Construction of universal quantitative models for the determination of cefoperazone sodium/sulbactam sodium for injection from different manufacturers using near-infrared reflectance spectroscopy

To develop near-infrared （NIR） reflectance spectroscopic methods for the quantitative analysis of cefoperazone sodium/ sulbactam sodium from different manufacturers for injection powder medicaments. Various powders of cefoperazone sodium/ sulbactam sodium were directly analyzed by non-destructive NIR reflectance spectroscopy using the spectrometer EQUINOX55. Two quantitative methods via integrating sphere （IS） and fiberoptic probe （FOP） models were explored from 6 batches of commercial samples and 42 batches of laboratory samples at a content ranging from 30% to 70% for cefoperazone and 60% to 20% for sulbactam. The root mean square errors of cross validation （RMSECV） and the root mean square errors of prediction （RMSEP） of IS were 1.79% and 2.85%, respectively, for cefoperazone sodium, and were 1.86% and 3.08%, respectively, for sulbactam sodium; and those of FOP were 2.93% and 2.92%, respectively, for cefoperazone sodium, and were 2.23% and 3.01%, respectively, for sulbactam sodium. Based on the ICH guidelines and Ref. 12, the quantitative models were then evaluated in terms of specificity, linearity, accuracy, precision, robustness and model transferability. The non-destructive quantitative NIR methods used in this study are applicable for rapid analysis of injectable powdered drugs from different manufacturers.

头孢哌酮(Cefoperazone)致肾功能衰竭一例

患者秦××,女性,80岁,因持续上腹部疼痛三天,寒颤、高热一天,于1986年1月28日入院。查:T:39℃,P:120次/分,R:27次/分,BP:120/60mmHg。一般情况尚可。皮肤、巩膜无黄染。浅表淋巴结未及肿大。双肺呼吸音粗,左肺底少许湿罗音。心界不大,心率120次/分,律齐,未闻杂音。腹软,全腹轻压痛,以右上腹为著,肝脾未触及,莫菲氏征阳性,血白细胞12200/mm^3,中性82%,尿常规阴性。血谷丙转氨酶500单位,γ—谷氨酰转肽酶1700单位,

Cefoperazone sodium/sulbactam sodium vs piperacillin sodium/tazobactam sodium for treatment of respiratory tract infection in elderly patients

BACKGROUND Respiratory tract infections in the elderly are difficult to cure and can easily recur,thereby posing a great threat to patient prognosis and quality of life.AIM To investigate the therapeutic effects of different antibiotics in elderly patients with respiratory tract infection.METHODS Seventy-four elderly patients with respiratory tract infection were randomly allocated to a study(n=37;treated with cefoperazone sodium/sulbactam sodium)or control(n=37;treated with piperacillin sodium/tazobactam sodium on the basis of routine symptomatic support)group.Both groups were treated for 7 d.Time to symptom relief(leukocyte recovery;body temperature recovery;cough and sputum disappearance;and rale disappearance time),treatment effect,and laboratory indexes[procalcitonin(PCT),C-reactive protein(CRP),white blood cell count(WBC),and neutrophil percentage(NE)]before and 7 d after treatment and the incidence of adverse reactions were assessed.RESULTS In the study group,the time to WBC normalization(6.79±2.09 d),time to body temperature normalization(4.15±1.08 d),time to disappearance of cough and sputum(6.19±1.56 d),and time to disappearance of rales(6.68±1.43 d)were shorter than those of the control group(8.89±2.32 d,5.81±1.33 d,8.77±2.11 d,and 8.69±2.12 d,respectively;P=0.000).Total effective rate was higher in the study group(94.59%vs 75.68%,P=0.022).Serum PCT(12.89±3.96μg/L),CRP(19.62±6.44 mg/L),WBC(20.61±6.38×10^(9)/L),and NE(86.14±7.21%)levels of the study group before treatment were similar to those of the control group(14.05±4.11μg/L,18.79±5.96 mg/L,21.21±5.59×10^(9)/L,and 84.39±6.95%,respectively)with no significant differences(P=0.220,0.567,0.668,and 0.291,respectively).After 7 d of treatment,serum PCT,CRP,WBC,and NE levels in the two groups were lower than those before treatment.Serum PCT(2.01±0.56μg/L),CRP(3.11±1.02 mg/L),WBC(5.10±1.83×10^(9)/L),and NE(56.35±7.17%)levels were lower in the study group than in the control group(3.29±0.64μg/L,5.67±1.23 mg/L,8.13±3.01×10^(9)/L,and 64.22±8.08%,respectively;P=0.000).There was no significant difference in the incidence of adverse reactions between the groups(7.50%vs 12.50%,P=0.708).CONCLUSION Piperacillin sodium/tazobactam sodium is superior to cefoperazone sodium/sulbactam sodium in the treatment of elderly patients with respiratory tract infection with a similar safety profile.

