Rectal preparations

9 important questions on Rectal preparations

What are the reasons for rectal administration?

1 Swallowing problems
2 Nausea, vomiting
3 Impaired consciousness
4 Severe gastrointestinal complains after oral administration (indomethacin)
5 Unpleasant taste (especially children)
6 Patient is non-cooperative (small child, mentally disabled)
7 Local therapy (hermorrhoids, colitis)


1 Slikproblemen
2 Misselijkheid, braken
3 Verminderd bewustzijn
4 Ernstige maag-darmklachten na orale toediening (indomethacine)
5 Onaangename smaak (vooral kinderen)
6 Patiënt wil niet meewerken (klein kind, verstandelijk gehandicapt)
7 Lokale therapie (hermorroïden/bawasir, colitis/kolon)

What are the 3 reasons to use rectal=

Rectal preparations in pharmacopea rectal dosage forms

Intended for rectal use in order to obtain a systemic or local effect, or intended for diagnostic purposes

What are the kinds of rectal preparations?

Suppositories ( We will focus on this/ zetpil)
Rectal capsules
Rectal solutions, emulsions and suspensions
(Enema, micro-enema)
Powders and tablets for rectal solutions and suspensions
Semi-solid rectal preparations (ointments, creams, gels)
Rectal foams
Rectal tampons
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What are the routes for rectal drugs

Systemic
Local


dikke darm infectie after de dunne darm very near the anus = rectal

What are the drugs that are given by rectal route for local action?

Local action
Haemorrhoids
- Zinc oxide, hydrocortisone acetate, lidocaine

Chronic inflammatory bowel disease
- Mesalazine, beclomethasone

Laxative
- Bisacodyl, docusate sodium

Biopharmaceutics rectal systemic effect

Systemic effect § Small surface for absorption § Often higher and less frequent dosing than oral § Residence time should be sufficiently long
The person goes to the toilet and the drug will be expand from the body

§ No irritation §

Enema: faster action than suppository
Liver first-pass effect partly avoided  

ENEMA ACT FASTER THAN SUPPOSITORY BECASUE suppository is fat and enema is vloeibaar?

Lipothilic suppository bases

Melting range no melting point

What does Iodine value mean?

A lot of double bounds,
The number of the double bound and thus the ... Of oxydation

How is API released from the suppository? 28

Small particles in fat, fat melt, fat spread over certain area in rectal, sedimentation, wetted, dissolve in the rectal vloeid .. Opgenomen

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