Module 9 Flashcards
The _______ is rarely administered solely as pure
substance but almost always given in a dosage form.
active (API)
A _______ is formulated invariably using drug and
excipient(s) in appropriate proportions.
dosage form
The proper design and formulation of a dosage form
requires consideration of the physical, chemical, and
biologic characteristics of ________ to be used in fabricating the drug product.
ALL OF THE PHARMACEUTICAL
INGREDIENTS
Selection of correct ______ in correct proportions is an
important step in formulation development.
excipients
Though excipients are defined as therapeutically inactive,
it is a well-established fact that they may interact with the
________and other _________ in the formulation.
API; excipients
Based on already existing information about _________ it is relatively easy for a
formulator to select an appropriate excipient for the ________ to be formulated
excipients; dosage form
_________ is the process in which different chemical
substances (i.e., actives and excipients), are combined to fabricate a final medicinal product of a desired dosage form (i.e. syrup, tablet, capsule, injectable liquid, or powder, etc.).
Drug Formulation
A dosage form is the _______ of a dose of a drug intended for administration or consumption.
physical form
A dosage form is a _______ by which the drug is delivered to the body.
system or device
The ________ for drug delivery is dependent on the dosage form of the substance in question.
route of administration
BCS class for high solubility and high permeability through a simple solid oral dosage form.
BCS1
BCS class for low solubility and high permeability with techniques to increase surface area like particle size reduction, solid solution, solid dispersion, wth solutions using solvents and/or surfactants.
BCS2
BCS class for high solubility and low permeability that incorporates permeability.
BCS3
BCS class for low solubility and low permeability that incorporates oral dosage techniques that combine BCS2 and BCS3.
BCS4
Principally a _________ is formulated to achieve predictable
therapeutic response of a drug included in the formulation.
dosage form
A dosage form provides an _______ of the drug being administered.
accurate dose
Note that a vast majority of drugs are administered in _________ (sometimes even in micrograms). This is much too small to be weighed only on a sensitive laboratory scale.
milligrams
Classification based on
Route of Administration (Dosage Forms)
Topical
Parenteral
Vaginal
Nasal
Oral
Rectal
Respiratory
Opthalmic
Others
Classification based on
Physical Form (Dosage Forms)
Solid
Semi-Solid
Liquid
Gaseous
Classification of Dosage Form
Physical state
Route of administration
Uses
Site of application
Oral Routes of Administration
- Powders
- Tablets
- Capsules
- Suspensions
- Solutions
- Emulsions
- Elixirs
- Syrups
- Magmas
- Sachets
- Gels
- Pills
Parenteral Routes of Administration
- Solutions
- Suspensions
- Emulsions
Transdermal Routes of Administration
- Ointments
- Powders
- Creams
- Lotions
- Pastes
- Plasters
Intra-Ocular Routes of Administration
- Solutions
- Suspensions
- Ointments
Sublingual Routes of Administration
- Tablets
- Lozenges
Vaginal Routes of Administration
- Suppositories
- Tablets
- Ointments
- Creams
- Douches
Conjunctival Routes of Administration
- Ointments
Intra-Respiratory Routes of Administration
- Aerosols
Rectal Routes of Administration
- Suppositories
- Enemas
- Ointments
Intra Nasal Routes of Administration
- Solutions
- Sprays
- Inhalations
Urethral Routes of Administration
- Suppositories
Solid dosage forms
- Unit dosage forms (tablets, capsule, powders, pills)
- Bulk (internal and external)
Solid bulk dosage forms
- Internal (fine powders and granules)
- External (dusting powders, insufflations, dentifrice, snuffs, ear powders)
Liquid dosage forms
- Biphasic (emulsion, suspension)
- Monophasic
Monophasic liquid dosage forms
- Internal (syrups, elixirs, linctus, drops)
- External (liniments, lotions, gargles, throat paints, mouth washes, sprays, eye lotions, eye drops, nasal drops)
Semi-solid dosage forms
- Internal (suppositories, pessaries)
- External (ointment, creams, pastes, jellies)
The ____ route of drug administration is the most convenient for
patients, with tablets emerging as the most popular solid _______ dosage form used today.
oral
Solid dosage forms
containing finely
divided particles in
micron size
Powders
Aggregate of particles
Granules
Solid dosage form containing
medicaments with or
without excipients
Tablets
Drug enclosed with gelatin
capsule
Capsules
Small tablet containing excipients
Pills
Solid preparations containing
sugar and gum used to medicate mouth and throat
Lozenges
Forms which may be
administered systematically
orally or injected, using
different techniques, into the
skin, muscle, or veins.
