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Pharmacokinetics of azithromycin in plasma and sinus mucosal tissue following administration of extended-release or immediate-release formulations in adult patients with chronic rhinosinusitis.
Int J Antimicrob Agents. 2009 Jul; 34(1):67-71.IJ

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 2g 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 (AUC(24)) for ER was 5.2- and 7.0-fold higher than IR in plasma and sinus tissue, respectively. Comparison between matrices showed that the AUC(24) and AUC(168) in sinus tissue were 28.2- and 62.2-fold higher than in plasma for the ER formulation, whilst the AUC(24) 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.

Authors+Show Affiliations

Pfizer Inc, 685 3rd Avenue, M/S 13-48, New York, NY 10017, USA. Annie.F.Fang@pfizer.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

19307106

Citation

Fang, Annie F., et al. "Pharmacokinetics of Azithromycin in Plasma and Sinus Mucosal Tissue Following Administration of Extended-release or Immediate-release Formulations in Adult Patients With Chronic Rhinosinusitis." International Journal of Antimicrobial Agents, vol. 34, no. 1, 2009, pp. 67-71.
Fang AF, Palmer JN, Chiu AG, et al. Pharmacokinetics of azithromycin in plasma and sinus mucosal tissue following administration of extended-release or immediate-release formulations in adult patients with chronic rhinosinusitis. Int J Antimicrob Agents. 2009;34(1):67-71.
Fang, A. F., Palmer, J. N., Chiu, A. G., Blumer, J. L., Crownover, P. H., Campbell, M. D., & Damle, B. D. (2009). Pharmacokinetics of azithromycin in plasma and sinus mucosal tissue following administration of extended-release or immediate-release formulations in adult patients with chronic rhinosinusitis. International Journal of Antimicrobial Agents, 34(1), 67-71. https://doi.org/10.1016/j.ijantimicag.2009.01.014
Fang AF, et al. Pharmacokinetics of Azithromycin in Plasma and Sinus Mucosal Tissue Following Administration of Extended-release or Immediate-release Formulations in Adult Patients With Chronic Rhinosinusitis. Int J Antimicrob Agents. 2009;34(1):67-71. PubMed PMID: 19307106.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Pharmacokinetics of azithromycin in plasma and sinus mucosal tissue following administration of extended-release or immediate-release formulations in adult patients with chronic rhinosinusitis. AU - Fang,Annie F, AU - Palmer,James N, AU - Chiu,Alexander G, AU - Blumer,Jeffrey L, AU - Crownover,Penelope H, AU - Campbell,Michael D, AU - Damle,Bharat D, PY - 2008/12/15/received PY - 2009/01/30/revised PY - 2009/01/30/accepted PY - 2009/3/25/entrez PY - 2009/3/25/pubmed PY - 2009/7/11/medline SP - 67 EP - 71 JF - International journal of antimicrobial agents JO - Int J Antimicrob Agents VL - 34 IS - 1 N2 - 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 2g 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 (AUC(24)) for ER was 5.2- and 7.0-fold higher than IR in plasma and sinus tissue, respectively. Comparison between matrices showed that the AUC(24) and AUC(168) in sinus tissue were 28.2- and 62.2-fold higher than in plasma for the ER formulation, whilst the AUC(24) 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. SN - 1872-7913 UR - https://www.unboundmedicine.com/medline/citation/19307106/Pharmacokinetics_of_azithromycin_in_plasma_and_sinus_mucosal_tissue_following_administration_of_extended_release_or_immediate_release_formulations_in_adult_patients_with_chronic_rhinosinusitis_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0924-8579(09)00060-0 DB - PRIME DP - Unbound Medicine ER -