Contact hypersensitivity stomatitis in response to Suboxone use: A case report

Grisham, Gabriel; Gutierrez, Lino A.; Nelson, Matthew T.; Mikals, Kyle; Powell, Angela

doi:10.1016/j.omsc.2019.100122

Cited by 2 publications

(1 citation statement)

References 7 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Due to low oral bioavailability, BUP is marketed primarily as mucosal (sublingual/buccal), transdermal (patch), or injectable (e.g., intravenous/intramuscular/implant) formulations. Compared to injectables, non-injectable formulations offer better convenience for clinical use, however mucosal formulations have been documented to cause dental health concerns, potentially due to pH change in the oral cavity ( Suzuki et al, 2013 ; Grisham et al, 2019 ) and transdermal patches cause skin irritation in 25–45% of patients ( Prommer 2015 ; Serpell et al, 2016 ). Sublingual BUP is also commonly used as a substitute for stronger opioids such as heroin, followed by a tapering strategy to allow withdrawal.…”

Section: Introductionmentioning

confidence: 99%

Triglyceride-Mimetic Prodrugs of Buprenorphine Enhance Oral Bioavailability via Promotion of Lymphatic Transport

Quach

Han

et al. 2022

Front. Pharmacol.

View full text Add to dashboard Cite

Buprenorphine (BUP) is a potent opioid analgesic that is widely used for severe pain management and opioid replacement therapy. The oral bioavailability of BUP, however, is significantly limited by first-pass metabolism. Previous studies have shown that triglyceride (TG) mimetic prodrugs of the steroid hormone testosterone circumvent first-pass metabolism by directing drug transport through the intestinal lymphatics, bypassing the liver. The current study expanded this prodrug strategy to BUP. Here different self-immolative (SI) linkers were evaluated to conjugate BUP to the 2 position of the TG backbone via the phenol group on BUP. The SI linkers were designed to promote drug release in plasma. Lipolysis of the prodrug in the intestinal tract was examined via incubation with simulated intestinal fluid (SIF), and potential for parent drug liberation in the systemic circulation was evaluated via incubation in rat plasma. Lymphatic transport and bioavailability studies were subsequently conducted in mesenteric lymph duct or carotid artery-cannulated rats, respectively. TG prodrug derivatives were efficiently transported into the lymphatics (up to 45% of the dose in anaesthetised rats, vs. less than 0.1% for BUP). Incorporation of the SI linkers facilitated BUP release from the prodrugs in the plasma and in concert with high lymphatic transport led to a marked enhancement in oral bioavailability (up to 22-fold) compared to BUP alone. These data suggest the potential to develop an orally bioavailable BUP product which may have advantages with respect to patient preference when compared to current sublingual, transdermal patch or parenteral formulations.

show abstract