Category: 86393-32-0

On June 10, 2018, Shetty, Nivedita; Park, Heejun; Zemlyanov, Dmitry; Mangal, Sharad; Bhujbal, Sonal; Zhou, Qi published an article.Safety of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate The title of the article was Influence of excipients on physical and aerosolization stability of spray dried high-dose powder formulations for inhalation. And the article contained the following:

The aim of this study is to investigate the influence of excipients on phys. and aerosolization stability of spray dried Ciprofloxacin dry powder inhaler formulations. The model drug, Ciprofloxacin hydrochloride, was co-spray dried with excipients such as disaccharides (sucrose, lactose, trehalose), mannitol and L-leucine. The spray dried samples were stored at two different relative humidity (RH) conditions of: (1) 20% and (2) 55% RH at 20°C. Ciprofloxacin co-spray dried with disaccharides and L-leucine in the mass ratio of 1:1 demonstrated an increase in fine particle fraction (FPF) as compared with the spray dried Ciprofloxacin alone when stored at 20% RH. However, deterioration in FPF of Ciprofloxacin co-spray dried with disaccharide and mannitol was observed upon storage at 55% RH as compared to the corresponding formulations stored at 20% RH due to particle agglomeration. Whereas, 10% and 50% weight/weight L-leucine in the formulation showed no change in aerosol performance (FPF of 71.1±3.5% and 79.5±3.1%, resp.) when stored at 55% RH for 10 days as compared to 20% RH (FPF of 68.1±0.3% and 73.6±7.1%, resp.). L-Leucine demonstrated aerosolization stability by alleviating crystallization of Ciprofloxacin to some extent and preventing significant change in particle morphol. L-Leucine is well-recognized as aerosolization enhancer; our study has shown L-leucine is also a phys. and aerosolization stabilizer for spray dried Ciprofloxacin DPI formulations. Such stability enhancing activities were attributed to the enrichment of L-leucine on the particle surface as confirmed by XPS data, and intermol. interactions between L-leucine and Ciprofloxacin as measured by FT-IR. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Safety of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

The Article related to excipient aerosolization spray drying powder formulation inhalation, antibiotics, dry powder inhaler (dpi), excipients, fine particle fraction (fpf), spray drying, Pharmaceuticals: Formulation and Compounding and other aspects.Safety of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On September 4, 2018, Shetty, Nivedita; Ahn, Patricia; Park, Heejun; Bhujbal, Sonal; Zemlyanov, Dmitry; Cavallaro, Alex; Mangal, Sharad; Li, Jian; Zhou, Qi Tony published an article.Related Products of 86393-32-0 The title of the article was Improved Physical Stability and Aerosolization of Inhalable Amorphous Ciprofloxacin Powder Formulations by Incorporating Synergistic Colistin. And the article contained the following:

This study aimed to develop dry powder inhaler (DPI) combination formulations of ciprofloxacin and colistin for use in respiratory infections. Effects of colistin on phys. stability and aerosolization of spray-dried ciprofloxacin were examined The combination DPI formulations were produced by co-spray drying colistin and ciprofloxacin in mass ratios of 1:1, 1:3, and 1:9. Colistin and ciprofloxacin were also co-sprayed with L-leucine in the mass ratio of 1:1:1. The phys. and aerosolization stability of the selected co-sprayed formulations stored at 20, 55, and 75% relative humidity (RH) were examined Formulation characterizations were carried out using powder X-ray diffraction (PXRD) for crystallinity, SEM for morphol. and particle size distribution, and dynamic vapor sorption for moisture sorption. Particle surface anal. was performed using XPS, energy dispersive X-ray spectrometry, and nano-time-of-flight secondary ion mass spectrometry. Potential intermol. interactions were studied using Fourier-transform IR spectroscopy (FTIR). Aerosol performance was evaluated using a multistage liquid impinger with a RS01 monodose inhaler device. PXRD diffractograms showed that the co-spray-dried colistin-ciprofloxacin formulation in the mass ratio (1:1) was amorphous at 55% RH for up to 60 days; whereas the co-spray-dried colistin-ciprofloxacin (1:3) and colistin-ciprofloxacin (1:9) crystallized after storage for 3 days at 55% RH. However, the extent of crystallization for the combination formulations was less as compared to the spray-dried ciprofloxacin alone formulation. Surface morphol. of the co-spray-dried formulations at different concentrations did not change even after storage at 55% RH for 60 days, unlike the spray-dried ciprofloxacin alone powder which became rougher after 3 days of storage at 55% RH. Surface anal. data indicated surface enrichment of colistin in the co-spray-dried formulations. Increasing colistin concentration on the composite particles surfaces improved aerosol performance of ciprofloxacin. FTIR data demonstrated intermol. interactions between colistin and ciprofloxacin, thereby delaying and/or preventing crystallization of ciprofloxacin when co-spray-dried. Co-spray drying ciprofloxacin with colistin in the mass ratio (1:1) completely prevented crystallization of ciprofloxacin at 55% RH for up to 60 days. However, the colistin-ciprofloxacin formulation (1:1) began to fuse when stored at 75% RH due to moisture absorption resulting in a compromised aerosol performance. In contrast, the colistin-ciprofloxacin-leucine (1:1:1) formulation demonstrated no particle fusion, enabling a stable aerosol performance at 75% RH for 7 days. This study demonstrated that incorporation of colistin in the spray-dried formulations can improve phys. stability and aerosolization of amorphous ciprofloxacin at 55% RH. At 75% RH, further addition of L-leucine in the formulation prevented particle fusion and deterioration in aerosol performance, attributed to the enrichment of nonhygroscopic L-leucine on the particle surface. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Related Products of 86393-32-0

The Article related to stability inhalant ciprofloxacin colistin powder synergy, aerosol performance, co-spray drying, dry powder inhaler, multidrug resistance, storage humidity, Pharmaceuticals: Formulation and Compounding and other aspects.Related Products of 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On September 30, 2019, Ling, Junhong; Mangal, Sharad; Park, Heejun; Wang, Shaoning; Cavallaro, Alex; Zhou, Qi Tony published an article.Related Products of 86393-32-0 The title of the article was Simultaneous Particle Size Reduction and Homogeneous Mixing to Produce Combinational Powder Formulations for Inhalation by the Single-Step Co-Jet Milling. And the article contained the following:

Homogeneous mixing of 2 cohesive jet-milled drug powders is a challenge for pharmaceutical manufacturing on account of their cohesive nature resulting in the formation of strong and random agglomerates. In this study, colistin and ciprofloxacin were co-jet milled to develop combinational antibiotic dry powder formulations for inhalation. The properties of particle size, morphol., content uniformity, and in vitro aerosolization were evaluated. The distribution of 2 drugs in the co-jet milled powders was assessed using time-of-flight-secondary ion mass spectrometry. The co-jet milled powders demonstrated an acceptable content uniformity indicating homogeneity. In general, time-of-flight-secondary ion mass spectrometry images showed relatively homogeneous distributions of ciprofloxacin and colistin in the co-milled formulations. Importantly, the 2 drugs generally had the similar fine particle fraction and deposition behavior in each combinational formulation supporting that the particle mixtures were relatively homogenous and could maximize the antimicrobial synergy. In conclusion, co-jet milling could be a viable technique to produce the combination powders for inhalation. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Related Products of 86393-32-0

The Article related to antibiotic ciprofloxacin colistin inhalation powder formulation jet milling, aerosol performance, dry powder inhaler, jet milling, mixing, uniformity, Pharmaceuticals: Formulation and Compounding and other aspects.Related Products of 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Puga, Ana M.; Rey-Rico, Ana; Magarinos, Beatriz; Alvarez-Lorenzo, Carmen; Concheiro, Angel published an article in 2012, the title of the article was Hot melt poly-ε-caprolactone/poloxamine implantable matrices for sustained delivery of ciprofloxacin.Application of 86393-32-0 And the article contains the following content:

It has been suggested that prevention and treatment of osteomyelitis could be achieved through local drug delivery using implantable devices, which provide therapeutic levels at the infection site with min. side-effects. Phys. blends of polycaprolactone (PCL) and poloxamine (Tetronic) were prepared by applying a solvent-free hot melting approach to obtain cytocompatible implants with a tunable bioerosion rate, ciprofloxacin release profile and osteoconductive features. Differential scanning calorimetry and X-ray anal. indicate that the hydrophilic poloxamine varieties T908, T1107, and T1307 are miscible with PCL, while the hydrophobic block copolymer T1301 is immiscible. Incorporation of the block copolymer at weight ratios ranging from 25 to 75 weight% led to matrixes with viscoelastic parameters in the range of those of fresh cortical bone. Once immersed in buffer the matrixes underwent a similar weight loss in the first week to the content of poloxamine, followed by a slower erosion rate due to PCL. The initial rapid erosion and the increase in porosity partially explain the observed burst of ciprofloxacin release, which is more intense in the PCL:T1301 formulation due to drug/T1301 repulsion due to polarity. The matrixes sustained ciprofloxacin release for several months (<50% released after 3 mo) and showed in vitro efficacy against Staphylococcus aureus, eradicating the bacteria in less than 48 h. PCL:poloxamine was cytocompatible with osteoblasts and the matrixes prepared with low proportions of T908 were also compatible with mesenchymal stem cell differentiation to osteoblasts. The influence of the nature and proportion of temperature-responsive poloxamine on the performance of PCL implantable systems was determined The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Application of 86393-32-0

The Article related to polycaprolactone tetronic dissolution hot melting ciprofloxacin hydrochloride monohydrate antibacterial, osteogenic sarcoma osteogenesis, Pharmaceuticals: Formulation and Compounding and other aspects.Application of 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Shahar, Or David; Kalousi, Alkmini; Eini, Lital; Fisher, Benoit; Weiss, Amelie; Darr, Jonatan; Mazina, Olga; Bramson, Shay; Kupiec, Martin; Eden, Amir; Meshorer, Eran; Mazin, Alexander V.; Brino, Laurent; Goldberg, Michal; Soutoglou, Evi published an article in 2014, the title of the article was A high-throughput chemical screen with FDA approved drugs reveals that the antihypertensive drug Spironolactone impairs cancer cell survival by inhibiting homology directed repair.HPLC of Formula: 86393-32-0 And the article contains the following content:

DNA double-strand breaks (DSBs) are the most severe type of DNA damage. DSBs are repaired by non-homologous end-joining or homol. directed repair (HDR). Identifying novel small mols. that affect HDR is of great importance both for research use and therapy. Mols. that elevate HDR may improve gene targeting, whereas inhibiting mols. can be used for chemotherapy, since some of the cancers are more sensitive to repair impairment. Here, the authors performed a high-throughput chem. screen for FDA approved drugs, which affect HDR in cancer cells. The authors found that HDR frequencies are increased by retinoic acid and Idoxuridine and reduced by the antihypertensive drug Spironolactone. The authors further revealed that Spironolactone impairs Rad51 foci formation, sensitizes cancer cells to DNA damaging agents, to Poly (ADP-ribose) polymerase (PARP) inhibitors and crosslinking agents and inhibits tumor growth in xenografts, in mice. This study suggests Spironolactone as a new candidate for chemotherapy. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).HPLC of Formula: 86393-32-0

The Article related to throughput screen antitumor neoplasm spironolactone homol directed repair, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.HPLC of Formula: 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Shahar, Or David; Kalousi, Alkmini; Eini, Lital; Fisher, Benoit; Weiss, Amelie; Darr, Jonatan; Mazina, Olga; Bramson, Shay; Kupiec, Martin; Eden, Amir; Meshorer, Eran; Mazin, Alexander V.; Brino, Laurent; Goldberg, Michal; Soutoglou, Evi published an article in 2014, the title of the article was A high-throughput chemical screen with FDA approved drugs reveals that the antihypertensive drug Spironolactone impairs cancer cell survival by inhibiting homology directed repair.HPLC of Formula: 86393-32-0 And the article contains the following content:

