amorphous solid dispersions Flashcards

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1
Q

what are the two types of molecular arrangement?

A

ordered crystalline molecular arrangement
disordered amorphous molecular arrangement

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2
Q

what is a polymorph?

A

different crystal molecular arrangement so different solubility and stability

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3
Q

how is the challenge of a no polymorphs that are soluble enough dealt with?

A

amorphous form used that are more soluble than crystalline form however they’re less stable

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4
Q

what delivery route is preferred for drug delivery?

A

oral route

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5
Q

what is does oral delivery need to display?

A

good solubility and dissolution properties
good absorption through gut

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6
Q

what does bioavailability of a drug?

A

the amount of drug that enters circulation when enters the body and can have an active effect

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7
Q

what is the journey of drug molecules?

A

In-Vivo:
dissolution, drug in solution (solubility), permeability (gut wall), blood, site of action, therapeutic effect

In-vitro:
dissolution (in dissolution testing), drug in solution (solubility), permeability (gut wall), blood, site of action, therapeutic effect

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8
Q

what is the table for Biopharmaceutics Classification System?

A

slide 7

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9
Q

what is the limitation of class 1?

A

formulation dependent

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10
Q

what is the limitation of class 2?

A

formulation dependent

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11
Q

what is the limitation of class 3?

A

Dependent on barrier properties

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12
Q

what is the limitation of class 4?

A

Formulation and barrier properties dependent

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13
Q

what are some oral formulation approaches for poorly water soluble compounds?

A

Crystalline Solid Dispersions
Amorphous drug and Amorphous Solid Dispersions

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14
Q

what is the effect of Amorphous drug and Amorphous Solid Dispersions?

A

disrupts crystalline ordered structure to form disordered amorphous structure so dissolution happens faster

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15
Q

what is the effect of Crystalline Solid Dispersions?

A

‘ordered particles of drugs are stable in solid water-soluble polymer matrix’

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16
Q

what happens when amorphous state reached?

A

increase in solubility and dissolution rate
decrease in physical stability

17
Q

what is glass transition temperature?

A

Tg- physical transition in amorphous materials from brittle to rubbery state

18
Q

what does a low Tg mean?

A

the lower the Tg the less stable the amorphous is

19
Q

what is spray drying?

A

fast solvent evaporation
‘Needs acceptable solubility of drug in low boiling solvent required.’

20
Q

what is hot melt extrusion?

A

no solvent needed
temperature and shear required for degradation

21
Q

what are the main manufacturing methods for solid dispersions?

A

heat based methods
solvent based methods

22
Q
A