Apparent Absorption Kinetics of Micronized Griseofulvin after Its Oral Administration on Single‐ and Multiple‐Dose Regimens to Rats as a Corn Oil‐in‐Water Emulsion and Aqueous Suspension

Bates, Theodore R.; Carrigan, Philip J.

doi:10.1002/jps.2600640910

Cited by 40 publications

(21 citation statements)

References 14 publications

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“…Although the absorption phase of our data was best fit by a zero-order equation, it may be events leading up to the absorption step which are rate limiting, thus forcing the absorption to appear to be zero order. The gastrointestinal absorption data for other antibiotics, including sulfisoxazole, griseofulvin, and erythromycin, have been described by a zero-order process and were likely due to dissolution problems (2,4,9). However, we have no evidence to suggest that ciprofloxacin has dissolution problems because peak serum concentrations were attained rapidly and were consistent.…”

Section: Discussionmentioning

confidence: 72%

Pharmacokinetics and tolerance of ciprofloxacin after sequential increasing oral doses

Tartaglione¹,

Raffalovich²,

Poynor³

et al. 1986

Antimicrob Agents Chemother

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The pharmacokinetics and safety of orally administered ciprofloxacin (Bay o 9867) were examined in 12 healthy male volunteers who received sequential doses of 250, 500, 750, and 1,000 mg. The individual and mean data were best described by biexponential disposition and elimination, assuming an apparent zero-order rate of absorption. The peak serum concentrations deterrmined from the individual data occurred at approximately 1.5 h after each dose and ranged from 0.42 to 4.2 ,ug/ml; the mean peak concentrations increased in proportion to the dose. The areas under the curve determined from the mean data were also proportional with respect to dose. The mean elimination half-lives calculated from pooled data were 4.1, 4.1, 6.9, and 6.3 h for doses of 250, 500, 750, and 1,000 mg, respectively. Longer half-lives but proportional area-under-the-curve values after the 750-and 1,000-mg doses implied that smaller fractions of ciprofloxacin were absorbed after these doses, although nonlinear kinetics could not be ruled out. The mean serum concentrations 12 and 24 h following each dose were -0.08 and 0.01 ,ug/ml, respectively. The urinary concentrations ranged from 30 to 500 ,ug/ml for at least 12 h after administration and were -9 ,ug/ml at 24 h following each dose. The urinary recovery level of unchanged ciprofloxacin over a 24-h period ranged from 28 to 44%. The mean renal clearances for each dose ranged from 300 to 500 ml/min. Ciprofloxacin was well tolerated, and no significant clinical or laboratory abnormalities were observed.Ciprofloxacin (Bay o 9867), a new quinolone derivative that is chemically related to nalidixic acid and norfloxacin, is currently undergoing microbiologic, pharmacokinetic, and clinical evaluation. The MICs of ciprofloxacin for 90% of the Enterobacteriaceae, Pseuidomnonas aeruiiginiosa, Hatemophiluis influenzae, Staphylococcus aureiis (including methicillin-resistant S. aiureuts), streptococcal, and Btacteroidesfragilis strains which have been tested including strains resistant to gentamicin and many third gei eration cephalosporins, range from 0.008 to 2.0 jig/ml (3,6,13).Ciprofloxacin was originally developed as an oral agent similar to nalidixic acid for the treatment of urinary tract infections. However, due to its excellent activity against gram-negative bacteria, development of a parenteral product is currently underway for use in the treatment of systemic bacterial infections. The purpose of this study was to determine the pharmacokinetic disposition and tolerance of orally administered ciprofloxacin in healthy volunteers after sequential increasing doses. MATERIALS AND METHODSSixteen healthy males (ages 22 to 26 years) were randomly selected to receive either ciprofloxacin (12 subjects) or a placebo (4 subjects). Before the study and before each of the four weekly doses, all of the subjects underwent physical examinations, including electrocardiograms, complete blood counts, platelet counts, a panel of 20 serum chemistry tests, urinalysis, and a stool test for occult blood. Another examin...

