Pharmaceutics Suppositories

Front 1

Rank in order of increasing drug delivery
Semisolid
Liquid
Solid

Back 1

Solid --> semisolid --> liquid (highest)

Front 2

Rectal=____
Vaginal=_____
Urethral=______

Back 2

Suppository
Pessary
Bougie

Front 3

Suppository
Size and shape

Back 3

Adult- 2g
Child- 1g
Bullet/finger shaped

Front 4

Pessary
Size and shape

Back 4

5g
Globular or Oviform

Front 5

Bougie
Size and shape

Back 5

4g Male
2g Female
Pencil shaped
3-6mm diameter, 140mm long

Front 6

Local effects of suppositories in the rectum?

Back 6

Constipation: glycerin suppository
Pain, irritation
Itching, inflammation (hemorrhoids)
Local anesthetic

Front 7

Local effect of vaginal Pessary?

Back 7

antiseptic

Front 8

Local effects of Urethral bougies?

Back 8

antibacterial
anesthetic before examinations

Front 9

Which insert is most likely to also have systemic effects?

Back 9

Usually rectal suppositories

Front 10

Advantages of rectal route for systemic effect

Back 10

Mucus membrane permits absoption of many drugs.
Drug not subject to GIT
No first pass effect
Wont irritate stomach
Patients unable to swallow or vomitting

Front 11

what are the factors that affect absorption?

Back 11

Physiological factors --> Body
Physiochemical factors --> drug, dosage form

Front 12

4 categories of physiological factors?

Back 12

1-Architecture
2-Colonic Content
3-Circulation route
4-Ph and lack of Buffering capacity

Front 13

Describe the architecture of the rectum

Back 13

rectum is 15-20cm
2-3ml of mucus
not mobile in resting state
no villi or microvilli

Front 14

Colonic content affect on absorption

Back 14

empty vs distended w/ fecal matter
diarrhea colonic obstruction due to tumorous growth

Front 15

Circulation route

Back 15

High vascularization
bypass the portal circulation, abosorption through hemorrhoidal veins and lymphatic circulation

Front 16

pH and lack of buffering capacity

Back 16

rectal fluids are neutral
no chemical changes made to the drug.
pH affects solubility and absorption

Front 17

_____ drugs in low concentration in a fatty base, have a low tendency for absorption.
How to prevent this?

Back 17

Lipophilic

Use the salt form of a drug.
otherwise, the drug will dissolve too well in the like base, and it will prefer the base over the aq. rectum

Front 18

water soluble bases will release..

A H2O soluble drugs
B Oil soluble drugs
C Both

Back 18

both

Front 19

What is the main requirement for a base?

Back 19

it must melt, dissolve, or soften quickly in the body

Front 20

What are some possible problems that can be created by the base?

Back 20

interaction with drug
base does not release drug
base irritates mucus membrane and promotes bowl movement when not needed

Front 21

other requirements of bases

Back 21

Offer control over drug release
min amount of base(too much=leakage)
residence time up to 24hr (no SR,ER)
if needed, offer emollient, protective, occlusive effect

Front 22

What are the types of bases used?

Back 22

Oleaginous/fatty
Water soluble (completely soluble)
Water miscible (o/w)
Miscellaneous

Front 23

examples of fatty bases

Back 23

Cocoa butter
Hydrogenated fatty acids of veg. oil (palm oil)
Glycerin + high molec weight fatty acids (glyceryl monostearate)
Combination of these to achieve proper melting point

Front 24

Emulsifying agents may be added to fatty bases
True or False

Back 24

True

Front 25

_____ is the traditional base, a natural product with a melting temp of 30-36 degrees C

Back 25

Cocoa butter

Front 26

disadvantages and problems when using CB as a base

Back 26

Natural product--> quality control
Can melt in hand or package on warm day.
Leakage
Polymorphism
Freezing point depression

Front 27

What is polymorphism?

Back 27

Existence as both alpha and beta forms.
Happens to CB when melted carelessly at high temp.
alpha is formed (metastable) less stable, low melt point.
transforms to Beta (more stable) in a few days

Front 28

What is freezing point depression?
what is used to lower melting points?

