[Translation] A randomized, open-label, non-controlled, single-dose escalation phase I study to evaluate the tolerability of ceftriaxone sodium for injection in healthy adult volunteers

以健康成年受试者为研究对象，对四川方向药业有限责任公司研制的注射用头孢他美钠（规格为0.5g/片、1.0g/片）进行单次给药和多次给药的耐受性研究，观察人体对注射用头孢他美钠的耐受程度和安全性，确定头孢他美钠静脉给药对健康人群的最大耐受剂量（MTD），为临床用药及新药注册提供依据。

[Translation]

Healthy adult subjects were used as research subjects to conduct single and multiple dosing tolerance studies on ceftriaxone sodium for injection (specifications: 0.5g/tablet and 1.0g/tablet) developed by Sichuan Xiangfang Pharmaceutical Co., Ltd., to observe the human body's tolerance and safety to ceftriaxone sodium for injection, and to determine the maximum tolerated dose (MTD) of ceftriaxone sodium for intravenous administration in healthy people, so as to provide a basis for clinical use and new drug registration.

Start Date-

Sponsor / Collaborator

Sichuan Direction Pharmaceutical Co. Ltd.

[+1]

CTR20131264 / CompletedPhase 1

注射用头孢他美钠单次给药临床药代动力学/药效学研究；

[Translation] Clinical pharmacokinetic/pharmacodynamic study of single-dose cefetamet sodium for injection;

通过健康志愿受试者分别单次恒速静脉滴注低、中、高剂量注射用头孢他美钠，考察其在中国健康人体内的药代动力学特征，并结合体外抗菌活性测定结果，进行注射用头孢他美钠PK/PD研究，为制定II期临床试验用药方案提供依据。

[Translation]

The pharmacokinetic characteristics of ceftriaxone sodium for injection in healthy Chinese subjects were investigated by single constant-rate intravenous infusion of low, medium and high doses of ceftriaxone sodium for injection in healthy volunteers. Combined with the results of in vitro antibacterial activity assay, a PK/PD study of ceftriaxone sodium for injection was conducted to provide a basis for formulating the medication regimen for Phase II clinical trials.

Start Date07 Mar 2012

Sponsor / Collaborator

Hainan Yishun Pharmaceutical Co. Ltd.

[+1]

CTR20131864 / Active, not recruitingPhase 1

单中心、随机、盲法、安慰剂平行对照注射用头孢他美钠在健康人体单次和多次给药的I期临床耐受性试验；

[Translation] A single-center, randomized, blinded, placebo-controlled phase I clinical tolerance trial of single and multiple doses of cefetamet sodium for injection in healthy humans;

观察健康人体单次和多次接受注射用头孢他美钠的安全性和耐受性，评估注射用头孢他美钠在健康人体单次和多次给药的安全剂量范围，确定健康人体单次和多次用药的最大耐受量，为制定I期药代动力学研究及II期临床试验给药方案提供依据。

[Translation]

To observe the safety and tolerability of single and multiple administrations of ceftriaxone sodium for injection in healthy humans, evaluate the safe dosage range of single and multiple administrations of ceftriaxone sodium for injection in healthy humans, determine the maximum tolerated dose of single and multiple administrations in healthy humans, and provide a basis for formulating the dosing regimen for Phase I pharmacokinetic studies and Phase II clinical trials.

Start Date31 Oct 2011

Sponsor / Collaborator

Hainan Yishun Pharmaceutical Co. Ltd.

