Pharmacokinetics and safety of liposomal bupivacaine after local infiltration in healthy Chinese adults: a phase 1 study.
Analgesia
Anesthesia
Bridging
Pharmacology
Tolerability
Journal
BMC anesthesiology
ISSN: 1471-2253
Titre abrégé: BMC Anesthesiol
Pays: England
ID NLM: 100968535
Informations de publication
Date de publication:
27 07 2021
27 07 2021
Historique:
received:
08
01
2021
accepted:
17
06
2021
entrez:
28
7
2021
pubmed:
29
7
2021
medline:
6
1
2022
Statut:
epublish
Résumé
Liposomal bupivacaine (LB) is a long-acting formulation of bupivacaine. The safety and efficacy of LB has been demonstrated across surgical procedures. However, pharmacokinetic (PK) parameters and safety of LB in the Chinese population have not been assessed. In this single-arm, single center, phase 1, open-label study, PK and safety of local infiltration with LB 266 mg were assessed in healthy Chinese adults. Eligible participants were aged 18 to 55 years with biologic parents and grandparents of Chinese ethnicity, in generally good health (i.e., no clinically significant abnormalities), and with a body mass index (BMI) 19.0 to 24.0 kg/m Participants (N = 20) were predominantly men (80 %); mean age was 32 years; and mean BMI was 21.8 kg/m After single-dose administration of LB, PK measures were similar to a previously reported profile in US adults. The highest observed peak plasma concentration of bupivacaine was several-fold below the plasma concentration threshold accepted as being associated with neurotoxicity or cardiotoxicity (2000-4000 ng/mL). These data support that LB is well tolerated and safe in individuals of Chinese descent. NCT04158102 (ClinicalTrials.gov identifier), Date of registration: November 5, 2019.
Sections du résumé
BACKGROUND
Liposomal bupivacaine (LB) is a long-acting formulation of bupivacaine. The safety and efficacy of LB has been demonstrated across surgical procedures. However, pharmacokinetic (PK) parameters and safety of LB in the Chinese population have not been assessed.
METHODS
In this single-arm, single center, phase 1, open-label study, PK and safety of local infiltration with LB 266 mg were assessed in healthy Chinese adults. Eligible participants were aged 18 to 55 years with biologic parents and grandparents of Chinese ethnicity, in generally good health (i.e., no clinically significant abnormalities), and with a body mass index (BMI) 19.0 to 24.0 kg/m
RESULTS
Participants (N = 20) were predominantly men (80 %); mean age was 32 years; and mean BMI was 21.8 kg/m
CONCLUSIONS
After single-dose administration of LB, PK measures were similar to a previously reported profile in US adults. The highest observed peak plasma concentration of bupivacaine was several-fold below the plasma concentration threshold accepted as being associated with neurotoxicity or cardiotoxicity (2000-4000 ng/mL). These data support that LB is well tolerated and safe in individuals of Chinese descent.
TRIAL REGISTRATION
NCT04158102 (ClinicalTrials.gov identifier), Date of registration: November 5, 2019.
Identifiants
pubmed: 34315419
doi: 10.1186/s12871-021-01407-5
pii: 10.1186/s12871-021-01407-5
pmc: PMC8314475
doi:
Substances chimiques
Anesthetics, Local
0
Liposomes
0
Bupivacaine
Y8335394RO
Banques de données
ClinicalTrials.gov
['NCT04158102']
Types de publication
Clinical Trial, Phase I
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
197Informations de copyright
© 2021. The Author(s).
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