Liquid Dosage Form
Liquid Dosage Form may be prepar using any of the following: (3)
Ø Dissolving the active in an aqueous or non-aqueous solvent
Ø Suspending the drug in appropriate medium
Ø Incorporating the drug into an oil or water phase.
Clear liquid preparation containing with or without medicaments used to internal or external preparations
Solutions
Sweet, viscous, concentrated liquid preparations containing with or without sugar and medicaments
Syrups
Biphasic liquid dosage form for oral containing medicaments in which fine oil globules dispersed in continuous phase
Emulsions
Biphasic liquid dosage form for oral containing medicaments in which fine solid particles suspended in continuous phase
Suspensions
Liquid preparation for oral containing medicaments with suitable excipients
Elixirs
Liquid preparation for rectal containing medicaments
Enemas
Viscous, liquid oral preparations used to relief cough
Linctuses
Liquid preparations for external application usually applied without friction
Lotions
Liquid preparations for external application usually applied
with friction
Liniments
Concentrated aqueous solutions for external use used to treat throat infections
Gargles
Concentrated aqueous solutions for external use used to treat mouth infections and oral hygienic
Mouth washes
Liquid preparations containing medicaments that are instilled into the nose with a dropper used to treat nose infections and blockage of nose
Nasal drops
_______ are a type of medication that is neither solid nor liquid. These medications are applied to the skin, nasal mucosa, cornea,
rectal or vaginal tissue (often via suppository), buccal tissue,
ear, or urethral membrane.
Semi-solid dosage (SSD) forms
SSD forms often involve two phases: ____ and ____.
oil; water
One phase is _____, or external, while the other phase is _____, or internal.
continuous; dispersed
Active ingredients can be dissolved in _______ phases.
one or both
__________ are applied to the surface of the
skin and remain there.
Topical semi-solid dosage forms
Topical dosages are typically used to treat _______ conditions like acne vulgaris, infections, wounds to the skin, and eczema.
dermatological
_________ are designed to be
absorbed through the skin into the bloodstream.
Transdermal semi-solid dosage forms
_______ are typically used to treat conditions that require ongoing
medication, such as pain management.
Transdermal dosages
Birth control and smoking cessation medications can also be delivered in a _________.
transdermal manner
Semisolid dosage forms for external use containing with
or without medicaments with suitable ointment base
Ointments
Semisolid dosage forms for external use containing with or
without medicaments with suitable fatty base
Creams
Semisolid dosage forms for external use containing high
proportion of finely powdered medicaments with suitable fatty base
Paste
Transparent semisolid dosage forms for external use containing
hydrophilic or hydrophobic base with gelling agents
Gels
Semisolid dosage forms for external use containing
medicaments applied to the skin to hold the dressing and protective
Poultices
Transdermal semi-solid dosage form that have an
external membrane that melts, dissolves, or softens at body
temperature, which releases the active ingredient so it can be
absorbed into the bloodstream. ___________are inserted into a body cavity, such as the vagina or rectum.
Suppositories
Medicated _______ is typically made with a combination of
__________, water, and an active ingredient. The ________is applied to the skin where it hardens and provides a slow, steady release of
medication over time.
Plaster
_______ dosage forms are packed in a container which gets released
upon applying pressure. The gas inside contains therapeutically active medicaments. The containers have valve systems with continuous or limited delivery. They are used for topical application on skin and as local application into nose and mouth.
