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PHAR1201 > Untitled Deck > Flashcards

Untitled Deck Flashcards

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1
Q

Define pharmacokinetics

A

the study of how the body interacts with administered substances for the entire duration of exposure

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2
Q

Define pharmacodynamics

A

the study of the biochemical, physiologic, and molecular effects of drugs on the body

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3
Q

What is the difference between pharmacokinetics and pharmacodynamics?

A

pharmacokinetics is the movement of drugs through the body, whereas pharmacodynamics is the body’s biological response to drugs.

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4
Q

What does LADME stand for?

A

L: Liberation
A: Absorption
D: Distribution
M: Metabolism
E: Elimination/excretion

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5
Q

What are excipients?

A

non-medical agents in the drug

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6
Q

What do excipients do?

A

excipients have no biological activities in the body, but delivers the dosage

They can affect the flavour, colour, emulsify the drug and more.

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7
Q

What does dosage form mean?

A

the physical form in which the drug is available for administration

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8
Q

Definition of pharmaceutics

A

the overall process of developing a new chemical entity into an approved therapy that is safe and effective in treating or preventing disease

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9
Q

What does drug target mean?

A

targets specific places in the body to produce a biological response

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10
Q

What are some physiochemical properties of drugs?

A

Ionisation, solid state properties, solubility, molecular weight and molecular structure

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11
Q

What does amorphous mean?

A

molecule has no defined structure, random molecules

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12
Q

What does crystalline mean?

A

Clear structure, lattice structure

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13
Q

What is amorphous melting pt and solubility like?

A

no defined melting point, instead they soften gradually over a range of temperatures and high solubility

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14
Q

What is crystalline melting pt and solubility like?

A

really defined melting pt and low solubility (has a specific temperature range to break the bonds between the molecules)

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15
Q

Define crystal habit

A

the external shape of the crystal, the way the crystal grows depends on the environments, leading to different external shapes, however they have the same crystal lattice, structure

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16
Q

What can affect a crystal habit?

A

concentration, pH, temperature, everything in the environment basically

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17
Q

Define suspension

A

a heterozygous mixture where particles are suspended in a liquid, rather than being dissolved in it

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18
Q

What is polymorphism?

A

A substance that can exist in multiple crystalline phases.

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19
Q

What does amorphous dispersion do?

A

enhances the solubility of the drug, making it much easier to dissolve

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20
Q

Why is polymorphism important for pharmaceutics?

A

different crystalline forms have different physical properties which can have a significant impact on solubility, dissolution rate and stability. All of these directly impact the drug’s bioavailability and efficacy.

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21
Q

What does anhydrous mean?

A

without water

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22
Q

What does a hydrate form imply?

A

Water molecule/s within the structure

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23
Q

Which has a faster dissolution rate; anhydrous or hydrate crystals?

A

Anhydrous forms have a faster dissolution rate

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24
Q

How does the size of the molecule impact the manufacturing of a drug?

A

Particle size affects solubility, smaller particles are easier to synthesise, purify and administer compared to larger particles

