Academic Journal
Comparative Pharmacokinetics of Azithromycin in Serum and White Blood Cells of Healthy Subjects Receiving a Single-Dose Extended-Release Regimen versus a 3-Day Immediate-Release Regimen
| العنوان: | Comparative Pharmacokinetics of Azithromycin in Serum and White Blood Cells of Healthy Subjects Receiving a Single-Dose Extended-Release Regimen versus a 3-Day Immediate-Release Regimen |
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| المؤلفون: | Liu, Ping, Allaudeen, Hameed, Chandra, Richa, Phillips, Kem, Jungnik, Arvid, Breen, Jeanne D., Sharma, Amarnath |
| المصدر: | Antimicrobial Agents and Chemotherapy ; volume 51, issue 1, page 103-109 ; ISSN 0066-4804 1098-6596 |
| بيانات النشر: | American Society for Microbiology |
| سنة النشر: | 2007 |
| الوصف: | The pharmacokinetic profiles of azithromycin given as a single-dose regimen (2.0-g extended-release microspheres) were characterized in serum and white blood cells (WBC) and compared with those of a 3-day regimen (a 500-mg immediate-release tablet once daily; total dose, 1.5 g) in an open-label, randomized, parallel-group study of 24 healthy adult subjects. Serial blood samples were collected up to 5 days after the start of dosing for both regimens. Safety assessments were conducted throughout the study. A single 2.0-g dose of azithromycin microspheres achieved significantly higher exposures in serum and WBC during the first 24 h after the start of dosing than a 3-day regimen: an approximately threefold higher area under the curve from time zero to 24 h postdose (AUC 0-24 ) and an approximately twofold higher mean peak concentration on day 1. The single-dose regimen provided total azithromycin exposures in serum and WBC similar to those of the 3-day regimen, as evidenced by the similar AUC 0-120 and trough azithromycin concentrations in serum and WBC (mononuclear leukocytes [MNL] and polymorphonuclear leukocytes [PMNL]). For both regimens, the average total azithromycin exposures in MNL and PMNL were approximately 300- and 600-fold higher than those in serum. Azithromycin concentrations in MNL and PMNL remained above 10 μg/ml for at least 5 days after the start of dosing for both regimens. This “front-loading” of the dose on day 1 is safely achieved by the extended-release microsphere formulation, which maximizes the drug exposure at the time when the bacterial burden is likely to be highest. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| DOI: | 10.1128/aac.00852-06 |
| DOI: | 10.1128/AAC.00852-06 |
| الاتاحة: | http://dx.doi.org/10.1128/aac.00852-06 https://journals.asm.org/doi/pdf/10.1128/AAC.00852-06 |
| Rights: | https://journals.asm.org/non-commercial-tdm-license |
| رقم الانضمام: | edsbas.AE6047C3 |
| قاعدة البيانات: | BASE |
| DOI: | 10.1128/aac.00852-06 |
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