for their deodorizing, refreshing and
antiseptic effect.
▪ Often used cosmetically than
therapeutically
▪ Examples: Listerine, Astring-O-sol,
Mouthwash, NF
▪ OTHER WASHES
▪ EYE WASH - Collyrium
▪ NASAL WASH - Collunarium
 DOUCHES
▪ Are aqueous solutions directed against a part or
into a cavity of the body
▪ Functions as cleansing or antiseptic agent
▪ Usually administered into a body part using a
bulb syringe
KINDS
1. Eye douche
2. Nasal douche
3. Pharyngeal douche
4. Vaginal Douche
 VAGINAL DOUCHES
🏵May be prepared from powders or from
liquid solutions or liquid concentrates
🏵Used for irrigative cleansing of the
vagina
 ENEMAS
Are RECTAL INJECTIONS
employed to:
1. Evacuate the bowel
2. Influence the general system by
absorption
3. Affect locally the seat of disease
4. Visualize the GIT for diagnosis
TYPES OF ENEMA
I. EVACUATION ENEMA
▪ Used to cleanse the bowel
▪ Fleet enema®
II. RETENTION ENEMA
a. Nutritive enema
b. Medicated enema
c. Diagnostic enema
– Barium Sulfate Enema
SYRUPS

Are concentrated, aqueous preparations

of a sugar or sugar substitutes with or
without added flavoring agent and
medicinal substances
 SWEET/VISCID SOLUTIONS
Examples Uses
Cherry syrup Vehicles for drugs that are stable in acidic
medium
Orange syrup Vehicles for drugs that are stable in acidic
medium
Cocoa syrup Used to mask the bitter taste of drugs
Raspberry syrup Mask the sour/salty tastes of drugs
Acacia syrup Mask the taste of urea
Glycyrrhiza syrup Mask the bitter taste of Vitamin B complex
Aromatic eriodyctyon Mask the bitter taste of alkaloids
Simple syrup Also known as “ ”
Has an 85% w/v or 65% w/w concentration
Has a specific gravity of 1.313
Self-preserving
PHARMACEUTICAL CLASSIFICATION

A. SUGAR-BASED SYRUP
 Sucrose is commonly employed
 Imparts a characteristic “body” to the
preparation
 Glycogenetic
 Sorbitol or glycerin may be added to
prevent crystallization
 Are clear, sweetened,
hydroalcoholic solutions
intended for oral use, and
are usually flavored to their ELIXIRS
palatability
ELIXIRS
ALCOHOL CONTENT
– VARY FROM 5 – 40 %
1. HIGH ALCOHOLIC ELIXIR (HAE) – 75 to 78% alcohol
2. LOW ALCOHOLIC ELIXIR (LAE) – 8 to 10 % alcohol
COMPONENTS:
▪ Alcohol and water – primary solvents
▪ Adjunct solvents – glycerin and propylene glycol
▪ Sweeteners
▪ Flavorants and colorants
▪ Medicinal substances
ELIXIRS
PREPARATION OF ELIXIRS
▪ By simple solution method
▪ By admixture of two or more liquids

▪ STORAGE:
Stored in a tight, light-resistant
containers and protected from excessive
heat
SPIRITS OR ESSENCES
●Are alcoholic or hydroalcoholic solutions of
volatile substances

●High alcohol content, usually over 60%, maintains

water-insoluble volatile oils in solution

●Addition of water results to the separation of the

oil
USES OF SPIRITS
MEDICINAL SPIRITS
AROMATIC SPIRIT OF AMMONIA – a reflex stimulant
FLAVORING SPIRITS
Ex.: Compound Orange Spirit, Compound Cardamom
Spirit
HOW ADMINISTERED?
Taken orally
🟒 Brandy and Whisky
🟒 Mixed with a portion of water to
reduce pungency of the spirit
Applied externally
Used by inhalation
🟒 Aromatic spirit of ammonia
METHODS OF PREPARATION
Distillation
- Brandy (48 – 54 % alcohol) and Whisky
(47 – 53% alcohol)
Solution with Maceration
– Peppermint Spirit
Solution by Chemical Reaction
– Ethyl Nitrite Spirit
Simple Solution
– Ammonia Spirit (Spirit of Sal Volatile)
 LINIMENTS
🖐 Formerly called EMBROCATIONS

🖐 Are alcoholic or oleaginous solution or emulsion of various

medicinal substances intended for external application to
the skin, generally with rubbing

🖐 Must bear a label indicating

“FOR EXTERNAL USE ONLY”

“ Not to be applied to broken skin”

