Pharmacokinetics of azithromycin in plasma and sinus mucosal tissue following administration of extended-release or immediate-release formulations in adult patients with chronic rhinosinusitis

Annie F. Fang, James N. Palmer, Alexander G Chiu, Jeffrey L. Blumer, Penelope H. Crownover, Michael D. Campbell, Bharat D. Damle

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

This study compared the pharmacokinetics of azithromycin (AZI) following administration of extended-release (ER) and immediate-release (IR) formulations in plasma and sinus mucosa in patients with chronic rhinosinusitis. Patients (n = 71) were randomised 1:1 to receive a single dose of AZI-ER 2 g or up to three doses of AZI-IR 500 mg daily. Paired plasma and sinus tissue samples were taken during endoscopic sinus surgery at 2-168 h (four patients per time point) after the first dose. Samples were measured by a validated liquid chromatography/mass spectrometry assay. Pharmacokinetics were determined using composite concentration-time profiles. Comparison between formulations showed that within the first 24 h, the AZI area under the plasma concentration-time curve (AUC24) for ER was 5.2- and 7.0-fold higher than IR in plasma and sinus tissue, respectively. Comparison between matrices showed that the AUC24 and AUC168 in sinus tissue were 28.2- and 62.2-fold higher than in plasma for the ER formulation, whilst the AUC24 in sinus tissue was 21.1-fold higher than in plasma for IR formulation. These results indicated that AZI has good penetration into sinus tissue regardless of formulation; however, dosing of AZI-ER (2 g) increased AZI exposure within the first 24 h compared with the Day 1 dose of 500 mg IR regimen.

Original languageEnglish (US)
Pages (from-to)67-71
Number of pages5
JournalInternational Journal of Antimicrobial Agents
Volume34
Issue number1
DOIs
StatePublished - Jul 2009
Externally publishedYes

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Azithromycin
Mucous Membrane
Pharmacokinetics
Liquid Chromatography
Mass Spectrometry

Keywords

  • Azithromycin extended-release
  • Chronic rhinosinusitis
  • Pharmacokinetics
  • Sinus mucosa

ASJC Scopus subject areas

  • Microbiology (medical)
  • Infectious Diseases
  • Pharmacology (medical)

Cite this

Pharmacokinetics of azithromycin in plasma and sinus mucosal tissue following administration of extended-release or immediate-release formulations in adult patients with chronic rhinosinusitis. / Fang, Annie F.; Palmer, James N.; Chiu, Alexander G; Blumer, Jeffrey L.; Crownover, Penelope H.; Campbell, Michael D.; Damle, Bharat D.

In: International Journal of Antimicrobial Agents, Vol. 34, No. 1, 07.2009, p. 67-71.

Research output: Contribution to journalArticle

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