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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

Plasma fentanyl concentration over time with fentanyl buccal tablet (FBT) 400 μg and oral transmucosal fentanyl citrate (OTFC®) 800 μg. Darwish M, Kirby M, Robertson P Jr, et al, Journal of Clinical Pharmacology. (vol 47, issue 3) p. 343–350. Copyright © 2007 by SAGE Publications.Reprinted by permission of SAGE Publications.16OTFCC values have been dose-normalized to 400 μg.Inset is an expanded view of the first 4 hours after administration of FBT or OTFC.
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f3-pmc-2010-011: Plasma fentanyl concentration over time with fentanyl buccal tablet (FBT) 400 μg and oral transmucosal fentanyl citrate (OTFC®) 800 μg. Darwish M, Kirby M, Robertson P Jr, et al, Journal of Clinical Pharmacology. (vol 47, issue 3) p. 343–350. Copyright © 2007 by SAGE Publications.Reprinted by permission of SAGE Publications.16OTFCC values have been dose-normalized to 400 μg.Inset is an expanded view of the first 4 hours after administration of FBT or OTFC.

Mentions: These preliminary findings were supported by an additional randomized, open-label, crossover study of healthy adults that assessed the bioavailability of fentanyl delivered using FBT and OTFC (Table 3).16 The study showed that OraVescent technology more than doubled the portion of the fentanyl dose absorbed via the buccal mucosa (48% with FBT vs. 22% with OTFC). This resulted in greater absolute bioavailability of FBT than OTFC (65% vs. 47%) and more rapid absorption into the systemic circulation (tmax: 47 minutes for FBT vs. 91 minutes for OTFC). Because of the improvement in the extent and speed of absorption afforded by the OraVescent technology, the early systemic exposure (i.e. the area under the plasma drug concentration-vs.-time curve [AUC] from time 0 to tmax [AUC0-tmax]) to fentanyl exceeded that provided by OTFC (0.40 vs. 0.14 ng•h/mL) (Fig. 3, Table 3).16


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)

Plasma fentanyl concentration over time with fentanyl buccal tablet (FBT) 400 μg and oral transmucosal fentanyl citrate (OTFC®) 800 μg. Darwish M, Kirby M, Robertson P Jr, et al, Journal of Clinical Pharmacology. (vol 47, issue 3) p. 343–350. Copyright © 2007 by SAGE Publications.Reprinted by permission of SAGE Publications.16OTFCC values have been dose-normalized to 400 μg.Inset is an expanded view of the first 4 hours after administration of FBT or OTFC.
© Copyright Policy - open-access
Related In: Results  -  Collection

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

f3-pmc-2010-011: Plasma fentanyl concentration over time with fentanyl buccal tablet (FBT) 400 μg and oral transmucosal fentanyl citrate (OTFC®) 800 μg. Darwish M, Kirby M, Robertson P Jr, et al, Journal of Clinical Pharmacology. (vol 47, issue 3) p. 343–350. Copyright © 2007 by SAGE Publications.Reprinted by permission of SAGE Publications.16OTFCC values have been dose-normalized to 400 μg.Inset is an expanded view of the first 4 hours after administration of FBT or OTFC.
Mentions: These preliminary findings were supported by an additional randomized, open-label, crossover study of healthy adults that assessed the bioavailability of fentanyl delivered using FBT and OTFC (Table 3).16 The study showed that OraVescent technology more than doubled the portion of the fentanyl dose absorbed via the buccal mucosa (48% with FBT vs. 22% with OTFC). This resulted in greater absolute bioavailability of FBT than OTFC (65% vs. 47%) and more rapid absorption into the systemic circulation (tmax: 47 minutes for FBT vs. 91 minutes for OTFC). Because of the improvement in the extent and speed of absorption afforded by the OraVescent technology, the early systemic exposure (i.e. the area under the plasma drug concentration-vs.-time curve [AUC] from time 0 to tmax [AUC0-tmax]) to fentanyl exceeded that provided by OTFC (0.40 vs. 0.14 ng•h/mL) (Fig. 3, Table 3).16

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