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PubMed2002

The effect of tablet formulation and hardness on in vitro release of cephalexin from Eudragit L100 based extended release tablets.

Eighteen batches of cephalexin extended release tablet were prepared by wet granulation method by using Eudragit L100. The effect of the concentration of Eudragit L100, microcrystalline cellulose and tablet hardness on cephalexin release was studied. The formulated tablets were also characterized for physical and chemical parameters. The dissolution results showed that a higher amount of Eudragit in tablet composition and higher tablet hardness resulted in reduced drug release. An increased amount of microcrystalline cellulose in tablet composition resulted in enhanced drug release. Tablet composition of 13.3% w/w Eudragit L100 and 6.6 to 8% w/w microcrystalline cellulose with hardness of 7-11 kg/cm2 gave predicted release for 6 h. The in vitro release was compared with a marketed tablet. Physical and chemical parameters of all formulated tablets were within acceptable limits. The effect of storage on in vitro release and physicochemical parameters of tablets was evaluated and two batches among formulated eighteen batches found to be in acceptable limits.

Cephalexin↗
PubMed1977

Cephalexin levels in serum, synovial fluid and joint tissues after oral administration.

Cephalexin (1 g) was administered orally every 6 hours to 13 patients with rheumatoid arthritis and chronic knee effusions without bacterial arthritis. Samples were taken from blood, synovial fluid, synovium, cartilage and bone. The concentrations found in these samples after one oral dose were high enough to have a possible therapeutic effect in bacterial arthritis sensitive to cephalexin.

Administration, Oral↗
PubMed1977

The determination of cephradine and cephalexin by reverse phase high-performance liquid chromatography.

The application of reverse phase high-performance liquid chromatography to the separation and analysis of cephradine and cephalexin is demonstrated. The procedure has been applied to chemicals, pharmaceutical formulations and reaction solutions. The preparation of samples is simple and rapid. Chromatographic conditions are described for both pellicular and small particle columns. The feasibility of determing cephradine and cephalexin in physiological fluids has also been demonstrated.

Capsules↗
PubMed1979

Bactericidal activity of cefadroxil, cephalexin, and cephradine in an in vitro pharmacokinetic model.

Cefadroxil (Duricef, Mead Johnson and Company), resembles cephalexin and cephradine in spectrum of antibacterial activity but differs in human pharmacokinetic properties. Whether the latter are likely to affect activity in vivo was assessed by determining bactericidal activity against clinical isolates under conditions simulating the variation of drug concentration in the blood stream after an oral dose of 500 mg to adults. In this kinetic model, cefadroxil was more active than cephalexin or cephradine against Staphylococcus aureus, Streptococcus pneumoniae, Klebsiella pneumoniae, Proteus mirabilis, Haemophilus influenzae and one of two strains of Escherichia coli. The other strain of E. coli was virtually unaffected by the cephalosporins. S. pyogenes was equally susceptible to all three cephalosporins. Analysis of the results suggest that the pharmocokinetic properties of an antibiotic affect its activity in the blood stream, provided the susceptibility of the infecting organism is concentration-dependent within the range of drug concentration occurring in serum.

Adult↗
PubMed1999

Neural modulation of cephalexin intestinal absorption through the di- and tripeptide brush border transporter of rat jejunum in vivo.

