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drug discovery > lecture 7 > Flashcards

lecture 7 Flashcards

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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
apart from the active principle,, what must also be studies
excipients
26
what solubility must be studied
solubility of both active principle and excipients in an aqueous media
27
what can be used in solubility tests in an aqueous media
37* aqueous buffer to allow equilibrium
28
solubility: meaning of max saturation // solubility
max amount of drug / excipient that can be dissolved in a fixed volume
29
what changes in ionisable groups
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
30
ionic compounds must have their solubility tested using what
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
31
what can solubility profiles be used for
knowing which solvent to use in formulations for injections, nasal drops etc
32
when does pka = ph
when 50% of the drug is ionised
33
ionic drugs have diff what in diff whattt
diff solubilities in diff environments
34
COOH solubility: most common form in stomach,, ph1
mostly COOH
35
COOH solubility: most common form in plasma,, ph7
mostly COO-
36
whats a positive consequence of ionisable groups having diff solubilities in diff conditions
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
37
compounds with ionisable groups first have their solubility measured when they are
not ionised intrinsic solubility
38
solubility profiles at different phs can also help us do what
find solvents to use for formulation
39
name diff solid dosage forms
- chewable tablet - sugar coated tablet - film coated tablet - buccal tablet
40
what is the meaning of dosage form
the way the drug is delivered to the site of action in the body
41
what determines if a drug reaches the site of action
physical state chemical composition
42
what gives a drug its suitable consistency
the vehicle aka the excipients
43
what are the positives of solid oral dosage forms
accurate good shelf life can self administer it easy to store and distribute
44
negatives of solid oral dosage forms
hard to administer t unconscious ppl takes long for it to be absorbed
45
for a drug to be successful,, what two things must be compatible
the active principle the excipient both physically and chemically compatible
46
diff types of solid dosage forms
tablets capsules granules powders
47
describe solid dosage form: capsule
- hard/soft gelatin shell - colourants
48
describe solid dosage form: tablets
- compressed + molded tablets - various excipients: anticaking//bulking agents, flavoures, colourants
49
when can sugar coated tablets be used
to mask flavour - water soluble sugar shell on outside
50
when does polymorphism occur
when a chemical compound crystallises with a different internal structures
51
diff types of polymorphism
crystalline polycrystalline amorphous
52
polymorphism structures: which is more soluble
amorphous polycrystalline crystalline
53
difference between diff polymorphism structures
diff polymorphic form = diff physiochemical characteristics (solubility, melting point, bioavailability, stability)
54
what is solubility rate // dissolution
the rate at which a drug or excipient dissolves in any particular medium
55
what does solubility rate depend on
particle size particle size distribution particle porosity // surface area wettability of surface (to initiate dissolution) nature of dissolution fluid
56
what changes as dissolution occurs
the particle porosity // surface area
57
what size particle is wanted
small,, increases the dissolution // solubility rate
58
why is moisture uptake // sorption measured
to find ideal conditions of storage and packaging
59
what are excipients
inactive substances that serve as vehicles//mediums for drugs should be inert normally no therapeutic effect
60
examples of excipients
binders - keep the tablet together colouring agents - helps the tablet look nice
61
what must be done to excipients
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
what is an extended release dosage form
drug is released over a long period of time. normally for oral doses: tablets + capsules
63
what must be considered for extended release dosage forms
- rate of absorption - rate of excretion - solubility - potency - TI - intended use
64
extended release dosage forms intended use
chronic conditions not acute conditions
64
sterile formulations product examples
sterile fluids medical devices
65
what is pharmacopoeia: certified analysis
- list of quantitative + qualitative medicine compositions - tests that should be carried out on medicine + the raw materials used to produce medicine
66
what must be followed in order to have a drug approved by the fda
pharmacopoeia must have been followed
67
medicine quality control: medicines should have xxx quality standards
high quality standards
68
what is gqs
good quality standards manufacturing industry is full of them
69
what 2 things play a crucial part in lab studies
the lab procedure the people carrying out the labs // the ppl executing the labs
70
every step of drug synthesis is covered by what
GxP
71
what can x stand for in gxp
good laboratory practice good manufacturing practice
72
what is covered by gxp
design + testing manufacturing and distribution of pharmaceutical products or medical devices
73
when and who first established glp
the fda 1970s
74
why were glps introduced
- 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
when must glps be used // applied
when handling live animals + plants
76
what testing should be performed under glp
safety + efficacy testing
77
when is glp not needed
discovery screening basic research in vitro studies studies where safety assessment is not a concern
78
4 glp practices
- 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
when do gmp practices apply
apply to every step of the drug manufacturing process not just the testing
80
why did the fda adopt the term current gmp
to make sure manufacturers continuously re evaluate their manufacturing practice to stay up to date as tech changes in their industry.
81
when do gmp regulations apply
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
what data is covered by glp
safety of the molecule + all necessary experiments
83
what data is covered by gmp
manufacturing + associated safety testing
84
what happens after preclinical research
federal law that a drug must be subject to approved marketing application before being transported to clinical trial centers around the world
85
what is EU - IMPO
european investigational medicinal product dossier
86
what is IND
investigational new drug
87
what is CTA
clinical trial authorisations
88
what does the clinical trial sponsor provide
a document that supports the investigational use of the medicinal product in clinical trials
89
what happens once the IND is submitted
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
what does a good GMP system ensure
ensures that products are consistently produced + controlled according to quality standards
91
why are gmps important
make sure high quality medicines are produced
92
describe poor quality medicines: if gmp was not a thing
- 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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