DNA double-strand breaks (DSBs) are the most severe type of DNA damage. DSBs are repaired by non-homologous end-joining or homol. directed repair (HDR). Identifying novel small mols. that affect HDR is of great importance both for research use and therapy. Mols. that elevate HDR may improve gene targeting, whereas inhibiting mols. can be used for chemotherapy, since some of the cancers are more sensitive to repair impairment. Here, the authors performed a high-throughput chem. screen for FDA approved drugs, which affect HDR in cancer cells. The authors found that HDR frequencies are increased by retinoic acid and Idoxuridine and reduced by the antihypertensive drug Spironolactone. The authors further revealed that Spironolactone impairs Rad51 foci formation, sensitizes cancer cells to DNA damaging agents, to Poly (ADP-ribose) polymerase (PARP) inhibitors and crosslinking agents and inhibits tumor growth in xenografts, in mice. This study suggests Spironolactone as a new candidate for chemotherapy. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).HPLC of Formula: 86393-32-0

The Article related to throughput screen antitumor neoplasm spironolactone homol directed repair, Pharmacology: Effects Of Neoplasm Inhibitors and Cytotoxic Agents and other aspects.HPLC of Formula: 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On November 30, 2011, He, Zhanwei; Liu, Guoguang; Liu, Haijin; Zhang, Nan; Wang, Gang published an article.Application of 86393-32-0 The title of the article was The effect of different nitrogen forms on the photo-degradation of ciprofloxacin in water. And the article contained the following:

This paper investigated the photo-degradation performance of Ciprofloxacin (CFX) under simulated solar irradiation and the effect of inorganic nitrogen in water. The results showed that the photo-degradation rate was decreased with the increase of initial concentration of CFX and dissolved oxygen. Nitrate accelerated the photo-degradation rate whereas nitrite inhibited it, and ammonium had few effects on it. Along with the increase of pE value, nitrogen form was changed from NH4+ to NO2- or NO3-, the photo-degradation rate of CFX was decreased at the beginning and increased afterwards. The experiments showed that there was no interaction between NH4+ and NO3-. When NO3- and NO2- coexisted, the photo-degradation rate of CFX was lower than the theoretic rate, which indicated that the facilitation of NO3- was inhibited because of the existence of NO2-. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Application of 86393-32-0

The Article related to effect nitrogen form photodegradation ciprofloxacin in water, Waste Treatment and Disposal: Chemical Treatment Of Aqueous Wastes and other aspects.Application of 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On October 31, 1994, Morissey, I.; Smith, J. T. published an article.Electric Literature of 86393-32-0 The title of the article was Activity of 4-quinolones against Pseudomonas aeruginosa. And the article contained the following:

The min. inhibitory concentrations (MICs), bactericidal activities and mechanisms of action of ofloxacin (CAS 82419-36-1), levofloxacin (CAS 100986-85-4) and ciprofloxacin (CAS 86393-32-0) were investigated against Pseudomonas aeruginosa. All three 4-quinolones were found to possess higher MICs against Pseudomonas aeruginosa than against other Gram-neg. bacteria. Despite this, however, all three drugs were more rapidly bactericidal and produced a greater level of kill against Pseudomonas aeruginosa than against any other bacterial species previously tested. Furthermore, MIC tests showed ciprofloxacin to be more potent than ofloxacin or levofloxacin against Pseudomonas aeruginosa. However, bactericidal tests showed levofloxacin to be about 10 times more bactericidal than either ciprofloxacin or ofloxacin. Thus, MIC tests cannot predict the relative bactericidal potency of 4-quinolones against Pseudomonas aeruginosa. Therefore, MIC tests should not be used as the sole measure for the efficacy of 4-quinolones, as is often the case. Surprisingly, the characteristic biphasic dose response curve, normally shown by 4-quinolones against other bacteria, was absent when Pseudomonas aeruginosa was tested. This unusual effect was explained by the presence of bactericidal mechanism A at high 4-quinolone concentrations This loss of bactericidal mechanism A may explain the recent high incidences of chromosomally mediated 4-quinolone resistance with Pseudomonas aeruginosa because it may be easier for Pseudomonas aeruginosa to mutate to resist one mechanism of action than to mutate to resist two or more mechanisms of action. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Electric Literature of 86393-32-0

