Please enable JavaScript.
Coggle requires JavaScript to display documents.
BIOPHARMACEUTICS INTRO (DIETARY SUPPLEMENTS (content in supplements bottle…
BIOPHARMACEUTICS INTRO
DEFINITION
physiocochemical property of a drug
dosage form
capcule
tablet
injection
eye drops
ear drops
patches
how these impact
rate - how fast
of systemic drug absorption
extent - how much
route of administration
HISTORY
before 1820
plants - crude products
powdered leaves
extracts
infusions
spirits
syrups
tinctures
minerals
salts of arsenic
barium
bismuth
cadmium
copper
iron
lithium
mercury
1800 - ACTIVE INGREDIENTS
discovered and isolation primarily in 1800s
alkalods chemists
started morphine in 1819
multiple active components -
found in crude products
opium / morphine
belladonna - atropine
cinchona - quinine
digitalis - digoxin
synthetic drug
ASPIRIN
willow bark - salix sp.
contain salicyl alcohol, salicin
identification of active metabolite
1852 - salicylic acid-synthesis of acetylsalicylic acid
1899 - bayer aspirin
use of active ingredients
more controlled than crude products
1900s - STANDARDIZATION OF CONTENT
1900- 1950 primarily
active ingredients in various proportions and amount in crude products
ex: kola drug - anti nausea
CONTENT
content varies with source of crude products
soil
growing conditions
climate
variety of plants
stability
well-established
specific drug given
dosage administered
IN VIVO ASSESSMENT of systemic delivery
in 1950s
development of pharmacokinetics
quantification of the kinetics of drug
absoption
distribution
metabolism
excretion
elimination of metabolites
common sites of measurements of drug and metabolites
plasma
urine
guaranteeting drug content
does not ensure systemic delivery
became more apparent
reasons for low bioavailability
bioavailability - systemic delivery
lack of release from dosage form in vivo
gastrointestinal tract
low pH - decomposition in stomach
enzymatic digestion
metabolism in gut wall
extensive extraction of the liver
large intestine - microflora decomposition
complex with compounds in gut contents
effect of
food
drug
gastrointestinal disease
abnormalities of GI tracts
too water soluble to be absorbed lipophilic GI membrane
too insoluble
slow dissolution
absent dissolution
DIETARY SUPPLEMENTS
1990s crude products can be on market
not have to prove safety or efficacy
not approved by FDA
many alleged to be useful for certain conditions without adequate clinical trials
content in supplements bottle
others have markers
some have active ingredients
highly variable in contents
few may not have any "active" compound
systemic bioavailability of these "active" compounds are not tested