Lecture 1 & 2 - Intro & Review

Dr. Sprowls

pharmaceutics

taking drug compound from its discovered chemical entity to a safe & efficacious medicine

biopharmaceutics

subfield of pharmaceutics; relationship between drug’s physiochemical properties:

• product’s formulation

• impact of formulation/route, effect on the body

process in which drug is released and dissolved in systemic circulation

absorption

back and forth process of drug in systemic circulation and drug in tissues

distribution

drug in tissues can cause…

pharmacologic or clinical effect

what does ADME stand for?

Absorption

Distribution

Metabolism

Excretion

the drug itself, the drug’s _________ on drug ________, __________ across encountered biological membranes, _________ of drug to it intended site of action, and ____________ & __________ of drug is known as ________

formulation; release; absorption; distribution; metabolism; excretion; adme

routes of administration

oral, IV, subcutaneous, transdermal, topical inhalation etc…

process in which drug in systemic circulation is excreted and metabolized

elimination

what does MEC stand for?

Minimum

Effective

Concentration

bioavailability

(F) is the amount of unchanged drug making it to systemic circulation

why is bioavailability important?

determines efficacy

bioequivalence

absence of difference in drug achieved @ target site b/w formulations for same drug

determine if two different drug products (like brand-name drug and generic) have the same bioavailability

why is bioequivalence important?

• ensures therapeutic goals are mets

• patient safety is maintained

• promotes access to affordable medications - achievable among brand and generic products

therapeutic goals

• rapid relief

• chronic disease treatment

• local or systemic action, etc…

drug (active pharmaceutical ingredient)

physiochemical properties of API; what helps or prevents getting to bioequivalence

route of adminstration

oral, topical, IV, transdermal, etc…

dosage & regimen

• large/small

• dose frequency of administration

• patient adherence and tolerance

type of drug product

orally disintegrating tablets, IR tablets, ER tablets, transdermal, topical, parental, implant, etc…

excipients

not active (no activity), but critically important to how, when, and amount of drug making it to blood after admin

what does area under the curve (AUC) tell us?

drug’s total exposure of body to particular drug over time

what is the trapezoidal rule?

estimates AUC by calculating the AUC between consecutive data points

important notes about trapezoidal rule?

• does not depend upon shape of curve

• accurate with enough data points; more accuracy with more data

• assumes straight line b/w data points

• if points too spaced out, normal curvature of line will cause great error

_________ ________ describes the _______ relationship between an __________ variable (input, x) and a _________ variable (output, y)

linear regression; linear; independent (input, x) ; dependent (output, y)

________ ________ describes the _______ of a ________ relationship

correlation coefficient (r); strength; linear

what does it mean when correlation coefficient (r) is (+1) or (-1)?

perfect relationship

what does it mean when correlation coefficient (r) is (0)?

no linear relationship

_________ __ _________ describes the _______ of the _______ that can be explained by the __________ factor

coefficient of determination (r²); variability; outcome; input

correlation v.s. causation in biopharmaceutics

reflective of elimination and distribution in your body over time; it is not time that makes the drug decrease, it is the underlying biological processes that are happening to the drug

non-linear regression

relationship in nonlinear trajectory using parametric model (curves) when function is known (exponential, power log)

ex. first-order eliminations and second-order eliminations

zero-order

proceeds over time independent from the concentration of drug; the negative sign implies concentration of drug decreases overtime

first-order

proceeds dependent upon concentration of drug