Efficacy and Safety of Intravenous Moxifloxacin Versus Cefoperazone with Azithromycin in the Treatment of Community Acquired Pneumonia

Summary： To compare the efficacy, safety, and tolerability of intravenous moxifloxacin with those of a commonly used empirical antibiotic regimen, cefoperazone and azithromycin in the treatment of community acquired pneumonia （CAP） in adult patients requiring initial parenteral therapy, 40 patients with CAP were divided into two groups, a moxifloxacin group （n=20） and a control group （n=20）, which were treated for 7 to 14 days. The patients in the moxifloxacin group were intravenously given 400 mg of moxifloxacin （AveloxR） once a day. Patients in the control group were administered 2.0 g of cefoperazone twice a day and azithromycin 0.5 g once a day. Clinical, bacteriological, and laboratory examinations were performed before the treatment, and at the end of the treatment. Our results showed that there was no significant difference in the clinical efficacy rate between two treatment groups at end of therapy （90 % for moxifloxacin, 95 % for cefoperazone plus azithromycin） （P〉0.05）. The bacteriologic eradication rate at the end of treatment was 90 % in the moxifloxacin group and 80 % in the cefoperazone-plus-azithromycin group, whereas there was no significant difference between the two groups （P〉0.05）. In addition, both drugs were well-tolerated in this trial, with the number of drug-related adverse events being comparable. It is concluded that moxifloxacin is an effective and well-tolerated treatment for CAP and was equivalent to the com- monly used empirical treatment of cefoperazone plus azithromycin. Moxifloxacin is likely to offer clinicians an alternative for reliable empirical CAP treatment in the face of increasing antibiotic resistance.

第三代半合成头孢菌素:Cefoperazone、Cefotaxime和Moxalactam

近年来半合成头孢菌素获得迅速的发展,并根据抗菌谱的范围已进入第四世代的研究。抗菌谱与头孢噻嗯相似的称为第一代;第二代抗菌谱除包括第一代范围外扩大至对第一代无效的肠杆菌属、吲哚阳性变形菌属、嗜血流感杆菌和某些拟杆菌属等;第三代活力更高,抗菌谱更广,并包括绿脓杆菌。目前正在发展药物动力学性能更优的第四代。本文就第三代中几个较成熟的半合成头孢菌素概述于下。头孢氧哌唑(Cefoperazone,T-1551)

Sclerotherapy with Leuprolide and Cefoperazone Sulbactam in the Management of Ovarian Endometriomas under Ultrasound Guidance: A Novel Approach

Endometriosis is an estrogen dependent gynecological disorder, which can occur throughout the reproductive age of women, causing chronic pelvic pain, substantial morbidity, and impaired fertility. It is clinically defined as the presence of ectopic endometrium resulting in sustained inflammatory reaction. In India, about 29,000,000 women suffer from endometriosis. Severe pelvic pain and recurrent endometriomas were observed even after surgery. We have conducted aspirations totally in 110 patients in which most of the patients were suffering from Stage III & Stage IV of endometriosis except for 7 patients for whom we have done as primary therapy for endometriomas. Among 110 patients, 4 patients didn’t turn up for follow up after first aspiration. This pilot study conducted with 110 patients in Ponni Hospital and Fertility Research Centre, Madurai aimed to evaluate pregnancy outcome in 51 infertile patients, and to alleviate pelvic pain, to restore a healthy sexual life and to reduce the recurrence rate of Ovarian Endometriomas (OE) in 59 patients, who did not seek fertility, After using the newer sclerosing agent Leuprolide with Cefoperazone Sulbactam (LCS) under ultrasound guidance. This prospective pilot study resulted in a highly significant achievement in pregnancy where 41 patients conceived out of 51 patients (80.39%) only 6 are in ongoing treatment. Those who didn’t seek fertility were 59 of which 43 have completed family 13 have one child and 3 unmarried girls. 96.61% were relieved of pain and recurrence and restored healthy sexual life, 2 are in ongoing treatment. We have not encountered any adverse effects during this treatment.

Green and efficient degradation of cefoperazone sodium by Bi_(4)O_(5)Br_(2) leading to the production of non-toxic products:Performance and degradation pathway

