Ofloxacin: Its Pharmacology, Pharmacokinetics, and Potential for Clinical Application

Drew, Richard H.; Gallis, Harry A.

doi:10.1002/j.1875-9114.1988.tb04063.x

Cited by 50 publications

(32 citation statements)

References 61 publications

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“…The presence of the methyl piperazine ring in ofloxacin probably leads to enhanced oral absorption and a long half-life (properties shown by other quinolones such as pefloxacin, fleroxacin, and difloxacin). Pharmacokinetic disposition and bioavailability have been previously studied in different study populations, and the bioavailability of ofloxacin has been reported to be 80 to 90% (1,2,4,5,7). There is a paucity of data, however, directly comparing oral (p.o.)…”

mentioning

confidence: 99%

Bioavailability and pharmacokinetics of ofloxacin in healthy volunteers

Yuk

Nightingale

Quintiliani

et al. 1991

Antimicrob Agents Chemother

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The pharmacokinetics and bioavailabiity of ofloxacin in 20 healthy male volunteers were studied in an open-label, randomized, two-way crossover study. Ofloxacin (400 mg) was administered either as a 1-h infusion or as an oral tablet. The mean peak concentration after intravenous infusion was 4.30 0.69 ,ug/ml, and that after oral administration was 3.14 ± 0.53 ,ug/mI, occurring 1.74 + 0.57 h after dosing. The bioavailability (F) of the oral dosage form of ofloxacin was virtuaUy identical to that of the intravenous form (F = 105% 7%). This complete bioavailability of ofloxacin is supportive of the use of the oral dosage form for the treatment of infections in hospitalized patients either as a replacement for intravenous ofloxacin therapy or in streamlining therapy from the intravenous to the oral route.Ofloxacin is a synthetic, fluorinated carboxyquinolone active against members of the family Enterobactericeae and gram-positive organisms. Its favorable pharmacokinetic features include good oral absorption and lack of metabolism resulting in decreased drug interaction. The presence of the methyl piperazine ring in ofloxacin probably leads to enhanced oral absorption and a long half-life (properties shown by other quinolones such as pefloxacin, fleroxacin, and difloxacin). Pharmacokinetic disposition and bioavailability have been previously studied in different study populations, and the bioavailability of ofloxacin has been reported to be 80 to 90% (1, 2, 4, 5, 7). There is a paucity of data, however, directly comparing oral (p.o.) and intravenous (i.v.) dosage forms in the same population. The present study was undertaken to evaluate the bioavailabilities of orally and parenterally administered ofloxacin in normal volunteers. An accurate determination of bioavailability is necessary for considering the use of oral ofloxacin in place of the parenteral form in the treatment of hospitalized patients.On the basis of laboratory tests (serum chemistry, hematology, urinalysis), medical history, and physical examination, 20 healthy male volunteers (age, 25 ± 4.6 years; weight, 74.5 ± 7.87 kg; height, 178.3 ± 5.92 cm [mean ± standard deviation]) were enrolled in this study after giving written informed consent. No alcohol or concomitant medication was allowed 72 h prior to the initial administration of the dose and for the entire duration of the study. All subjects reported to the study site at least 12 h prior to the administration of the initial dose, remained within the facility for 36 h after each dose, and returned to the study site for the 48-h scheduled blood draw. Subjects were dosed in the mornings of day 1 and day 8. Subjects fasted at least 8 h prior to each dose and remained fasted for 2 h postdose. Water was permitted ad lib until 2 h prior to and 2 h after dosing. Tablets containing 400 mg of ofloxacin (FD 18489-BS-22) and 10-ml single-dose vials containing 400 mg of ofloxacin (FD 18489-* Corresponding author. BR-45) for parenteral use were provided by Ortho Pharmaceutical Corporation.The tablets were admin...

