DDS LEC REVIEWER
Oral – through the mouth
DRUG
- An article intended for having their main use in
the DIAGNOSIS, CURE, MITIGATION, and
TREATMENT or PREVENTION of disease
- Article recognized by MONOGRAPH
- Article other than food used to effect the
structure or any function of the body of man or
animals
- Article used as a component in any of the
previously mentioned definitions
- ACTIVE INGREDIENT
- Any component that is intended to furnish
pharmacological activity or other direct effect in
the diagnosis, cure, mitigation, treatment or
prevention of disease or to affect the structure
or function of the body of man or other animals
- Includes those components that may undergo
chemical change in the manufacture of the drug
product and be present in the drug product in a
modified form intended to furnish the specified
activity and effect
ROUTES OF ADMINISTRATION
- INTRAVASCULAR
 Direct to the circulatory system
 Intravenous – directly to the vein
 2 TYPES:
1. Bolus – one time big time
injection, one
time of one dose of the drug
 Infusion – commonly known as dextrose
(suero)
 intermittent – administered at
certain point in time
(putol-putol)
 continuous – continous
administration
 Interarterial – direct to the artery
 Intracardiac – directly to the heart
chamber, used for emergency
cases e.g. Epinephrine (3rd
drip 90 degrees)
- EXTRAVASCULAR
 Enteral – it goes through the GIT
1.
2. Buccal – inside the cheeks
3. Sublingual – under the tongue
4. Rectal – to the anus
 Parenteral administration
1. Subcutaneous – subcutaneous tissue or
fats layers under the
skin
2. Intramascular – muscles (deltoid);
vaccines and oil based
drugs
3. Intradermal – under the skin
4. Intraperitoneal – addominal cavity
5. Intraocular – direct to the eyes; eye
Surgery (antiseptic)
6. Intrathecal – direct to the spinal fluid
(epidural)
 Others
1. Inhalation – respiratory system
2. Topical – to the skin only
3. Transdermal – skin but meant to
systemic absorption
4. Intranasal – inside the nose
5. Vaginal – for vaginal suppositories
6. Urethral – into the urethra
7. Ocular – drops
8. Otic – for the ears (aural)
INTRODUCTION TO DOSAGE FORMS
Dosage form
- The finished product that produces a mean of
administration for drug formulated
preparation
- Combination of a drug entity and drug additives
Drug product
- Finished dosage forms that contains drug
substance in association with the active
ingredients and excipients
ADVANTAGES OF DOSAGE FORMS
- To protect the drug substance from the
destructive influences of oxygen or humidity
- To protect the drug substances from thee
destructive influence of gastric acids after oral
administration
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 - To conceal the bitter, salty or offensive taste or 6. Fifth Generation
odour of a drug  Gene therapy
- To provide liquid preparations of drug  Treat the cause of a disease
substances, either as dispersion or as clear CATEGORIES OF DOSAGE FORMS
preparation  Based on Delivery Route
- To provide rate-controlled drug action 1. GI Tract – oral, oropharengeal, rectal
- To provide optimal drug action from topical 2. Tissues or Body Fluids
administration sites – IV, IA, IC, IM, SC, ID, IT
- To provide insertion of a drug into one of the 3. Mucosal Membrane
body’s orifices – otic, nasal, ophthalmic, vaginal,
- To provide for placement of drugs directly in Urethral
the bloodstream or body tissues 4. Skin Surface
- To provide for optimal drug actions through – topical, transdermal
inhalation therapy 5. Lungs
DEVELOPMENTS IN DOSAGE FORM DESIGN – inhalational
1. Primitive  Based on General Type
 lacked consistency, uniformity, and 1. Liquids
specificity – solutions, emulsions, suspensions,
 chewing of medicinal plant parts, inhalation inhalants, aerosols
of soot (no extraction process) 2. Semisolids
 taking of medicinal extracts – ointments, creams, gels, pastes,
 done by shamans foams, collodions
2. First generation 3. Solids
 19th century – powders, tablets, capsules, patches,
 Has consistency and uniformity (slmost all gauzes, tapes, sticks
doasage forms)  Based on Release Pattern
3. Second Generation 1. Conventional release – normal release
 1950’s 2. Modified release:
 Modified protection, prolong action,  Extended - long action (hours
improved bioavailability of effect)
 Enteric coated tablets, repeat-action forms,  Delayed – no effect instantly
prolonged action forms, time-release forms (after how many hours)
4. Third Generation  Targeted
 Mid 1960’s  Pulsatile
 Controlled DDS  Orally disintegrating
 Osmitically-controlled, swelling controlled,  Orally dispersing
magnetically- controlled, chemically- PHARMACEUTICAL EXCIPIENTS
controlled, electrically-controlled, diffusion- Excipient
controlled - Any component other than API
5. Fourth Generation - Inactive ingredient
