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Fentanyl buccal tablet for the treatment of breakthrough pain: pharmacokinetics of buccal mucosa delivery and clinical efficacy.

Darwish M, Hamed E, Messina J - Perspect Medicin Chem (2010)

Bottom Line: Fentanyl buccal tablet (FBT; FENTORA((R)), Cephalon, Inc.) employs OraVescent((R)) drug delivery technology, which enhances the rate and extent of fentanyl absorption.OraVescent technology enhances the oral dissolution and buccal absorption of fentanyl, which facilitates rapid uptake of fentanyl into the bloodstream, reducing gastrointestinal absorption and minimizing extensive first-pass metabolism.The pharmacokinetic properties of FBT allow for meaningful clinical efficacy, with an onset of action that closely matches the onset of BTP.

View Article: PubMed Central - PubMed

Affiliation: Cephalon, Inc., Frazer, PA 19355, USA.

ABSTRACT
The treatment of breakthrough pain (BTP), a transitory exacerbation of pain that occurs on a background of otherwise-controlled, persistent pain, requires an opioid formulation and/or method of administration that can provide rapid and extensive systemic exposure. Fentanyl buccal tablet (FBT; FENTORA((R)), Cephalon, Inc.) employs OraVescent((R)) drug delivery technology, which enhances the rate and extent of fentanyl absorption. OraVescent technology enhances the oral dissolution and buccal absorption of fentanyl, which facilitates rapid uptake of fentanyl into the bloodstream, reducing gastrointestinal absorption and minimizing extensive first-pass metabolism. The resulting pharmacokinetic profile of FBT is characterized by greater bioavailability and a higher early systemic exposure compared with the earlier oral transmucosal fentanyl citrate formulation. In clinical studies of opioid-tolerant patients with cancer-related and noncancer-related BTP, FBT has provided consistent and clinically relevant improvements in pain intensity and pain relief relative to placebo, with a safety and tolerability profile that is generally typical of that observed with other potent opioids. The pharmacokinetic properties of FBT allow for meaningful clinical efficacy, with an onset of action that closely matches the onset of BTP.

No MeSH data available.


Related in: MedlinePlus

Serum concentration of fentanyl with OraVescent® fentanyl buccal tablet (FBT), non-OraVescent® FBT, and oral transmucosal fentanyl citrate (OTFC®) over time. Adapted with permission from Pather et al.19Inset shows absorption during the first 30 minutes.
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Related In: Results  -  Collection


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f2-pmc-2010-011: Serum concentration of fentanyl with OraVescent® fentanyl buccal tablet (FBT), non-OraVescent® FBT, and oral transmucosal fentanyl citrate (OTFC®) over time. Adapted with permission from Pather et al.19Inset shows absorption during the first 30 minutes.

Mentions: A preliminary, open-label pharmacokinetic study that compared FBT with OTFC highlighted the potential of OraVescent technology.19 In this study, 12 healthy men were randomized to receive one of three treatments: OraVescent FBT, non-OraVescent FBT (a tablet containing fentanyl and lactose in place of the OraVescent components), or OTFC. Subjects who received OraVescent FBT had an increased peak serum fentanyl concentration (Cmax), a shorter time to reach Cmax (tmax), and a larger area under the serum fentanyl concentration-vs.-time curve compared with those who received OTFC or non-OraVescent FBT (Table 2). Fentanyl was absorbed more rapidly and induced greater systemic exposure when coupled with OraVescent technology than with either of the other fentanyl formulations (Fig. 2).19


Fentanyl buccal tablet for the treatment of breakthrough pain: pharmacokinetics of buccal mucosa delivery and clinical efficacy.

Darwish M, Hamed E, Messina J - Perspect Medicin Chem (2010)

Serum concentration of fentanyl with OraVescent® fentanyl buccal tablet (FBT), non-OraVescent® FBT, and oral transmucosal fentanyl citrate (OTFC®) over time. Adapted with permission from Pather et al.19Inset shows absorption during the first 30 minutes.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC2901636&req=5

f2-pmc-2010-011: Serum concentration of fentanyl with OraVescent® fentanyl buccal tablet (FBT), non-OraVescent® FBT, and oral transmucosal fentanyl citrate (OTFC®) over time. Adapted with permission from Pather et al.19Inset shows absorption during the first 30 minutes.
Mentions: A preliminary, open-label pharmacokinetic study that compared FBT with OTFC highlighted the potential of OraVescent technology.19 In this study, 12 healthy men were randomized to receive one of three treatments: OraVescent FBT, non-OraVescent FBT (a tablet containing fentanyl and lactose in place of the OraVescent components), or OTFC. Subjects who received OraVescent FBT had an increased peak serum fentanyl concentration (Cmax), a shorter time to reach Cmax (tmax), and a larger area under the serum fentanyl concentration-vs.-time curve compared with those who received OTFC or non-OraVescent FBT (Table 2). Fentanyl was absorbed more rapidly and induced greater systemic exposure when coupled with OraVescent technology than with either of the other fentanyl formulations (Fig. 2).19

Bottom Line: Fentanyl buccal tablet (FBT; FENTORA((R)), Cephalon, Inc.) employs OraVescent((R)) drug delivery technology, which enhances the rate and extent of fentanyl absorption.OraVescent technology enhances the oral dissolution and buccal absorption of fentanyl, which facilitates rapid uptake of fentanyl into the bloodstream, reducing gastrointestinal absorption and minimizing extensive first-pass metabolism.The pharmacokinetic properties of FBT allow for meaningful clinical efficacy, with an onset of action that closely matches the onset of BTP.

View Article: PubMed Central - PubMed

Affiliation: Cephalon, Inc., Frazer, PA 19355, USA.

ABSTRACT
The treatment of breakthrough pain (BTP), a transitory exacerbation of pain that occurs on a background of otherwise-controlled, persistent pain, requires an opioid formulation and/or method of administration that can provide rapid and extensive systemic exposure. Fentanyl buccal tablet (FBT; FENTORA((R)), Cephalon, Inc.) employs OraVescent((R)) drug delivery technology, which enhances the rate and extent of fentanyl absorption. OraVescent technology enhances the oral dissolution and buccal absorption of fentanyl, which facilitates rapid uptake of fentanyl into the bloodstream, reducing gastrointestinal absorption and minimizing extensive first-pass metabolism. The resulting pharmacokinetic profile of FBT is characterized by greater bioavailability and a higher early systemic exposure compared with the earlier oral transmucosal fentanyl citrate formulation. In clinical studies of opioid-tolerant patients with cancer-related and noncancer-related BTP, FBT has provided consistent and clinically relevant improvements in pain intensity and pain relief relative to placebo, with a safety and tolerability profile that is generally typical of that observed with other potent opioids. The pharmacokinetic properties of FBT allow for meaningful clinical efficacy, with an onset of action that closely matches the onset of BTP.

No MeSH data available.


Related in: MedlinePlus