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mentioning

confidence: 99%

Bioavailability and pharmacokinetics of ofloxacin in healthy volunteers

Yuk

Nightingale

Quintiliani

et al. 1991

Antimicrob Agents Chemother

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“…3 The proposed method was used to analyze azithromycin added to human urine. The samples were spiked at three concentration levels and the drug was determined by means of the standard addition method.…”

Section: Determination Of Azithromycin In Urinementioning

confidence: 99%

“…The remainder is excreted mainly as the parent substance unchanged in urine. 3 The most commonly employed techniques for the determination of azithromycin in biological matrixes have been based on HPLC using electrochemical detection. 4,5 Assays reported in the literature for the measurements of the drug in pharmaceutical dosage forms include HPLC, 6,7 LC-MS, 8 and microbiological methods.…”

Section: Introductionmentioning

confidence: 99%

Adsorptive Stripping Voltammetric Determination of Azithromycin at a Glassy Carbon Electrode Modified by Electrochemical Oxidation

Nigović

2004

ANAL. SCI.

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“…Another important structural characteristic is the presence of other sugar moiety containing a dimethylamine group, which confers to the macrolides a basic behavior 2 and makes them a potential n-electron donating substances. One of the most important members of this class is the azithromycin (Figure 1), which has been used as antibiotic in the human medicine for the treatment or prophylaxis of a number of health problems such as ear, lung, skin, and throat infections, 3,4 veneral disease, 5 pneumonia, 6 toxoplasmosis 7 and opportunistic diseases in patients with AIDS. 8 Several analytical methods can be found in the literature for the azithromycin determination in different kinds of samples.…”

Section: Introductionmentioning

confidence: 99%

Novel spectrophotometric method for the determination of azithromycin in pharmaceutical formulations based on its charge transfer reaction with quinalizarin

Paula¹,

Almeida²,

Cassella³

2010

J. Braz. Chem. Soc.

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Neste trabalho é proposto um novo método para a determinação espectrofotométrica simples e rápida de azitromicina em formulações farmacêuticas. O método está baseado na reação de transferência de carga entre a azitromicina e a quinalizarina em meio de metanol. O efeito de diversas variáveis foi avaliado com o intuito de alcançar máxima sensibilidade analítica. A reação de transferência de carga foi caracterizada, sendo determinadas a estequiometria da reação, a absortividade molar aparente e a constante de associação. Melhores resultados foram obtidos em meio de metanol e com uma concentração de quinalizarina de 50 mg L -1 . Nestas condições, o ânion radicalar (produto da reação de transferência de carga) foi formado imediatamente após a mistura dos reagentes, apresentando máxima absorção em 564 nm. O método apresentou um limite de detecção de 0,35 mg L -1 e um limite de quantificação de 1,2 mg L -1 , sendo aplicado com sucesso na determinação de azitromicina em três amostras de medicamentos comerciais contendo azitromicina. This paper proposes a new method for simple and fast spectrophotometric determination of azithromycin in pharmaceutical formulations. The method is based on the charge transfer reaction between the azithromycin and quinalizarin in methanol medium. In order to achieve maximum sensitivity the effect of some chemical variables such as the type of solvent, reagent concentration and reaction time were evaluated. The reaction was characterized in terms of stability of the product formed and its stoichiometry, and the apparent molar absorptivity and association constant were derived. Best conditions for the analytical determination of azithromycin were observed in methanol medium with a quinalizarin concentration of 50 mg L -1 . At these conditions, the radical anion (absorbing specie) was formed in the medium immediately after mixing of the reagents and showed maximum absorption at 564 nm. The method presented a limit of detection of 0.35 mg L -1 and a limit of quantification of 1.2 mg L -1 . It was successfully applied in the determination of azithromycin in three commercial pharmaceutical formulations of azithromycin and no matrix interferences were observed.

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Ofloxacin: Its Pharmacology, Pharmacokinetics, and Potential for Clinical Application

Cited by 50 publications

References 61 publications

Bioavailability and pharmacokinetics of ofloxacin in healthy volunteers

Bioavailability and pharmacokinetics of ofloxacin in healthy volunteers

Adsorptive Stripping Voltammetric Determination of Azithromycin at a Glassy Carbon Electrode Modified by Electrochemical Oxidation

Novel spectrophotometric method for the determination of azithromycin in pharmaceutical formulations based on its charge transfer reaction with quinalizarin

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