TYPES OF LINIMENTS
1. Alcoholic Liniments
▪ Used for its rubefacient property
2. Oily Liniments
▪ Useful when massage is required
3. Dental Liniments – not official
EXAMPLES:
1. White Liniment, BPC
2. Camphor Liniment
3. Efficascent Oil
4. Omega Pain Killer
 COLLODIONS
 Ethereal solutions
 Are liquid preparations composed of pyroxillin
(soluble gun cotton, collodion cotton) dissolved in
a solvent mixture usually composed of alcohol
and ether with or without added medicinal
substances
 Intended for external use only
 Applied to the skin with a fine camel’s hair brush
or glass applicator
 Stored in a tight-closed container at a
temperature not exceeding 30°C remote from fire
 EXAMPLES AND USES OF COLLODIONS
I. COLLODION, USP
 Useful in holding the edges of an incised wound
together
 Has a disadvantage of being non-flexible
II. FLEXIBLE COLLODION, USP
 Prepared by adding 2% camphor and 3%
castor oil
III. SALICYLIC ACID COLLODION, USP
 A 10% salicylic acid in Flexible Collodion
 Used as a keratolytic agent
GLYCERITES
 Are viscous solutions or mixtures of
medicinal substances in NOT LESS THAN
50% by weight of GLYCERIN
 Used as a medicinal agent or as an aid in
dissolving other drugs in water or alcohol
Examples:
1. Starch glycerite - topical protectant
2. Tannic Acid glycerite - astringent
3. Phenol glycerite
OLEOVITAMINS
 Vitamins A and D in fish liver oil
 COD LIVER OIL (Oleovitamin A and D)

TOOTHACHE DROPS
 Preparations used for the temporary relief of
toothache
 Applied using a small pledget of cotton
saturated with the product into the tooth cavity
 Contains clove oil and mixtures of phenol with
camphor or creosote
EXTRACTIVES

Obtained from plants and are

commonly called GALENICALS

TINCTURES
FLUIDEXTRACTS
EXTRACTS
Are alcoholic or
hydroalcoholic
TINCTURES
solutions of chemicals
or soluble constituents
of vegetable drugs
METHODS OF EXTRACTION

MACERATION
PERCOLATION
INFUSION
DIGESTION
DECOCTION
TOPICAL TINCTURES
 Can cause stinging sensation when applied
to abraded or broken skin
Examples:
1. Compound Benzoin Tincture – topical
protectant
2. Iodine Tincture - germicide
3. Thimerosal Tincture – antiseptic

NON MEDICATED TINCTURES

used as flavoring agents
Examples: Vanilla Tincture, Sweet Orange Peel
Tincture, Tolu Balsam Tincture
VARIATIONS IN TINCTURES
As to alcohol content:
 Contains approximately 15 – 80 % alcohol
Examples:
1. Opium Tincture – 17 to 21 % alcohol
2. Compound Benzoin Tincture – 74 to 80%
alcohol
3. Iodine Tincture – 44 to 50% alcohol
4. Thimerosal Tincture – about 50% alcohol
VARIATIONS IN TINCTURES

• AGING CAN CAUSE THE PRECIPITATION OF THE

INACTIVE CONSTITUENTS IN TINCTURES

●Glycerin may be added to

increase the solubility of the active
constituents and reduce precipitation during
storage

❖Stored in a light-resistant containers

FLUIDEXTRACTS
 Are liquid extracts of vegetable drugs that
contain alcohol as a solvent, preservative, or
both
 Prepared by Percolation
 Sometimes referred to as “ 100% tinctures”
 Are considered too potent for self
administration, and too bitter
 Used today as sweetening or flavoring
agents
EXTRACTS
 Concentrated preparations of
vegetable or animal drugs obtained by
removal of the active constituents of
the respective drugs with suitable
menstrua, evaporation of all or nearly
all of the solvent, and adjustment of the
residual masses or powders to the
prescribed standards
THREE FORMS OF EXTRACTS
 SEMI-LIQUID EXTRACTS
- syrupy consistency
 PILULAR OR SOLID EXTRACTS
🙢 plastic consistency
🙢 preferred in compounding ointments or
pastes
 POWDERED EXTRACTS
※ dry
※ preferred in compounding powders, tablets,
and capsules
DISPERSED SYSTEM
SUSPENSION
 A two-phase system consisting of finely divided solid
(suspensoid) dispersed in a liquid vehicle.
COMPOSITION
A. Dispersed phase
B. Dispersion medium
 A third component may be present, the suspending agent
SUSPENDING AGENTS
1. HYDROPHILIC COLLOIDS
 Increase the viscosity of water by binding water
molecules
 Support the growth of microorganisms
 Mostly anionic, except methylcellulose (neutral) and
chitosan (cationic)
 Incompatible with quaternary antibacterial agents
 Mostly are insoluble in alcoholic solutions
EXAMPLES OF HYDROPHILIC COLLOIDS
 Acacia –used as 35% mucilage; form colored complex with
organic compounds due to peroxidase natural

