title: Tolerability and pharmacokinetics of biapenem following single and multiple intravenous administrations in healthy Chinese subjects: an open-label, randomized, single-center study.
abstract: This study was designed to evaluate the tolerability and pharmacokinetics of biapenem after single and multiple intravenous administrations in healthy Chinese subjects. Subjects were randomly allocated to receive a single 0.15, 0.3, or 0.6 g dose of biapenem. Subjects assigned to the 0.3 g single dose group continued into the multiple-dose phase. Blood samples were collected over 6 h and plasma biapenem concentrations were determined by a validated HPLC method. Tolerability was assessed by monitoring vital signs, laboratory parameters, physical examinations, electrocardiogram, and adverse events collected by non-directive questioning/spontaneous reporting. Pharmacokinetic parameters for biapenem after intravenous administration of a single dose of 0.15, 0.3, or 0.6 g were as follows: Cmax=7.06 (1.30), 15.59 (1.33), and 29.12 (1.22) mg/L; AUC0-6 h=8.95 (1.33), 22.62 (1.25), and 42.05 (1.19) mg · h/L; t1/2=0.97 (0.13), 1.04 (0.08), and 1.12 (0.08) h; CL=15.78 (1.32), 12.91 (1.24), and 13.95 (1.19) L/h; Vd=21.87 (1.25), 19.31 (1.25), and 22.41 (1.23) L, respectively. Pharmacokinetic parameters for biapenem after intravenous administration of multiple 0.3 g doses were as follows: Cmax=18.50 (1.16) mg/L; AUC0-6 h=26.45 (1.15) mg · h/L; t1/2=1.06 (0.15) h; CL=11.06 (1.16) L/h; Vd=16.78 (1.19) L. The incidence of reported AEs was as follows: phlebitis (2/10), nausea (1/10), and diarrhea (1/10). All of the AEs were mild in intensity. The pharmacokinetic properties of biapenem were linear at dose of 0.15-0.6 g. All biapenem doses appeared to be well tolerated.
authors.affiliation: Clinical Research Organization for Pharmaceutical Products, Union -Hospital, Tongji Medical College, Huazhong University of Science and -Technology, Wuhan, People's Republic of China.
authors.forename: Y
authors.initials: Y
authors.lastname: Liu
authors.forename: Z
authors.initials: Z
authors.lastname: Li
authors.forename: C
authors.initials: C
authors.lastname: Yang
authors.forename: H
authors.initials: H
authors.lastname: Zheng
authors.forename: Y
authors.initials: Y
authors.lastname: Lv
authors.forename: H
authors.initials: H
authors.lastname: Chen
authors.forename: Y
authors.initials: Y
authors.lastname: Zhang
authors.forename: S
authors.initials: S
authors.lastname: Shi
mesh_terms: D000328:Adult; D005260:Female; D064368:Healthy Volunteers; D006801:Humans; D007275:Injections, Intravenous; D008297:Male; D012737:Sex Factors; D013845:Thienamycins / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D055815:Young Adult
chemical_list: D013845:Thienamycins; C065257:biapenem