Rectal and Vaginal Delivery

Question 1

what must you do with diazepam suppositories

Answer 1

make sure green shows and dose is locked in place

Question 2

therapeutic effects of suppositories can be

Answer 2

local and systemic

Question 3

which population is best for suppositories

Answer 3

children
elderly
uncooperative

Question 4

what limits suppository use

Answer 4

tradition and culture

Question 5

local effects of suppositories

Answer 5

pain control
infection
inflammation
constipation

Question 6

systemic effects of systemic effects

Answer 6

asthma
fever control
RA

Question 7

drug factors of absorption

Answer 7

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

Question 8

formulation factors for absorption

Answer 8

base type and amount
formulation disintegration
drug dissolution

Question 9

physiological factors of absorption

Answer 9

pH

water amount

Question 10

where is there direct systemic absorption

Answer 10

lower and middle veins

Question 11

where is there absorption that passes the liver

Answer 11

upper vein

Question 12

whats critical to how drug is released and absorbed

Answer 12

application

Question 13

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

Answer 13

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

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

Question 14

amount of water in the rectum

Answer 14

3ML

Question 15

main absorption mechanism in rectal

Answer 15

passive

Question 16

drug release

Answer 16

melts and spreads
sedimentation
wetting
dissolution

Question 17

what are the major parameters of suppository

Answer 17

partition coeffecient
pka
particle size
surfactants

Question 18

partition coefficient limits what

Answer 18

rate limiting from vehicle to body fluid

Question 19

pka limits what

Answer 19

rate limiting rom body fluid into blood

want non ionized

Question 20

what particle size is preferred in suppositories

Answer 20

50-100um

Question 21

what do surfactants in suppositories do

Answer 21

promote wetting, partition and permeation

Question 22

components of an ideal base

Answer 22

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

Question 23

whats a metastable form

Answer 23

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

Question 24

advantages of cocoa butter

Answer 24

nonreactive
nontoxic
versatile

Question 25

why isnt cocoa butter used anymore as a vehile

Answer 25

polymorphism low softening point cost

Question 26

what is used as a vehicle now

Answer 26

semisynthetic fatty triglycerides

Question 27

hydrophilic vehicle properties

Answer 27

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

Question 28

molding mehtods for suppositories

Answer 28

``` hand molding compression molding pour molding automatic molding in package molding ```

Question 29

4 things for quality control

Answer 29

weight disintigration melting behavious softening time

Question 30

why is water as a solvent avoided

Answer 30

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

Question 31

physics problems

Answer 31

hygroscopicity of gelatin and PEG viscosity volume contraction

Question 32

whats contraction hole formation

Answer 32

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

Question 33

how should suppositories be stored

Answer 33

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

Question 34

good and bad of enema

Answer 34

easy drug absorption | application in convenience

Question 35

how do effervecent tables work in the rectum

Answer 35

dissolve and realease co2 to stimulate defecation | limited use becuase not enough water

Question 36

intravaginal products used for

Answer 36

STI contraception cancer hormone replacement

Question 37

vaginal mucosa

Answer 37

epithelium laminar propria blood vessels muscularis

Question 38

arteries the the vagina

Answer 38

iliac artery vaginal venous plexus vaginal artery and vein

Question 39

epithelium thickness changes during menstruation affecting what

Answer 39

drug absorption

Question 40

amount and ph of vaginal fluid

Answer 40

.5-10ml | 3.5-4.9

Question 41

cervial mucus can act as a what

Answer 41

barrier

Question 42

what can the drug be degraded by

Answer 42

cervicovaginal fluid | contians enzymes and nucleases

Question 43

what are synthetic epithelial tissues used for

Answer 43

in vitro irritation models

Question 44

siRNA mechanism

Answer 44

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

Question 45

factors affecting siRNA delivery

Answer 45

``` pH nucleases infections lower pH menstruation alters microflora and endothelial thickness mucosal entrapment vaginal fluid volume ```

Question 46

advantage of vag gel

Answer 46

doesnt require HCP discrete portable

Question 47

disadvantage of vag gel

Answer 47

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

Question 48

advantage of vag film and tablet/supp

Answer 48

doesnt require HCP portable discreet not messy

Question 49

disavantage of vag film and tablet/supp

Answer 49

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

Question 50

advantage of vag ring

Answer 50

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

Question 51

disadvantage of vag ring

Answer 51

siRNA cant withstand high processing temps

Question 52

advantage of foam

Answer 52

not that messy | doesnt require HCP

Question 53

disadvantage of foam

Answer 53

time to disperse has to be inserted before intercouse short acting

Question 54

4 things in and ideal vaginal delivery system

Answer 54

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