Exam 1 Flashcards
an active ingredient intended for incorporation into a finished dosage form that meets the statutory definition of a drug (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 any function of the human body)
drug substance, active pharmaceutical ingredient (API)
a finished dosage form that contains a drug substance in association with one or more other ingredients
drug product
discipline of pharmacy that deals with the process of turning a drug into a medication to be used safely and effectively by patients, drug to dosage form
pharmaceutics
pt conditions, desired effect, dose required, duration of medication, drug’s physiochemical properties
things the choice of dosage form will depend on
generic drug product nomenclature
generic drug name - strength - route - dosage form
brand name drug product nomenclature
brand name - generic name - strength - route - dosage form
path by which a drug is administered into or onto the body
routes of administration
patient, drug, dose, route, time
rights of correct drug administration
a liquid product of high strength and low volume that must be diluted before administration
concentrate
precise control of dosing, suitability for different administration routes (convenience of dosing), controlled delivery rate for optimum therapy, improved adherence, individualized products to meet different patients’ needs, protection of product quality and integrity
why we need dosage forms
reliable release, reliable bioavailability, adequate stability, manufacturability, patient adherence
ideal dosage form
clinical need, drug properties, marketability, patients’ characteristics
criteria for drug product development
substances that are included in dosage forms not for their direct therapeutic action but to aid the manufacturing process, protect/support/enhance physical/chemical/microbiological stability, improve drug release/solubility/bioavailability, enhance patient acceptability
excipients
adherence, product safety (prevent harm and assist in product identification), product quality (manufacturability and stability), therapeutic efficacy (shouldn’t impede drug release and bioavailability)
functions of excipients
animal (lactose, gelatin), plant (starch, sugar, cellulose), mineral (calcium phosphate, silica), synthesis (polyethylene glycols, polysorbates, povidone)
sources of excipients
all marketed drug products (not just drug) must be safe and pure
1938 Federal Food, Drug, and Cosmetic Act
FDA regulates excipients in drug products (pure and safe), FDA’s GRAS (generally recognized as safe) list for specified use/route/amount, new excipient or new function for GRAS excipient (safety and toxicity studies are required)
safety of excipients
_____ excipients are safe for use only in approved amounts/for approved routes and in most patients
GRAS
pharmacologically inactive, provide the desired functionality, non-toxic, compatible (does not interact with active ingredient or other excipients), stable and reproducible, cost effective
ideal excipient properties
measures the rate and extent of absorption (drug reaching the systemic circulation or available at the site of action)
bioavailability
gives extent/to what degree a drug is absorbed
area under the curve (AUC)
fraction of amount of drug that reaches systemic circulation compared to dose administered
F
max drug concentration
Cmax
method of manufacturing, crystal form of the drug substance (polymorphism), nature (type/amount) of excipients used, type of dosage form, age of product, storage conditions
things the bioavailability of a drug depends on
route of administration (IV have 100%), drugs’ physiochemical properties, characteristics of dosage forms, properties of excipients used, patients’ related factors
factors affecting bioavailability
water soluble drugs tend to stay in _____ and ______
the blood, interstitial space (fluid that surrounds cell)
highly lipophilic drugs distribute extensively into ________
adipose tissue
only _____ drugs can be absorbed across membranes, high solubility = fast _______
dissolved, dissolution
particle size, molecular weight, concentration
things the dissolution rate of drugs depends on
smaller molecules dissolve ______
faster
increasing the release rate of a drug from a tablet could increase _____
absorption rate/Cmax (high Cmax means high absorption rate)
drugs’ physiochemical properties, formulation, route of administration
things rate of absorption depends on
in general _____-soluble drugs can cross cell membranes more quickly than ______-soluble drugs
fat, water
optimal drug has _____ solubility but not too _____ so it is permeable
high, polar
drugs with high solubility and high permeability
class I
drugs with low solubility and high permeability
class II
drugs with high solubility and low permeability
class III
drugs with low solubility and low permeability
class IV
main form of drug absorption
passive diffusion
Fick’s law - diffusion across the high concentration to one of low concentration
Ca - Cp
Fick’s law - molecule’s lipid solubility, size, degree of ionization
P (partition coefficient) and D (diffusion coefficient)
Fick’s law - area of absorptive surface
A (surface area)
Fick’s law - thickness of epithelial membrane
h
carrier molecule in the membrane facilitates absorption of molecule, substrate specific, availability of carriers limits absorption process (can reach saturation), process does not require energy, transport from high to low concentration
facilitated passive diffusion
selective carrier-mediated saturable, against concentration gradient, energy expenditure
active transport
fluid or particles are engulfed by a cell, cell membranes encloses the fluid/particles, fuses again, forming a vesicle that later detaches and moves to cell interior, energy expenditure, small role in drug transport (except for protein drugs/large molecules)
pinocytosis
bioavailability of drug product in comparison with IV administration
absolute bioavailability
bioavailability comparison of two non-IV products
relative bioavailability
