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Pharmaceutics part B > Rectal and Vaginal Delivery > Flashcards

Rectal and Vaginal Delivery Flashcards

1
Q

what must you do with diazepam suppositories

A

make sure green shows and dose is locked in place

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2
Q

therapeutic effects of suppositories can be

A

local and systemic

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3
Q

which population is best for suppositories

A

children
elderly
uncooperative

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4
Q

what limits suppository use

A

tradition and culture

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5
Q

local effects of suppositories

A

pain control
infection
inflammation
constipation

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6
Q

systemic effects of systemic effects

A

asthma
fever control
RA

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7
Q

drug factors of absorption

A

solubility - must be solubilized to be absorbed
pKa
partition coefficient - not too high so doesnt stay in base but high enough to cross

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8
Q

formulation factors for absorption

A

base type and amount
formulation disintegration
drug dissolution

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9
Q

physiological factors of absorption

A

pH

water amount

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10
Q

where is there direct systemic absorption

A

lower and middle veins

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11
Q

where is there absorption that passes the liver

A

upper vein

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12
Q

whats critical to how drug is released and absorbed

A

application

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13
Q

what is the ph of the rectum and what determine the final ph

A

7.5 wiht little buffer capacity (will change based on drug)

not able to maintain its ph so drug solution will determine the ph

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14
Q

amount of water in the rectum

A

3ML

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15
Q

main absorption mechanism in rectal

A

passive

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16
Q

drug release

A

melts and spreads
sedimentation
wetting
dissolution

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17
Q

what are the major parameters of suppository

A

partition coeffecient
pka
particle size
surfactants

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18
Q

partition coefficient limits what

A

rate limiting from vehicle to body fluid

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19
Q

pka limits what

A

rate limiting rom body fluid into blood

want non ionized

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20
Q

what particle size is preferred in suppositories

A

50-100um

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21
Q

what do surfactants in suppositories do

A

promote wetting, partition and permeation

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22
Q

components of an ideal base

A 
non toxic 
non irritating 
no metastable form s
wetting and emulsifying properties 
high water number 
stability over storage
east manufacturing properties
23
Q

whats a metastable form

A

heating causes it to change forms and then change the melting point temperature

24
Q

advantages of cocoa butter

A

nonreactive
nontoxic
versatile

25
Q

why isnt cocoa butter used anymore as a vehile

A

polymorphism
low softening point
cost

26
Q

what is used as a vehicle now

A

semisynthetic fatty triglycerides

27
Q

hydrophilic vehicle properties

A

higher melting point - not intended to melt release by dissolution
slower drug dissolution
hygroscopic
drug instability

28
Q

molding mehtods for suppositories

A 
hand molding 
compression molding 
pour molding 
automatic molding
in package molding
29
Q

4 things for quality control

A

weight
disintigration
melting behavious
softening time

30
Q

why is water as a solvent avoided

A 
accelerates vehicle oxidation 
precipitates dissolved substances
instability in presence of water 
growth of bacteria and fungus 
little impact on drug absorption
31
Q

physics problems

A

hygroscopicity of gelatin and PEG
viscosity
volume contraction

32
Q

whats contraction hole formation

A

when pour in mold it contracts as it cools so have to overfill the mold to compensate

33
Q

how should suppositories be stored

A

some refridgerated
avoid temp fluctuation
avoid from light and oxygen
completely closed

34
Q

good and bad of enema

A

easy drug absorption

application in convenience

35
Q

how do effervecent tables work in the rectum

A

dissolve and realease co2 to stimulate defecation

limited use becuase not enough water

36
Q

intravaginal products used for

A

STI
contraception
cancer
hormone replacement

37
Q

vaginal mucosa

A

epithelium
laminar propria
blood vessels
muscularis

38
Q

arteries the the vagina

A

iliac artery
vaginal venous plexus
vaginal artery and vein

39
Q

epithelium thickness changes during menstruation affecting what

A

drug absorption

40
Q

amount and ph of vaginal fluid

A

.5-10ml

3.5-4.9

41
Q

cervial mucus can act as a what

A

barrier

42
Q

what can the drug be degraded by

A

cervicovaginal fluid

contians enzymes and nucleases

43
Q

what are synthetic epithelial tissues used for

A

in vitro irritation models

44
Q

siRNA mechanism

A

rna corresponds with specific target and drug properties are incorporated into it
crosses the cell membrane and use RNAi mechanism for gene slicing that exhibits therapeutic effect

45
Q

factors affecting siRNA delivery

A 
pH 
nucleases
infections lower pH 
menstruation alters microflora and endothelial thickness
mucosal entrapment 
vaginal fluid volume
46
Q

advantage of vag gel

A

doesnt require HCP
discrete
portable

47
Q

disadvantage of vag gel

A 
messy 
have to apply before intercourse 
requires time to disperse
dose may not be accurate
short lasting
48
Q

advantage of vag film and tablet/supp

A

doesnt require HCP
portable
discreet
not messy

49
Q

disavantage of vag film and tablet/supp

A

require insertion before intercourse
time to melt
short acting
possibly limited use in hihg temperature climates

50
Q

advantage of vag ring

A 
doesnt require insertion by HCP 
doesnt have to be inserted before intercourse
discreet
not messy 
long lasting
51
Q

disadvantage of vag ring

A

siRNA cant withstand high processing temps

52
Q

advantage of foam

A

not that messy

doesnt require HCP

53
Q

disadvantage of foam

A

time to disperse
has to be inserted before intercouse
short acting

54
Q

4 things in and ideal vaginal delivery system

A

non irritating
doesnt get trapped in mucosal layer
resist degradation but nucleases
resist inactivation in low pH

Pharmaceutics part B (4 decks)

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