Aqueous solubilities of some variously substituted quinolone antimicrobials

Ross, Danna L.; Riley, Christopher M.

doi:10.1016/0378-5173(90)90130-v

Cited by 275 publications

(144 citation statements)

References 10 publications

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“…Interestingly, as soon as the solutions containing chitosan were added to the suspensions of the poorly water-soluble ofloxacin, the antibiotic dissolved completely and rapidly. The solubility in aqueous media of fluoroquinolones is considerably increased by decreasing the pH from neutral to slightly acidic 9 . Indeed, Ross and Riley 9 have determined that lowering the pH from 7 to 5 increased the solubility of ofloxacin from 3.23 mg/mL to 95.4 mg/mL.…”

Section: Lachrymal Availability Of Tobramycin and Ofloxacinmentioning

confidence: 99%

“…The solubility in aqueous media of fluoroquinolones is considerably increased by decreasing the pH from neutral to slightly acidic 9 . Indeed, Ross and Riley 9 have determined that lowering the pH from 7 to 5 increased the solubility of ofloxacin from 3.23 mg/mL to 95.4 mg/mL. Therefore, it is proposed that this solubilization phenomenon is due to the fact that aqueous solutions of chitosan have a pH ranging from 5.5 to 6.5.…”

Section: Lachrymal Availability Of Tobramycin and Ofloxacinmentioning

confidence: 99%

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Delivery of antibiotics to the eye using a positively charged polysaccharide as vehicle

Felt

Gurny

Baeyens³

2001

AAPS PharmSci

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The positively charged polysaccharide chitosan is able to increase precorneal residence time of ophthalmic formulations containing active compounds when compared with simple aqueous solutions. The purpose of the study was to evaluate tear concentration of tobramycin and ofloxacin after topical application of chitosan-based formulations containing 0.3% wt/vol of antibiotic and to compare them with 2 commercial solutions: Tobrex® and Floxal®, respectively. The influence of the molecular weight, deacetylation degree, and concentration of 4 different samples of chitosan on pharmacokinetic parameters (area under the curve values [AUC eff ] and time of efficacy [t eff ]) of tobramycin and ofloxacin in tears was investigated over time. It was demonstrated that the 2 chitosan products of high molecular weight (1350 and 1930 kd) and low deacetylation degree (50%) significantly increased antibiotic availability when compared to the controls, with AUC eff showing a 2-to 3-fold improvement. The time of efficacy of ofloxacin was significantly increased from about 25 minutes to 46 minutes by the chitosan of higher Mw (1930 kd) at a concentration of 0.5% wt/vol, whereas a similar performance was achieved by a chitosan of low Mw (580 kd) at a concentration of 1.5% wt/vol in the case of tobramycin.

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Section: Lachrymal Availability Of Tobramycin and Ofloxacinmentioning

confidence: 99%

Section: Lachrymal Availability Of Tobramycin and Ofloxacinmentioning

confidence: 99%

Delivery of antibiotics to the eye using a positively charged polysaccharide as vehicle

Felt

Gurny

Baeyens³

2001

AAPS PharmSci

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“…Sufficiently sensitive computations tools are needed to fully interpret such complicated systems. Figure 1c shows the logS-pH profile of amifloxacin, an ampholyte which forms a hydrochloride salt below pH 5 [51]. The region of maximum solubility near pH 5 showed supersaturation effects, especially at equilibration times < 24 h. The data in the figure are based on 48 h equilibration time.…”

Section: Atorvastatinmentioning

confidence: 99%

Equilibrium solubility measurement of ionizable drugs – consensus recommendations for improving data quality

et al. 2016

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“…Ofloxacin is freely soluble in acetic acid, slightly soluble in water, methanol, ethanol or acetone. The octanol/water partition coefficient for ofloxacin was reported to be -0.48 [1,2] Ofloxacin which is the focus of this review is a second generation fluoroquinolone with a 6-fluoro substituent and a 7-piperazinyl substituent on the quinolone ring structure [11] Entrapped niosomes were prepared by hand shaking and ether injection process with different ratios of (1:1, 1:2 and 1:3) cholesterol and Span-80 (Non-ionic surfactant). The niosomes prepared were in the size of 0.5-2.5 microns in case of hand shaking process and 0.5-2.5 microns in case of Ether injection process.…”

Section: Related Workmentioning

confidence: 99%

To Study the Formulation of Niosome of Ofloxacin and Its Evaluation for Efficacy of Anti-Microbial Activity

Srivastav¹,

Das²

2014

IJIRSET

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Nanotechnology has offered enormous improvement in field of therapeutics by means of designing of nano-carriers that can cross biological barriers and are able to target cellular reservoirs. The aim of the present investigation was to formulate and evaluate Niosomes, a synthetic microscopic non-ionic surfactant vesicles formed on the admixture of a non-ionic surfactant, cholesterol and phosphate with subsequent hydration in aqueous media. The delivery of drugs by "vesicular drug delivery system" such as niosomes provides several important advantages over conventional drug therapy. Ofloxacin was selected as a suitable drug for the present study because it is a potent secondgeneration fluoroquinolone active against a broad range of gram positive and gram-negative aerobic and anaerobic bacteria. In the present investigation three formulations of Niosomal drug delivery system of ofloxacin with non ionic surfactant, span 60, in various proportions were prepared and evaluated for Morphological characterization, Encapsulation efficiency, In-vitro drug release study. The Ofloxacin niosomes were prepared by lipid film hydration method. The prepared ofloxacin niosomes showed a vesicle size of 100-300 nm, the entrapment efficiency was 78.4%. The partition coefficient value of ofloxacin was found to be 0.5.

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Aqueous solubilities of some variously substituted quinolone antimicrobials

Cited by 275 publications

References 10 publications

Delivery of antibiotics to the eye using a positively charged polysaccharide as vehicle

Delivery of antibiotics to the eye using a positively charged polysaccharide as vehicle

Equilibrium solubility measurement of ionizable drugs – consensus recommendations for improving data quality

To Study the Formulation of Niosome of Ofloxacin and Its Evaluation for Efficacy of Anti-Microbial Activity

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