头孢地尼原料及制剂的聚合物杂质分析

目的 建立头孢地尼原料及制剂聚合物杂质的分析方法。方法 分别采用0.1mol/L磷酸盐溶液和氯仿-三乙胺为溶剂,制备头孢地尼降解溶液;采用高效凝胶色谱法(HPSEC, TSK G2000 SWxl)和柱切换-LC/MSn法对头孢地尼降解溶液的弱保留值杂质进行分离和结构鉴定,并评估高效凝胶色谱法分析聚合物杂质的专属性;采用Diamonsil, C18型色谱柱,以0.25%四甲基氢氧化铵溶液(pH5.5)-甲醇-乙腈为流动相进行梯度洗脱,建立头孢地尼聚合物的RP-HPLC分析方法,采用二维色谱法和柱切换-LC/MSn法对其专属性进行分析,并进行方法学验证。结果 在头孢地尼降解物中鉴定出头孢地尼二聚体及其异构体,以及若干小分子杂质;高效凝胶色谱法分离头孢地尼聚合物杂质时,小分子杂质与聚合物杂质共出峰,方法专属性与定量准确性差;RP-HPLC法分析头孢地尼聚合物杂质时,能够检出头孢地尼二聚体及其异构体,头孢地尼三聚体,专属性好。结论 高效凝胶色谱法不能对头孢地尼的聚合物杂质进行有效质控,建立的反相色谱法分析头孢地尼聚合物杂质的专属性良好,可将头孢地尼降解溶液可作为聚合物杂质系统适用性溶液。     

Cefdinir-induced red stool and purple discoloration of nutritional formula: A case report

This case report describes a 4-year-old girl with food aversion who received three separate courses of cefdinir mixed with PediaSure®, an iron-fortified nutritional formula. The patient's stool turned red with variable onset during all three courses of treatment. Moreover, the PediaSure® formula turned purple after mixed with cefdinir, an interaction that has not been previously reported. We recommend that medication counseling for pediatric patients taking cefdinir include a mention of these possible discolorations.     

头孢地尼与其他6种β-内酰胺类的体外抗菌活性研究

目的　比较头孢地尼与头孢克肟、头孢克洛、头孢呋辛、头孢拉定、头孢氨苄、阿莫西林对临床常见致病菌的体外抗菌活性。方法　采用琼脂平板稀释法测定最低抑菌浓度 (MIC)。结果　头孢地尼对金黄色葡萄球菌、表皮葡萄球菌的敏感率分别为 73 3%、90 % ,抗菌活性显著强于头孢克肟 ;对肺炎克雷伯氏菌的活性与头孢克肟相似 ,强于受试第一代、二代头孢菌素 ;对大肠埃希氏菌活性强于其他 6种抗生素 ;对变形菌活性与头孢克肟相似。阴沟肠杆菌、柠檬酸杆菌属对受试药物耐药性均较高 ,其中头孢地尼和头孢克肟的敏感率 40 %左右 ,较其他 5种抗生素为强。结论　头孢地尼对大部分革兰氏阳性及革兰氏阴性菌具有较强的抗菌活性。     

Electrochemistry and determination of cefdinir by voltammetric and computational approaches

The oxidation and reduction behavior of cefdinir (CEF) was studied by experimental methods and computational calculations at B3LYP/6-31+G (d)//AM1. Voltammetric studies were carried out based on two irreversible reduction peaks at approximately −0.5 and −1.2 V on a hanging mercury drop electrode (HMDE) and on one irreversible oxidation peak at approximately 1.0 V on a glassy carbon electrode (GCE) versus Ag/AgCl, KCl (3.0M) in Britton–Robinson (BR) buffer at pH 4.2 and 5.0, respectively. Differential pulse adsorptive stripping voltammetric methods have been developed and validated for determination of CEF in different samples. The linear range was established as 0.25–40.0 μM for HMDE and 0.40–10.0 μM for GCE. Limit of quantification was calculated to be 0.20 and 0.26 μM for HMDE and GCE, respectively. These methods were successfully applied to assay the drug in tablets and human serum with good recoveries between 92.7% and 107.3% having relative standard deviation less than 10%.     