Back 28

Remains liquid at normal freezing temperature.
Phenol or Chloral hydrate can lower melting point.

Front 29

What can be added to a base to restore melting point being lowered from freezing point depression?

Back 29

wax
cetyl ester or beeswax

Front 30

Other fatty bases

Back 30

Fattibase, wecobee, witepsol
Triglycerides and varying amounts of di/monoglycerides from veg. source.

Front 31

Water soluble and water miscible bases

Back 31

Glycerinated gelatin
Polyethylene glycol (polymer)

Front 32

Gelatin 20% and glycerin 70% + 10% water or drug solution is preferred for ____ inserts for a longer local effect

Back 32

Vaginal (pessaries)

its dissolution is slower than CB

Front 33

Gelatin 60% +glycerin 20% + 20% drug solution is preferred for _____ inserts

Back 33

Urethral (Bougies)

Front 34

Due to the hydroscopic nature of water soluble and water miscible based suppositories.....

Back 34

should protect from moisture
has dehydrating effect and irritation upon insertion
Should be moisturized with water b4 insertion

Front 35

PEG uses ____ as a mechanism of drug release

Back 35

dissolution
no need to melt at body temp

Front 36

PEG commonly uses MW of 300-8000
300,400,600 is_____
over 1000 is _____

Back 36

a clear liquid
a wax like solid

a combination of different MW's to adjust physical properties

Front 37

Advantages of PEG

Back 37

slow release
easy storage
no leakage from orifice
wont melt

Front 38

if PEG is less than ___% water, it should be dipped in water before insertion

Back 38

20

Front 39

Misc. bases

Back 39

mixture of oleaginous and H2O soluble/water miscible materials

Some are w/o emulsions or will form emulsion upon dispersion into water

Front 40

3 ways to prepare suppositories?

Back 40

Molding- compounding
Compression- industrial
Hand rolling- small scale

Front 41

Process of molding suppositories

Back 41

Melt base to workable texture
Incorporate medication
Prep the mold --> lubrication
Pour into mold
Allow to cool
Removal

Front 42

____ and ____ dont require lubricating the mold because they contract when cooled

Back 42

PEG and CB

Front 43

want to solidify quickly because drug can ____ and will not be uniform

Back 43

settle (like a suspension)

mold can be pre chilled

Front 44

Suppository molds can be made from...

Back 44

aluminum
brass
plastic
rubber
foil paper
can be part of final package

Front 45

Mold must be calibrated because

Back 45

drug amounts expressed as weight
mold can be by volume (calculate density) or in relation to CB
base and drug have different densities

Front 46

Pouring temp and cooling is critical for

Back 46

content uniformity
should stir and pour all at once.
should be smooth, even, free of marks, not gritty

Front 47

Advantages of Compression

Back 47

Heat liable meds
no medication can precipitate in bottom of mold.
base softens by friction

Front 48

Disadvantages of compression

Back 48

special machine
limited shape (forced through a die)

Front 49

Drugs for local vaginal effect

Back 49

Nystatin
eletrimazole
sulfanilamide
providonejodine
nonoxynol 9
estrogenic substances

Front 50

drug for systemic vaginal effect

Back 50

progesterone

Front 51

drugs for local rectal effect

Back 51

ZnO
balsamperu
Bismuth Salts

Front 52

Drug for systemic rectal effect

Back 52

Morphine

Front 53

Rectal suppository
Bisacodyl

Back 53

Cathartic (purging,cleansing)

Front 54

Rectal suppository
Prochlorperazine

Back 54

antiemetic
(vomiting, nausea, motion sickness)

Front 55

Rectal suppository
hydrocortisone

Back 55

local antipyretic (reduce fever)

Front 56

Rectal suppository
Glycerin

Back 56

Glycerin 91g etc
for constipation

Front 57

Urethral Bougie
Alprostadil microsuppositories

Back 57

1.4mm x 3-6mm in special applicator
for erectile dysfunction

Front 58

Vaginal inserts
suppositories and tablets

Back 58

treat infection, restore mucosa, contraception
Nystatin, clotrimazole, sulfanolamide
PEG and SAA may be buffered to acidic pH
Plastic insertion device