Intestinal absorption of beta-lactamine antibiotics (e.g., cefixime and cephalexin) has been shown to proceed through the dipeptide carrier system. In a previous study, nifedipine (NFP), an L-type calcium channel blocker, enhanced the absorption of cefixime in vivo but not in vitro, and it was suggested that neural mechanisms might be involved in the effect of NFP. The aim of the present study was to assess the involvement of the nervous system on the intestinal absorption of cephalexin (CFX). To investigate this, we used a single-pass jejunal perfusion technique in rats. NFP and diltiazem enhanced approximately 2-fold the plasma levels of CFX in treated rats versus untreated controls. NFP also increased approximately 2-fold the CFX level in portal plasma and increased urinary excretion of CFX, thus indicating that CFX did effectively increase CFX intestinal absorption. Perfusing high concentrations of dipeptides in the jejunal lumen competitively reduced CFX absorption and inhibited the enhancement of CFX absorption produced by NFP. Hexamethonium and lidocaine inhibited the effect of NFP, whereas atropine, capsaicin, clonidine, and isoproterenol enhanced CFX absorption by the same order of magnitude as NFP. Thus, complex neural networks can modulate the function of the intestinal di- and tripeptide transporter. Sympathetic noradrenergic fibers, intestinal sensory neurons, and nicotinic synapses are involved in the increase of CFX absorption produced by NFP.

ATP-Binding Cassette Transporters↗
PubMed2001

Effects of ceramic component on cephalexin release from bioactive bone cement consisting of Bis-GMA/TEGDMA resin and bioactive glass ceramics.

The purpose of this study was to elucidate the effect of amount of ceramic cement powder on drug release from bioactive bone cement. The associated bone-bonding strength was also investigated. The bioactive bone cement under investigation consisted of bisphenol-alpha-glycidyl methacrylate (Bis-GMA), triethylene-glycol dimethacrylate (TEGDMA) resin and a combination of apatite- and wollastonite-containing glass-ceramic (A-W GC) powder. A-W GC powder (50%, 70% and 80% w/w) containing 5% cephalexin (CEX) powder hardened within 5 min after mixing with Bis-GMA/TEGDMA resin. The compressive strength of the cement with or without drug increased with increasing the amount of ceramic powder. The compressive strength of the 80% ceramic cement without the incorporation of cephalexin was 194 MPa. This compressive strength was about 3 times higher than that for polymethylmethacrylate cement. After the cement was implanted in the proximal metaphysis of the tibiae of male rabbits, the failure load for the cement was found to increase with increasing of the amount of ceramic powder. This finding suggested that the cement formed a bonding with bone. In vitro CEX release from bioactive bone cement pellets in a simulated body fluid at pH 7.25 and 37 degrees C continued for more than 2 weeks. Drug release profile followed the Higuchi equation initially, but not at later stages. The drug release rate increased with increasing amount of ceramic powder in the mixture. Since the pore volume of the cement increased with increasing of amount of ceramic powder, the drug diffused in the pores between the ceramics particle and polymer matrix. As hydroxyapatite precipitated on the cement surface, the drug release rate decreased, as observed at the later release stage. These results suggest that varying the amount of ceramic powder in the cement system could control the drug release rate from bioactive bone cement.

Absorbable Implants↗
PubMed1975

Concentration of cephalexin in maxillary sinus mucosa and secretion.

Twenty patients hospitalized for unilateral or bilateral sinus surgery were given 500 mg or 15 mg/kg body weight of cephalexin by mouth two hours before operation. Samples of serum, sinus mucosa and secretion for cephalexin concentrations were taken during operation. There was a large variation in the mucosal and secretion concentrations and no definite correlation with serum levels. Drug levels effective against most gram-positive cocci were usually found in the mucosa. The mucosal concentrations were much larger than those in the secretion. There were no noteworthy differences between the patients with purulent infection and those in whom the infection was quiescent.

Adult↗
PubMed2002

Determination of cephalexin in oral suspensions by micellar electrokinetic chromatography.

A simple and efficient micellar capillary electrophoresis method for the analysis of cephalexin in oral suspensions is described. The analysis was carried out in a bare silica capillary with 75 microm i.d. and total length of 50 cm (28 cm to the detector) with a buffer solution containing 20 mM sodium tetraborate, 20 mM sodium dodecyl sulfate, and 0.1% laurylpolyoxiethylenic ether. The applied voltage was 15 kV. Detection was achieved by ultraviolet absorption at 210 nm. The calibration curve was linear within the concentration range from 40.0 to 120 microg/mL with a correlation coefficient of 0.9998. The percentage recovery was found to be 100.09 +/- 0.56. The method showed good selectivity and resolution of the drug impurities, and was found suitable to study cephalexin stability in pharmaceutical preparations.

