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PHA333 > suppositories > Flashcards

suppositories Flashcards

1
Q

What are suppositories?

A

solid, single dose preparations

they contain 1 or more active substances dispersed/dissolved in a suitable basis that may be soluble or dispersible in water and may melt at body temperature

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2
Q

types of suppositories

A

rectal

vaginal (pessaries)

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3
Q

rectal blood circulation

A

superior rectal artery - main blood supply

haemorrhoidal veins (superior, middle, inferior veins) - drug absorption

drug absorption from inferior/middle veins - bypass 1st pass metabolism

absorption from superior veins - liver, 1st pass metabolism

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4
Q

SYSTEMIC effects of rectal suppositories

A

analgesia - paracetamol/NSAIDs

CNS disorders - diazepam

infections - ampicillin

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5
Q

LOCAL effects of rectal suppositories

A

haemorrhoids
constipation
colitis

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6
Q

dosage forms used rectally

A 
suppositories
ointments
enemas
tablets
soft capsules
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7
Q

advanages of vaginal route

A

high blood supply

avoidance of liver metabolism

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8
Q

disadvantages of vaginal route

A

low moisture content - affects disintegration of some dosage forms

pH varies - 3.5-4.5, hormonal stages (pregnancy, menopause)

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9
Q

local effects of vaginal route

A

infections - candida (thrush), trichomonas infections

local HRT

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10
Q

systemic effect of vaginal route

A

HRT - oestrogens, prostaglandins

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11
Q

dosage forms via vaginal route

A 
suppositories/pessaries
gels
creams
foam
tablets
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12
Q

body temp and suppositories/pessaries

A

vehicles melt/soften at body temp

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13
Q

g of med in rectal/vaginal suppositories

A

rectal

  • 1g infant
  • 2g child
  • 4g adult

vaginal
- 3-5g

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14
Q

ideal suppository base

A
  • melts/dissolves/disperses at 37 degrese C
  • non-irritating
  • physically stable during manufacture/storage
  • chemically stable and inert (compatible with drugs)
  • convenient to handle
  • high viscosity when melted
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15
Q

types of suppository bases

A
  1. oleaginous (fatty bases)
    - cocoa butter (theobroma oil)
    - cocoa butter substitutes
  2. water soluble/dispersible (hydrophilic bases)
    - glycerinated gelatin
    - PEG mixtures
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16
Q

advantages of oleaginous/fatty bases

A
  • appropriate for water soluble drugs
  • innocuous/non reactive
  • melt at body temp
  • less irritant than hydrophilic bases
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17
Q

disadvantages of oleaginous bases

A
  • FAs can become rancid
  • melt in warm weather
  • liquefy when certain drugs are incorporated
  • polymorphism
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18
Q

cocoa-butter (Theobroma oil)

A
  • obtained from roasted seeds of Theobroma Cacao
  • saturated triglycerides and unsaturated oleic acid
  • yellowish-white solid
  • has 4 polymorphic forms
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19
Q

polymorphic forms of cocoa butter

A

alpha, beta’, beta, gamma

  • diff crystal structures, same chem structure
  • diff physical properties
  • melting points diff
  • all forms convert to beta in days/1 week
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20
Q

cocoa butter substitutes

A
  • mixture of synthetic/natural vegetable oils
  • triglycerides of natural saturated fatty acids
  • fatty alcohols C10-C18
  • eg Witepsol H15, Wecobee, Dehydag, Cotmar, Fattibase
21
Q

composition of ondansetron suppositories (Zofran)

A

ondansetron 16mg

Witepsol S58 (cocoa butter substitute)

22
Q

composition of Alvedon suppositories

A

paracetamol 60/125/250mg

Witepsol H12

23
Q

advantages of hydrophilic bases

A

appropriate for lipophilic drugs

24
Q

disadvantages of hydrophilic bases

A

hygroscopic (need to absorb rectal/vaginal fluids)

slow dissolution

mucosal irritation

25
glycerinated gelatin
- mixture of glycerin and gelatin - hygroscopic - ratio of water:glycerins:gelatin - > 10:70:20 - laxative purposes - vaginal preparations
26
PEG base with: 96% PEG 1000, 4% PEG 4000 COMPARED TO 75% PEG 1000, 25% PEG 4000
base 1: (96%, 4%) - low mp, refrigerate in summer - rapid drug release base 2 (75%, 25%) - higher mp - slower drug release
27
types of macrogols
300-600 -> clear liquid, miscible with water, soluble in alcohol > 1000 -> white waxy appearance, soluble in water
28
how to package PEG
in tightly closed containers they absorb water can be stored without rifrigeration
29
problems with PEG
incompatible with many drugs membrane irritation - deplete cavity of fluids
30
ortho-gynest pessary composition
estriol 0.5mg benzoic acid - preservative butylated hydroxytoluene BHT - antioxidant PEG 400 - base hydrophilic PEG 1000 - base hydrophilic sorbitan monostearate - surfactant, enhances sol of drug during release Witepsol S55 - base lipophilic, cocoa butter substitute -> hydrophilic and hydrophobic bases together to adjust the solubility of the drug
31
formulation considerations for suppository base properties
type melting/dissolution characteristics viscosity at 37 degC
32
formulation considerations for drug properties
- solubility of drug in base and rectal/vaginal fluids - solubility of drug in molten and cooled base - particle size - > dissolution rate - > physical stability - total amount of drug - displacement value
33
what bases for liphophilic and hydrophilic drugs
lipophilic drug -> hydrophilic base hydrophilic drug -> oleaginous base
34
displacement value DV definition
mass of drug that displaces 1g of base
35
When does displacement value DV apply?
when dug dispersed in the molten base
36
excipients
``` hardening agents surfactants non-hygroscopic agents permeation enhancers preservatives and antimicrobial agents ```
37
hardening agents
- prevent base leaking - when mp of fatty base is lowered by other ingredients eg. beeswax, cetyl esters wax
38
surfactants
- help to break up suppositiry and disperse drug - increases wetting of base in rectal fluids - lipophilic base and/or drug eg. Span, Tween
39
non-hygroscopic agents
- reduce water uptake - physical and chemical syability on storage eg. colloidal silicon dioxide
40
permeation enhancers
disrupt membrane calcium channels in rectal cavity increase diffusion of drug -> not in vaginal drug delivery
41
preservatives & antimicrobial agents
prevent microbial growth in water soluble bases
42
2 methoda of supposiroty manufacture
1. moulding | 2. compression
43
moulding method manufacture
- lubrication of mould - calibration of mould - melting of base and addition of medicaments in a heat tank - filling of moulds with molten mass - cooling - removal - > automated process
44
compression method manufacture
- base and medicaments mixed and heated together to a soft paste - paste forced though a cylinder to fill suppository die - appropriate for thermolabie (heat sen) drugs
45
manufacturing considerations with theobroma oil/cocoa butter
controlled melting to get right polymorph - temp - rate of cooling - agitation - don't heat above 35 C - heat enough to remove alpha, gamma, beta', BUT KEEP BETA - can add beta seed crystals from stock - store at 28-30 C
46
drug release from oleaginous/fatty base and hydrophilic base
oleaginous - melts and spreads - drug partitions from molten base hydrophilic base - absorbs water and dissolved fluids
47
properties that affact release/diffusion
drug properties - pKa - partition coefficient rectal/vaginal fluid properties - pH - volume - viscosity/composition membrane permeability contents pressure from membrane wall
48
QC of suppositories
- appearance - drug content and uniformity of content - fragility - melting and dissolution behaviour

PHA333 (27 decks)

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