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Medical research on ceftin
Eur J Pharm Biopharm. 2008 Apr 11;
Dhumal RS, Biradar SV, Yamamura S, Paradkar AR, York P
The aim of the present work was to prepare amorphous discreet nanoparticles by sonoprecipitation method for enhancing oral bioavailability of cefuroxime axetil (CA), a poorly water-soluble drug. CA nanoparticles (SONO-CA) were prepared by sonoprecipitation and compared with particles obtained by precipitation without sonication (PPT-CA) and amorphous CA obtained by spray drying. Spray drying present broad particle size distribution (PSD) with mean particle size of 10mum and low percent yield, whereas, precipitation without sonication resulted in large amorphous aggregates with broad PSD. During sonoprecipitation, particle size and yield improve with an increase in the amplitude of sonication and lowering the operation temperature due to instantaneous supersaturation and nucleation. The overall symmetry and purity of CA molecule was maintained as confirmed by FTIR and HPLC, respectively. All the three methods resulted in the formation of amorphous CA with only sonoprecipitation resulting in uniform sized nanoparticles. Sonoprecipitated CA nanoparticles showed enhanced dissolution rate and oral bioavailability in Wistar rat due to an increased solubility attributed to combination of effects like amorphization and nanonization with increased surface area and reduced diffusion pathway.
Diagnosis and treatment of Lyme disease.
Mayo Clin Proc. 2008 May; 83(5): 566-71
Bratton RL, Whiteside JW, Hovan MJ, Engle RL, Edwards FD
Lyme disease is the most common tick-borne disease in the United States. This review details the risk factors, clinical presentation, treatment, and prophylaxis for the disease. Information was obtained from a search of the PubMed and MEDLINE databases (keyword: Lyme disease) for articles published from August 31, 1997, through September 1, 2007. Approximately 20,000 cases of Lyme disease are reported annually. Residents of the coastal Northeast, northwest California, and the Great Lakes region are at highest risk. Children and those spending extended time outdoors in wooded areas are also at increased risk. The disease is transmitted to humans through the bite of the Ixodes tick (Ixodes scapularis and Ixodes pacificus). Typically, the tick must feed for at least 36 hours for transmission of the causative bacterium, Borrelia burgdorferi, to occur. Each of the 3 stages of the disease is associated with specific clinical features: early localized infection, with erythema migrans, fever, malaise, fatigue, headache, myalgias, and arthralgias; early disseminated infection (occurring days to weeks later), with neurologic, musculoskeletal, or cardiovascular symptoms and multiple erythema migrans lesions; and late disseminated infection, with intermittent swelling and pain of 1 or more joints (especially knees). Neurologic manifestations (neuropathy or encephalopathy) may occur. Diagnosis is usually made clinically. Treatment is accomplished with doxycycline or amoxicillin; cefuroxime axetil or erythromycin can be used as an alternative. Late or severe disease requires intravenous ceftriaxone or penicillin G. Single-dose doxycycline (200 mg orally) can be used as prophylaxis in selected patients. Preventive measures should be emphasized to patients to help reduce risk.
Effect of malnutrition on the pharmacokinetics of cefuroxime axetil in young rats.
J Pharm Pharm Sci. 2008; 11(1): 9-21
González-Hernández I, Jung-Cook H, Sotelo A
PURPOSE: To determine the pharmacokinetics of cefuroxime axetil in malnourished rats using a diet with a restriction in energy and nutrients (group M), a diet with a low quality protein (group K) and a good quality diet (group C) as a control. METHODS: The rats were fed with the corresponding diet during 21 days. After this period a single oral dose of cefuroxime axetil (equivalent to a 2.2 mg dose of cefuroxime) was administered, and plasma samples were taken at 0, 5, 10, 30, 45, 60, 90, 120, 180, 240, 300 and 360 minutes; samples were assayed using an HPLC assay. Biochemical parameters were also measured an a microscopy study of the small intestine was done. After a 21 day period of recovery of the malnourished groups a second pharmacokinetic study was performed using the same sample times as in the first study. RESULTS: In malnourished animals of group K the levels of plasma proteins were low, and showed higher concentrations of fat in the liver. The relative bioavailability of cefuroxime was 78.2% for group M and 64.4% for group K. Groups M and K presented lower values of area under the curve, which means that the amount of antibiotic absorbed was lower than group C. In the second pharmacokinetic study although the animals received a good quality diet, it was observed that the area under the curve of group K was lower, and the relative bioavailability was 54.3%, while group M had similar pharmacokinetic values than control group. CONCLUSIONS: The pharmacokinetics of cefuroxime was affected by malnutrition, suggesting that the absorption process via the transporter was modified in the malnourished groups, specially in the group fed with a low quality protein.
