SUPPOSITORIES

1

• SUPPOSITORIES
• - Definition
• - merits
• - limitations
• - formulations
• - suppository bases
• - compounding
• - labeling
• - displacement value
• - evaluation

2

• - solid or stiffened semi-solid dosage form for
  insertion into body cavities other than mouth
• Types
• Rectal
• Vaginal (pessaries)
• Urethral bougies
• Ear (ear cones)
• Nose bougies

3

• Merits
• Local effects
• Systemic effects
• Mechanical effects
• Bye pass first pass metabolism
• Alternative route for unconscious, elderly
  patients etc
• Unpleasant drugs
• Avoids gastric irritation GI instability
• Prolonged drug release

4

• Limitations
• Aesthetic objection
• Leakage
• Unpredictable absorption
• Mucosal damage
• Formulation
• Drug
• Base
• Other additives surfactants, soothing agents,
  antioxidants, preservatives, anti-settling agents
  (blend of higher m.p waxes fatty acids )

5

• Methods of preparation
• Hand rolling method (trituration)
• Moulding method (fusion)
• Cold compresion method
• Labeling
• - For rectal use only
• - Store in a cool dry place or
• - To be refrigerated etc

6

• Ideal properties of a suppository base
• Easily melt and dissolve or disperse
• Release medicament readily
• Retain shape while handling
• Non-toxic non-irritant
• Stable compatible
• Moldable, non adhering

7

• Bases
• I. Oleaginous (fatty) bases
• a) Natural - cocoa butter or their
  substitutes
• b) Synthetic - witepsol, massuppol
• II. Hydrophilic (water soluble/miscible) bases
• a) Natural - glycero gelatin
• b) Synthetic - macrogols
• Cocoa butter
• m.p 30 36oc
• Readily liquefiable on warming and rapid setting
  on cooling
• Blandness

8

• Limitations
• Polymorphism unstable gamma/beta forms
• Adhere to mould due to contractility on
  solidification
• Softening point too low for hot climates (beeswax
  may be added)
• Batch to batch variation in composition
• Becomes rancid on storage
• Immiscible in body fluids and poor water
  absorption
• Tendency to leak, immiscibility makes it not
  suitable for vaginal and urethral route
• May melt at warmer climates

9

• Synthetic bases
• - readily available
• - do not become rancid
• - chemically more inert
• - do not exhibit polymorphism
• - good water absorption and emulsification
  properties
• - lubrication can be avoided
• - white, smooth odorless
• - may become brittle fracture if cooled
  rapidly

10

• Glycero-gelatin
• - may cause irritation due to dehydration of
  mucosa
• - hygroscopic, careful storage
• - incompatible with many drugs
• - chance for microbial growth
• - base preparation is time consuming
• - sticky, cant be used for hand rolling

11

• Macrogols
• - combination for adjusting m.p, hardness etc
• - may produce irritation due to hygroscopic
  nature
• - suitable for tropical climates
• - good solvent properties
• - less liable to leakage due to high viscosity
• - do not become rancid
• - physiologically inert
• - do not support microbial growth
• - give clean attractive suppositories
• - form complex with some drugs retard
  release

12

• Displacement value
• - the number of parts by weight of drug that
  displaces one part of base.
• Calculation of DV
• Wt. of 6 CB suppository, WCB
• Wt. of 6 medicated(40) suppository, WMS
• Wt. of drug in suppository, WD WMS x 40/100
• Wt. of CB in suppository, WB WMS WD
• Wt. of CB displaced by drug, WDCB WCB WB
• Displacement value, DV WD /WDCB

13

• Evaluation
• - appearance
• - wt. variation
• - content uniformity
• - melting temp.
• - drug release
• - stability studies