 Tragacanth – used as 5% dispersion in water; does not contain

peroxidase
 Methylcellulose semi synthetic

 Carboxymethylcellulose
 SUSPENDING AGENTS

2. CLAYS
 Silicates that are anionic in aqueous dispersion
 Strongly hydrated
 Exhibit thixotropy
 Examples: Bentonite (as 5% magma), Veegum
3. OTHER AGENTS
 Agar, chondrus (carrageenan),gelatin, pectin,
gelatinized starch
TYPES OF SUSPENSION
1. ORAL SUSPENSIONS
 Ready to use
 Dry powders for reconstitution
 Uses: Antacid, anthelmintic, antibacterial (see table 14.1
pp.399-401 for examples)
2. SUSPENSIONS FOR INJECTION
 Particles must exhibit “ syringebility”
TYPES OF SUSPENSION
3. OPHTHALMIC SUSPENSIONS
 Particle size must not exceed 10 microns
4. SUSPENSIONS FOR TOPICAL USE
 Fine particles are desired to avoid grittiness when applied
to the skin
 The smaller the particle size, the greater the covering and
protective power of the preparation.
CLASSES OF SUSPENSION
I. LOTIONS
II. GELS
III. MAGMAS AND MILKS
IV. MIXTURES
 LOTIONS
 Suspensions for external application
 Prepared by:
(1) Trituration method
(2) By chemical reaction method

TYPES OF LOTIONS
I. MEDICINAL LOTION
II. COSMETIC LOTION
 MEDICINAL LOTIONS
 CALAMINE LOTION – antipruritic; use to
relieve itching and pain of sunburn, insect
bites and other minor irritations
 BENZYL BENZOATE LOTION – used for scabies

 PHENOLATED CALAMINE LOTION –

anesthetic and antiseptic
 WHITE LOTION – for the treatment of acne and
antiseptic
COSMETIC LOTION
 Areapplied to hair, scalp,
face and hands
 Popular
as sunscreen
preparations
GELS
 Are semisolid systems consisting of either
suspensions made up of small inorganic
particles or large organic molecules
enclosed and interpenetrated by a liquid
CLASSES OF GELS
As to composition:
1. INORGANIC GELS – two-phase system
2. ORGANIC GELS – single phase system
As to dispersion medium used:
1. HYDROGEL
2. ORGANOGEL
CLASSES OF GELS
 SINGLE PHASE GEL
🟒 Macromolecules are distributed in the dispersion medium
in such manner that no apparent boundaries exist between
them
 TWO-PHASE GEL
🟒 Consist of floccules of small distinct particle and
frequently called MAGMA or MILK
TERMINOLOGIES RELATED TO GELS
 IMBIBITION
 SWELLING
 SYNERESIS
MAGMAS AND MILKS
 Are aqueous suspensions of insoluble inorganic drugs and
differ from gels mainly that the suspended particles are larger
USES OF MAGMAS AND MILKS
• Suspending agent for internal and external use – Bentonite
Magma
• As medicinal antacid – Milk of Magnesia
MIXTURES
 Are aqueous liquid preparations which contain suspended
insoluble solid substances and are intended for internal use.
 Less viscous
 Examples: Kaolin Mixture, Kaolin Mixture with Pectin, Brown
Mixture
 EMULSION