Gaseous
Suspension of fine solid or liquid
particles with gas used to apply drug to respiratory tract having atomizer within device
Aerosols
Internal liquid preparations
containing medicaments dissolved in suitable solvent or if insoluble suspended in the propellent
Inhalations
Gaseous preparations of drugs containing alcohol applied to mucous membrane of nose or throat with atomizer or nebulizer
Sprays
Drug characteristic considerations (3)
- Drug physical and chemical characteristics
- Drug stability
- Appearance and palatability
Therapeutic considerations (3)
- Nature of illness
- Age of patient
- Condition of patient
Biopharmaceutic considerations
- Bioavailability
Therapeutic Considerations
- The nature of the illness
- The way illness is treated (locally or through systemic action)
- Age and gender
- Anticipated condition of the patient
- Other societal factors (religion, ethnicity, etc.)
Consideration of _______ (or what
the body does to the drug).
Some drugs produce effects by altering cellular function and
binding to a specific receptor. Some drugs just work through
simple reactions without the need of a receptor binding.
Pharmacology & pharmacokinetics
The ____ determines the
required dose and frequency as well as the therapeutic index for a drug in a population.
dose-response
The ________ helps determine the efficacy and safety of a drug.
therapeutic index
The ratio of the minimum
toxic concentration to the median
effective concentration
Therapeutic Index
_____ are macromolecules involved in chemical signaling between and within cells; they may be located on the cell surface membrane or within the cytoplasm.
Receptors
_________ directly or indirectly regulate cellular biochemical processes (e.g., ion conductance, protein phosphorylation, DNA transcription, enzymatic activity).
Activated receptors
A drug’s ability to affect a given receptor is related to the drug’s
_____ and _____ which are determined by its chemical structure.
affinity; intrinsic efficacy
______ is the probability of the drug occupying a receptor at any given instant.
Affinity
______ is the degree to which a ligand activates receptors and leads to cellular response.
Intrinsic efficacy or activity
The _____ is also determined by the duration of time that the
drug-receptor complex persists (________).
pharmacologic effect; residence time
The lifetime of the drug-receptor complex is affected by conformation changes that control the _______ and ________ from the target.
rate of drug association; dissociation
“A longer residence time explains a prolonged _______. However, a longer residence time can be a potential disadvantage when it prolongs a drug’s _______.”
pharmacologic effect; toxicity
Some drugs (i.e., simethicone, cholestyramine, neomycin, etc.)
should only be taken orally since they need to pass through the
_______. Drugs that work through the GIT may be taken rectally.
gut
Persistent nausea and emesis or vomiting may make it difficult
to use an ______ dosage form, and in such a case, it may be
necessary to utilize an alternate route such as inhalational,
buccal, sublingual, nasal, suppository, or parenteral instead.
oral
A specific dosage form may be a requirement for certain kinds
of drugs, as there may be issues with various factors like
______ or _________.
chemical stability; pharmacokinetics
______ CANNOT be given orally because being a protein in nature it is extensively metabolized in the GIT before reaching the blood stream and is thus incapable of sufficiently reaching its therapeutic target destinations.
Insulin
Immediate and rapid onset of drug response (such as in
emergency cases) is achieved by designing a liquid dosage form
administered_________.
intravenously (IV)
IV drugs achieve 100% _______ , in which they can reach
the systemic circulation directly without the absorption process.
bioavailability
Interactions between excipients and APIs can occur via both
_________ mechanisms.
chemical and physical
Many small-molecule APIs are inherently ______ and have
diverse _______ that can undergo multiple reactions either simultaneously or in sequence.
complex; functional groups
In most cases, the excipient itself doesn’t initially interact in a
negative manner with the API. For that to occur, it must first
undergo a _______ to generate a _______ that can affect the API.
chemical reaction; new species
______ enhances the antibacterial activity of the benzalkonium chloride.
EDTA
In nanoparticulate suspensions, excipients physically adsorb to the
surfaces of the API nanoparticles via ______ or ______ interactions.
steric; charge-charge
______ assist in “bridging” of particles during ______ processing and can be used to coat API particles to increase their interface with surrounding media during dissolution
lower-molecular-weight polymers; wet granulation
________ can form ______ that restrict the release of API, enabling extended release
higher-molecular-weight polymers; hydrogels
Lactose and APIs with amine group in the presence of moisture and
stearates resulting in the brownish discoloration of the tablet, this is
called ________.
