Background and importance Ulcerative proctitis is associated with faecal incontinence, pain, itching, bleeding and purulent discharge, and is often managed with topical salicylates or steroids. However, treatment can be refractory in some patients. Rectal administration of tacrolimus may be effective in difficult to treat ulcerative proctitis1. Some patients find it difficult to retain rectal pharmaceutical forms, suppositories or enemas, which lead to painful administration and infradosification.
Aim and objectives To develop a tacrolimus adhesive gel and its galenic validation, to improve and extend contact time of tacrolimus with rectal mucosal surfaces.
Material and methods Tacrolimus 0.06% adhesive gel was compounded, in a biological safety cabinet with protection equipment for the manipulator, with tacrolimus 5 mg capsules (Prograf, Astellas Pharma), glycerin (Acofarma) and a lipophilic gel (Excipiente Acofar adhesivo oral, Acofarma). The compounded drug was packed on monodoses of 4.5 g with the aim of administering 2 mg of tacrolimus in 5 mL latex free luer lock syringes (Omnifix, B Braun). Each syringe was supplied with a rectal cannula (José Mestre, SA) for patient administration (1 g of gel is retained in the cannula). Tacrolimus gel was stored at room temperature, in a dry place and protected from light.
Galenic characterisation was carried out, according to good manufacturing practices,2 testing for homogeneity and appearance, extensibility, pH and monodose mass extraction, weekly over 28 days. Determination of pH was made with pHmeter glp21.
Results For 28 days at room temperature: tacrolimus gel kept the same appearance (granular, translucent and colourless), there were no quite different values for extensibility and pH (5.99) and monodose mass extraction (3.50 g) results differed minimally (<5–10% difference). Currently, one patient is treated in our hospital with this formulation once every 2 days, responding positively, with no adverse effects and good tolerance.
Conclusion and relevance This gel preparation is stable for 28 days at room temperature, maintaining its galenic characteristics and it can be useful in patients with difficult to treat ulcerative proctitis.
References and/or acknowledgements 1. Jaeger SU, et al. Tacrolimus suppositories in therapy-resistant ulcerative proctitis. Inflamm Intest Dis 2018;3:116–124. doi:10.1159/000493979
2. Ministerio De Sanidad, Servicios Sociales e Igualdad. Guía de buenas prácticas de preparación de medicamentos en servicios de farmacia hospitalaria. Junio 2014.
No conflict of interest.
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