PMCY 2020 Exam 2: Flashcards on Formulation Methods and Injection Types

different formulation methods

buccal, oral, pulmonary, transdermal, ocular, nasal, sublingual, vaginal/anal

things to consider in dosage formulations

protection of the drug

conceal bitter, salty or offensive taste

provide liquid preparations

provide optimal drug action from topical administration sites

provide for insertion into one of the body's orifices

preformulation studies

physical and chemical properties, drug solubility, dissolution rate, partition coefficient, membrane permeability, stability

physical properties

physical description, particle size, crystalline structure, melting point, solubility, crystal or amorphous forms

chemical properties

purity, structure, form, reactivity

drug solubility

pH, particle size, max solubility

dissolution rate

rate-limiting step in absorption

may explain variations of biological activity

may change from person to person

opposite of permeability

partition coefficient

P = (concentration of drug in octanol) / (concentration in water)

determines membrane permeability

bigger = slower to cross membrane

stability

light, oxygen, humidity, crystal form, temperature

amber vial to protect from light

most injectables are refridgerated

sublingual

under tongue, immediate release

ex. nitroglycerin

buccal

in cheek

topical

on skin

ex. Neosporin

formulations with local effect

buccal, sublingual, topical

parenteral

administering medication by any other means than the GI tract (injection)

intradermal injection

allergy testing, TB 0.1mL

intravenous

drugs injected in peripheral vein over 1-2 minutes or longer by infusion IV Bolus

must be in aqueous solution

must remain in solution after injection

intramuscular

drugs injected into muscle (Gluteal or Lumbar), 2-5mL

aqueous or oleaginous solution/suspension

has absorption phase

subcutanous

drugs injected just under skin (< 2mL)

injection sites: forearm, upper arm, thigh, buttocks

ex. insulin

oral administration affected by

p/c characteristics, physiological, formulation

passive diffusion

no energy, high to low

facilitated diffusion

no energy, high to low, binding to transportors

active transport

energy required, low to high

organs responsible for most of first rate metabolism

liver + (NOT SMALL INTESTINE) kidney?

route with fastest absorption

solutions

tablets contain

drug, lubricant, granulating agent, filler, wetting agent, disintegration agent

route with fastest onset action

sublingual

ADME

absorption, distribution, metabolism, excretion

where to look for drug concentration?

concentration at receptor site, in tissue, in plasma

oral absorption path

intravenous -> pulmonary -> systemic

liver -> heart -> lung -> heart -> target site

metabolism can cause drug to become

more polar (enhance excretion in bile or urine), inactivate, more potent

bioavailability affected by

physical properties of drug, formulation, given w/o food, food/drug interactions, transporters, GI health, enzyme induction

hydrophilic

CANNOT cross cell membrane

lipophilic

CAN cross cell membrane

examples of single compartment model

IV bolus, instant

dosing questions

how much? how long? how often?

dosing interval is based on what

therapeutic index and half life

pharmacogenetics

the study of how genetic variation affects an individual's response to drugs

when are animal studies conducted

preclinical (tox, efficacy)

3 r's of good animal welfare

replace, reduce, refine

fidelity

how close a model is to the organism or condition being studied in our target species

animal welfare act 1966

regulates the treatment of animals in research, exhibition, transport and by dealers

- exclude hoof stock, cold-blooded, fish, birds

public health service (PHS policy)

oversees care and use of animals in any public or private organisms, business, or agency

- follows the guide

- requires establishment and maintenance of proper measures to ensure care and use of animals in research

the guide

internationally accepted primary reference on animal care and use

- provides framework for the judgements requires in the management of animal facilities

VRBPAC

vaccines and related biological products advisory committee

- large scale manufacturing (FDA)

- track vaccine quality

vaccine safety datalink

CDC + health organization monitor and proactive searches of vaccine related data

VAERS

Vaccine Adverse Event Reporting System

CISA

Clinical Immunization Safety Assessment

- conduct clinical research on vaccine-related health risks

examples of side effects from vaccines

sore arm, redness, swelling, fever, chills

why are people getting measles, pertussis, polio

antivax, fear of autism

cytochrome P-450

highest class of drug metabolizing enzymes in the body

most abundant substrates of cytochrome P-450

CYP 3A4/5, CYP2D6, CYP1A/2

genetic polymorphism

differences in phenotypes among the same population

factors leading to variations in response to drug

dose, frequency, metabolism, elimination, absorption, sex, liver size