Buprenorphine transdermal administration

Kapil RP, Cipriano A, Michels GH, Perrino P, O Keefe SA, Shet MS, et al. Effect of ketoconazole on the pharmacokinetic profile of buprenor-phine following administration of a once-weekly buprenorphine transdermal system. Clin Drug Investig 2012 32(9) 583-92. 

A quantum leap in pain therapy with distinct advantages in the form of reduced side-effects and application frequency was achieved with transdermal opioid administration. Transdermal application requires a number of characteristics on the part of the active substance (Fig. 7), the most restrictive being the daily dose, and only very potent opioids which are effective in very low doses, such as fentanyl and buprenorphine, are an option (Sittl and Likar, 2001). 

Buprenorphine, the other option for transdermal application on account of its potency, is more difficult to apply dermally in therapeutic doses (Roy et al., 1994 Grond et al., 2000). A surrogate parameter for skin penetration, provided the other prerequisites are fulfilled (Fig. 7), is the melting point of the active substance. With buprenorphine base this is 209°C and about 260°C for buprenorphine hydrochloride, compared with, for example, 83°C for fentanyl base and 150°C for fentanyl dihydrogen citrate. The DDS developer LTS devised a technical solution for reliable transdermal buprenorphine administration in the form of a matrix patch (Fig. 9). 

Drug administration ronte Transdermal buprenorphine has been studied in children with cancer pain in three case studies. An adverse event occurred in only one case— erythema and pruritus at the patch site [192 ]. 

---