Formulation Requirements Flashcards

1
Q

what is the response with IV administration

A

large proximal vein, rapid response

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2
Q

what is the response with intramuscular administration

A

into a muscle, small volume of injection with fairly rapid absorption, can be used for controlled release formulations

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3
Q

what is the response with subcutaneous administration

A

into subcutaneous tissue, slower onset of action and absorption of drugs
can be used for implants

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4
Q

what does intradermal mean

A

between epidermis and dermis

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5
Q

what does intrathecal mean

A

into cerebrospinal fluid

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6
Q

what does epidural mean

A

outside the dura

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7
Q

what does intra-articular mean

A

into the synovial fluid of a joint cavity

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8
Q

what does intracardiac mean

A

into the muscles of the heart

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9
Q

what does intra-arterial mean

A

similar to IV but rarely used

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10
Q

what does intraocular mean

A

into the eye

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11
Q

what are the advantages of parenteral formulations

A

immediate physiological response, drugs with poor bioavailability used, unconscious or vomiting patients, control of dosage and frequency of administration, requirement for localised effect, correction of electrolytes, range of drug release profiles, total parenteral nutrition

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12
Q

what are the disadvantages of parenteral formulations

A

more complicated manufacture, skill needed for administration, pain on administration, allergy is rapid onset, difficult to reverse drug effects

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13
Q

what are the general requirements for parenterals

A

sterile, free from endotoxins and pyrogens, free from particulates

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14
Q

what physiochemical drug properties are needed for formulation

A

good solubility in solution, moderate solubility if using co-solvents, low solubility if in suspension

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15
Q

what drug peoperties are needed for IV products

A

aqueous solutions that do not precipitate in blood stream

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16
Q

what drug properties are needed for SC or IM products

A

suspensions (aqueous r oil based) and oil-based solutions, aqueous solutions

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17
Q

what are the colligative properties of formulations

A

vapour pressure lowering, boiling point elevation, freezing point depression, osmotic pressure

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18
Q

what are colligative properties

A

properties of solutions dependent on the ratio of solute particles to solvent particles in the solution, not the identity of the solute

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19
Q

what is vapour pressure depression

A

addition of non-volatile solute to a solvent, reduces vapour pressure above the liquid
results from some particles in the gas phase

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20
Q

what is boiling point elevation

A

dissolution of non-volatile solute in a solvent increases bp of solution with respect to that of pure solvent
change in T = Kb m
kb is bp constant

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21
Q

what is freezing point depression

A

dissolution of a non-volatile solute in solvent decreases the freezing point of the solution with respect to that of pure solvent
cange in T = Kf m
Kf is freezing point depression

22
Q

what is osmosis

A

solvent from lower concentration solution will move through semi-permeable membrane to higher conc solution

23
Q

what is osmotic pressure

A

external pressure that must be applied to prevent the movement of solvent via osmosis

24
Q

what is the osmotic pressure equation for a non-electrolyte solution

A

V
n= moles, R= gas constant, t=temp, v=vol

25
Q

what is the van’t hoff factor

A

osmotic pressure = icRT

i= given value, R=gas constant, t=temp, c=conc

26
Q

what is osmolality

A

number of osmoles/kg of solvent

27
Q

what is osmolarity

A

number of osmoles/litre of solution

28
Q

what is the normal osmolality for blood

A

275 to 295 mOsm/kg

29
Q

what is an isosmotic solution

A

conc of solution and intracellular conc are equal

30
Q

what is a hyper-osmotic solution

A

conc of solution greater than intracellular conc

cell shrinks

31
Q

what is a hypo-osmotic solution

A

conc of solution smaller than intracellular conc

cell swells

32
Q

what is isosmoticity

A

two solutions separated by a semi-permeable membrane and there is no net movement of solute

33
Q

what is isotonicity

A

two solutions separated by a biological membrane and remain in osmotic equilibrium

34
Q

what is the difference between isomotic and isotonic solutions

A

a solution that is isosmotic with blood will only be isotonic if the blood cells are impermeable to the solute molecules and permeab;e to the solvent

35
Q

what is osmoticity

A

property of solution and independent of any membrane

36
Q

what is tonicity

A

property of solution in reference to a particular membrane

37
Q

what solutions are not isotonic with biological membranes

A

ammonium chloride, urea, glycerine, propylene glycol

38
Q

what terms are used for osmoticity if the membrane is impermeable to solutes

A
isosmotic = isotonic
hyper-osmotic = hypertonic
hypo-osmotic = hypotonic
39
Q

what type of solution is preferred for parenteral preparation

A

isotonic
hypotonic can be adjusted with dextrose or sodium chloride
hypertonic solutions cannot be adjusted

40
Q

what are the effects of excessive IV infusion of a hypotonic solution

A

RBC swelling, haemolysis, water ingress into cells/tissues, water intoxication leading to convulsion and oedema

41
Q

what are the effects of excessive IV infusion of an isotonic solution

A

possible increase in extravascular fluid volume and circulatory overload

42
Q

what are the effects of excessive IV infusion of a hypertonic solution

A

hyperglycaemia, intracellular dehydration, osmotic diuresis, water/electrolyte loss, dehydration, coma
also RBC creatination, low bp, shallow respiration, pulmonary oedema, haemorrhage

43
Q

what injection routes require isotonic solutions

A

intraspinal/intrathecal injections, intradermal injections, intramuscular and subcutaneous injections (hypertonic can increase IM drug absorption)

44
Q

what does TPN stand for

A

total parenteral nutrition

45
Q

what is the osmolarity method of preparing isosmotic solutions

A
  1. calculate osmolarity of components
  2. determine remaining osmolarity needed to make solution isotonic with body fluids
  3. calculate amount of adjusting substance required to make up the shortfall
46
Q

what is the freezing point of bodily fluids

A

-0.52 degrees C

47
Q

how to calculate freezing point depression

A

freezing point depression constant is 1.86 for water

overall, Tf from all components must be 0.52 degrees C

48
Q

what is the NaCl equivalents method

A

the sodium chloride equivalent of a solute is the mass of NaCl that lowers the freezing point of a solvent to the same extent as 1g of the solute

49
Q

what is the White-Vincent method

A

water added to the drug and excipients in a sufficient amount to form an isotonic solution
preparation is then diluted to final volume with an isotonic or buffered isotonic diluting vehicle

50
Q

which calculation method is inaccurate

A

osmolarity method

it is just an estimation

51
Q

what is the molecular weight of NaCl

A

58.44

52
Q

what are the ideal conditions for an isotonic solution

A

freezing point -0.52
0.9% NaCl
285 mOsm/L
the membrane must be impermeable for solute isotonicity