头孢地尼对细菌感染小鼠的体内抗菌作用

目的:探讨头孢地尼对郑州市分离的致病菌感染小鼠的体内抗菌作用。方法:以最小致死量(MLD)0.5 ml腹腔注射金黄色葡萄球菌、肺炎链球菌、肺炎克雷伯菌和大肠埃希菌感染小鼠,建立小鼠全身感染模型,灌胃以不同剂量的头孢地尼0.5 ml,以头孢妥仑匹酯为阳性对照,并以半数有效量(ED50)为观察指标,研究头孢地尼的体内抗菌活性。结果:头孢地尼对金黄色葡萄球菌、肺炎链球菌、肺炎克雷伯菌和大肠埃希杆菌的ED50分别为0.12、0.08、1.25、2.18 mg/kg,头孢妥仑匹酯对上述菌株的ED50值分别为16.7、19.5、7.12、1.65 mg/kg。结论:头孢地尼体内抗球菌的活性远高于头孢妥仑匹酯,但其对大肠埃希杆菌的活性低于头孢妥仑匹酯,提示头孢地尼具有较优的抗球菌作用。     

Cefdinir vs. cephalexin for mild to moderate uncomplicated skin and skin structure infections in adolescents and adults

ABSTRACT

Objectives: To compare the efficacy and safety of cefdinir to that of cephalexin in adolescents and adults with mild to moderate uncomplicated skin and skin structure infections (USSSI).

Research design and methods: This was an investigator-blinded, multicenter study in which patients at least 13 years of age with USSSI were randomized to receive 10 days of cefdinir 300?mg twice daily (BID) or cephalexin 250?mg four times daily (QID). Patients were evaluated at baseline, by telephone on Days 3–5, and during office visits on Days 12–14 (end-of-therapy [EOT] visit) and Days 17–24 (test-of-cure [TOC] visit).

Main outcome measures: Clinical response was evaluated at the TOC visit. Patient reported outcomes, including a usefulness questionnaire, were also assessed.

Results: Three hundred and ninety-one patients were treated. The treatment groups were well matched with regard to demographic characteristics and types of infection. Abscess(es) (26%), wound infection (24%), and cellulitis (21%) were the most common infections. At the TOC visit, the clinical cure rate for both treatment groups was 89% (151/170 for cefdinir and 154/174 for cephalexin) in clinically evaluable patients (95% CI for difference in cure rates [–6.7 to 7.3]). In the intent-to-treat analysis, cure rates were 83% for cefdinir vs. 82% for cephalexin. Clinical cure rates for infections caused by methicillin-susceptible (MSSA) and methicillin-resistant (MRSA) Staphylococcus aureus were 93% (37/40) and 92% (35/38) for cefdinir vs. 91% (29/32) and 90% (37/41) for cephalexin (?p > 0.999 comparing treatment groups for MSSA; p > 0.999 for MRSA). The usefulness questionnaire demonstrated that cefdinir was more highly rated in the mean composite score (87.4 vs. 83.6, p = 0.04), with the difference primarily due to the respondents’ preference for the convenience of taking the study medication (mean score 93.5 vs. 74.1 for cephalexin, p < 0.001). The study had the following limitations: the requirement for culture at baseline likely skewed the enrollment of patients towards those with abscesses; the results of culture in patients with USSSIs are often non-specific; in some patients entering the study with a diagnosis of cellulitis, the cellulitis was associated with an abscess; and, incision and drainage (I&D), spontaneous drainage, and needle aspiration are likely to have contributed to clinical response for purulent infections, and in particular MRSA-associated infections. Both study drugs were well tolerated. The most common treatment-related adverse events were diarrhea (10% cefdinir, 4% cephalexin, p = 0.017), nausea (3% and 6%, respectively, p = 0.203), and vaginal mycosis (3% and 6% of females, respectively, p = 0.500).

Conclusions: This study demonstrated that empiric coverage of USSSIs with cephalosporin therapy remains an appropriate clinical strategy. MRSA infections responded well in both arms of the study, suggesting that the choice of a cephalosporin did not adversely affect patient outcome. However, cephalosporins do not have accepted, clinically relevant in vitro activity against MRSA. Hence, the clinical response rates seen in this study against MRSA infections must be interpreted with caution. Cefdinir was more highly rated than cephalexin in a composite usefulness assessment.Introduction     

Efficacy,tolerability, and parent reported outcomes for cefdinir vs. high-dose amoxicillin/clavulanate oral suspension for acute otitis media in young children*

ABSTRACT

Objectives: To compare efficacy, tolerability, and parental satisfaction of cefdinir and high-dose amoxicillin/clavulanate oral suspensions given to young children with non-refractory acute otitis media (AOM) based on clinical endpoints and outcomes measures.

Research design and methods: This was an investigator-blinded, multicenter study in which 318 children 6 months through 6 years of age with a clinical diagnosis of AOM were randomized to receive 10 days of either cefdinir (14?mg/kg divided BID) or high-dose amoxicillin/clavulanate (90/6.4?mg/kg divided BID).

Main outcome measures: Investigators evaluated clinical response at an end-of-therapy (EOT) office visit conducted on day 12–15. Outcomes of satisfaction, tolerability, and adherence were also assessed at that visit using an Otitis Parent Questionnaire.

