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Pharm 125 > rectal and vaginal dosage forms > Flashcards

rectal and vaginal dosage forms Flashcards

1
Q

suppositories definition

A

dosage form adapted for application into the rectum

-melt, soften or dissolve at body temperature

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2
Q

inserts definition

A

solid dosage from inserted into naturally occuring body cavity other than mouth or rectum

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3
Q

suppositories definition round 2

A

semi-solid or solid dosage form

intended to be inserted into body orfices

  • rectum
  • vagina (inserts or pessaries)
  • urethra (inserts or bougies)
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4
Q

advantages (6(

A

patients cannot swallow
-(children, elderly, nausea, and vomiting)

GI tract irritant drugs

treatment of diseases of lower parts of GI

once daily use

local and systemic effect

avoid hepatic first pass metabolism (if administered correctly

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5
Q

disadvantages

A

poor compliance

discomfort and leakage

variation of absorption
- shit first

irritation of mucous membranes caused by some drugs or bases

upward movement of suppository from local site can inc first pass metabolism

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6
Q

classification of suppositories

A

rectal
vaginal (inserts or pessaries)
urethral (inserts or bougies)

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7
Q

rectal suppositories shape

A

bullet and torpedo shape

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8
Q

rectal suppositories weight

  • baby
  • adult
  • rectal rocket
A

baby: 1g
adult: 2g

rectal rocket 4-5g

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9
Q

rectal suppositories local action

A

hemorrhoids
itching
infections

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10
Q

rectal suppositories systemic action

A

antinauseants
analgesics
hormones

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11
Q

rectal suppositories drug content

A
  1. 1% up to 30-40% (from blank weight

- variable

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12
Q

other rectal preparations (8)

A 
rectal capsules
rectal tablets
solutions (enemas)
suspension
emulsions
ointments
foams
tampons
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13
Q

benefit of rectal rocket

A

internal and external treatment

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14
Q

vaginal inserts shape

A

usually globular, oval or cone shaped

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15
Q

vaginal inserts weight

A

3-5g each

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16
Q

vaginal inserts bases

A

water soluble or water miscible vehicles

PEG or glycerinated gelatin

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17
Q

vaginal inserts uses

A

contraceptives
gynecological ailments
antiseptics

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18
Q

other dosage forms for vaginal application

A 
solutions
ointments
creams
gels
foams
implants
tablets
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19
Q

urethral inserts shape

A

cylindrical
-vary in length according to gender

females
50mm length

males
12.5mm in length

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20
Q

urethral inserts diameter

A

3-6mm

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21
Q

urethral inserts weight

  • female
  • male
A

~2g female

~4g male

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22
Q

urethral inserts uses (3)

A

severe ED
-alprostadil

antibacterial

local anesthetic preparative for urethral exam

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23
Q

composition of suppositories (3)

A

1) API
2) additives
3) suppository bases

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24
Q

Other types of suppositories

A

hollow type
-drug in sol’n/suspension in hollow cavity

multilayered
-good for sep incompatible reagents/excipients

sustained release
-viscosity inducing ingredient to modify release

thermo-reversible liquid

  • forms gel when warm
  • mucoadhesive properties

effervescent

  • foams and froths in contact with body fluid
  • aids in dispersion of drug
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25
Q

rectal cavity physiological factors

  • mucus fluid
  • pH
  • surface area
  • fecal matter
A

small mucus fluid volume (1-3mL)
-problem for drugs that are poorly water sol

pH = 6.8 - 7.4 and lower buffer capacity
-excipients and API can change pH of fluids

small surface area relative to GI

presence of fecal matter
-council evacuate b4 insert

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26
Q

blood supply to rectal area

A

inferior rectal vein

superior rectal vein

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27
Q

inferior rectal vein

A

transports drugs into IVC and bypass iver

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28
Q

superior rectal vein

A

transports drugs to upper part of rectal cavity to the liver

29
Q

why is it hard to predict if drug will avoid liver metabolism

A

depends on if abs by IRV or SRV

30
Q

Cocoa butter and fatty base, drug release and absorption

A

oleaginous (fatty base) melts and spreads, drug partitions from molten base, dissolves in mucus, diffuses across membrane

31
Q

PEG base, drug release and absorption

A

hydrophilic base absorbs water and dissolves in fluids

drug dissolves in mucus and diffuses across membrane

32
Q

formulation and drug properties factors: melting or dissolution of base (2)

A

1) melting point
- melt at body T or few below
- fatty bases melt

2) aqueous solubility and dissolution
- water sol bases need dissolve to release drug, slower release than fatty bases

33
Q

formulation and drug properties factors: release and diffusion of drug (4)

A

1) solubility of drug in vehicle and in rectal fluids’
2) drug particle size
3) spreading capacity
4) base viscosity at rectal temperature

34
Q

formulation and drug properties factors: rectal mucosa

A

1) pKa of drug
2) pH induced in rectal fluids
3) presence of buffers
4) partition coefficient of drug

35
Q

solubility of drug in vehicle

-what mixes

A

if put liophilic drug in fatty base
- low tendency drug escape from base into rectal cavity