 Control on the time of availability and - Provides the drug or API in a form of suitable
localization of the drug administration
 Targetable (site-specific) ROLES/QUALITIES OF AN IDEAL EXCIPIENT
 Modulated (pulsatile) 1. Harmless in amounts used
 Self-regulated (feedback controlled)
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 2. Does not exceed the minimum quantity
required to provide intended effect
3. Does not impair the bioavailability/therapeutic
efficacy of the dosage form
4. Does not interfere with the assays and tests
prescribed for determining their compliance for
the official standards
CATEGORIES OF PHARMACEUTICAL EXCIPIENTS
- Those added for stability
 Enhances the physical and chemical
stability of the drug product
 Buffers and preservatives
- Those added for In Vivo absorption
 For bioavailability
 Improves the capability of the drug
substances to reach general circulation
- Those added for manufacturability
 Promotes the production of the drug
substances into dosage form
 Co-solvents, solubilizers, emulsifiers,
diluents, binders, suspending agents
Compounding – small scale of production
Manufacturing – large scale production
- Those added for acceptability
 Increase patient acceptability of the
drug product
 Aesthicity
 Flavours, colours, sweetening agent,
viscosity enhancers
 Flavours and colours must match
PACKAGING, LABELING, AND STORAGE OF
PHARMACEUTICALS
Packaging
- An economical means of providing:
1. Presentation – presentable
2. Protection – bottles, blister packs
3. Identification/information – leaflets
4. Containment – secondary packaging
5. Convenience – easy transport
6. Compliance – for regulation of
pharmaceuticals
- For a product during storage, carriage, display,
and use until such time as the product is used or
administered
- Types of Package System:
 Primary
- Intermediate container
- Direct contact with the product
o Contain product
o Administer drug
- Direct effect on the product shelf-
life
o Prevent product
deterioration
 Secondary
- Outer packaging
- No direct contact with the product:
boxes
- Additional physical protection
o Ensure the safe storage in
warehouses and delivery of
the product
PRIMARY PACKAGE SYSTEM
1. Container – holds the drug
2. Liner – effects a hermetic seal between the
closure and the container
3. Inner Seal – for a more positive seal surface
and to provide tamper-evidence
4. Coil – Prevents damage during shipping
5. Dessicant – counteracts moisture brought by
the coil
6. Cap or closure – provides an effective seal
 Screw, threaded, lug, crimp-on, crown,
press-on, snap, roll-on, child-resistant (for
children not to open since they cannot
produce two simultaneous actions),
tamper-resistant (seals) or tamper-evident,
vacuum, linerless, dispenser, applicators
SECONDARY PACKAGE SYSTEM
1. Inserts – leaflets inside the packaging
2. Boxes
3. Cartons
4. Corrugated shippers
5. Pallets
CATEGORIES OF CONTAINERS:
 According to protection ability
o Well-closed container – protects
loss of drugs and extraneous solids
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 o Tight container – protects against o Oral solid and liquid DF; external
solids, liquids, and gases, loss of preparations
drugs, vapours o POWDER GLASS TEST
o Hermetic container – inprevious to 2. Plastic
air or gas under ordinary conditions  ADVANTAGES:
e.g. vials, aerosols. ONE TRUE light weight and durable
TAMPER RESISTANT CONTAINER:  DISADVANTAGES:
AEROSOL Permeability and leaching
o Light resistant container – protect  THERMOSETS:
from light e.g. amber bottle Rigid, non-meltable plastic
 According to quantity held made by melting of powder
o Single-unit – holds single dose  THERMOPASTICS:
o Multiple-unit – holds more than Flexible, polymer materials
single dose 3. Metal
MATERIALS USED IN PACKAGING  Laminated, coated or uncoated
1. Glass aluminium; tin
 ADVANTAGES: For semisolid preparations
Good barrier properties Caps, tubes, jars
Inert Strips, blisters
Transparency 4. Rubber
Sparkle  Synthetic/natural
Easy cleaning Synthetic since mas sure sa
Effective closuring and reclosing compisition
Rigidity and stackability  Stoppers, droppers
OFFICIAL GLASS TYPES 5. Paper and board
 Type 1  Pouches, boxes, cardboard backing
o Highly resistant borosilicate glass  Label and inserts
o Neutral glass Drug Labelling
o Buffered and non-buffered aq sol’n - Includes labels and information
o All purpose placed on package
o POWDERED GLASS TEST - Ensures safe use of the drug
 Type 2 product
o Treated soda lime glass - Summary information of the
o Surface-treated soda glass medicine
o Buffered solutions of pH less than 7; - Summary information of the inserts
dry powders Summary Information on Label of Dispensed Medicine
o WATER ATTACK TEST - Name of Preparation
 Type 3 - Quantity
