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drug discovery > lecture 6c > Flashcards

lecture 6c Flashcards

1
Q

what is included in drug formulation to manufacturing

A

stages that occur to get from a lead compound to it being manufactured and used by consumers.

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2
Q

when do drug formulation studies occur

A

thoughout the whole process

from preclinical studies to launch!!

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3
Q

what must be known before drug formulation

A

the drugs intended use must be known in order to be optimised!!

we must know it’s use before preclinical studies

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4
Q

examples of drug administration routes

A

oral dose
nasal spray
injection

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5
Q

what differs between drugs that are administered differently

A

their formulation differs.

they will be formulated differently in order to be optimised for their intended use

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6
Q

is the drug the main part of medicine

A

no!!

there are excipients in the medicine aswell!!

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7
Q

what 3 factors control bioavailability ‘F’

A
  • the drugs rate and extent of release from its dosage form
  • absorption from solution state
  • bio transformation during absorption
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8
Q

what does the shape of a plasma conc profile depend on

A

relative rates of absorption and elimination

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9
Q

what do plasma conc profiles vary between

A

they vary depending on the route of administration

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10
Q

what administration leads to an early peak due to fast absorption on a plasma conc profile

A

intravenous
intramuscular

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11
Q

what administration route leads to a delayed peak on a plasma conc profile

A

oral, rectal, subcutaneous

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12
Q

is the rate of elimination constant

A

yes!
it depends on the nature of the active ingredient

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13
Q

3 things that make up drug disposition

A

distribution
metabolism
excretion

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14
Q

a drugs disposition is itsssss

A

ADME!!
absorption
adsorption
metabolism
extraction / elimination

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15
Q

plasma conc profile for multiple doses

A

furry graph

conc changes up and down with time

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16
Q

plasma conc profile for single dose

A

normal graph
increases, peak, decreases

conc increases then decreases with time

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17
Q

what are the visible phases of a plasma conc profile

A

absorption phase
elimination phase

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18
Q

what is Css

A

steady state concentration

when the absorption of the drug is equal to the elimination of the drug

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19
Q

what happens to the drug when it is administered using multiple doses

A
  • drug accumulates in the body until plateau is reached
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20
Q

what happens when the plasma conc is too high for multiple doses

A

excessive adverse side effects occur

conc increases too high too fast

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21
Q

in multiple doses, where do we want the drug conc to be at

A

the therapeutic window.

the conc where effects are seen but there are no excessive side effects.

plasma drug conc increases slowly + therapeutic success is seen

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22
Q

areas of preformulation research
aka things we think about before formulating the drug

A
  • physiochemical properties
  • bulk characterisation
  • solubility analysis
  • stability analysis
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23
Q

preformulation research: physiochemical properties

A

physical properties
PURITY
SURFACE AREA
PARTICLE SIZE
PARTICLE SHAPE

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24
Q

preformulation research : bulk characterisation

A

powder flow properties
bulk density

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25
Q

preformulation research: solubility analysis

A

pka
dissolution
pH solubility profiles

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26
Q

preformulation: stability analysis

A

solution
solid state
bulk
compatibility stability

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27
Q

what must we think about when optimising a drugs formulation

A

we must think about it’s intended use.

aka if it’s use is to stop a sore throat and u need to suck on it, we must formulate it to taste nice

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28
Q

the active principle must be studied,, what else must be studies

A

the excipients
everything other than the active principle

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29
Q

when do preformulation research occur

A

all the time!!
from preclinical to launch

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30
Q

what’s solubility must be studied

A

the active principle + excipients in an aqueous media

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31
Q

when solubility is tested,, what condition are used

A

37*C
aqueous buffer to reach equilibrium

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32
Q

what is max saturation // solubility

A

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

fully saturated = it can’t dissolve anymore

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33
Q

why must solubility be studied at different pHs

A

solubility of ionisable groups changes under certain pHs.
the body also has environments of different pHs.
COOH vs COO- have diff solubilities

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34
Q

why must a solubility profile be made

A

to see the diff states the active principle is in diff pHs.

allows us to optimise the drugs formulation basing it of its use.
aka the use of a certain solvent for nasal sprays

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35
Q

what does pKa equal to and when

A

it equals pH

when 50% of the drug is ionised

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36
Q

ionic drugs have diff what???

A

diff solubilities in diff environments

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37
Q

how does COOH change between pHs and body environments

A

pH 1: mainly COOH can enter the plasma

pH 7: mainly COO- can’t return back to stomach.

no longer membrane soluble

38
Q

what does testing solubility help us do

A
  • find correct solvents to use when manufacturing the active ingredient
39
Q

name one dosage form ‼️‼️‼️

A

solid!!

40
Q

name the diff types of solid dosage forms

A
  • buccal tables
  • chewable tablet
  • sugar coated
  • film coated
41
Q

what are the advantages of a solid oral dosage form

A
  • accurate
  • good shelf life
  • easy to store + distribute
  • ppl can administer it themselves
42
Q

what are the disadvantages of a solid oral dosage form

A
  • hard to administer it to unconscious ppl
  • may take longer for the drug to be absorbed
43
Q

what determines the way a drug is delivered to the site of action

A

it’s physical state + chemical composition

aka a solid with 0 solubility cannot be administered intravenously

44
Q

what gives a drug it’s suitable consistency

A

the active principle and the excipients // the vehicle.