The Article related to quinolone sensitivity pseudomonas, Microbial, Algal, and Fungal Biochemistry: Antimicrobial Sensitivity and other aspects.Electric Literature of 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On November 30, 2011, He, Zhanwei; Liu, Guoguang; Liu, Haijin; Zhang, Nan; Wang, Gang published an article.Application of 86393-32-0 The title of the article was The effect of different nitrogen forms on the photo-degradation of ciprofloxacin in water. And the article contained the following:

This paper investigated the photo-degradation performance of Ciprofloxacin (CFX) under simulated solar irradiation and the effect of inorganic nitrogen in water. The results showed that the photo-degradation rate was decreased with the increase of initial concentration of CFX and dissolved oxygen. Nitrate accelerated the photo-degradation rate whereas nitrite inhibited it, and ammonium had few effects on it. Along with the increase of pE value, nitrogen form was changed from NH4+ to NO2- or NO3-, the photo-degradation rate of CFX was decreased at the beginning and increased afterwards. The experiments showed that there was no interaction between NH4+ and NO3-. When NO3- and NO2- coexisted, the photo-degradation rate of CFX was lower than the theoretic rate, which indicated that the facilitation of NO3- was inhibited because of the existence of NO2-. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Application of 86393-32-0

The Article related to effect nitrogen form photodegradation ciprofloxacin in water, Waste Treatment and Disposal: Chemical Treatment Of Aqueous Wastes and other aspects.Application of 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On October 31, 1994, Morissey, I.; Smith, J. T. published an article.Electric Literature of 86393-32-0 The title of the article was Activity of 4-quinolones against Pseudomonas aeruginosa. And the article contained the following:

The min. inhibitory concentrations (MICs), bactericidal activities and mechanisms of action of ofloxacin (CAS 82419-36-1), levofloxacin (CAS 100986-85-4) and ciprofloxacin (CAS 86393-32-0) were investigated against Pseudomonas aeruginosa. All three 4-quinolones were found to possess higher MICs against Pseudomonas aeruginosa than against other Gram-neg. bacteria. Despite this, however, all three drugs were more rapidly bactericidal and produced a greater level of kill against Pseudomonas aeruginosa than against any other bacterial species previously tested. Furthermore, MIC tests showed ciprofloxacin to be more potent than ofloxacin or levofloxacin against Pseudomonas aeruginosa. However, bactericidal tests showed levofloxacin to be about 10 times more bactericidal than either ciprofloxacin or ofloxacin. Thus, MIC tests cannot predict the relative bactericidal potency of 4-quinolones against Pseudomonas aeruginosa. Therefore, MIC tests should not be used as the sole measure for the efficacy of 4-quinolones, as is often the case. Surprisingly, the characteristic biphasic dose response curve, normally shown by 4-quinolones against other bacteria, was absent when Pseudomonas aeruginosa was tested. This unusual effect was explained by the presence of bactericidal mechanism A at high 4-quinolone concentrations This loss of bactericidal mechanism A may explain the recent high incidences of chromosomally mediated 4-quinolone resistance with Pseudomonas aeruginosa because it may be easier for Pseudomonas aeruginosa to mutate to resist one mechanism of action than to mutate to resist two or more mechanisms of action. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Electric Literature of 86393-32-0

The Article related to quinolone sensitivity pseudomonas, Microbial, Algal, and Fungal Biochemistry: Antimicrobial Sensitivity and other aspects.Electric Literature of 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics