title: [Pharmacokinetics of injected cefozopran hydrochloride in healthy volunteers].
abstract: OBJECTIVE
  To study the pharmacokinetics of injected cefozopran hydrochloride in healthy volunteers.
  
  
  METHODS
  24 healthy volunteers were enrolled to receive low (0.5 g), middle (1.0 g), high (2.0 g) doses of single injection and multiple doses (1.0 g) injection of cefozopran hydrochloride in an open randomized study. The plasma concentrations of cefozopran were determined by RP-HPLC. The DAS2.0 was used to fit the concentration-time data and to calculate the pharmacokinetic parameters.
  
  
  RESULTS
  The main pharmaeokinetic parameters for a single injection of low, middle and high doses of cefozopran were as follows: Cmax (48.27 +/- 9.84), (77.99 +/- 15.08) and (171.59 +/- 18.27) mg/L; Tmax (0.50 +/- 0.00), (0.51 +/- 0.02) and (0.51 + 0.02) h; AUCo-t (92.43 +/- 24.02), (152.45 +/- 16.26) and (341.03 +/- 44.16) mg x h/L; t1/2beta (1.97 +/- 0.19), (2.44 +/- 0.24) and (2.18 +/- 0.31) h, respectively. The main pharmacokinetic parameters for a multiple doses injection of cefozopran were as follows: Cmax (80.39 +/- 11.86) mg/L; Tmax (0.51 +/- 0.02) h; AUCo-t (159.74 +/- 15.06) mg x h/L; t1/2beta (2.55 +/- 0.55) h. The accumulative rate of cefozopran through urine pathway within 24 h was (89.4 +/- 15.5)%. The statistical analysis showed that Cmax, AUCo-t, and AUCo-infinity increased significantly with increased doses of injection (P < 0.05). Those parameters were linearly correlated with the doses of injection (r = 0.9950, 0.9960, 0.9963). However, dosage did not have an impact on other pharmacokinetic parameters (P > 0.05). No gender differences in the parameters were found (P > 0.05).
  
  
  CONCLUSIONS
  Cefozopran hydrochloride performs a linear kinetics in healthy volunteers. The main pharmacokinetic parameters have no significant gender differences, and there is no drug accumulated with multiple doses of injection.
authors.affiliation: Department of Clinical Pharmacology, West China Hospital, Sichuan University, Chengdu 610041, China.
authors.forename: Wang-Wei
authors.initials: WW
authors.lastname: Guo
authors.forename: Qi
authors.initials: Q
authors.lastname: Shen
authors.forename: Yong-Ping
authors.initials: YP
authors.lastname: Qin
authors.forename: Ying
authors.initials: Y
authors.lastname: Wang
authors.forename: Lei
authors.initials: L
authors.lastname: Wang
authors.forename: Jia
authors.initials: J
authors.lastname: Miao
authors.forename: Feng
authors.initials: F
authors.lastname: Nan
authors.forename: Jin
authors.initials: J
authors.lastname: Xiang
authors.forename: Qin
authors.initials: Q
authors.lastname: Yu
authors.forename: Mao-Zhi
authors.initials: MZ
authors.lastname: Liang
mesh_terms: D000328:Adult; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002511:Cephalosporins / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid / Q000379:methods; D005260:Female; D006801:Humans; D007262:Infusions, Intravenous; D008297:Male; D055815:Young Adult; D000097586:Cefozopran
chemical_list: D000900:Anti-Bacterial Agents; D002511:Cephalosporins; D000097586:Cefozopran