Photocatalytic process represents a promising approach to overcome the pollution challenge associated with the antibiotics-containing wastewater.This study provides a green,efficient and novel approach to remove cephalosporins,particularly cefoperazone sodium(CFP).Bi_(4)O_(5)Br_(2) was chosen for the first time to systematically study its degradation for CFP,including the analysis of material structure,degradation performance,the structure and toxicity of the transformation products,etc.The degradation rate results indicated that Bi_(4)O_(5)Br_(2) had an excellent catalytic activity leading to 78%CFP removal compared with the pure BiOBr(38%)within 120 min of visible light irradiation.In addition,the Bi_(4)O_(5)Br_(2) presents high stability and good organic carbon removal efficiency.The effects of the solution p H(3.12-8.75)on catalytic activity revealed that CFP was mainly photocatalyzed under acidic conditions and hydrolyzed under alkaline conditions.Combined with active species and degradation product identification,the photocatalytic degradation pathways of CFP by Bi_(4)O_(5)Br_(2) was proposed,including hydrolysis,oxidation,reduction and decarboxylation.Most importantly,the identified products were all hydrolysis rather than oxidation byproducts transformed from the intermediate ofβ-lactam bond cleavage in CFP molecule,quite different from the mostly previous studies.Furthermore,the final products were demonstrated to be less toxic through the toxicity analysis.Overall,this study illustrates the detailed mechanism of CFP degradation by Bi_(4)O_(5)Br_(2) and confirms Bi_(4)O_(5)Br_(2) to be a promising material for the photodegradation of CFP.

Impact of antibacterial drugs on human serum paraoxonase-1(hPON1)activity:an in vitro study

Objective:To investigate the in vitro effects of the antihacterial drugs,mcropenem trihydrate.piperacillin sodium,and cefoperazone sodium,on the activity of human serum paraoxonase mPOND.Methods:hPQN1 was purified from human serum using simple chromatographic methods.including DEAE-Sephadex anion exchange and Sephadex G-200 gel filtration chromatography.Results:The three antihacterial drugs decreased in vitro hPON1 activity.Inhibition mechanisms meropcnem trihydrate was noncompetitive while piperacillin sodium and cefoperazone sodium were competitive.Conclusions:Our results showed that antihacterial drugs significantly inhibit hPON1 activity,both in vitro,with rank order meropenem trihydrate piperacillin sodium cefoperazone sodium in vitro.

Pharmaceutical care of a patient with antibiotic-associated encephalopathy

Objective:To provide reference of pharmaceutical care for the clinical treatment of a severe patient with antibiotic-associated encephalopathy.Methods:Clinical pharmacists participated in the clinical treatment of the patient with antibiotic-associated encephalopathy,provided pharmaceutical care for clinicians,including the evaluation of adverse drug events and the prevention of adverse drug interaction and development of anti-infection programs by using Pharmacokinetics/pharmacodynamics theory and therapeutic drug monitoring technique.Results:Through active clinical treatment and pharmaceutical care,the symptoms of patients with encephalopathy were relieved,and the infection was effectively controlled.Conclusion:Clinical pharmacists play a positive role in the treatment for the case with antibiotic associated encephalopathy.

Effect of antimicrobial agents on the toll-like receptors and inflammatory cytokines in liver tissue of the alcohol-induced liver disease in rats with Vibrio vulnificus sepsis

Background Septicemia and inflammation-mediated septic shock caused by Vibrio vulnificus （VV） is strongly associated with chronic liver disease. This study examined the effects of antimicrobial therapy on expression of hepatic toll-like receptors and inflammatory cytokines in rats with alcohol-induced liver disease complicated by VV sepsis. Methods Male Sprague-Dawley rats were assigned to the following treatment groups： normal control （N）, alcoholic liver disease control （A）, antimicrobial-treated alcoholic liver disease control （AA）, alcoholic liver disease with VV sepsis （AV）, and antimicrobial-treated alcoholic liver disease with VV sepsis （AVA）. Alcohol-induced liver disease was observed in all groups except N. Expression of mRNAs encoding hepatic toll-like receptors 2 and 4, myeloid differentiation protein-2, tumor necrosis factor-α （TNF-α）, interleukin （IL）-1β, IL-6 and IL-10 was determined by RT-PCR. Results mRNAs encoding toll-like receptors 2 and 4 and myeloid differentiation protein-2 were significantly up-regulated in group AV as compared to control groups at 2-24 hours of sepsis; peak expression occurred at 12 hours. These mRNAs were also up-regulated in group AVA but to lesser degrees than in group AV at comparable time post-infection, mRNAs encoding TNF-α, IL-1β and IL-6 were significantly elevated in group AV as a function of infection. In group AVA as compared to AV, expression of TNF-α and IL-1β mRNAs was lower at 12-24 hours post-infection and expression of IL-6 mRNA was lower at 24 hours post-infection. Compared with control groups, IL-10 mRNA expression in group AV was markedly higher at 12-24 hours of sepsis. Expression of IL-10 mRNA was lower in group AVA as compared to AV at 24 hours of sepsis. Conclusions Antimicrobial therapy reduces expression of toll-like receptors and cytokines in rats with alcohol-induced liver disease complicated by VV sepsis. Monitoring hepatic toll-like receptor and cytokine expression during antibiotic therapy may be valuable for determining the course of VV sepsis in subjects with liver disease.