scholarly journals Biological and physicochemical stability of ceftazidime and aminophylline on glucose parenteral solution

2012 ◽  
Vol 48 (4) ◽  
pp. 691-698
Author(s):  
Carolina Alves dos Santos ◽  
Laura Oliveira-Nascimento ◽  
Marcos Camargo Knirsch ◽  
Marco Antônio Stephano ◽  
Adalberto Pessoa Júnior ◽  
...  

Ceftazidime is a broad spectrum antibiotic administered mainly by the parenteral route, and it is especially effective against Pseudomonas aeruginosa. The period of time in which serum levels exceed the Minimum Inhibitory Concentration (MIC) is an important pharmacodynamic parameter for its efficacy. One of the forms to extend this period is to administer the antibiotic by continuous infusion, after prior dilution in a Parenteral Solution (PS). The present work assessed the stability of ceftazidime in 5% glucose PS for 24 hours, combined or not with aminophylline, through High Performance Liquid Chromatography (HPLC). The physicochemical evaluation was accompanied by in vitro antimicrobial activity compared MIC test in the 24-hour period. Escherichia coli and Pseudomonas aeruginosa were the microorganisms chosen for the MIC comparison. The HPLC analysis confirmed ceftazidime and aminophylline individual stability on PS, while the MIC values were slightly higher than the mean described in the literature. When both drugs were associated in the same PS, the ceftazidime concentration by HPLC decreased 25% after 24 hours. Not only did the MIC values show high loss of antibiotic activity within the same period, but also altered MIC values immediately after the preparation, which was not detected by HPLC. Our results indicate that this drug combination is not compatible, even if used right away, and that PS might not be the best vehicle for ceftazidime, emphasizing the importance of the MIC evaluation for drug interactions.

2021 ◽  
pp. 1-12
Author(s):  
Olivia T. Cheng ◽  
Andrew P. Stein ◽  
Eric Babajanian ◽  
Kathryn R. Hoppe ◽  
Shawn Li ◽  
...  

BACKGROUND: Implantable medical devices and hardware are prolific in medicine, but hardware associated infections remain a major issue. OBJECTIVE: To develop and evaluate a novel, biologic antimicrobial coating for medical implants. METHODS: Electrochemically compacted collagen sheets with and without crosslinked heparin were synthesized per protocol developed by our group. Sheets were incubated in antibiotic solution (gentamicin or moxifloxacin) overnight, and in vitro activity was assessed with five-day diffusion assays against Pseudomonas aeruginosa. Antibiotic release overtime from gentamicin infused sheets was determined using in vitro elution and high performance liquid chromatography (HPLC). RESULTS: Collagen-heparin-antibiotic sheets demonstrated larger growth inhibition zones against P. aeruginosa compared to collagen-antibiotic alone sheets. This activity persisted for five days and was not impacted by rinsing sheets prior to evaluation. Rinsed collagen-antibiotic sheets did not show any inhibition zones. Elution of gentamicin from collagen-heparin-gentamicin sheets was slow and remained above the minimal inhibitory concentration for gentamicin sensitive organisms for 29 days. Conversely, collagen-gentamicin sheets eluted their antibiotic payload within 24 hours. Overall, heparin associated sheets demonstrated larger inhibition zones against P. aeruginosa and prolonged elution profile via HPLC. CONCLUSION: We developed a novel, local antibiotic delivery system that could be used to coat medical implants/hardware in the future and reduce post-operative infections.


2018 ◽  
Vol 0 (0) ◽  
Author(s):  
Anne-Claire Bonnaure ◽  
Romain Bellay ◽  
Pauline Rault ◽  
Marie-Antoinette Lester ◽  
Pierre-Nicolas Boivin

Abstract Background Prednisone is a corticosteroid used in several inflammatory diseases and cancers. In France, no available prednisone drinkable formulation exists. Instead, an oral syrup of prednisone with ethanol, sodium benzoate and simple syrup is produced. However, sodium benzoate can induce neonatal icterus and alcohol is not authorized for children below 3 years of age. The aim of this study was to determine the stability of 5 mg/mL prednisone oral suspension in a commercial compounding excipient: Syrspend® SF PH4. Methods Three batches of oral suspensions were prepared, using micronized prednisone and Syrspend® SF PH4. They were packaged in amber glass vials and stored at room temperature. On day 0, 1, 4, 10, 30, 60 and 90, we observed physical and chemical stability (pH measurement, osmolality measurement, residual concentrations of prednisone and degradation product identification). A stability indicating method was developed using high performance liquid chromatography with Ultraviolet detection at 254 nm. Results Prednisone concentrations remained stable within ± 5 % of nominal values for 60 days. No degradation product and change of physicochemical properties were detected. Conclusion This study showed that 5 mg/mL prednisone oral suspension in Syrspend® SF PH4 is stable for 60 days, at room temperature and protected from light.


