Paediatric Analgesic Formulations I

Question 1

common paed dosage forms

Answer 1

suspensions (e.g. paracetamol - calpol)

spolutions (paed paracetamol elixir BP)

suppositries - melts at body temp

tablets/ capsules - older children

Question 2

orodispersible dosage forms

Answer 2

disolve rapidly in mouth

classified;
1) orodispersble tabs
2) oral lyophilisates
3) films
4) granules

Question 3

1) orodispersible tablets

Answer 3

• direct compression
• sublimation
• phase transition

direct compression
Superdisintegrants e.g. crosmellose Na, crospovidone

Question 4

1) orodispersible tablets; manifacture

Answer 4

sublimation; volite solid substances
phase transition - compression of mixture of high/ low melting point sugar alcohols

tablet heated to 95C causing xylitol > melt and diffuse leaving pores in tablet.

Question 5

2) Oral lyophilisates

Answer 5

Oral lyophilisates are produced using a lyophilisation (freeze-drying) process
Most widely-known technology is Zydis > by RP Scherer (now Catalent)

lyophilisation (freeze- drying) - keep products stable

Question 6

freeze drying - oral lyophilisates

Answer 6

• liquid or semi-solid drug forumlation&raquo_space; added to final blister pack
• 4 main stages

Question 7

4 stages of freeze drying:

Answer 7

1. frezing stage
   - carefully controlled; obtain desired ice crystals
   - packs exposed to temps from 10C-30C in large freeze dry units
   - liquid nitrogen used in process
2. vacuum application
   - bring pressure down below triple point
3. Sublimation stage
   - heat applied
   - ice is low process
   - 0.5% moisture typically left after this
   - vapour is removed
4. Secondary drying
   - residual moisture removed by raising temp from 50-60C

Question 8

Oral lyophilisates: clinical points

Answer 8

• not used for paeds currently
• many examples of commercially avail. products
  (Rizatriptan – MAXALT MELT (migraine)
  Desmopressin acetate – DesmoMelt / DDAVP Melt / Noqdirna (polyuria / polydipsia / nocturnal enuresis)

Question 9

3) Orodispersible films

Answer 9

• single/ multi layer sheets that dissolve
• limited therapeutic use
• “solvent casting methods”
• ## `ondansetron - setofilm

Question 10

Chronic & moderate to severe pain

Answer 10

Parenteral dosage forms
Intravenous route: paracetamol can be given i.v. and this route may also be used for administration of morphine or fentanyl (strong opioid analgesics)

Buccal route
Fentanyl lozenges can also be used for paediatric analgesia
“Integral oromucosal applicator” resembles a lollipop stick (Actiq)

Transdermal route
Fentanyl may also be delivered transdermally for paediatric analgesia
More details in Skin ISU

Intranasal route
deliver fentanyl for delivery of relief of moderate to serve pain to children

Question 11

Entonox

Answer 11

medicinal gases - short term analgesia/ reduced anxiety druing hospital procedures

• mixture of oxygen and nitrous oxide 50:50 mixture
• ” gas and air”
• administered using a mask or mouthpiece