Antimicrob Agents Chemother. 2008 Jul; 52(7): 2639-43
Critchley IA, Jacobs MR, Brown SD, Traczewski MM, Tillotson GS, Janjic N
Of 393 isolates of Streptococcus pneumoniae from U.S. children collected in 2005-2006, nonvaccine serotypes accounted for 89.1%, with serotype 19A the most prevalent, representing 30.5% of all isolates. The MIC(90) of faropenem against serotype 19A isolates was 1 mug/ml, compared to > or =8 microg/ml against amoxicillin/clavulanate, cefdinir, cefuroxime axetil, and azithromycin.
Cefprozil versus Cefuroxime Axetil in the Treatment of Acute Sinusitis.
Clin Drug Investig. 1998; 15(2): 81-90
Brankston ER, Conter HS, Corriveau R, Martel JM, Laroche C, Roy R, Savard C, Roy D, Kelly R, Forget P, Rivard M, Boulerice F
The objective of this multicentre, randomised, open-label, general practice (GP) study was to evaluate the efficacy and tolerability of cefprozil (Cefzil(trade mark), Bristol-Myers Squibb) compared with that of cefuroxime axetil (Ceftin((R)), Glaxo Wellcome) in the treatment of adult subjects with acute sinusitis. Typical of the GP setting, diagnosis was made based solely on clinical signs and symptoms of acute disease. Sinus radiography was performed post-randomisation. A total of 381 adolescent and adult patients were randomly assigned to 10 days' treatment with either cefprozil, 500mg orally twice daily (n = 191), or cefuroxime axetil, 250mg orally twice daily (n = 190). Based on predefined criteria, treatments were found to be equally effective in terms of proportions of patients in the per-protocol population that were cured, improved or failed (p = 0.20). Similar results were observed when the evaluation was performed on the subset of patients with radiographic evidence of sinusitis and when the evaluation was based on the investigator's judgement. Similar rates of adverse events were observed in the two treatment groups. In summary, cefprozil 500mg twice daily is as well tolerated and as effective as cefuroxime axetil 250mg twice daily for the treatment of adolescent and adult patients with clinical signs and symptoms of acute sinusitis.
What is a Suitable Dissolution Method for Drug Nanoparticles?
Pharm Res. 2008 Jul; 25(7): 1696-701
Heng D, Cutler DJ, Chan HK, Yun J, Raper JA
PURPOSE: Many existing and new drugs fail to be fully utilized because of their limited bioavailability due to poor solubility in aqueous media. Given the emerging importance of using nanoparticles as a promising way to enhance the dissolution rate of these drugs, a method must be developed to adequately reflect the rate-change due to size reduction. At present, there is little published work examining the suitability of different dissolution apparatus for nanoparticles. METHODS: Four commonly-used methods (the paddle, rotating basket and flow-through cell from the US Pharmacopia, and a dialysis method) were employed to measure the dissolution rates of cefuroxime axetil as a model for nanodrug particles. RESULTS: Experimental rate ratios between the nanoparticles and their unprocessed form were 6.95, 1.57 and 1.00 for the flow-through, basket and paddle apparatus respectively. In comparison, the model-predicted value was 7.97. Dissolution via dialysis was rate-limited by the membrane. CONCLUSIONS: The data showed the flow-through cell to be unequivocally the most robust dissolution method for the nanoparticulate system. Furthermore, the dissolution profiles conform closely to the classic Noyes-Whitney model, indicating that the increase in dissolution rate as particles become smaller results from the increase in surface area and solubility of the nanoparticles.
Stability of cefuroxime axetil oral suspension at different temperature storage conditions.
Bosn J Basic Med Sci. 2008 Feb; 8(1): 93-7
Uzunović A, Vranić E
Stability testing of an active substance or finished product provides information of the variation of drug substance or final product with time influenced by a variety of environmental factors such as temperature, humidity and light. Knowledge gained from stability studies enables understanding of the effects of the environment on the drugs. The aim of our study was to determine the stability of cefuroxime axetil oral suspension at different temperature storage conditions (stored at room /20 degrees C/ and refrigerated /5 degrees C/ conditions). Determination of cefuroxime (as cefuroxime axetil) was performed by dissolution testing. Fractions of the released cefuroxime axetil were compared using f2 value. After interpolating data for dissolution profiles at room and refrigerated conditions the following f2values were obtained: 62,56; 56,32 and 36,18 on 3rd, 6th and 10th day, respectively. These values indicate similarities in drug release from analyzed cefuroxime axetil oral suspension on 3rd, 6th day, and differences on 10th day. Based on our results, we may assume that cefuroxime axetil oral suspension preserves its stability for 10 days after reconstitution under room and refrigerated conditions. It is obvious, according to the f2 value obtained on the 10th day, that there is a difference between the released cefuroxime axetil from oral suspension at room (87,68%) and refrigerated (92,35%) conditions. Concentration changes can be caused by the mechanisms associated with drug release and hydrolytical decomposition of the sample and higher temperatures during longer period of storage.