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25
What are Co-crystals?
the study of how two or more different molecules can crystallize together through non-covalent bonds
26
Aim of co-crystals
Aims to improve a drug's bioavailability and solubility
27
What is bioavailability?
The proportion of a drug or other substance which enters the circulation when introduced into the body.
28
What does bioavailability determine?
The ability of a substance to have an active effect in the body.
29
What does a solid dispersion usually consist of?
usually a hydrophilic matrix and a hydrophobic drug
30
How is polymerisation used in amorphous dispersions?
polymers are often used to make amorphous dispersions as they help to stabilise the amorphous drug in the solid state and may help prevent crystallisation on dissolution
31
Eutectic mixture
the specific composition of at least two solid components that produces a change of phase to liquid at a certain temperature
32
Why are polymorphs important in pharmacy?
The importance of polymorphic forms is that different polymorphic forms exhibit DIFFERENT physical and chemical properties. They may have different MELTING POINTS, different SOLUBILITIES and usually exist in different HABITS.
33
What is a saturated solution?
a solution where the maximum amount of solute has been dissolved in a given solvent at a specific temperature
34
What is a supersaturated solution?
A supersaturated solution is when a solution has more than the maximum amount of solute dissolved in a solvent at a given temperature
35
What is dissolution?
transfer of solute molecules from solid phase to liquid and transfer of dissolved solute back to solid phase
36
Difference between compounds, solutions and mixtures
Compound - pure substances that consists of two or more elements combined chemically in definite proportions Mixtures - a combination of two or more pure substances in which each pure substance retains its individual chemical properties Solutions - a homogenous mixture, exists in a single phase
37
Intrinsic solubility meaning
The solubility of a compound in its neutral, electrically uncharged (unionized) form, independent of pH
38
Types of solute-solute bonds
dipole-dipole forces (in polar compounds), dispersion forces and hydrogen bonds
39
Types of solvent-solvent bonds
hydrogen bonds, dispersion forces
40
Types of solutions
solid in liquid (w/v), liquid in liquid (v/v), gas in liquids, solids in solids (w/w)
41
If ΔH of solution is negative, increasing the temperature will ____________ solubility of solute.
decrease
42
If ΔH of solute is positive, solvent temp is higher, more solute will be ____________.
dissolved
43
Dielectric constant meaning
Measure of influence by the solvent on energy required to separate two OPPOSITELY charged bodies
44
Electrolyte definition
substances that have a natural positive or negative electrical charge when dissolved in water
45
Ionic compounds
electrons are transferred between atoms
46
Covalent compounds
electrons are shared between atoms
47
With acidic compounds, if pH is 2 or more units below the pKa, it is _________ (unionized or completely ionised)
unionized
48
With acidic compounds, if pH is 2 or more units above the pKa, it is _________ (unionized or completely ionised)
completely ionized
49
With basic compounds, if pH is 2 or more units below the pKa, it is _________ (unionized or completely ionised)
completely ionized
50
With basic compounds, if pH is 2 or more units above the pKa, it is _________ (unionized or completely ionised)
unionized
51
Amphoteric compounds can
act as both an acid or a base
52
What are additives?
a substance that is added to a mixture or compound to change the properties of that mixture or compound
53
What happens when an additive decreases solubility?
salt moves out --> usually occurs because added ions or molecules compete for water molecules and remove water molecules from hydration of another compound
54
How can additives increase solubility?
by altering the interaction between the solute and solvent, such as by forming complexes, changing the solvent's properties, or increasing the surface area of the solute
55
What makes a good solvent for electrolytes?
high dipole moment, smaller molecular size, high dielectric constant
56
Organic electrolytes solubility is determined by
degree of ionization, molecular size, interaction of substituent groups with solvent, crystal properties
57
Colligative properties
vapour pressure lowering, boiling point elevation, freezing point depression and osmotic pressure
58
Osmotic pressure
the minimum pressure applied to a solution to stop the flow of solvent molecules through a semipermeable membrane
59
Vapour pressure lowering
The addition of a nonvolatile solute, which has little tendency to evaporate, results in a lowering of the vapor pressure of the solvent
60
Boiling point elevation
the temperature at which the vapour pressure is equal to atmospheric pressure. Adding solute will decrease vapour pressure
61
Freezing point depression
a drop in the maximum temperature at which a substance freezes
