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PY366 Drug discovery > Bioequivelence > Flashcards

Bioequivelence Flashcards

1
Q

what is pharmaceutical equivelence

A
  • contain the same active ingredients
  • same dosage form and route of administration
  • identical in strength or concentration
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2
Q

describe what occurred in the phenytoin toxicity study

A
  • same dose per capsule
  • normal batches were made with CaSO4
  • some batches made with lactose
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3
Q

describe what occurred with levothyroxine sodium tablets

A
  • 58 adverse drug reactions
  • patients were switching brands
  • inconsistencies between batches from same manufacturer
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4
Q

how is bioavailability measured on a graph

A

area under the curve

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5
Q

what is bioequivelence

A

2 medicinal products containing the same active substance that are pharmaceutically equivalent or pharmaceutical alternatives and their bioavailabilities after administration in the same molar dose lie within acceptable predefined limits
- these limits are set to ensure comparable in vivo performance

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6
Q

what are the stages that occur after taking a tablet

A
  1. disintegration
  2. dissolution
  3. diffusion
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7
Q

what is disintegration dependent on

A
  1. formulation dependent
  2. excipients
    - diluents
    - binders
    - disintegrants
    - lubricants
    - coatings
  3. processes
    - mixing
    - granulation
    - drying
    - compaction
    - coating
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8
Q

what factors impact dissolution

A
  1. water solubility of the drug
  2. particle size
  3. salt form
  4. crystal form
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9
Q

what can cause biological variation between patients

A
  • body weight
  • gender
  • age
  • disease state
  • genetic differences
  • nutrition and hydration
  • other drugs
  • stress
  • time of administration
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10
Q

what is absolute bioavailability

A

comparison between blood levels achieved in IV dosing and oral dosing

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11
Q

what is relative bioavailability

A

comparison between blood levels achieved in standard formulation and in test formulation

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12
Q

when are dosage forms bioequivelent

A

if their bioavailability doesn’t differ significantly after administration

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13
Q

what are the EMA guidelines on bioequivelence

A
  1. acceptance intervals of 80-125%
    - 90-111% for narrow therapeutic index drugs
  2. requires 90% confidence intervals between test and reference formulations
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14
Q

what is the biopharmaceutical classification system

A
  1. class I
    - high solubility
    - high permeability
  2. class II
    - low solubility
    - high permeability
  3. class III
    - high solubility
    - low permeability
  4. Class IV
    - low solubility
    - low permeability
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15
Q

what is defined as good or poor water solubility

A
  1. soluble >10mg/ml over the physiological pH range
  2. poorly soluble < 1mg/ml over physiological pH range
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16
Q

describe the effects of Class I drugs in the biopharmaceutical classification system

A
  1. dissolution and absorption are rapid
  2. not generally a problem for bioequivelence
    - eg. propanolol, diazepam
17
Q

describe the effects of Class II drugs in the biopharmaceutical classification system

A
  1. dissolution is slow (particle size)
  2. absorption is rapid
    - eg. amiodarone, digoxin
18
Q

describe the effects of Class III drugs in the biopharmaceutical classification system

A
  1. rapid dissolution
  2. slow absorption
    - low log P values may affect permeability
    - eg. atenolol, ranitidine
19
Q

describe the effects of Class IV drugs in the biopharmaceutical classification system

A
  1. slow dissolution and absorption
    - make prodrugs if possible
    - eg. furosemide, allopurinol
20
Q

outline the formulation approaches that deal with low solubility

A
  1. alternative salt forms
  2. metastable crystalline polymorphic forms
  3. co-crystals
  4. complex formation
  5. cosolvents
  6. solubilisation by surfactants
  7. amorphous forms
21
Q

what structural modifications can be made to deal with low permeability

A

make a prodrug
- eg. aciclovir has low permeability, valaciclovir has greater bioavailability than aciclovir

22
Q

what are biosimilars

A

biological medicine that is similar to another biological medicine that has already been authorised for use
- made from a biological source, such as bacterium or yeast

23
Q

what are some exceptions to the generic medicines in the NHS

A
  1. drugs with narrow therapeutic index
  2. some antiepileptics
  3. some modified release products
  4. certain drug administration devices
  5. some multi ingredient products
  6. biosimilars
  7. special needs- intolerance to excipients

PY366 Drug discovery (15 decks)

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