Anti-Bacterial Agents↗
PubMed1975

Cephalexin-related nephropathy.

Hematuria and eosinophilia developed in two patients being treated for bacterial endocarditis with 20 or 24 gm/day of cephalexin given orally together with probenecid (Benemid). One patient had a concurrent transient increase in serum creatinine; both patients had a history of penicillin allergy and had previously received cephalexin intravenously. All abnormalities promptly remitted following discontinuation of therapy.

Administration, Oral↗
PubMed2002

Histological changes in the pancreas of white rats after administering cephalexin and ethanol.

The research was conducted on male Wistar rats weighing approximately 200 g. Animals of experimental group I were administered 20% ethyl alcohol for drinking, animals of experimental group II--cephalexin in the dose of 42 mg daily, animals of experimental group III--simultaneously alcohol and cephalexin in the mentioned doses. After 10 days the animals were guillotined and pancreas was taken for research. On paraffin sections 7 mu thick there were carried out H + E stain and PAS reaction aimed at discovering neutral mucopolysaccharides. After administering alcohol there was stated a decrease in the activity of exocrime cells and after administering of cephalexim--an increase in this activity. A simultaneous administration of ethyl alcohol and antibiotic causes trophic changes, which can be noticed as introductory, but at this stage--reversible, degenerative changes.

Animals↗
PubMedDate not supplied

Comparison of micellar electrokinetic chromatography, liquid chromatography, and microbiologic assay for analysis of cephalexin in oral suspensions.

Two well-accepted methodologies, based on a microbiologic assay (MA) and liquid chromatography (LC), and a novel methodology using micellar electrokinetic chromatography (MEKC), were compared for the determination of cephalexin in commercially available and simulated samples of oral suspensions. The MA, described in the Brazilian Pharmacopeia, was performed with a strain of Staphylococcus aureus ATCC 6538 as the test organism, following the cylinder-plate method. The LC analysis followed the European Pharmacopoeia, 3rd Ed., and was used with minor modifications. The MEKC analysis was based on a previous work of the group. Estimates of the repeatability relative standard deviations of the MA, LC, and MEKC methods in the analysis of a commercial sample were 0.34, 0.42, and 0.37%, respectively. The recovery obtained with LC was 99.90 +/- 1.11%; for MEKC, it was 100.09 +/- 0.56%. Although the 3 methodologies were statistically equivalent for the determination of cephalexin in oral suspensions, MA gave suitable repeatability despite being nonspecific and time-consuming. MEKC provided faster analysis and higher column efficiency, whereas LC presented superior sensitivity. The results indicated that MEKC can be used as an alternative method to MA and LC in routine quality control laboratories.

Anti-Bacterial Agents↗
PubMed1990

[Screening of alpha-amino acid ester hydrolase producing strain and synthesis of cephalexin by Pseudomonas aeruginosa].

From ten genera and 146 bacterial strains, 22 strains producing alpha-amino acid ester hydrolase were selected. Among them, AS 1.586 and 41-2 were the best. The optimal conditions for synthesis of cephalexin by pseudomonas aeruginosa 1.204 were investigated. The optimal pH and temperature for enzymatic synthesis reaction was pH 6.8 and 25 degrees C, respectively. By using 1% 7-ADCA, 3% PGME and 4% biomass, about 70% of 7-ADCA was converted to cephalexin under the mentioned conditions.

Carboxylic Ester Hydrolases↗
PubMed1989

[Effect of cephalexin on the colonization resistance of the large intestine in experimental animals].

