Module 1 Flashcards
what are drugs intended to be used for in humans or in animals?
diagnosis, mitigation, treatment, cure, prevention
drugs used to diagnose or determine a disease by…
assaying the percentage of antibodies present
given for diagnosis of diseases or thyroid related problems
radiopharmaceuticals
deals with a disease, injury, etc. in order to make someone feel better or become healthy again
treatment
what is better than a cure?
prevention
GAMOT
G - inhawa (mitigation)
A - lisin ang sanhi (cure)
M - aibalik sa normal (treatment)
U - miwas sa sakit (prevention)
T - ukuyin ang dahilan (diagnosis)
preparations designed to contain a specified quantity of medication for ease and accuracy of dosage administration
dosage form
another name for dosage forms?
pharmaceuticals
ACTIVE INGREDIENTS
active pharmaceutical agents (API), pharmacologically active therapeutic ingredients
NON ACTIVE INGREDIENTS
inert, inactive ingredients, additives, excipients
what do non active ingredients do to the pharmaceutical?
Give the formulation its unique composition and characteristic physical appearance
According to USP, it holds the article and is or maybe in direct contact with the article immediate container (the one that is in direct contact with the article at all times) closure
Container
protects the content from extraneous solids and from loss of the article under ordinary conditions of handling, shipment, storage and distribution
well-closed container
protects the contents from contamination by extraneous liquids, solids or vapors, from loss of the article and from efflorescence, deliquescence or evaporation under the ordinary or customary conditions of handling, shipment, storage and distribution and is capable of tight re-closure
tightly-closed container
an uptake of salt that causes a decrease in water
efflorescence
absorption of moisture
deliquescence
is impervious to air or any other gas under the ordinary or customary conditions of handling, shipment, storage and distribution
hermetic container
how are substances in hermetic containers delivered?
injection or parenteral preparation
provides protection from the degradative effects of light by reducing light transmission
light-resistant containers
light-resistant containers are also called…
amber bottles
added to decrease the transmission of short ultraviolet rays
ultraviolet absorbers
USP standard on limit if light transmission is between…
290-450 nm
container that is significantly difficult for
children to open or to obtain a harmful amount of its contents within a measurable time and that is not difficult for normal adults to use properly
child-resistant container
child-resistant containers are specially made for children aged…
5 years old and below
four basic designs of child resistant containers
align the arrows
press down and turn
squeeze and turn
latch top
packaging that has one or more indicators or barriers to entry which if breached or missing, can reasonably be expected to provide visible evidence that tampering has occurred.
tamper-evident container
one that holds a quantity of drug intended as a single dose and when opened cannot be resealed with assurance that sterility has been maintained
single dose
examples of single dose containers
ampules, prefilled syringes or cartridges
contains more than a single dose of the
medication and permits the withdrawal of
successive portions without changing the
strength or endangering the quality or purity of the remaining portion
multiple dose
examples of multiple dose containers
vials
type I of glass is composed of
highly-resistant borosilicate glass
what is type I, II, and III glass used for?
parenteral products
type II of glass is composed of
treated soda-lime glass
type III of glass is composed of
soda lime glass
type NP of glass is composed of
general purpose soda-lime glass
what is type NP glass used for?
other preparations
what type of glass is most resistant?
type I
plastic material that is rigid and has good
clarity;
polyvinyl chloride (PVC)
PVC is useful in
blister packaging of tablets and capsules
PVC is not suitable when
gamma sterilization is required
PET plastic used in water bottles and the likes
polyethylene terephthalate
APET
amorphous polyethylene terephthalate glycol
PETG
polyethylene terephthalate glycol
have excellent transparency and luster and can be sterilized with gamma radiation
APET and PETG
advantage of plastic containers
-Lightness in weight
-Resistance to impact
-Versatility in container design and consumer acceptance
-Consumer preference for plastic squeeze bottles
-Popularity of blister packaging and unit dose dispensing
disadvantages of plastic containers
-Permeability of the container to atmospheric oxygen and to moisture vapor
-Leaching of the constituent of the container to the internal contents
-Absorption of drugs from the contents to the container
-Transmission of light through the container
-Alteration of the container upon storage (deformity)
Statement of pharmacologic category; No Rx symbol
OTC label
prescription drug label contains…
Nonproprietary and Proprietary name of the drug
Name and address of manufacturer
Dosage strength or potency
Type of dosage form
Net content
Prescription logo and Legend statement
Label reference to see the accompanying package insert
Special storage instructions
Bar code and Registration number
Lot or control number
Expiration date
for controlled substances…
the symbol “C” and the statement “Warning: Maybe habit-forming”
OTC drug label contains…
Product name (generic and brand)
Name and address of manufacturer
Net content
Formulation
Name of any habit-forming substances
Pharmacologic category (principal intended action)
Cautions and warnings
Na+ content for oral preparations
Storage conditions
Description of tamper-evident feature
Lot number and expiration date
dietary supplement labels should contain
This statement has not been evaluated by the FDA. The product is not intended to diagnose, treat, cure or prevent any disease
herbal products should state…
specific parts of the plant used
