Formulation Requirements

Question 1

what is the response with IV administration

Answer 1

large proximal vein, rapid response

Question 2

what is the response with intramuscular administration

Answer 2

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

Question 3

what is the response with subcutaneous administration

Answer 3

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

Question 4

what does intradermal mean

Answer 4

between epidermis and dermis

Question 5

what does intrathecal mean

Answer 5

into cerebrospinal fluid

Question 6

what does epidural mean

Answer 6

outside the dura

Question 7

what does intra-articular mean

Answer 7

into the synovial fluid of a joint cavity

Question 8

what does intracardiac mean

Answer 8

into the muscles of the heart

Question 9

what does intra-arterial mean

Answer 9

similar to IV but rarely used

Question 10

what does intraocular mean

Answer 10

into the eye

Question 11

what are the advantages of parenteral formulations

Answer 11

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

Question 12

what are the disadvantages of parenteral formulations

Answer 12

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

Question 13

what are the general requirements for parenterals

Answer 13

sterile, free from endotoxins and pyrogens, free from particulates

Question 14

what physiochemical drug properties are needed for formulation

Answer 14

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

Question 15

what drug peoperties are needed for IV products

Answer 15

aqueous solutions that do not precipitate in blood stream

Question 16

what drug properties are needed for SC or IM products

Answer 16

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

Question 17

what are the colligative properties of formulations

Answer 17

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

Question 18

what are colligative properties

Answer 18

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

Question 19

what is vapour pressure depression

Answer 19

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

Question 20

what is boiling point elevation

Answer 20

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

Question 21

what is freezing point depression

Answer 21

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

Question 22

what is osmosis

Answer 22

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

Question 23

what is osmotic pressure

Answer 23

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

Question 24

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

Answer 24

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

Question 25

what is the van't hoff factor

Answer 25

osmotic pressure = icRT | i= given value, R=gas constant, t=temp, c=conc

Question 26

what is osmolality

Answer 26

number of osmoles/kg of solvent

Question 27

what is osmolarity

Answer 27

number of osmoles/litre of solution

Question 28

what is the normal osmolality for blood

Answer 28

275 to 295 mOsm/kg

Question 29

what is an isosmotic solution

Answer 29

conc of solution and intracellular conc are equal

Question 30

what is a hyper-osmotic solution

Answer 30

conc of solution greater than intracellular conc | cell shrinks

Question 31

what is a hypo-osmotic solution

Answer 31

conc of solution smaller than intracellular conc | cell swells

Question 32

what is isosmoticity

Answer 32

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

Question 33

what is isotonicity

Answer 33

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

Question 34

what is the difference between isomotic and isotonic solutions

Answer 34

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

Question 35

what is osmoticity

Answer 35

property of solution and independent of any membrane

Question 36

what is tonicity

Answer 36

property of solution in reference to a particular membrane

Question 37

what solutions are not isotonic with biological membranes

Answer 37

ammonium chloride, urea, glycerine, propylene glycol

Question 38

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

Answer 38

``` isosmotic = isotonic hyper-osmotic = hypertonic hypo-osmotic = hypotonic ```

Question 39

what type of solution is preferred for parenteral preparation

Answer 39

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

Question 40

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

Answer 40

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

Question 41

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

Answer 41

possible increase in extravascular fluid volume and circulatory overload

Question 42

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

Answer 42

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

Question 43

what injection routes require isotonic solutions

Answer 43

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

Question 44

what does TPN stand for

Answer 44

total parenteral nutrition

Question 45

what is the osmolarity method of preparing isosmotic solutions

Answer 45

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

Question 46

what is the freezing point of bodily fluids

Answer 46

-0.52 degrees C

Question 47

how to calculate freezing point depression

Answer 47

freezing point depression constant is 1.86 for water | overall, Tf from all components must be 0.52 degrees C

Question 48

what is the NaCl equivalents method

Answer 48

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

Question 49

what is the White-Vincent method

Answer 49

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

Question 50

which calculation method is inaccurate

Answer 50

osmolarity method | it is just an estimation

Question 51

what is the molecular weight of NaCl

Answer 51

58.44

Question 52

what are the ideal conditions for an isotonic solution

Answer 52

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