Suppositories Flashcards
What are suppositories?
Solid dosage forms intended for insertion into body orifices (i.e ear, nose, rectum, vagina, urethra)
What are bougies?
Urethral and Nasal bougies are thin and long dosage forms used to insert into urethra and nose respectively.
What are the uses of suppositories?
Carry drug for action at site of placement
Carry drug for systemic action
Disadvantages of suppositories for drug delivery
Strong feeling of aversion in Asians
suppositories can leak
slow onset (~30min) and incomplete drug absorption
considerable intersubject and intrasubject variation in drug absorption
development of proctitis
When will suppositories be recommended for drug delivery?
When patient unable to utilise oral route of drug administration
Also for drugs which are less suited for oral administration (due to high first pass)
What are desirable properties of a suppository base?
Can be moulded by pouring or compression stable if heated above its melting point does not adhere to mould releases drug at desired rate keep its shape when handled and easy to insert does not leak out of orifice into which it is inserted stable during storage non-toxic and non-irritating compatible with drug
What are the different types of bases (include some examples)
Oleaginous bases (fats and oils) water-soluble or water-miscible bases (glycerinated gelatin, PEG) Emulsifying bases (witepsol, massupol)
What are the 3 crystalline forms of theobroma oil? Include their melting points
alpha - unstable, MP of 22-24 deg C
beta - stable, MP of 34 - 36 deg C
gamma - unstable, MP of 18 deg C
How long does it take for unstable alpha form to revert to stable beta form if the theobroma oil was heated above 60 deg C
several days
How to ensure that we obtain beta crystalline forms of theobroma oil
Use low heat of 40-50 deg C and cool slowly.
Disadvantages of theobroma oil base
melting process must monitor carefully
theobroma oil tends to stick to sides of mould
theobroma oil tends to soften in tropical climate and when substances like volatile oils, phenol, or chloral hydrate are added
more difficult to administer as the oil melts on finger tip
theobroma oil tends to leak out of the orifice.
What alternative bases are able to overcome some of the disadvantages of theobroma oil?
Fattibase, suppocire
Will water soluble bases melt?
No, they dissolve slowly in biological fluid
Oppositely charged compounds are incompatible with each other: True or False
True
What does gelatin and glycerin impart on the suppository?
Gelatin: Hardness
Glycerin: Hydrophilicity
Advantages of glycerinated gelatin base?
More prolonged drug release (commonly used in pessaries)
more easily inserted (suitable for urethral administration)
Disadvantages of glycerinated gelatin bases?
Hygroscopic - can lead to dehydrating effect on mucous membrane
Supports the growth of mould