2020 ◽  
Vol 64 (12) ◽  
Author(s):  
Iris H. Chen ◽  
David P. Nicolau ◽  
Joseph L. Kuti

ABSTRACT Combination therapy may enhance imipenem/cilastatin/relebactam’s (I/R) activity against Pseudomonas aeruginosa and suppress resistance development. Human-simulated unbound plasma concentrations of I/R at 1.25 g every 6 h (h), colistin at 360 mg daily, and amikacin at 25 mg/kg daily were reproduced alone and in combination against six imipenem-nonsusceptible P. aeruginosa isolates in an in vitro pharmacodynamic model over 24 h. For I/R alone, the mean reductions in CFU ± the standard errors by 24 h were −2.52 ± 0.49, −1.49 ± 0.49, −1.15 ± 0.67, and −0.61 ± 0.10 log10 CFU/ml against isolates with MICs of 1/4, 2/4, 4/4, and 8/4 μg/ml, respectively. Amikacin alone also resulted in 24 h CFU reductions consistent with its MIC, while colistin CFU reductions did not differ. Resistant subpopulations were observed after 24 h in 1, 4, and 3 I/R-, colistin-, and amikacin-exposed isolates, respectively. The combination of I/R and colistin resulted in synergistic (n = 1) or additive (n = 2) interactions against three isolates with 24-h CFU reductions ranging from −2.62 to −4.67 log10 CFU/ml. The combination of I/R and amikacin exhibited indifferent interactions against all isolates, with combined drugs achieving −0.51- to −3.33-log10 CFU/ml reductions. No resistant subpopulations were observed during I/R and colistin combination studies, and when added to amikacin, I/R prevented the emergence of amikacin resistance. Against these six multidrug-resistant P. aeruginosa, I/R alone achieved significant CFU reductions against I/R-susceptible isolates. Combinations of I/R plus colistin resulted in additivity or synergy against some P. aeruginosa, whereas the addition of amikacin did not provide further antibacterial efficacy against these isolates.


1997 ◽  
Vol 41 (9) ◽  
pp. 2006-2008 ◽  
Author(s):  
J R Forney ◽  
S Yang ◽  
M C Healey

The combined effect of the serine protease inhibitor alpha-1-antitrypsin (AAT) and the aminoglycoside paromomycin on Cryptosporidium parvum infection in vitro was investigated. AAT and paromomycin were mixed with C. parvum oocysts as either single or combined treatments and used to inoculate epithelial cell cultures. Single- and combined-treatment groups had significantly lower (P < 0.01) parasite numbers than untreated controls. The mean fractional inhibitory concentration indices suggested significant synergistic activity.


Animals ◽  
2020 ◽  
Vol 10 (2) ◽  
pp. 281
Author(s):  
Adrian Zaragoza-Bastida ◽  
Saudy Consepcion Flores-Aguilar ◽  
Liliana Mireya Aguilar-Castro ◽  
Ana Lizet Morales-Ubaldo ◽  
Benjamín Valladares-Carranza ◽  
...  

Rattlesnakes have venoms with a complex toxin mixture comprised of polypeptides and proteins. Previous studies have shown that some of these polypeptides are of high value for the development of new medical treatments. The aim of the present study is to evaluate, in vitro, the antibacterial and hemolytic activity of Crotalus triseriatus and Crotalus ravus venoms. A direct field search was conducted to obtain Crotalus triseriatus and Crotalus ravus venom samples. These were evaluated to determine their antibacterial activity against Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa through the techniques of Minimum Inhibitory Concentration (MIC) and Minimum Bactericidal Concentration (MBC). Hemolytic activity was also determined. Antibacterial activity was determined for treatments (Crotalus triseriatus 2) CT2 and (Crotalus ravus 3) CR3, obtaining a Minimum Inhibitory Concentration of 50 µg/mL and a Minimum Bactericidal Concentration of 100 µg/mL against Pseudomonas aeruginosa. CT1 (Crotalus triseriatus 1), CT2, and CR3 presented hemolytic activity; on the other hand, Crotalus ravus 4 (CR4) did not show hemolytic activity. The results of the present study indicate for the first time that Crotalus triseriatus and Crotalus ravus venoms contain some bioactive compounds with bactericidal activity against Pseudomonas aeruginosa which could be used as alternative treatment in diseases caused by this pathogenic bacterium.


Materials ◽  
2020 ◽  
Vol 13 (14) ◽  
pp. 3205 ◽  
Author(s):  
Seen-Young Kang ◽  
Ji-Min Yu ◽  
Hyoung-Sik Kim ◽  
Jun-Seok Lee ◽  
Chan-Mi Yeon ◽  
...  