A TWO-PHASE SYSTEM CONSISTING

OF AT LEAST ONE IMMISCIBLE LIQUID
INTIMATELY DISPERSED IN ANOTHER IN
THE FORM OF DROPLETS
PHASES OF EMULSIONS

1. DISPERSED PHASE – the liquid droplet, internal phase,

or discontinuous phase
2. DISPERSION MEDIUM – external, or continuous phase
TYPES OF EMULSION
◎ W/O emulsion – if water is the internal phase
◎ O/W emulsion – if water is the external phase
CLASSES OF EMULSIFIERS
▪ Natural Emulsifiers
▪ Animal-Derived
▪ They are usually protein materials and favor the formation of o/w
emulsions
▪ Examples:
▪ Gelatin [makes the emulsion too fluid]
▪ Egg yolk
▪ Casein
▪ Wool fat
▪ Cholesterol
CLASSES OF EMULSIFIERS
▪ Natural Emulsifiers
▪ Animal-Derived
▪ They are usually protein materials and favor the formation of o/w
emulsions
▪ Examples:
▪ Gelatin [makes the emulsion too fluid]
▪ Egg yolk
▪ Casein
▪ Wool fat
▪ Cholesterol
 SYNTHETIC EMULSIFIERS
 ANIONIC AGENTS – include sulfuric acid
esters, sulfonic acid derivatives, and soaps
⮲Alkali soaps – form O/W emulsion
⮲Metallic soaps – form W/O emulsion
⮲Monovalent and polyvalent soaps – form
W/O emulsion
 CATIONIC AGENTS
⮚Used as surfactant in 1% concentration
⮚Example: Benzalkonium chloride
 SYNTHETIC EMULSIFIERS
NONIONIC EMULSIFIERS
🙢Resistant to the addition of acids and
electrolytes
Examples:
🙢Sorbitan esters – Spans, hydrophobic, low
HLB values, form W/O emulsions
🙢Polysorbates – Tweens, hydrophilic, high
HLB values, form O/W emulsions
HLB SYSTEM
 Used to classify surfactants
HYDROPHILIC SURFACTANTS
❖ High HLB values (>10)
❖ Form O/W emulsion
LIPOPHILIC SURFACTANTS
❖ Low HLB values (1-10)
❖ Form W/O emulsion
APPLICATION OF SURFACTANTS
HLB VALUE RANGE SURFACTANT
APPLICATION
1–3 Antifoaming agents
4–6 Water-in-Oil emulsifiers
7–9 Wetting agents
8 – 18 Oil-in-Water emulsifiers
13 – 15 Detergents
10 – 18 Solubilizing agents
CLASSES OF EMULSIFIERS
▪ Finely Divided Solids
▪ These include the colloidal clays
▪ Examples
▪ Bentonite [aluminum silicate]
▪ Veegum [magnesium aluminum silicate]
METHODS OF PREPARATION
1. WET GUM METHOD (English method) - 4:2:1 of oil:water:gum
2. DRY GUM METHOD (Continental method)
3. BOTTLE METHOD – 3:2:1 OR 2:2:1 ratio of oil:water:gum
4. NASCENT SOAP METHOD
 The soap is formed first by mixing equal volumes of oil and alkali
 The soap acts as emulsifying agent
 A 50:50 ratio of oil to water ensures sufficient emulsion
THEORIES OF EMULSIFICATION
1. SURFACE-TENSION THEORY
• The use of surfactants result in the
lowering of interfacial tension between
two immiscible liquids
2. ORIENTED WEDGE THEORY
• This theory assumes monomolecular
layers of emulsifying agent curved
around a droplet of the internal phase
THEORIES OF EMULSIFICATION
3. PLASTIC OR INTERFACIAL FILM
THEORY
• This theory places the emulsifying
agent at the interface between the oil
and water, surrounding the droplets of
the internal phase as a thin layer of
film adsorbed on the surface of the
drops
 PROBLEMS IN EMULSIONS
▪Creaming or Flocculation
▪ Refers to the aggregation of oil
globules that rise to the top of the
emulsion
▪Sedimentation
▪ Refers to the aggregation of oil
globules that fall to the bottom of the
emulsion
PROBLEMS IN EMULSIONS
▪ Cracking or Breaking or Coalescence
▪ Refers to the complete separation of internal and external phases of
the emulsion
▪ Phase Inversion
▪ A process where the emulsion changes from o/w to w/o or vice
versa
▪ It is usually prevented when the concentration of the dispersed
phase approaches or exceeds 75% of the volume of the product
AEROSOLS
 AEROSOLS
 Pressurized dosage forms designed to deliver
drug systemically or topically with the aid of
a liquefied or propelled gas (propellant)
COMPONENTS OF AEROSOL PRODUCT
❑ Product concentrate

❑ Propellant

✦Compressed gases – CO2, N2, NO

✦Liquefiable gases – saturated HC’s, CFC’s,
dimethyl ether, and HFC’s
 AEROSOLS

ADVANTAGES
 Convenience
 Stability
 Wide range of products to be dispensed as sprays,
foams, or semisolids

DISADVANTAGE
 Environment hazard
 METHODS OF FILLING AEROSOLS
I. Cold Filling
 Product concentrate and propellant
are cooled at -34.5 to -40°C

II. Pressure Filling

 METERED DOSE INHALERS (MDI’S)
SHOULD BE SHAKEN

 These devices allow a drug to be

inhaled as a fine mist of drug or
drug-containing particles for
systemic or pulmonary delivery
 Use special metering valves to
regulate the amount of formulation
and the drug that is dispensed in
each dose.
 Commonly employed in asthma
therapy
STERILE
PHARMACEUTICALS
 STERILE DOSAGE FORMS
Parenterals
■ injection ( IV)