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Section: Discussionmentioning

confidence: 72%

Pharmacokinetics and tolerance of ciprofloxacin after sequential increasing oral doses

Tartaglione¹,

Raffalovich²,

Poynor³

et al. 1986

Antimicrob Agents Chemother

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“…In our study, rats received about 1.5 times less oil than in the study of Bates and Carrigan (1975). For the same ratio of emulsified lipids ingested with griseofulvin in man, it was shown that the bioavailability was better when the amount of lipids ingested was higher (Bates et al 1977).…”

Section: Influence Of the Formulation On Absorption Of Griseofulvinmentioning

confidence: 46%

“…One pharmacokinetic study was performed on each rat because of a decrease of the bioavailability of griseofulvin after repeated administration (Bates and Carrigan 1975;SchaferKorting 1993).…”

Section: Rat Experimentationmentioning

confidence: 99%

“…Several studies showed that the incorporation of drugs administered orally in o/w emul-sion significantly increased the bioavailability compared with the equivalent aqueous suspension (Kakemi et al 1972a, b;Bates and Carrigan 1975;Bates and Sequeira 1975;Kimura et al 1989;Kararli et al 1992), the oily suspension (Carrigan and Bates 1973), or the oily solution (Wagner, Gerard, and Kaiser 1966;Toguchi, Ogawa, and Shimamoto 1990).…”

Section: Introductionmentioning

confidence: 99%

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Effect of Oil-in-Water Submicron Emulsion Surface Charge on Oral Absorption of a Poorly Water-Soluble Drug in Rats

et al. 2008

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The effect of oil-in-water submicron emulsion (SE) droplet surface charge on absolute bioavailability of a poorly watersoluble drug (griseofulvin, as model drug) after oral administration was studied in conscious rat. Positively, negatively, and neutrally charged SE were designed and characterized (size, polydispersity index, zeta potential, and pH). Three emulsion formulations, whose compositions included 40% oil phase and differed only in the nature of the emulsifying agent, were retained. Only the positively charged SE showed a higher area under the plasma concentrationtime curve (AUC 0→∞ ) in comparison with the tablet and with the other SE.

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“…In addition, it improves the thermal stability, water solubility and oral bioavailability of functional compounds (McClements et al, 2009) Nano emulsions derived from the natural hydrocolloids act as colloidal drug carriers for pharmaceutical applications. Due to best internal absorption, the bioavailability of less water soluble drugs increases even though it passes through oral way (Constantinides, 1995; Bates et al, 1975).Absorption in the gastrointestinal tract is improved by a small droplet size also been found (Toguchi et al, 1990). Recently, more preferences have been given for the use of many natural hydrocolloids as drug delivery carriers in the bio-pharmaceutical sector (Ogaji et al, 2012).…”

Section: Introductionmentioning

confidence: 99%

Interaction of Semi-Refined Carrageenan (E407a) With Nano Quanta of Some Food Hydrocolloids and Their Physiochemical, Functional and Rheological Properties

Marimuthu¹,

Ilansuriyan²,

Yap³

et al. 2017

J microb biotech food sci

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Interaction of semi-refined carrageenan with other food hydrocolloids in different ratio and their rheological, physicochemical and some functional characteristics were evaluated in the present study. Gel strength and viscous synergism index (Iv) were measured and used to analyze their interaction level. Kappa carrageenan had good synergistic effect with cassia, LBG, guar, HPMC and konjac and antagonistic effect with xanthan, alginate, CMC and agar. Only Iota carrageenan in the range of 60:40 with kappa showed neutral effect. A blend of SRC with konjac / LBG can be made for good gel strength whereas konjac / GG for good viscosity. Therefore, SRC can be used in place of refined carrageenan in some food applications.

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Apparent Absorption Kinetics of Micronized Griseofulvin after Its Oral Administration on Single‐ and Multiple‐Dose Regimens to Rats as a Corn Oil‐in‐Water Emulsion and Aqueous Suspension

Cited by 40 publications

References 14 publications

Pharmacokinetics and tolerance of ciprofloxacin after sequential increasing oral doses

Pharmacokinetics and tolerance of ciprofloxacin after sequential increasing oral doses

Effect of Oil-in-Water Submicron Emulsion Surface Charge on Oral Absorption of a Poorly Water-Soluble Drug in Rats

Interaction of Semi-Refined Carrageenan (E407a) With Nano Quanta of Some Food Hydrocolloids and Their Physiochemical, Functional and Rheological Properties

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