title: Pharmacokinetics of azithromycin in serum and sinus fluid after administration of extended-release and immediate-release formulations in patients with acute bacterial sinusitis.
abstract: As high drug levels at the infection site are desirable for optimal activity, this study explored whether one dose of azithromycin extended release (AZ-ER) achieved higher azithromycin exposure in sinus fluid than azithromycin immediate release (AZ-IR) in adults with acute bacterial sinusitis. Subjects received AZ-ER (2g single dose; n=5) or AZ-IR (500mg daily for 3 days; n=4) and blood and sinus aspirates were collected until 120 h after initial dosing. Within 24 h, exposure was four- and three-fold higher with AZ-ER than with AZ-IR in serum and sinus fluid, respectively. Sinus fluid exposure was five- and three-fold higher than serum for AZ-IR and AZ-ER, respectively. Azithromycin concentrations in sinus fluid were maintained up to 120 h.
authors.affiliation: Department of Clinical Science, Intervention and Technology, Division of Otorhinolaryngology, Karolinska Institutet, and Nacka Närsjukhus Proxima AB, Stockholm, Sweden. jadelinia@hbase.com
authors.forename: A
authors.initials: A
authors.lastname: Ehnhage
authors.forename: M
authors.initials: M
authors.lastname: Rautiainen
authors.forename: A F
authors.initials: AF
authors.lastname: Fang
authors.forename: S P
authors.initials: SP
authors.lastname: Sanchez
mesh_terms: D000208:Acute Disease; D000328:Adult; D000900:Anti-Bacterial Agents / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000627:therapeutic use; D019540:Area Under Curve; D017963:Azithromycin / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000627:therapeutic use; D001826:Body Fluids / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003692:Delayed-Action Preparations; D004305:Dose-Response Relationship, Drug; D005260:Female; D006801:Humans; D008297:Male; D013058:Mass Spectrometry; D008875:Middle Aged; D010256:Paranasal Sinuses / Q000378:metabolism; D012852:Sinusitis / Q000188:drug therapy / Q000378:metabolism*
chemical_list: D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D017963:Azithromycin