[+1]

100 Clinical Results associated with Cefetamet Sodium

100 Translational Medicine associated with Cefetamet Sodium

100 Patents (Medical) associated with Cefetamet Sodium

Literatures (Medical) associated with Cefetamet Sodium

03 May 2016·Journal of ChemotherapyQ4 · MEDICINE

Using Monte Carlo simulation to determine optimal dosing regimen for cefetamet sodium for injection

Q4 · MEDICINE

Article

Author: Miao, Jia ; Xiao, Yonghong ; Wang, Ying ; Yu, Rujia ; Sun, Jiayu ; Li, Caizheng ; Qin, Yongping

The objective of the study was to use Monte Carlo simulation to determine the optimal treatment dosing regimen of the cefetamet sodium for injection by analysing the pharmacokinetics (PK) parameters in healthy Chinese volunteers, and antibacterial activity in vitro was also examined. A three-cross Latin square single-dose PK study was designed. Twelve healthy volunteers were randomized to receive 500, 1000, and 2000 mg of cefetamet sodium for IV infusion over 30 minutes in three periods sequentially; and the washout time in between periods was 3 days. The drug concentrations in plasma were analysed by high-performance liquid chromatography, and the PK parameters were calculated using DAS2.0 PK software. The peak concentrations (Cmax) at 0.5 hours were 37.78±7.29, 76.18±12.81, and 149.32±29.94 mg/l, the areas under concentration-time curve (AUC0-t) were 69.75±14.44, 139.06±22.62, and 278.54±53.12 mg h/l, and the elimination half-life (t1/2) were 1.69±0.19, 1.69±0.27, and 1.81±0.23 hours for 500, 1000, and 2000 mg of cefetamet sodium for injection, respectively. The disposition of cefetamet was appear to fit a two-compartment model with linear kinetics. Antibacterial activity in vitro showed that most Gram-negative bacteria, including non-extended-spectrum beta-lactamases (ESBL)-producing Enterobacter, Haemophilus influenzae, Moraxella catarrhalis, and Neisseria gonorrhoeae, were sensitive to cefetamet. The result of Monte Carlo simulation showed that the probability of target attainment for bactericidal response (%fT>MIC≧50%) for susceptible bacteria was reached at all three dosing regimens of 500 mg, q6h, 1000 and 2000 mg, q8h and q6h. Considering the efficacy, safety, and pharmacoeconomy comprehensively, we recommended the dosing regimen of 500 mg, q6h for further clinical treatment based on the principle of minimum daily dosage.

01 Dec 2015·European Journal of Drug Metabolism and PharmacokineticsQ4 · MEDICINE

Pharmacokinetics and pharmacodynamics of oral and intravenous cefetamet in dog

Q4 · MEDICINE

Article

Author: Wang, Chun-Mei ; Wang, Wei ; Zhu, Xiao-Mao ; Chen, Zhong-Hua ; Gou, Si ; Zhao, Yuan

The pharmacokinetic (PK) and pharmacodynamic (PD) properties of intravenously (IV) administered cefetamet-Na and per os (PO) administered cefetamet pivoxil were investigated in eighteen healthy dogs at three different dose levels. The three doses for IV cefetamet-Na were 95, 190 and 380 mg, while those for oral cefetamet pivoxil were 125, 250 and 500 mg (both equivalent to 90, 180 and 360 mg of cefetamet). An efficacy predictor, measured as the ratios of the time that the concentration of the free drug is over the MIC90 (T > MIC90) and the dosing interval (f% T > MIC90) of IV and PO administration were calculated. The PK parameters' maximum concentration (C max), half-life (t 1/2) and area under the curve (AUC0-t ) after three IV doses were 42.85 ± 11.79 μg/mL, 1.66 ± 0.36 h and 80.10 ± 28.92 mg h/L (95 mg); 93.50 ± 30.51 μg/mL, 1.47 ± 0.13 h and 1.47 ± 0.13 mg h/L (190 mg); 185.74 ± 113.83 μg/mL, 1.60 ± 0.38 h and 263.20 ± 73.27 mg h/L (380 mg). After PO administration, the C max, t 1/2 and AUC0-t at three doses were 9.25 ± 1.02 μg/mL, 1.79 ± 0.50 h and 31.90 ± 4.76 mg h/L (125 mg); 9.75 ± 1.77 μg/mL, 1.93 ± 0.65 h and 42.69 ± 8.93 mg h/L (250 mg); 15.55 ± 6.65 μg/mL, 2.02 ± 0.54 h, and 68.72 ± 24.11 mg h/L (500 mg). The IV f% T > MIC90 was greater than PO f% T > MIC90 when MIC90 was within the range of 0.25-256 mg/L.

