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drug discovery > lecture 7 > Flashcards

lecture 7 Flashcards

1
Q

stages in drug development

A

research + discovery to launching them on the market

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2
Q

what must drug formulations be optimised for

A

optimised for their intended use

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3
Q

when are drug formulation studies help

A

from preclinical to the launch of the drug

they just continue and continue

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4
Q

what must be known about the drug before preclinical studies

A

its intended use

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5
Q

different routes of drug administration

A

oral
nasal
injection / intravenous

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6
Q

whats different about different routes of administration

A

they have different formulations

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7
Q

what is the F in bioavailaility controlled by

A
  • rate + extent of release of drug from dosage form 9aka the amount that is acc released)
  • absorption from solution state
  • biotransformations during absorption
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8
Q

what does the shape of plasma concentration profiles depend on

A

the relative rates of absorption and elimination

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9
Q

what does a plasma conc profile vary between

A

vary between different forms of drug administration.

aka intravenous would have a higher + earlier peak as it is absorbed with 100% bioavailability - fast absorption

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10
Q

describe an oral dose peak on a plasma conc profile

A

smaller peak + later on due to slower absorption

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11
Q

different administration routes but the same active principle haveth same

A

rate of elimination

this depends on the active principle!!
their absorption will vary,, but elimination will be the same

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12
Q

disposition

A

distribution
metabolism
excretion

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13
Q

plasma conc axis

A

conc up and down

time left and right

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14
Q

single dose plasma conc description

A

single peak
- absorbance phase (increasing conc)
- elimination phase (decreasing conc over time)
Cmax and Tmax : time and conc was the highest here

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15
Q

multiple repeated dose plasma conc profile

A

furry graph of absorbance and elimination
Css = steady state average when abs = elim // input = output.

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16
Q

what happens to a drug whn it is given in multiple doses:

A

conc accumulates in the body until plateu is reached

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17
Q

too high drug conc when given in multiple doses

A

excessive diverse effects are observes

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18
Q

in multiple dose plasma conc profiles,, where is the plasma conc preferred

A

in the therapeutic window
affects are seen buyt there are no adverse ones

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19
Q

when are adverse effects seen on a plasma conc profile for multiple doses

A

when the plasma concentration increases too fast and too high

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20
Q

areas of preformulation research

A
  • physiochemical properties
    bulk characterisation
    solubility analysis
    stability analysis
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21
Q

preformulation research: physiochemical properties

A

purity
surface area
particle size
particle shape

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22
Q

preformulation research: bulk characteristics

A

powder flow properties
bulk density

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23
Q

preformulation research: solubility analysis

A

pka
dissolution
ph solubility profile

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24
Q

preformulation research: stability analysis

A

solution
solid state
bulk
compatibility stability

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25
Q

apart from the active principle,, what must also be studies

A

excipients

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26
Q

what solubility must be studied

A

solubility of both active principle and excipients in an aqueous media

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27
Q

what can be used in solubility tests in an aqueous media

A

37*
aqueous buffer to allow equilibrium

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28
Q

solubility: meaning of max saturation // solubility

A

max amount of drug / excipient that can be dissolved in a fixed volume

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29
Q

what changes in ionisable groups

A

their solubility changes between their neutral state and ionised state

solubility of groups like NH2 and COOH must be tested when neutral + ionised as their solubility changes

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30
Q

ionic compounds must have their solubility tested using what

A

using different ph environments as there are many different areas of ph in the body

allows us to gain insight of their state in different ph environments

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31
Q

what can solubility profiles be used for

A

knowing which solvent to use in formulations for injections, nasal drops etc

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32
Q

when does pka = ph

A

when 50% of the drug is ionised

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33
Q

ionic drugs have diff what in diff whattt

A

diff solubilities in diff environments

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34
Q

COOH solubility: most common form in stomach,, ph1

A

mostly COOH

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35
Q

COOH solubility: most common form in plasma,, ph7

A

mostly COO-

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36
Q

whats a positive consequence of ionisable groups having diff solubilities in diff conditions

A

prevents the group from returning back to environments with different phs.

aka when COOH is ionised into COO- when it enters the plasma, it can no longer return back to the stomach as they have diff phs

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37
Q

compounds with ionisable groups first have their solubility measured when they are

A

not ionised
intrinsic solubility

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38
Q

solubility profiles at different phs can also help us do what

A

find solvents to use for formulation

39
Q

name diff solid dosage forms

A
  • chewable tablet
  • sugar coated tablet
  • film coated tablet
  • buccal tablet
40
Q

what is the meaning of dosage form

A

the way the drug is delivered to the site of action in the body

41
Q

what determines if a drug reaches the site of action

A

physical state
chemical composition

42
Q

what gives a drug its suitable consistency

A

the vehicle aka the excipients

43
Q

what are the positives of solid oral dosage forms

A

accurate
good shelf life
can self administer it
easy to store and distribute

44
Q

negatives of solid oral dosage forms

A

hard to administer t unconscious ppl
takes long for it to be absorbed

45
Q

for a drug to be successful,, what two things must be compatible

A

the active principle
the excipient

both physically and chemically compatible

46
Q

diff types of solid dosage forms

A

tablets
capsules
granules
powders

47
Q

describe solid dosage form: capsule

A
  • hard/soft gelatin shell
  • colourants
48
Q

describe solid dosage form: tablets

A
  • compressed + molded tablets
  • various excipients: anticaking//bulking agents, flavoures, colourants
49
Q

when can sugar coated tablets be used

A

to mask flavour

  • water soluble sugar shell on outside
50
Q

when does polymorphism occur

A

when a chemical compound crystallises with a different internal structures

51
Q

diff types of polymorphism

A

crystalline
polycrystalline
amorphous

52
Q

polymorphism structures: which is more soluble

A

amorphous
polycrystalline
crystalline

53
Q

difference between diff polymorphism structures

A

diff polymorphic form = diff physiochemical characteristics (solubility, melting point, bioavailability, stability)