o Soda-lime glass - Instructions for the patient
o Soda/alkali glass - Patient’s Name
o Dry owders/substances; - Date of Dispensing
oily/oleaginous solutions - Name and address of the pharmacy
o POWDER GLASS TEST - “keep out of reach of children”
 Type NP - Warning, batch number, expiry date, additional
o General purpose soda-lime glass legal
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 - Requirements
- Description – names of the active ingredient,
route of administration, formula
- Clinical Pharmacology – action in humans
- Indications and Usage – approved indication in
the treatment,
prevention, or diagnosis
of a
disease or condition
- Contraindications – situations in which the drug
should not be used
- Warnings – description of undesirable reactions
- Precautions – special care to be exercised by
prescriber and patient
- Adverse Reactions – predictable and potential
Unpredictable and
undesired effects
- Drug abuse and dependence – psychological
and physical
dependence
potential
- Overdosage – signs, symptoms, and laboratory
findings of acute overdosage
- Dosage and Administration – recommended
usual dose
- How Supplied – availability of dosage forms
STORAGE OF PHARMACEUTICALS
• Cold
 Not exceeding 8℃ (46℉)
 Refrigerator: 2℃ to 8℃ (36 - 46℉)
 Freezer: -25℃ to -10℃ (-13℉ to -14℉)
• Cool
 8℃ to 15℃ (46℉ to 59℉)
• Room Temperature
 Temperature prevailing in the working
area
• Controlled Room Temperature
 20℃ (68℉) to 25℃ (77℉)
 Allows for temperature variations
between 15℃ (49℉) to 30℃ (86℉) that
may be experienced that may be
experienced in pharmacies, hospitals
• Warm
 30℃ (86℉) to 40℃ (104℉)
• Excessive Heat
 Above 40℃ (104℉)
• Protection from Freezing
 Indicated when in addition to the risk of
breakage of the container, freezing
subjects a product to loss of strength or
potency, or to destructive alteration of
the dosage form
• No specific storage or limitations
 Protection from moisture, freezing, and
excessive heat
CURRENT GOOD COMPOUNDING PRACTICES
Compounding
- Preparation, mixing, assembling, packaging or
labelling of a drug or device
- Extemporaneous compounding
- Compounding environment
- Stability of compounded preparations
- Quality control
- Patient counselling
- -compounding small scale
Manufacturing
-
INTERNATIONAL CLIMATIC ZONES
1. Zone I – temperate
2. Zone II – subtropical (w/ possible high humidity)
3. Zone III – hot/dry
4. Zone IV – hot/humid (PHILIPPINES)
NEW DRUG DEVELOPMENT PROCESS
1. Discovery of new chemical entity
2. Pre-clinical studies: animal studies
3. Investigation New Drug Application
4. Preclinical studies and clinical trials
 After proving that it’s safe
5. NDA
 Proof that it could be marketed
6. Post marketing
Drug Discovery and Design
- Multidisciplinary approach
- OTC drugs, Prescription drugs, biologics
- Largest pharmaceutical companies
- Sources of new drugs
 Natural sources
 Plant, animal, marine
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  Synthetic sources adsorption, distribution, metabolism, and
 Genetic sources excretion
 Recombinant DNA Animal Models
 Monoclonal antibody - Rats: hypertension, CNS
production - Mice: CNS
 Gene therapy - Dogs: hypertension, Respiratory, diuretic action
Goal drug - Guinea pigs: respiratory
- Specifically desired effect (one target effect) - Rabbits: fever, blood coagulation
- Most desired effect Drug metabolism
- Minimal dosage and dosing frequency (to - To ensure that the drug has been released
ensure the effect) completely from the body
- Optimal onset and duration of action Toxicology
- No side effect - To test toxicity of drugs
- Eliminated efficiently, completely and w/out PRE-FORMULATION STUDIES
residual effect (secreted completely out of the - Studies aimed at collectiong basic information
body) on the physical and chemical characteristics of
the drug substances to be prepared into
Methods of Drug Delivery pharmaceutical dosage forms
1. Random/untargeted screening - Goal: to find the optimal delivery system
2. Bioassays
3. High-throughput screening (library of
compounds to be tested in one test)
4. Molecular modification
 Mechanism-based drug design
Lead Compound
- Prototype chemical compound
- Has the fundamental biologic or pharmacologic
activity
- Posses all the desired features of drug
- Modifies to achieve desired features and lessen
undesired ones
Prodrugs
- Compound that requires metabolic
biotransformation after administration to
produce the desired active compound
- Needed to take before it takes an action or
transform into a drug that has an effect to the
body
- Needed to make to ensure solubility, bio
stability, and prolonged release of a drug
BIOLOGIC CHARACTERIZATION
Pharmacology
- Study of biochemical and psychologic effects of
a drug, mechanism of action, ADME:

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