product standardization includes
USP verified program
NSF certification program
Consumer Laboratories
assurance of product safety but not guarantee effectiveness
SEAL
any temperature not exceeding 8 degrees celcius
cold temperature
refrigerator
2 to 8 c
freezer
-25 to -10 c
any temperature between 8 to 15 c
cool temperature
temperatures between 20 to 25 c, sometimes 15 - 30 c
controlled room temperature
temperature between 30 to 40 c
warm temperature
temperature above 40 c
excessive heat
risks of freezing; breakage of container; loss of potency/strength; destructive alteration of the dosage form
protection from freezing
to protect drug substances from the destructive influence of gastric acid after oral administration
enteric coated tablets
to provide liquid preparations of substances that are either insoluble or unstable in the desired vehicle
suspension or clear preparation solution
to conceal bitter, offensive, or salty taste or odor of a drug substance
capsule, Coated tablets, syrups
to provide rate controlled drug action
controlled release tablet, capsule, suspension
to provide optimal drug action from topical administration sites
ointment, creams, transdermal patches, ophthalmic prep. ear prep, nasal prep
to provide for insertion of drug into one of the body’s orfices
rectal, vaginal suppositories
to provide placement of drug directly in the bloodstream or body tissues
injection
to provide optimal drug action through inhalation therapy
inhalants, inhalation aerosols
the formulation that best meets the goals for the product is selected to be its
master formula
pre formulation considerations
-physical descriptions
-microscopic examination
-heat vaporization
-melting point depression
-phase rule
-particle size
-polymorphism
-solubility
-dissolution
-membrane permeability
-partition coefficient
-dissociation constant
general considerations in dosage forms designs
- physical and chemical properties of the drug substance
- therapeutic considerations
therapeutic considerations
i. nature of illness
ii. manner in which it is treated
iii. age and the anticipated condition of the patient
the purity of the chemical substance substance is essential for its identification and for evaluation of its chemical, physical and biological properties
physical description
structure, form, and reactivity
chemical property
physical description, particle size, crystalline structure, melting point and solubility
physical property
ability to get to a site of action and elicit responses
biological property
Gives an indication of particle size and size range of the raw materials along with the crystal structure
microscopic examination
which flow more freely: spherical and ovals powders of needle shaped powders?
spherical and oval powders
heat vaporization
-The amount of heat absorbed when 1 g of liquid vaporizes
-Operation of implantable pumps delivering medicine
-Aerosol dosage forms
-Nasal inhalants for treating nasal decongestion
-Particle size affects vapor pressure; the smaller the particle size the greater the vapor pressure
melting point depression is used to determine
the purity of the substance
change in melting point of product means it is
not pure
a useful device for relating the effect of the least number of independent
variables (e.g., temperature, pressure, and concentration) upon the various phases (solid, liquid, and gaseous) that can exist in an equilibrium system containing a number of components.
phase rule
Certain physical and chemical properties of drug substances, including dissolution rate, bioavailability, content uniformity, taste, texture, color and stability are affected by the particle size distribution Flow characteristics and sedimentation rates Particle size influences oral absorption
particle size
polymorphism
crystal or amorphous, and affects melting point and solubility
should possess aqueous solubility for therapeutic effect
solubility
frequently added to increase solubility
salt and water
can increase solubility
adjustment in particle size and pH
rate limiting step in the absorption process
dissolution
the time it takes for the drug to be dissolved in the fluids at the absorption site
dissolution rate
To produce biological response, the drug
molecules must first cross the biologic membrane (acts as lipid barrier) permits absorption of lipid soluble substance by passive diffusion
membrane permeability
measure of drug’s lipophilic character
partition coefficient
the extend of dissociation and ionization of the drug
pKa/dissociation constant
has strong effect on drug absorption, distribution, and elimination
extent of ionization
absorbs moisture from air
hygroscopic powder
absorb moisture from air before liquefying
deliquescent powder
give up water for crystallization and may even become damp and pasty
efflorescent powder
drugs are either weak acids or weak bases and have limited water solubility, often used the salts of the product to increase the aqueous solubility
organic salt consideration
Prepared for increase solubility, stability,
resistance to degradation after administration, use of prodrug
organic ester consideration
preformulation stability studies
- Solid state stability of the drug alone
- Solution phase stability
- Stability in the presence of expected excipients
A solvolysis process in which drug interact with water to yield breakdown products of different chemical constitution
hydrolysis
examples of hydrolysis
acetylsalicylic acid + water
salicylic acid + acetic acid
also prone to hydrolytic decomposition
amides, lactones, and lactams
Involves the loss of electrons from an atom or a molecule
oxidation
oxidation is common to
aldehydes, alcohols, phenols, sugars, alkaloids, and unsaturated fats and oils
defined as the extent to which a product retains, within specified limits, and throughout its period of storage and use, the same properties and characteristics that it possessed at the time of its
manufacture
stability
each active ingredient retain its chemical
integrity and labeled potency, within specified limits.