This study aims to compare the torque values for various lengths of the titanium-based orthodontic anchor screw (OAS), different anchorage methods and varying artificial bone densities after predrilling. Furthermore, the effects of these parameters on bone stability are evaluated. A total of 144 OASs were prepared with a diameter of 1.6 mm and heights of 6, 8 and 10 mm. Artificial bones were selected according to their density, corresponding to Grades 50, 40 and 30. Torque values for the automatic device and manual anchorage methods exhibited a statistically significant difference for the same-sized OAS, according to the bone density of the artificial bones (p < 0.05). However, when insertion torque was at the maximum rotations, there was no significant difference in the torque values for the Grade 30 artificial bone (p > 0.05). When the torque values of both anchorage methods were statistically compared with the mean difference for each group, the results of the manual anchorage method were significantly higher than those of the automatic device anchorage method (p < 0.05). A statistically significant difference was observed in the bone stability resulting from different OAS anchorage methods and artificial bone lengths. These findings suggest that the automatic anchorage method should be used when fixing the OAS.


1976 ◽  
Vol 4 (3) ◽  
pp. 165-175 ◽  
Author(s):  
Jose Ximenes ◽  
Orlando Natale Bassoi ◽  
Jairo Perche de Menezes ◽  
Wilson Fry

The activity of amikacin, gentamicin and kanamycin was tested in vitro against clinical isolates of Pseudomonas aeruginosa. Concentrations of the antibiotics in serum and in saline solution were prepared according to serum levels produced in volunteers 15 minutes, 1, 2, and 6 hours after a single intramuscular injection of 500 mg amikacin, 80 mg gentamicin and 500 mg kanamycin. Following isolation of the Pseudomonas strains in cultures, they were incubated and seeded in Mueller-Hinton broth, then 107 dilutions of the organisms were kept in contact with the prepared antibiotic solutions in serum and in saline solution for three hours, the approximate half-life of the antibiotics in serum. Amikacin was active at concentrations seen six hours post-dose, inhibiting growth in a total of 72·5% of seeded plates. Gentamicin was active for only two hours and inhibited growth in 2·5% of the plates. Kanamycin showed no anti-pseudomonal activity.


2008 ◽  
Vol 53 (1) ◽  
pp. 46-56 ◽  
Author(s):  
Jürgen B. Bulitta ◽  
Neang S. Ly ◽  
Jenny C. Yang ◽  
Alan Forrest ◽  
William J. Jusko ◽  
...  

ABSTRACT Evidence is mounting in support of the inoculum effect (i.e., slow killing at large initial inocula [CFUo]) for numerous antimicrobials against a variety of pathogens. Our objectives were to (i) determine the impact of the CFUo of Pseudomonas aeruginosa on ceftazidime activity and (ii) to develop and validate a pharmacokinetic/pharmacodynamic (PKPD) mathematical model accommodating a range of CFUo. Time-kill experiments using ceftazidime at seven concentrations up to 128 mg/liter (MIC, 2 mg/liter) were performed in duplicate against P. aeruginosa PAO1 at five CFUo from 105 to 109 CFU/ml. Samples were collected over 24 h and fit by candidate models in NONMEM VI and S-ADAPT 1.55 (all data were comodeled). External model qualification integrated data from eight previously published studies. Ceftazidime displayed approximately 3 to 4 log10 CFU/ml net killing at 106.2 CFUo and concentrations of 4 mg/liter (or higher), less than 1.6 log10 CFU/ml killing at 107.3 CFUo, and no killing at 108.0 CFUo for concentrations up to 128 mg/liter. The proposed mechanism-based model successfully described the inoculum effect and the concentration-independent lag time of killing. The mean generation time was 28.3 min. The effect of an autolysin was assumed to inhibit successful replication. Ceftazidime concentrations of 0.294 mg/liter stimulated the autolysin effect by 50%. The model was predictive in the internal cross-validation and had excellent in silico predictive performance for published studies of P. aeruginosa ATCC 27853 for various CFUo. The proposed PKPD model successfully described and predicted the pronounced inoculum effect of ceftazidime in vitro and integrated data from eight literature studies to support translation from time-kill experiments to in vitro infection models.


2013 ◽  
Vol 785-786 ◽  
pp. 493-497
Author(s):  
Yu Ping Li ◽  
Li Zhen Sun ◽  
Xiang Yuan Xiong ◽  
Zi Ling Li ◽  
Ting Kang Xing ◽  
...  

In the present study, controlled release characteristics of new nanosized PLA-Pluronic-PLA block copolymer vesicles comprising of amphiphilic poly (lactic acid) (PLA) and Pluronic block copolymers (PEO-PPO-PEO) have been evaluated as an oral insulin carrier. The mean size of vesicles was 78 nm for PLA-F127-PLA and 165 nm for PLA-P85-PLA copolymer. The mean insulin entrapment efficiency was 59.6% for PLA-P85-PLA and 26.4% for PLA-F127-PLA. The in vitro release characteristics of insulin from vesicles exhibited an initial burst in the range of pH 1.2-7.4 dissolution mediums. The presence of PLA-Pluronic-PLA vesicles improved the stability of insulin in the gastrointestinal fluids than that of the phosphate buffer solution (PBS) of insulin. More importantly, the released insulin from the vesicles maintained their biological activity. The results from this studies demonstrated that biodegradable PLA-Pluronic-PLA can self-assemble with insulin, form insulin-encapsulated vesicles, and is good carrier materials for oral insulin/protein delivery.


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