Mark Hewitt Flashcards

1
Q

Make a list of physical and chemical properties of a drug substance that affect their pharmacological activity?

A
Melting and boiling point
Volatility 
Particle size and shape
pH
Log P
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2
Q

What is a true solution?

A

A mixture of 2 or more components that form a homogeneous mixture (one phase)

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3
Q

What types of solutes are possible?

A

Electrolyte

Non-electrolyte

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4
Q

What is a saturated solution?

A

The solute is in equilibrium with the solid phase

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5
Q

What is an unsaturated solutions?

A

Dissolved solute is in a concentration below that necessary for complete saturation

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6
Q

What is a supersaturated solution?

A

Contains more of the solute than is normal

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7
Q

What are the possible units for solubility?

A

mol/L
mg/L
ppm

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8
Q

Why is solubility important in pharmaceutics?

A

As many formulations are solutions, and the drug needs to be dissolved before it can be absorbed

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9
Q

What is intrinsic solubility?

A

Solubility of the free unionised solute

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10
Q

How can you measure solubility?

A

Experimentally: Saturated shake flask method and automated Potentiometric acid/base titration
Computationally

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11
Q

Rank in order of solubility:- NaCl, Nicotine, Pentanol, Ethanol, Glucose and Aspirin

A

NaCl, Ethanol, Glucose, Pentanol, Aspirin and Nicotine

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12
Q

Name the factors that influence solubility?

A
Number of polar groups (OH)
Number of non-polar groups (CH3)
If hydrogen bonding can occur
Acid/basic characteristics
If branched or unbranched
Molecular size
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13
Q

What is the partition coefficient (P)?

A

Ratio of concentration between two immiscible phases

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14
Q

Why is octanol used as a solvent when measuring log P?

A

As it mimics phospholipids (membrane)

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15
Q

What methods can you use to determine log P?

A

Shake flask method - need to use octanol and water - don’t need to know structure
HPLC - need to know structure
Electrochemical method - ionisable drugs

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16
Q

Can you determine log P without doing any experiments?

A

Yes, software package called EPI

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17
Q

Log P increases when?

A

Increase in size

Increase in carbon atoms - non-polar content

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18
Q

High log P value means?

A

Less soluble in water - hydrophobic

Less polarising

19
Q

Low log P value means?

A

More water soluble - hydrophilic

More polarising

20
Q

What does a big log P value mean for the delivery of the drug?

A

Accumulate in the hydrophobic region of the cell membrane, wont get to target

21
Q

What does a low log P value mean for the delivery of the drug?

A

Pass through the cell membrane readily but will also pass out of cell membrane readily

22
Q

What is molality?

A

Amount of substance (in moles) per unit mass of solvent

23
Q

What are the units of molality?

A

mol kg-1

24
Q

What is Raoult’s law?

A

The partial vapour pressure of a substance in a mixture is proportional to its mole fraction and its vapour pressure when pure

25
Q

What is Henry’s law?

A

The vapour pressure of a volatile solute is proportional to its mole fraction in a solution

26
Q

What is an ideal dilute solution?

A

A solution which has a low concentration of solute, so obeys Henry’s law

27
Q

What is a colligative property of a solution?

A

That a solute in solution will affect the properties of the solution

28
Q

List three colligative properties?

A

Raise in boiling point
Reduction in melting point
Produce an osmotic effect

29
Q

What are the units for colligative properties?

A

mol kg-1 = same as molality

30
Q

What is osmotic pressure?

A

The pressure that must be applied to the solution to stop the osmotic flow

31
Q

What is tonicity?

A

The measure of the osmotic pressure gradient of two solutions separated by a semi permeable membrane

32
Q

What happens when something is hypotonic?

A

Draws water in as it has a high solute concentration

33
Q

What happens when something is hypertonic?

A

Draw water out as it has a low solute concentration

34
Q

Tonicity of the plasma?

A

275-295 mosmol-1

35
Q

Name a company that produces osmotic pumps commercially?

A

Alzet

36
Q

What is the azeotropic point?

A

Point at which two liquids can not be separated by distillation

37
Q

Give examples of high azeotropes?

A

Chloroform/acetone
Nitric acid/water
HCl/water

38
Q

Give examples of low azeotropes?

A

Dioxane/water

Ethanol/water

39
Q

What is the eutectic point?

A

the lowest temperature for the existence of the liquid phase in a solution

40
Q

Name three dosage forms that rely on eutectic points?

A

Suppository
Pessary
Skin patches

41
Q

What is an incongruent melting point?

A

Melting point that is lower than expected

42
Q

what is a plane of symmetry in a crystal?

A

Divides crystal into two parts that are mirror images of one another

43
Q

What is an axis of symmetry in a crystal?

A

A line about which the crystal can be rotated

44
Q

What is a centre of symmetry in a crystal?

A

Centre of which the crystal can rotate