chemical stability
chemical stability is important for
-selecting storage conditions (temperature, light, humidity)
-selecting the proper container (glass vs. plastic, clear vs. amber)
-anticipating interactions when mixing drugs
the original physical properties, including
appearance, palatability, uniformity, dissolution and suspendability are retained
physical stability
sterility or resistance to microbial growth is retained
Antimicrobial agents that are present retain effective within specified limits
microbiologic stability
the therapeutic effect remains unchanged
therapeutic stability
approaches in the stabilization of drug products against hydrolytic decomposition
-reduction of water from the pharmaceutical system
-applying waterproof protective coating
-replacing water with different substitute liquids
-usage of anhydrous vegetable oils in injectable products
-suspending drug in a nonaqueous vehicle
-supply drug in a dry form for reconstitution
-refrigeration
-use for buffering agents
-use of antioxidant
in liquid preparations, water can be frequently replaced or reduced through the use of substitute liquids such as
glycerin, propylene glycol, and alcohol
for most hydrolyzable drugs, optimum stability is on the…
acid side (pH 5 and 6)
high pH
sodium sulfite
aqueous prep
alpha-tocopherol
oleaginous prep
intermediate pH
aqueous prep
hutyl hydroxy anisole
oleaginous prep
low pH
hypophosphorous acid
ascorbic acid
aqueous prep
ascorbyl palmitate
oleaginous prep
factors that affects oxidation
-oxygen present as airspace within the container
-nitrogen trace elements in drugs, solvent, container and
stopper -chelating agent eg. EDTA
ethylenediaminetetraacetic acid)and calcium disodium edetate
light-light resistance or opaque plastic
temperature -cool place
ph of the preparation- maintain solution in pH most favorable to its stability
low MW salts
salty
high MW salts
bitter
increase hydroxyl group
increase sweetness
pleasant to taste
aldehyde, organic esters, alcohols
nitrogen compound
(plant alkaloids) bitter
aspartame
sweet
mask salty taste of drugs (Chlorides of Na, K, and Ammonium)
cinnamon, raspberry, and orange flavors
mask the bitter taste of drugs (alkaloids, epsom salt)
cocoa
combat acid or sour taste
fruit or citrus flavors
commonly used sweetener from sugar canes/beets
sucrose
less sweet than sucrose but more viscous
glycerin
300 times as sweet as sucrose; has a bitter after taste; carcinogenic in animal
saccharin
180 to 200 times sweeter than sucrose; contraindicated to phenylketonuria
aspartame
has carcinogenic potential; artificial sweetener
cyclamate
130 times as sweet as sucrose
acesulfame potassium
natural, non-toxic, safe and 30 times sweeter than sucrose
stevia powder
plant dyes
achuete
minerals
Ferric Oxide (red); it is mixed in small
portion with Zinc oxide imparting a characteristic pink color in Calamine powder
synthetic
coal tar dyes, anthracene dyes, aniline dyes
used in food, drugs, and cosmetics
FD & C (brilliant blue)
approved for use in drugs, some in cosmetics, and some in medical devices
D & C
use of which is restricted to external parts of the body, not including the lipids or any body surface covered by mucous membrane
external D & C
changes of colorant according to toxicological findings
a) withdrawal of certification
b) the transfer of colorant from one certification category to another
c) the addition of new color to the list
can cause allergic reactions to patient who has sensitivity reaction to aspirin; FDA requires the listing of this dye on the labels of food and ingested drugs containing the substance
FD & C Yellow No. 5 (tartrazine)
drug products requiring colorants
capsules
compressed tablets
sugar-coated tablets
suspension
drug products that do not contain color additives
ophthalmic products
parenteral products
ointments
suppositories
amount of liquid dyes added to liquid preparations ranges from
0.0005 to 0.001% depending ypon the colorant and the depth of color desired
a pigment consisting of a substratum of alumina hydrate on which the dye is adsorbed or precipitated.
FD and C
lake pigments are suitable for coloring products in which the moisture levels are…
low
products requiring preservatives
syrups
emulsions
semisolid preparations
ophthalmic products
parenteral (multiple-dose packages)
products not requiring preservitives
alcoholic and hydroalcoholic solutions
large volume parenterals
what percentage of alcohol in solutions will prevent microbial contamination
15-20%
parenterals and ophthalmic preparations are sterilized by
autoclaving, bacterial filtration, and dry heat, however may still require additional preservatives
frequently used in preservatives in ophthalmic preparations because of their low degree of irritant qualities
chlorobutanol, benzalkonium chloride, and phenyl mercuric nitrate
_____ are more effective in ______
acidic preservatives, acid media
_______ are less effective in acid or neutral media but more effective in _______
alkaline preservatives, alkaline media