54
Q

what is solubility rate // dissolution

A

the rate at which a drug or excipient dissolves in any particular medium

55
Q

what does solubility rate depend on

A

particle size
particle size distribution
particle porosity // surface area
wettability of surface (to initiate dissolution)
nature of dissolution fluid

56
Q

what changes as dissolution occurs

A

the particle porosity // surface area

57
Q

what size particle is wanted

A

small,, increases the dissolution // solubility rate

58
Q

why is moisture uptake // sorption measured

A

to find ideal conditions of storage and packaging

59
Q

what are excipients

A

inactive substances that serve as vehicles//mediums for drugs
should be inert
normally no therapeutic effect

60
Q

examples of excipients

A

binders - keep the tablet together
colouring agents - helps the tablet look nice

61
Q

what must be done to excipients

A

they must be tested alongside the drug to make sure they are physically and chemically compatible + dont react under any diff environments.

must be tested together in a range of different phs, environments etc etc

62
Q

what is an extended release dosage form

A

drug is released over a long period of time.
normally for oral doses: tablets + capsules

63
Q

what must be considered for extended release dosage forms

A
  • rate of absorption
  • rate of excretion
  • solubility
  • potency
  • TI
  • intended use
64
Q

extended release dosage forms intended use

A

chronic conditions

not acute conditions

64
Q

sterile formulations product examples

A

sterile fluids
medical devices

65
Q

what is pharmacopoeia: certified analysis

A
  • list of quantitative + qualitative medicine compositions
  • tests that should be carried out on medicine + the raw materials used to produce medicine
66
Q

what must be followed in order to have a drug approved by the fda

A

pharmacopoeia must have been followed

67
Q

medicine quality control: medicines should have xxx quality standards

A

high quality standards

68
Q

what is gqs

A

good quality standards

manufacturing industry is full of them

69
Q

what 2 things play a crucial part in lab studies

A

the lab procedure

the people carrying out the labs // the ppl executing the labs

70
Q

every step of drug synthesis is covered by what

A

GxP

71
Q

what can x stand for in gxp

A

good laboratory practice

good manufacturing practice

72
Q

what is covered by gxp

A

design + testing

manufacturing and distribution

of pharmaceutical products or medical devices

73
Q

when and who first established glp

A

the fda
1970s

74
Q

why were glps introduced

A
  • assess nonclinical safety
  • protect integrity of scientific data
  • aid in product advancement - providing open ended research studies
  • ## regulate non clinical lab studies for humans, animals, perfumes etc
75
Q

when must glps be used // applied

A

when handling live animals + plants

76
Q

what testing should be performed under glp

A

safety + efficacy testing

77
Q

when is glp not needed

A

discovery
screening
basic research
in vitro studies

studies where safety assessment is not a concern

78
Q

4 glp practices

A
  • audit and introspection (internal + external performed by external regulatory bodies to check that procedures are being followed)
  • standard operating procedures,, SOP
    clearly written guidelines labs should follow + everyone should see
  • data recording
    what u did, how it was done, when it was done, who did it : record data correctly + without error
  • staff
    trained staff should perform tests + their qualifications should be kept
79
Q

when do gmp practices apply

A

apply to every step of the drug manufacturing process

not just the testing

80
Q

why did the fda adopt the term current gmp

A

to make sure manufacturers continuously re evaluate their manufacturing practice to stay up to date as tech changes in their industry.

81
Q

when do gmp regulations apply

A

when products are being manufactured for consumers to use
u must batch test,, test ingredients from suppliers + any other tests during the manufacturing process.

82
Q

what data is covered by glp

A

safety of the molecule + all necessary experiments

83
Q

what data is covered by gmp

A

manufacturing + associated safety testing

84
Q

what happens after preclinical research

A

federal law that a drug must be subject to approved marketing application before being transported to clinical trial centers around the world

85
Q

what is EU - IMPO

A

european
investigational
medicinal
product
dossier

86
Q

what is IND

A

investigational new drug

87
Q

what is CTA

A

clinical trial authorisations

88
Q

what does the clinical trial sponsor provide

A

a document that supports the investigational use of the medicinal product in clinical trials

89
Q

what happens once the IND is submitted

A

u wait 30 days for the fda to approve it,, make sure all data is correct or else u just waste ur time.

u wait 30 days then u can start clinical trials

fda makes sure clinical trial subjects will not be subjected to unreasonable risks

90
Q

what does a good GMP system ensure

A

ensures that products are consistently produced + controlled according to quality standards

91
Q

why are gmps important

A

make sure high quality medicines are produced

92
Q

describe poor quality medicines: if gmp was not a thing

A
  • health hazard
  • waste of money
  • waste of time
  • may have had toxic substances unintentionally added
  • too small amount of active principle -> no therapeutic effect
  • countries only allow the importation + sale of medicine that has been manufactured respecting gmp practices.

drug discovery (18 decks)

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