SO

FB use hydrophillic drug

36
Q

solubility of drug in rectal fluids considerations

A

small vol rectal fluids
-difficult for poorly water sol drugs dissolve
+add wetting agents or surfactants to increase solubility of drug

37
Q

drug particle size consideration

A

smaller particle size = more dissolution = more absorption = prevents sedimentation

ALSO

remains longer in vehicle and eliminates some mechanical irritation

38
Q

spreading capacity considerations

A

increase area for absorption

-add surfactant to increase spreading capacity

39
Q

viscosity of base at rectal temperature considerations

A

higher viscosity = diffuse slowly = helps disperse drug uniformely throughout melted base

40
Q

pKa of drug considerations

A

unionized cross membrane easier

41
Q

pH induced in rectal fluids considerations

A

recal fluids dont have high buffer capacity

supp base/ presence of buffer affect drug ionization

42
Q

partition coefficient considerations

A

drug needs some lipophillic properties to permeate through rectal mucosa

43
Q

drug release from oleaginous base

A

hydrophillic drugs
- good release resulting in abs

lipophilic drugs

  • tend to remain in base, slow release, little abs
  • if possible use ionized salt form of drug or fatty acid base with surfactant
44
Q

drug release from water soluble suppository

A

hydrophillic drugs
- moderate release (dpnds on disoolution of base and diffusion of drug)

lipophilic drugs
-good to moderate release resulting in absorption

45
Q

higher molecular weight PEGs result in what

A

longer dissolution time

46
Q

Preparation of suppositiories (3)

-what is the most common

A

hand rolling and shaping
-traditional - not really used now

compression

  • no heat (good for heat labile drugs)
  • not very popular - requires specialized machine and limited shapes made
  • base and drug mixed then compressed into mold

fusion molding (most common)

  • base melted in controlled water bath
  • drug disoolved/dispersed into base
  • pured into molds (metal, plastic)
47
Q

Hand rolling and shaping: specialized equipment?

A

no specialized equipment

48
Q

Hand rolling and shaping: role

A

historic

49
Q

Hand rolling and shaping: difficult?

A

requires lot of skill

50
Q

Hand rolling and shaping: what base

A

generally cocoa butter bc easy manipulate

51
Q

Hand rolling and shaping: steps (5)

A

1) triturate fine powder/extracts making paste with cocoa butter
2) add grated cocoa butter and triturate to incorporate
3) knead mass until pliable
4) roll out cylinder pipe using both hands and cut into pieces
5) roll to suppository shape

52
Q

Compression molding: process

A

base and ingredients combined by mixing into paste-like consistency

mixed mass forced into special molds

53
Q

Compression molding: advantages

A

suitible for heat labile substances

good for substances that are insoluble in base

54
Q

Compression molding: disadvantages

A

requires special suppository machine

limited shapes can be made

55
Q

fusion molding: preparation

A

melting supp base and dispersing/dissolving drug into melted base

56
Q

fusion molding: steps (7)

A

1) calbration of mold
2) melt base in water bath at low heat
3) incorporate API and additives into melted base
4) pour melt base into molds ctsly to prevent layering
5) allow suppositories to cool
6) trim excess with spatula
7) remove formed suppositories from mold and wrap individually (if metal mold used) or dispense in disposable plastic mold

57
Q

packaging suppositories (3)

A

lined with grease proof paper or wrapped in foil and placed in partitioned rigid paper boxes

in compounding more commoly dispensed in disposable plastic molds inside paper box or disposable plastic shells

hygroscopic products (glycerol suppositories)
-dispensed in tightly closed glass or plastic containers
58
Q

quality control tests: visual examination (3)

A

color: intensity, nature, homogeneity

texture-surface: smoothness of the surface

appearance: dry or oily?moist

59
Q

quality control tests: weight uniformity

A

yes this is one eeeeee

60
Q

quality control tests: more industrial tests not done in pharmacy

A

uniformity of APIs

mechanical str

disintegration tests

melting behaviour

drug release from suppositories

61
Q

determination of amount of base required (4)

A

density factor calculation

estimation ratio

0.7 estimated DF

double casting method

62
Q

what does a DF of 1.2 mean

A

1.2g of API will displace 1g of base

63
Q

when do we need density factors

A

when quant of drug is more than 100mg in a 2g mold (5%)

64
Q

estimation by ratio

A

used to calc DF of a drug using the ratio of blank supp of an unknown base to a blank of cocoa butter

65
Q

0.7 estimated DF

A

powders have an estimated average displacement of 0.7g of suppository base for each gram of drug

INVERSE OF DF

66
Q

DOUBLE CASTING TECHNIQUE: when to use (3)

A

when the quantity of drug is greater than 100mg

drug is used for systemic effect

DFs are not known

67
Q

double casting technique: steps (4)

A

1) first cast
- mix all of drug with a portion of the base
- fill partially each of the cavities

2) overfill cavities with plain base
- if needed for DF determination, calibrate at least 3 cavities with plain base

3) let coool, removed excess from top, remove suppositories and re-melt
4) second cast to distribute evenly the drug

68
Q

why do we overfill in double casting technique

A

because pores form, if overfill pore form on overfill that is removed

69
Q

how do you calculate the DF from the double casting method

A

paddock method

Pharm 125 (5 decks)

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