Maillard reaction
_______, a polymeric substance for drug swelling properties, interacts
with acidic drugs like diclofenac sodium.
Eudragit®
There are several strategies that can be employed to minimize
undesirable excipient-API interactions: (3)
◦ complete avoidance of problematic excipients in the formulation
◦ consider the use of excipients that stabilize or protect APIs, devices that physically separate formulation ingredients until the time of administration
◦ develop and use packaging that incorporates chemical agents that inhibit certain chemical reactions.
Excipients with ____ moisture content should be used to reduce the probability of chemical interaction due to hydrolysis and ____ should be added to adsorb any moisture picked up in the formulation.
low; silica
For APIs that can react with oxygen, excipients that contain or can generate ______ should be avoided, while ______ should be added to the formulation in the optimal quantity.
peroxides; antioxidants
For _______ such as magnesium stearate and stearic acid, proper characterization of material blending is important.
fat-based lubricants
For ________ and __________, the addition of acidic or basic excipients or buffering agents as appropriate can help maintain the
desired pH and prevent degradation of the API.
non-sterile oral liquids; liquid injectables
Other vitally important factor is the _________. The processing conditions and the time for which the formulation is subjected to a particular process must be well defined. The ___________may affect the API or the excipient or both.
processing parameters
A light sensitive drug like _________ must be manufactured in light-
protected environment.
nifedipine, omeprazole etc.,
___________ drugs like clomtrimazole, cephradine , acarbose, penicillin’s, ranitidine,
norfloxacin etc. demand for stringent humidity control during formulation.
Hygroscopic
Sterile dosage forms require ______ conditions, ________ conditions must be controlled for emulsions and suspensions, _______ for heat sensitive API’s is not
recommended for sterilization.
aseptic; stirring; autoclaving
_________ of dosage form during shelf life is an essential requirement of quality dosage form.
Stability
It must be kept in mind that a quality dosage form is
not always the ___________ successful one.
commercially
_________ (3) of administration are the other factors, which along with first two influence acceptability of the product to both prescriber and patient.
Cost, aesthetic value and ease
The ________ (2) solely depends on the excipients and the formulation
process adopted.
cost and aesthetic value
Ease of administration/application depends not only on formulation but also on ________.
packaging
In addition to the previously mentioned, the dosage form is needed for the following reasons:
- For the protection of API from the destructive influence of the environment
- To conceal the bitter, salty or obnoxious taste or odor of API.
- To provide liquid dosage form for API’s that are either insoluble or instable in the desired
vehicle. - To provide liquid dosage form soluble in desired vehicle.
- To provide extended drug release.
- To provide optimal drug action from topical administration sites.
- To provide for the insertion of a drug into one of the body cavity.
- To provide drug directly into the blood stream.
- To provide optimal drug action through inhalation therapy.
Dosage form to protect the drug substance from the destructive influences of atmospheric oxygen or humidity
coated tablets, sealed ampoules
Dosage form to protect the drug substance from the destructive influence of gastric acid after oral administration .
enteric-coated tablets
Dosage form to conceal the bitter, salty, or offensive taste or odor of a drug substance
capsules, coated tablets, flavored syrups
Dosage forms to provide liquid preparations of substances which are either insoluble or unstable in the desired vehicle
suspensions
Dosage form to provide clear liquid dosage forms of substances
syrups, solutions
Dosage forms to provide rate-controlled drug action
various controlled-release tablets, capsules, and suspensions
Dosage forms to provide optimal drug action from topical administration sites
ointments, creams, transdermal patches, and ophthalmic, ear, and
nasal preparations
Dosage forms to provide for insertion of a drug into one of the body’s orifices
rectal or vaginal suppositories
Dosage forms to provide for placement of drugs directly in the bloodstream or body tissues
injections
Dosage forms to provide for optimal drug action through inhalation therapy
inhalants and inhalation aerosols