01 Jul 2014·Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition

[Phase I clinical trial on the safety of injectable cefetamet sodium with a single dose in healthy volunteers].

Article

Author: Sun, Jia-Yu ; Li, Cai-Zheng ; Qin, Yong-Ping ; Wang, Ying ; Miao, Jia

OBJECTIVETo investigate the safety and maximum tolerable dosage of injectable cefetamet sodium Sixty healthy volunteers were enrolled in this study. with a single infusion in Chinese healthy volunteers.METHODSA double-blinded, randomized, placebo-controlled design was adopted. Eight dosages ranging from 100 mg to 5 000 mg were tested. The pharmacokinetics of the drug was analyzed using a Latin square three-cross self-controlled design, with 12 healthy volunteers receiving 500 mg, 1 000 mg and 2 000 mg of injectable cefetamet sodium in a randomized sequence. Blood and urine samples were collected and analyzed using high performance liquid chromatography with UV detection. The main pharmacokinetics parameters were calculated with DAS2.0 software.RESULTS59 healthy volunteers completed the tolerance tests. Clinical adverse reactions occurred in 22.73% of participants in the test group and 6.67% of participants in the placebo group; but the difference was not statistically significant. Common adverse events included infusion pain and dizziness. Rare adverse events such as palpitations, diarrhea and rash occurred in participants in the test group. All of the adverse reactions were mild. Abnormal laboratory test results occurred in 43.18% participants in the test group and 53.33% participants in the placebo group; again the difference was not statistically significant. Common abnormal laboratory test results included abnormal bowel flora, stool abnormalities, abnormal urine and elevated serum potassium. After a single infusion of 500 mg, 1 000 mg and 2 000 mg of injectable cefetamet sodium, peak concentration of the drug at 0.5 h reached (37.92 +/- 7.43), (74.90 +/- 10.67) and (148.54 +/- 31.63) mg/L, with areas under concentration-time curve of (72.08 +/- 14.98), (144.28 +/- 24.57) and (286.66 +/- 54.25) (mg x h)/L, respectively. Their elimination half-life was (2.03 +/- 0.38), (2.04 +/- 0.26), and (2.12 +/- 0.26) h, respectively. The disposition of cefetamet was presented as a two-compartment model with linear kinetics. The 24-hour urinary accumulation excretion was 76.6%-67.5%.CONCLUSIONThe maximum single tolerated dose of injectable cefetamet sodium is 5 000 mg. The pharmacokinetics is a two-compartment model with linear kinetics within a dose range 500-2 000 mg.

100 Deals associated with Cefetamet Sodium

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R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Phase 1	CN	Sichuan Direction Pharmaceutical Co. Ltd.	12 Jun 2015
Acute Bronchitis	Phase 1	CN	Hainan Yishun Pharmaceutical Co. Ltd.	31 Oct 2011
Acute Bronchitis	Phase 1	CN	Sichuan Antimicrobial Industry Research Institute	31 Oct 2011
Pharyngolaryngitis	Phase 1	CN	Sichuan Antimicrobial Industry Research Institute	31 Oct 2011
Pharyngolaryngitis	Phase 1	CN	Hainan Yishun Pharmaceutical Co. Ltd.	31 Oct 2011
Pneumonia	Phase 1	CN	Hainan Yishun Pharmaceutical Co. Ltd.	31 Oct 2011
Pneumonia	Phase 1	CN	Sichuan Antimicrobial Industry Research Institute	31 Oct 2011
Tonsillitis	Phase 1	CN	Sichuan Antimicrobial Industry Research Institute	31 Oct 2011
Tonsillitis	Phase 1	CN	Hainan Yishun Pharmaceutical Co. Ltd.	31 Oct 2011

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