Results: The treatment groups were similar at baseline with respect to patient demographics. At the EOT visit, for cefdinir and amoxicillin/clavulanate, respectively, intent-to-treat (ITT) clinical cure rates were 82% (129/158) and 85% (134/158) (?p = 0.547; 95% confidence interval [CI] –11.7 to 5.4) and per-protocol cure rates were 82% (123/150) and 90% (129/143) (?p = 0.045; 95% CI –16.4 to 0.0). This difference was driven primarily by reduced cefdinir response in patients with recurrent AOM (p = 0.010) and those younger than 24 months (p = 0.039). Comparing cefdinir with amoxicillin/clavulanate, parents more often reported significantly better ease of use (89% vs. 57%; p < 0.0001), better taste (85% vs. 39%; p < 0.0001), and better adherence (at least 95% of doses) (82% vs. 61%; p < 0.0001). Diarrhea/loose stools were more common in the amoxicillin/clavulanate group than in the cefdinir group (28% vs. 18%, respectively; p = 0.0341). One patient in the cefdinir group and eight patients in the amoxicillin/clavulanate group withdrew from the study prematurely due to at least one adverse event (?p = 0.0364). Study limitations included assessment of clinical recurrence by telephone call rather than office visit, exclusion of children with refractory AOM, and no assessment of middle ear microbiology.

Conclusions: Among young children with non-refractory AOM, cefdinir was as efficacious as high-dose amoxicillin/clavulanate in the ITT group, but somewhat less effective in per-protocol analysis. From the parental perspective, cefdinir was easier to administer, had a better taste, caused less diarrhea, and resulted in higher treatment adherence than high-dose amoxicillin clavulanate.     

头孢地尼原料及制剂的聚合物杂质分析

目的 建立头孢地尼原料及制剂聚合物杂质的分析方法。方法 分别采用0.1mol/L磷酸盐溶液和氯仿-三乙胺为溶剂,制备头孢地尼降解溶液;采用高效凝胶色谱法(HPSEC, TSK G2000 SWxl)和柱切换-LC/MSn法对头孢地尼降解溶液的弱保留值杂质进行分离和结构鉴定,并评估高效凝胶色谱法分析聚合物杂质的专属性;采用Diamonsil, C18型色谱柱,以0.25%四甲基氢氧化铵溶液(pH5.5)-甲醇-乙腈为流动相进行梯度洗脱,建立头孢地尼聚合物的RP-HPLC分析方法,采用二维色谱法和柱切换-LC/MSn法对其专属性进行分析,并进行方法学验证。结果 在头孢地尼降解物中鉴定出头孢地尼二聚体及其异构体,以及若干小分子杂质;高效凝胶色谱法分离头孢地尼聚合物杂质时,小分子杂质与聚合物杂质共出峰,方法专属性与定量准确性差;RP-HPLC法分析头孢地尼聚合物杂质时,能够检出头孢地尼二聚体及其异构体,头孢地尼三聚体,专属性好。结论     

头孢地尼联合奥硝唑治疗盆腔炎的临床效果观察

目的 研究头孢地尼联合奥硝唑治疗盆腔炎的临床效果.方法 选取78例盆腔炎患者作为研究对象,按随机数字表法分为对照组和观察组,各39例.对照组口服奥硝唑治疗,观察组口服奥硝唑联合头孢地尼治疗.比较两组治疗效果、治疗前后炎症因子[白细胞介素-1(IL-1)、C反应蛋白(CRP)]水平、治疗前后血液流变学指标(血浆粘度、红细...     

宣肺止嗽合剂联合头孢地尼治疗急性细菌性上呼吸道感染的临床研究

目的 探讨宣肺止嗽合剂联合头孢地尼治疗急性细菌性上呼吸道感染的临床疗效。方法 选取2021年6月—2023年6月上海交通大学医学院苏州九龙医院收治的急性细菌性上呼吸道感染患者120例,随机分为对照组（60例）和治疗组（60例）。对照组患者口服头孢地尼分散片,100 mg/次,3次/d。在对照组的基础上,治疗组口服宣肺止嗽合剂,20 mL/次,3次/d。两组连续服药7 d。观察两组患者临床疗效,比较治疗前后两组患者临床症状恢复时间,体温（T）,白细胞计数（WBC）,血清炎性因子白细胞介素-6(IL-6)、降钙素原（PCT）、干扰素-γ(INF-γ)和C反应蛋白（CRP）水平。结果 治疗后,治疗组临床总有效率为98.33%,明显高于对照组总有效率（83.33%,P<0.05）。治疗后,治疗组症状好转时间均明显短于对照组（P<0.05）。治疗后,两组患者体温、WBC、IL-6、PCT、CRP指标水平均比治疗前显著下降,而IFN-γ水平明显升高（P<0.05）,且治疗组这些指标水平均明显好于对照组（P<0.05）。结论 头孢地尼与宣肺止嗽合剂协同治疗急性细菌性上呼吸道感...