Variations in the anaerobic faecal flora of ten healthy human volunteers with special reference to the Bacteroides fragilis-group and clostridium difficile

1986 ◽  
Vol 261 (1) ◽  
pp. 43-52 ◽  
Author(s):  
G.J. Meijer-Severs ◽  
E. van Santen
Keyword(s):  
Clostridium Difficile ◽  
Special Reference ◽  
Bacteroides Fragilis ◽  
Healthy Human ◽  
Faecal Flora ◽  
Human Volunteers ◽  
Bacteroides Fragilis Group

Antianaerobic activity of the ketolide RU 64004 compared to activities of four macrolides, five beta-lactams, clindamycin, and metronidazole.

1997 ◽  
Vol 41 (5) ◽  
pp. 1037-1041 ◽  
Author(s):  
L M Ednie ◽  
S K Spangler ◽  
M R Jacobs ◽  
P C Appelbaum
Keyword(s):  
Clostridium Difficile ◽  
Bacteroides Fragilis ◽  
The Other ◽  
Beta Lactams ◽  
Gram Positive ◽  
Amoxicillin Clavulanate ◽  
Bacteroides Fragilis Group ◽  
Agar Dilution ◽  
Bacteroides Ovatus ◽  
Fusobacterium Varium

Agar dilution methodology (with added Oxyrase in the case of the macrolide group to allow incubation without added CO2) was used to compare the activity of RU 64004, a new ketolide, with the activities of erythromycin, azithromycin, clarithromycin, roxithromycin, clindamycin, amoxicillin with and without clavulanate, piperacillin with and without tazobactam, metronidazole, and imipenem against 379 anaerobes. Overall, RU 64004 yielded an MIC at which 50% of the isolates are inhibited (MIC50) of 1.0 microg/ml and an MIC90 of 16.0 microg/ml. In comparison, MIC50s and MIC90s of erythromycin, azithromycin, clarithromycin, and roxithromycin were 2.0 to 8.0 and >64.0 microg/ml, respectively. MICs of macrolides, including RU 64004, were higher for Bacteroides ovatus, Fusobacterium varium, Fusobacterium mortiferum, and Clostridium difficile than for the other species. RU 64004 was more active against gram-positive rods and cocci, Prevotella and Porphyromonas spp., and fusobacteria other than F. mortiferum and F. varium than against the Bacteroides fragilis group. Overall MIC50s and MIC90s (in micrograms per milliliter), respectively, of other compounds were as follows: clindamycin, 1.0 and 16.0; amoxicillin, 4.0 and 64.0; amoxicillin-clavulanate, 0.5 and 4.0; piperacillin, 8.0 and >64.0; piperacillin-tazobactam, 1.0 and 16.0; metronidazole, 1.0 and 4.0; and imipenem, 0.25 and 1.0.

Comparative antianaerobic activities of the ketolides HMR 3647 (RU 66647) and HMR 3004 (RU 64004).

1997 ◽  
Vol 41 (9) ◽  
pp. 2019-2022 ◽  
Author(s):  
L M Ednie ◽  
M R Jacobs ◽  
P C Appelbaum
Keyword(s):  
Clostridium Difficile ◽  
Bacteroides Fragilis ◽  
Bacteroides Fragilis Group ◽  
Fusobacterium Varium

HMR 3647 (RU 66647) and HMR 3004 (RU 64004), two ketolides, had MICs at which 50% of the strains are inhibited (MIC50s) of 0.06 to 0.125 microg/ml and MIC90s of 16.0 microg/ml against 352 anaerobes. MIC50s and MIC90s of erythromycin, azithromycin, clarithromycin, and roxithromycin were 0.5 to 2.0 microg/ml and 32.0 to >64.0 microg/ml, respectively. HMR 3647 and HMR 3004 were more active against non-Bacteroides fragilis-group anaerobes (other than Fusobacterium mortiferum, Fusobacterium varium, and Clostridium difficile).

Gastroretentive Floating Capsules of Risedronate Sodium: Development, Optimization, in vitro and in vivo Evaluation in Healthy Human Volunteers

2015 ◽  
Vol 8 (2) ◽  
pp. 2835-2842
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Arun Kumar Jarathi ◽  
Suresh Gande ◽  
Viswaja Medipally ◽  
Ramesh Bomma
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Zero Order ◽  
Wet Granulation ◽  
Capsule Formulation ◽  
In Vivo Evaluation ◽  
Healthy Human ◽  
X Ray ◽  
Human Volunteers

Background and the purpose of the study: Risedronate sodium inhibits osteoclast bone resorption and modulates bone metabolism. Risedronate has a high affinity for hydroxyapatite crystals in bone and is a potent antiresorptive agent. In the present investigation efforts were made to improve the bioavailability of risedronate sodium by increasing the residence time of the drug through sustained-release matrix capsule formulation via gastroretentive mechanism. Capsules were prepared by wet granulation technique. The influence of gel forming agents, amount of risedronate and total weight of capsules on physical properties, in vitro buoyancy, drug release, FTIR, DSC, X-ray studies were investigated. The release mechanisms were explored and explained by applying zero order, first order, Higuchi and Korsmeyer equations. The selected formulations were subjected to stability study at 40 °C/75% RH, 25 °C/60% RH for the period of three months. For all formulations, kinetics of drug release from capsules followed Higuchi’s square root of time kinetic treatment heralding diffusion as predominant mechanism of drug release. Formulation containing 25 mg HPMC K4M and 75 mg HPMC K100 LV (F-8) showed zero order release profile. There was no significant change in the selected formulation, when subjected to accelerated stability conditions over a period of three months. X-ray imaging in six healthy human volunteers revealed a mean gastric retention period of 5.60 ± 0.77 hrs for the selected formulation. Stable, sustained release effervescent floating capsules of risedronate sodium could be prepared by wet granulation technique.  

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