Pharmacokinetics and Bioequivalence of Cefprozil for Suspension and Granule Formulation in Healthy Chinese Volunteers: T
- PDF / 1,267,954 Bytes
- 13 Pages / 595.276 x 790.866 pts Page_size
- 76 Downloads / 208 Views
ORIGINAL RESEARCH
Pharmacokinetics and Bioequivalence of Cefprozil for Suspension and Granule Formulation in Healthy Chinese Volunteers: Two Single-Dose Crossover Studies Ping-Ping Lin . Chen-Jing Wang . Yan-Ping Liu . Ting Li . Xiao-Meng Gao . Ya-Ping Ma . Ping Shi . Xin Li . Le-Xin Wang . Yu Cao Received: November 2, 2020 / Accepted: December 2, 2020 Ó Springer Healthcare Ltd., part of Springer Nature 2020
ABSTRACT Introduction: Cefprozil, an oral second-generation semi-synthetic cephalosporin, possesses a broad spectrum of antimicrobial activity. A granule formulation has been developed to improve medication adherence of the patients. This study was conducted to assess the bioequivalence of the granule formulation to a dry suspension in healthy Chinese volunteers and estimate the pharmacokinetic (PK) profiles of cefprozil. Methods: An open-label, randomized, singledose, two-period, two-group, crossover study was conducted in 60 healthy Chinese volunteers under fasted or fed conditions (30 volunteers for each condition) to assess the bioequivalence between two formulations of cefprozil. Blood samples were collected at specified time intervals, and the plasma concentrations of cis- and trans-cefprozil were determined Ping-Ping Lin and Chen-Jing Wang contributed equally to this work. P.-P. Lin C.-J. Wang Y.-P. Liu T. Li X.-M. Gao Y.-P. Ma P. Shi X. Li Y. Cao (&) Clinical Trial Center, The Affiliated Hospital of Qingdao University, Qingdao, China e-mail: [email protected] L.-X. Wang (&) School of Biomedical Sciences, Charles Sturt University, Wagga Wagga, NSW, Australia e-mail: [email protected]
by a validated liquid chromatography-tandem mass spectrometry (LC–MS/MS) method. PK and bioavailability parameters were estimated via non-compartmental methods. Adverse events (AEs) were also recorded. Results: Under fasted conditions, the mean Cmax was (3534.70 ± 634.67) ng/ml, Tmax was (0.98 ± 0.25) h, t1/2 was (1.37 ± 0.13) h and AUC0-t was (9302.86 ± 1618.39) ngh/ml, respectively, after a single dose of 125 mg cefprozil for suspension. Under fed conditions, the mean Cmax was (2438.80 ± 493.78) ng/ml, Tmax was (1.66 ± 0.76) h, t1/2 was (1.36 ± 0.24) h and AUC0-t was (9332.36 ± 1373.61) ngh/ml, respectively. The PK parameters of the granule formulation of cefprozil were similar to those of the suspension. The 90% CI values of the GMRs of Cmax, AUC0-t and AUC0-? under both fasted and fed conditions were within the prespecified bioequivalence range (80.00–125.00%). Conclusions: According to the criteria for bioequivalence, the test granule formulations of cefprozil and ‘‘Cefprozil for SuspensionÒ’’ were determined to be bioequivalent whether under fasted or fed conditions by measurement of cis-, trans- and total cefprozil. Trial registration: ClinicalTrials.gov identifier, NCT04414254. Keywords: Bioequivalence; Cefprozil; Chinese; Healthy subjects; Infectious disease; Pharmacokinetics
Adv Ther
Key Summary Points Many children and the elderly find swallowing the existing dosage form of cefprozil, includ
Data Loading...