Biologicals
■
IM SC

Irrigation Fluids
■

Dialysis Solutions
■
kidneys

Pellets or Implants
■
intradermal

Ophthalmic Preparations
■ eyes

semi permeable yung eyes so easy to penetrate yung gamot so need sterile

gram NEGATIVE cause fever

 PARENTERALS
CONSIDERATIONS
1. Sterile
2. Pyrogen free
3. Isotonic
METHODS OF STERILIZATION
1. Steam sterilization
2. Dry-heat sterilization
3. Sterilization by filtration
4. Gas Sterilization
5. Sterilization by Ionizing Radiation
 SMALL VOLUME PARENTERALS
Available in ampules, vials, or pre-filled
syringes
Package in single-dose or multiple-dose
containers (2 mL to 30 mL)
Examples:
Heparin Sodium Injection
Insulin Injection
Lidocaine HCl Injection
 LARGE VOLUME PARENTERALS
Administered by intravenous infusion to
replenish body fluids, electrolytes, or to
provide nutrition
Usually in volumes of 100 mL to 1 Liter

Employed in maintenance therapy and

replacement therapy
Examples: Ringer’s Inj., Mannitol Inj.,
Sodium Chloride Inj., Dextrose Inj.
 BIOLOGICAL PRODUCTS
Vaccines, Toxoids, Antitoxins, Immune Serum, Antivenins, Blood

derivatives, Immunologic diagnostic aids

Stored in refrigerator (between 2°C and 8°C), or freezer with a

temperature of -15°C

Examples: MMR Virus vaccine, Poliovirus vaccine, Tetanus toxoid,

Tetanus antitoxin, Antivenin polyvalent, Smallpox vaccine, Typhoid
vaccine
OPHTHALMIC PRODUCTS
Include:
1. Solutions
2. Suspension
3. Gels
4. Ointments
5. Drug impregnated inserts
6. Contact lenses
7. Contact lenses care
products
SPECIAL CONSIDERATIONS FOR OPHTHALMIC SOLUTIONS
AND SUSPENSIONS

 Sterility
 Preservation
 Isotonicity
 Buffering
 Viscosity
 Ocular
bioavailability
 Packaging
RADIOPHARRMACEUTICALS
 RADIOPHARMACEUTICALS

 Usedfor
diagnostic or
therapeutic
procedures
 Frequently
prepared as
parenteral
dosage form
 RADIOPHARMACEUTICALS
DRUG PRIMARY USES
111In capromab pendetide Monoclonal antibody for imaging prostate cancer
(ProstaScint)
123I,
sodium iodide and 131I, Thyroid imaging and uptake
sodium iodide
99mTc pertechnetate Imaging of thyroid, salivary glands, ectopic gastric
mucosa, parathyroid glands, dacryocystography,
cystography
99mTc red blood cells (Ultratag) Imaging of GI bleeding, cardiac chambers, cardiac
first-pass
99mTc sulfur colloid Imaging of reticuloendothelial system, bone marrow,
gastric emptying, GI bleeding, lymphoscintigraphy,
arthrograms
133Xe
Pulmonary ventilation imaging
90Y microspheres (TheraSphere) Therapy for biopsy-proven, unresectable
hepatocellular carcinoma
166Ho-DOTMP and 186Re-HEDP Bone cancer therapy
 POSITRON EMISSION TOMOGRAPY (PET)
RADIOPHARMACEUTICALS
- Used for imaging procedures
PET Pharmaceuticals include:
1. Carbon-11
 As a tracer, used to study myocardial
metabolism

11C glucose is use for cerebral glucose
metabolism
2. Nitrogen-13
 Used as tracer for cerebral and
myocardial blood flow
 PET RADIOPHARMACEUTICALS
3. Oxygen-15
Four 15O are available for clinical use:

15OO (oxygen gas)
 used in the study of oxygen metabolism
 C15O (carbon monoxide) –
 administered via inhalation; serves as tracer for RBC
volume
 CO15O (carbon dioxide)
 H215O (water)
 commonly used as tracer of cerebral and
myocardial perfusion
 PET RADIOPHARMACEUTICALS
4. Flourine-18
 For cerebral glucose metabolism,
myocardial glucose metabolism and tumor
glucose metabolism
5. Gallium-68
 Binds with transferrin forming 68Ga-
transferrin

68Ga-transferrin is employed in pulmonary
studies of vascular permeability
DRUG ANTIDOTE FOR
RADIATION EXPOSURE
PRUSSIAN BLUE
ferric
hexacyanoferrate
Radiogardase capsule