the vehicle takes the drug to the target

45
Q

what is a excipient // a target

A

a non therapeutic

gives the drug its suitable consistency

46
Q

lists of drug consistency’s

A

solid
liquid
gas
semisolid

47
Q

what is important about the active principle and the excipient

A
  • they must be physically and chemically compatible!!
    they must not react and cause side effects

they must be tested for this under lots of pH values

48
Q

solid capsule

A

gel coating
gelatine covering
colourant included

49
Q

solid tablets

A

compressed + molded with the excipient
anticaking agents
can be sugarcoated to mask bad flavour

50
Q

when does polymorphism occur

A

when a chemical compound crystallises with different internal structures

51
Q

diff types of possible polymorphisms

A

crystalline (crystal arrangement)
polycrystalline ( many crystals joined)
amorphous ( bit of a mess but we love her x)

52
Q

out of the 3 polymorphic forms,, what structure is least soluble

A

crystalline
then polycrystalline
then amorphous

53
Q

what is the difference between the 3 polymorphic forms

A
  • diff physiochemical properties

aka solubility, melting point

effects their ‘F’ and stability

54
Q

what does the rate at which a drug or excipient dissolve in any particular medium depend on

A
  • particle size + particle size distribution
  • particle porosity // surface area
  • wettability of surface (initiates dissolution)
  • nature of dissolution fluid
55
Q

dissolution meaning

A

breaking down
dispersing itself

56
Q

what size of particle dissolves at a faster rate

A

a smaller particle

57
Q

moisture uptake and sorption

A

measured to see how a medicine (drug + excipient) should be stored and packaged based on moisture uptake findings

58
Q

moisture uptake / sorption

A

gives insight into how a medicine ( drug + excipient) should be packaged

59
Q

what is an excipient

A
  • inactive substance with no therapeutic use
  • used as a vehicle or medium for drugs
    should be inert
  • must also be tested alongside the drug
60
Q

example of an excipient

A

colourant
bulking agent
anti-caking agent
binders

61
Q

why must excipients be included in the ingredients section

A

someone could be allergic to the excipient but not the drug itself (the active principle)

62
Q

what are drugs that are formulated as extended release

A

they release the active principle over a longer period of time.

most commonly seen for oral doses

  • TI, solubility, potency + rate of absorption/ excretion must be considered
63
Q

when are extended release dosage forms of drug usually used

A

for chronic conditions

not for acute conditions

64
Q

sterile formulation product examples

A

medical devices
sterile fluids

65
Q

what is pharmacopoeia + certified analysis

A
  • list of the quantitative and qualitative compositions of medicines
  • series of tests that the medicine and raw materials must undergo
  • must occur in order to be fda approved into clinical trials
66
Q

medicine quality control role

A
  • drugs must obey high quality standards
67
Q

what 2 things play a crucial part in a lab study

A
  • the procedures
  • the ppl in the lab
68
Q

the manufacturing industry is full of..

A

Good Practice Standards

69
Q

all steps of the lab must be covered under,,

A

GXP

70
Q

what does the X in GXP stand for

A

LABORATORY
MANUFACTURING

71
Q

what is GOOD LABORATORY PRACTICE

A
  • established by the fda to:
    • assess non clinical pharmceutical lab study safety
    • protect integrity of scientific data (moral principles + honestly)
  • provide open end research for product advancement (long answers)
72
Q

what lab studies does GLP regulate

A

non clinical lab studies for future human / animal drugs, perfumes, biologics etccc

73
Q

what do u need when handling live organisms or plants

A

GLP
good laboratory practice

74
Q

what must be tested under GLP

A

safety and efficacy

75
Q

what studies don’t require GLP

A

discovery
basic research
screening
in vitro studies

studies where safety is not a concern

76
Q

things included in GLP

A
  • audit + inspection (internal and external- FDA) to see if procedures are being followed
  • standard operating procedures (guidelines labs should follow - must be clearly written and accessible)
  • data must be recorded physically (what was done, how it was done, where it was done)
  • staff must be trained!!
77
Q

GLP examples:

A

notes made on temperature gives info on how drugs should be stored.

78
Q

what do GMP regulations apply to

A

they apply to every step of the manufacturing process!! not just the testing

79
Q

what does the FDA say about GMP

A

that manufacturers should reevaluate their practices to stay up to date with new technology

80
Q

when should GMP be applied

A

when smt is being manufactured for consumers!
batches and ingredients must be tested!!

81
Q

data on safety of smt applies to what GXP

A

GLP

82
Q

manufacturing aka batch/kit release and associated safety testing applies to what GXP

A

GMP

  • anything with making stuff for ppl/ consumers = GMP
83
Q

what happens after preclinical testing

A
  • after preclinical we have clinical tests!!!
84
Q

before the drug is transported to diff countries to start clinical trials what must occur

A

drug must be subject of an approved marketing application by EU IMPD, IND, CTA

85
Q

marketing application : EU IMD

A

european investigational medicinal product dossier

86
Q

marketing application: IND

A

Investigational new drug

87
Q

marketing application: CTA

A

clinical trial authorisations

88
Q

what happens before u can start clinical trials

A

get document from clinical trial sponsor!! u wait 30 days for the FDA to analyse the data to see if ur clinical trial is safe + won’t put anyone in harms way. then after 30 days u can start clinical trials

89
Q

medicine and GMP

A

used to make sure that products are consistently produced under good standards

90
Q

why are GMPs important in medicine

A
  • ensures that medicine is high in quality
  • makes sure there are no health hazards, prevents time wasting, prevents money waste, makes sure no toxic compounds were added unintentionally
  • countries can refuse to sell drugs that aren’t under GMP.

drug discovery (18 decks)

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