Formulation in Pharmacy Practice   2nd Edition

TACROLIMUS
 
 
Tacrolimus is highly lipophilic and is insoluble in water but soluble in alcohol.

Formula 2

Tacrolimus Suspension 0.5mg per mL
 
Tacrolimus 5mg capsules  
Ora-Plus 30  mL
Simple Syrup NF 30  mL
 
Expiry:  30 days.
 
Stability:
Chemically stable for 56 days at room temperature (24 - 26°C).
 
Storage:  In this study the solutions were stored in 2 oz, amber
glass or plastic prescription bottles.
 
Shake well before use
 

 
NOTES
  1. During preparation wear latex gloves to protect hands.  Premix the Ora-Plus and syrup thoroughly and then add to the mortar in portions.
  2. Ora Plus contains: microcrystalline cellulose, sodium carboxymethylcellulose, xanthan gum, citric acid, sodium phosphate, simethicone, methyl paraben and potassium sorbate; pH = 4.2.
    If Ora-Plus is not available use a base of syrup and methylcellulose, parabens 0.1% and buffer or adjust the pH (use citric acid) to pH 4 - 5.  An expiry date of 30 days suggested.
  3. McGhee et al3 showed that tacrolimus was adequately absorbed from this preparation although actual bioavailability was not determined.
  4. Tacrolimus adsorbs to PVC, but does not significantly adsorb to glass or plastic bottles made from polypropylene resin.1,2

REFERENCES
  1. Taormina D., Abdullah H.Y., Venkataramanan R. et al.  Stability and sorption of FK 506 in 5% dextrose injection and 0.9% sodium chloride injection in glass, polyvinyl chloride, and polyolefin containers.Am J Hosp Pharm 1992; 49: 119-123.
  2. Jacobson P.A., Johnson C.E., West N.J., Foster J.A.  Stability of tacrolimus in an extemporaneously compounded oral liquid.  Am J Health Syst Pharm 1997; 54: 178-180.
  3. McGhee B, McCombs J.R., Boyle G, Webber S.A., Reyes J.R.  Therapeutic use of an extemporaneously prepared oral suspension of tacrolimus in pediatric patients.  Transplantation 1997; 64: 941-42.

 
Formulation in Pharmacy Practice
2nd Edition