62
Osmolarity
the amount of dissolved solutes per liter of solution
63
Osmolality
the number of particles of solute per kilogram of solvent
64
Difference between osmolarity and osmolality
Osmolality measures solute concentration per kilogram of solvent (water), while osmolarity measures solute concentration per litre of solution
65
Isotonic solutions have equal osmotic pressure which means
equal movement of water into and out of cell
66
Hypotonic solutions have lower osmotic pressure which means
the net water movement is going into the cells, this can lead to rupturing of the cell membrane
67
Hypertonic solutions have higher osmotic pressure which means
the net water movement is going out of the cell
68
Advantages of oral formulations
- easy to administer even with swallowing difficulties - active ingredient dissolve rate is more rapid - taste masking may be achieved
69
Disadvantages of oral formulations
- not suitable for drugs that are unstable in solution - poor solubility of drug may mean it cannot be formulated as a solution - expensive to ship - bulky to carry around
70
Common co-solvents for oral formulations
- glycerol (or glycerin) - alcohol - propylene glycol - polyethylene glycol
71
Surface active agents
- hydrophilic and hydrophobic regions - micelles - micelle ruptures when swallowed - improves solubility of poorly soluble drugs - Tweens (polysorbates), sodium lauryl sulphates
72
What are complexing agents
- used to increase drug solubility - cyclodextrins (sporanox) - PVP (iodine)
73
Buffers
solutions that resist changes in pH when small amounts of acid or base are added. ## Footnote Essential for: - maintaining a stable pH - drug stability - drug efficacy - prevention of degradation
74
Disadvantages of buffers
buffer must be compatible with drug and other excipients because they may react with other components causing a change in pH and concentration (potential toxicity change)
75
Buffer examples
acetic acid, sodium acetate, citric acid, sodium citrate, sodium phosphate
76
Sweetening agent examples
sucrose, glycerol, sorbitol, sodium saccharin, aspartame
77
Flavours to mask salty taste
butterscotch, apricot, peach, vanilla, wintergreen mint
78
Flavours to mask bitter taste
cherry, anise, mint
79
Flavours to mask sweet taste
vanilla, fruit, berries
80
Flavours to mask sour taste
citrus, raspberry
81
Viscosity enhancing agents
assist with palatability as solution does not spread as widely in mouth
82
Antioxidants
prevents drugs from being susceptible to oxygen degradation
83
Oxidation process steps
Initiation – a net increase in free radicals (reactive oxygen species or other elemental species) triggered by heat or light. Propagation – no gain or loss of free radicals. Termination – a net decrease in free radicals.
84
Types of antioxidants
True antioxidants --> a specific type of reducing agent that prevents oxidation of other molecules, thereby protecting them from damage caused by free radicals or reactive oxygen species Reducing agents --> a substance that donates electrons to another substance, reducing its oxidation state while itself getting oxidised Antioxidant synergists --> doesn't fight free radicals, but it enhances the properties of an antioxidant to do its job more efficiently
85
Types of true antioxidants
tocopheryls, alkyl gallates, BHA, BHT
86
Types of reducing agents
ascorbic acid, sodium sulphite, sodium metabisulphite
87
Types of antioxidant synergists
EDTA, citric acid, tartaric acid, lecithin
88
Water soluble antioxidants
sodium sulphite, sodium metabisulphite, sodium formaldehyde sulphoxylate, ascorbic acid
89
Water insoluble antioxidants
used in oil-based formulations butylated hydroxyanisole (BHA), butylated hydroxytoluene (BHT) and propyl gallate
90
T/F Antioxidants are usually present in very low concentrations
True, usually <0.2% w/w
91
Purpose of preservatives
to give drugs a longer shelf life by preventing microbial growth and preserve multi-dose preparation with water as the main solvent
92
ideal properties of preservatives
broad spectrum of activity (effective against gram positive and gram negative bacteria and fungi) chemically and physically stable over shelf-life of product compatible with drug, other excipients and contents low toxicity (affects bacterial cells but not our cells)
93
common preservatives
Benzoic acid and its salts Sorbic acid and its salts Alkyl esters of parahydroxybenzoic acid (paraben)
94
factors affecting preservative efficacy
pH of formulation presence of micelles presence of hydrophilic polymers concentration of the preservative as sometimes the preservative can interact with excipients or drug, affecting the concentration
95
Why use surfactants in a drug
to assist with solubility and stability of poorly soluble drugs
96
T/F the presence of micelles increases the availability or effective concentration of a preservative in solution
False, The widespread use of cationic surfactants as antimicrobial agents can contribute to the development of bacterial resistance.

PHAR1201 (2 decks)

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