Chemotherapy. 2008; 54(2): 84-90
Sevillano D, Aguilar L, Alou L, Giménez MJ, González N, Echeverría O, Torrico M, Valdes L, Coronel P, Prieto J
BACKGROUND: Activity of simulated serum concentrations after oral therapy with 400 mg cefditoren pivoxil b.i.d., 500 mg cefuroxime axetil b.i.d. and 875/125 mg amoxicillin/clavulanic acid b.i.d. and t.i.d. regimens was explored over 24 h against Streptococcus pneumoniae. METHODS: Computerized pharmacodynamic simulations were performed against strains with penicillin/amoxicillin/cefuroxime/cefditoren minimum inhibitory concentrations (MICs, microg/ml) and serotypes: strain 1 (0.25/0.12/1/0.12; serotype 6A), strain 2 (2/4/ 2/0.25; serotype 6B), strain 3 (4/16/4/0.5; serotype 14), and strain 4 (4/16/8/1; serotype 14). RESULTS: Bactericidal activity (> or =3 log(10) reduction) at 12 and 24 h was obtained against all strains with cefditoren, against strains 1 and 2 with cefuroxime and amoxicillin/clavulanic acid t.i.d., but only against strain 1 with amoxicillin/clavulanic acid b.i.d.. Bactericidal activity at 24 h was related to T > MIC of >30% dosing interval, 1.7-2.0 log(10) reductions with T > MIC of 20-30%, and MIC of 0%. CONCLUSIONS: It is difficult to achieve pharmacodynamic coverage and bactericidal activity by physiological concentrations of oral beta-lactams against penicillin-resistant pneumococcal strains exhibiting higher amoxicillin versus penicillin MICs. Cefditoren may offer alternatives.
Aging Clin Exp Res. 2008 Feb; 20(1): 81-6
Flamaing J, Knockaert D, Meijers B, Verhaegen J, Peetermans WE
BACKGROUND AND AIMS: Community acquired lower respiratory tract infection (CALRTI) is the most common infection requiring hospitalization in the elderly. Sequential antibiotic therapy offers the potential for earlier functional rehabilitation, shorter length of hospital stay and lower costs. We studied the efficacy and safety of an empiric sequential antibiotic therapy with cefuroxime-cefuroxime axetil in elderly patients hospitalized with a CALRTI. METHODS: A prospective, randomized, open-label, in-hospital study of cefuroxime IV 750 mg tid for 10 days (IV group) vs cefuroxime 750 mg IV tid for 3 days, followed by cefuroxime-axetil PO 500 mg bid for 7 days (sequence group), when clinical (symptoms improved and fever disappeared) and/or laboratory response [decrease in C-reactive protein (CRP)] occurred. RESULTS: A total of 142 patients, 71 (mean age: 83.3 (+/-6 SD), M/F ratio: 1.1) in the IV group, and 71 (mean age: 81.5 (+/-7 SD), M/F ratio: 1.5) in the sequence group, were included in the study. Eighty-three (58.4%) presented with radiologically confirmed pneumonia (CAP) and 59 (41.6%) with non-pneumonic LRTI (NPLRTI) (p=ns between study groups). Treatment was considered effective in 84.5% (60/71) of patients in the IV group and 80.3% (57/71) in the sequence group (p=ns). Therapy failed in 15% (21/142) of the study population (p=ns between study groups) and, after day 3 of therapy, 8.45% (6/71) failed in both study groups. By the end of treatment, two patients had died in each study group, and total in-hospital mortality was 8.5% (12/142, p=ns between study groups). The length of hospital stay (LOS) did not differ between the two study groups. CONCLUSIONS: When a favorable clinical or biochemical response occurs on day 3 of IV cefuroxime therapy, further therapy with oral cefuroxime-axetil is as effective and safe as a full course of cefuroxime IV in elderly patients hospitalized with CALRTI. However, LOS was not reduced after sequential antibiotic therapy in this population.
Neurological picture. Horner syndrome due to jugular vein thrombosis (Lemierre syndrome).
J Neurol Neurosurg Psychiatry. 2008 Mar; 79(3): 293
Habek M, Petravić D, Ozretić D, Brinar VV