It was shown morphologically and microbiologically that cephalexin administered intragastrically in a dose of 2 g/kg induced deep microecological changes in the cecum of Wistar albino rats. Scanning electron microscopy revealed that a single use of cephalexin in the above dose resulted in almost complete elimination of the biofilm from the surface of the cecum mucosa and it inflammation. This was accompanied by an increase in the number of potentially pathogenic bacteria and broadening of the spectrum of the phage variants of coliform bacilli present in the animal feces, as well as by change the periods of coliform bacilli persisting in the large intestine.

Animals↗
PubMed1977

[Pharmacokinetics of cephalexin and cephradine in surgical patients].

Pharmacokinetics of 2 oral cephalosporin antibiotics, i.e. cephalexin and cephradin in surgical patients with normal function of the liver and kidneys was studied. Both the drugs were satisfactorily absorbed into the blood reaching the maximum level in 1 hour. The antibiotics were determined in close concentrations in the blood serum of the patients during 5 hours of the observation. No differences in the time of a two-fold decrease in the antibiotic serum level and the value of the area limited by the antibiotic blood level were found. Cephalexin and cephradin were excreted with the urine in equal amounts.

Absorption↗
PubMed1987

[Changes in the microflora of the large intestine in rats administered cephalexin and erythromycin orally].

The effect of long-term use of cephalexin and erythromycin (for 17 days) on large intestine microflora was studied on rats. It was found that intragastric administration of cephalexin in a dose of 800 mg/kg and erythromycin in a dose of 400 mg/kg was followed by changes in the quantitative and qualitative composition of the large intestine aerobic and anaerobic microflora. However, it did not induce production of beta-aspartyl glycine which is a biochemical indicator of deep changes in intestinal microflora. The long-term use of the above antibiotics resulted in increased levels and persistence of intestine colonization with facultative pathogenic enterobacteria and staphylococci resistant to the chemotherapeutic agents.

Administration, Oral↗
PubMed1985

A multicenter, randomized parallel double-blind study comparing three antibiotics, cephemic-cofosfolactamine, fosfomycin and cephalexin, in the treatment of systemic infections.

In the present multicenter, randomized and double-blind study, performed on 127 hospitalized patients, we compared the effects of three antibiotics (cephemic cofosfolactamine, cephalexin and fosfomycin) in the treatment of acute or recurrent systemic infections. Results show that the percentage of recoveries of clinical symptoms and of bacterial eradications were significantly higher, and associated with a lower rate of side effects in the patients treated by cephemic cofosfolactamine than in those treated by cephalexin or fosfomycin.

Anti-Bacterial Agents↗
PubMed1985

[Primary hemostatic disorders caused by beta-lactams. Apropos of a postoperative hemorrhagic complication during treatment with cephalexin].

The authors report a case of haemorrhage due to cephalexin therapy. The bleeding started after an orthopedic operation in a patient without renal failure, receiving 3 g/day of cephalexin. Platelet function was very abnormal at the time of the haemorrhage with a bleeding time of over 20 minutes, which returned to normal when treatment was stopped. This case seems to be similar to other reports of haemorrhages during treatment with other beta-lactams.

Aged↗
PubMed1977

[Clinical experience with sustained release cephalexin (S-6436) in urology (author's transl)].

Clinical studies of S-6436 were conducted in 30 urinary tract infection patients in urology with the following conclusion. The patients received the drug twice a day after breakfast and dinner. 1. Of the 30 patiens, excellent efficacy was observed in 9 patients, good efficacy in 14, fair in 5 and poor in 2. The effectiveness (excellent or good) was 76.7%. 2. Twenty-seven (27) strains were isolated from the 30 patients and 23 strains (85.2%) of the 27 disappeared with the administration of the drug. 3. Side effects were found in 3 patients (10%) of the 30. The incidence was almost similar to that of regular cephalexin. No remarkable changes in laboratory data were observed. 4. S-6436 which requires the administration of only twice a day is a preparation which is more convenient for patients than regular cephalexin which requires the administration of four times a day.

Adult↗