Bioavailability and pharmacokinetics of cefoxitin sodium

Schrogie, John J.; Davies, Richard O.; Yeh, Kuang C.; Rogers, D. W. O.; Holmes, Geoffrey I; Skeggs, Helen R.; Martin, Christopher M.

doi:10.1093/jac/4.suppl_b.69

Cited by 48 publications

(26 citation statements)

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“…It is recommended that cefoxitin should be administered i.m. with lignocaine and although Schrogie et al (1978) have shown that concomitant lignocaine administration does not affect bioavailability, in the present study it was felt to be wiser not to add a possible interfering factor, thus the drug was administered on its own. For clinical use, however, dilution in lignocaine would seem appropriate.…”

mentioning

confidence: 60%

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Cefoxitin: intravenous pharmacokinetics and intramuscular bioavailability in kwashiorkor.

Buchanan¹,

Mithal²,

Witcomb³

1980

Brit J Clinical Pharma

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confidence: 60%

“…Intramuscular bioavailability of cefoxitin has been documented by Schrogie et al (1978), as being 95% in healthy volunteers. In the present study, it was found to be 123 + 72% in the acute phase of kwashiorkor and 109 + 11.6% on recovery; the reasons for high bioavailability values in this study are unclear.…”

mentioning

confidence: 99%

Cefoxitin: intravenous pharmacokinetics and intramuscular bioavailability in kwashiorkor.

Buchanan¹,

Mithal²,

Witcomb³

1980

Brit J Clinical Pharma

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“…The assay method was reproducible and specific for cefoxitin. Cefoxitin is only slightly metabolized under the dosing conditions described previously (17). The sensitivity was about 0.1 ,ug/ml.…”

mentioning

confidence: 78%

“…A high-pressure liquid chromatographic method was used to measure the levels of cefoxitin in serum and urine (2,14,17; Fix et al, in preparation). A C-18 Partisil column containing a 10-,um particle-sized reversed-phase system was used.…”

Section: Methodsmentioning

confidence: 99%

Use of adjuvants for enhancement of rectal absorption of cefoxitin in humans

Davis¹,

Burnham²,

Wilson³

et al. 1985

Antimicrob Agents Chemother

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The biological availability of cefoxitin administered rectally in the form of suppositories was examined in six human subjects by a cross-over design. Four different suppository systems containing adjuvants expected to enhance the absorption of the drug were studied. The presence of sodium salicylate and a nonionic surface-active agent, BriJ 35, gave increased bioavailability as high as 20% compared with 3% for a system without adjuvants. The quantity of sodium salicylate was found to have an influence on the quantity of cefoxitin absorbed, and the salicylate was absorbed over an extended period of time from the rectum. The suppositories were well tolerated, and there were no adverse effects on bowel flora.The rectal route of drug administration has certain advantages over the more popular oral route and can be especially useful in pediatric patients and in those with certain disease conditions, for example in patients with epilepsy and arthritis. The rectal mucosa may offer a more reliable and welldefined region for drug absorption than does the small intestine; in addition, the rectal administration of drugs may lead to a reduction in the initial metabolic destruction by the liver after absorption from the intestine (first-pass effect).Results of studies in animals (rats and more recently dogs) have shown that certain innocuous pharmaceutical adjuvants (namely, salicylates, benzoates, and related compounds) can lead to enhanced absorption of drugs, particularly those that are soluble in water, such as theophylline, lidocaine, levodopa, cephamycin antibiotics, gentamicin and penicillin G (3-14; J. Fix, L. J. Caldwell, J. Haslam, P. A. Porter, K. Engle, P. S. Leppert, R. Schaffer, L. Frost, A. Mlodozeniec, and T. Higuchi, manuscript in preparation).The adjuvant and drug need to be administered concurrently, and histological examinations have failed to reveal any adjuvant-induced changes in the mucosa (8). The mechanism of the adjuvant effect has not yet been fully elucidated but could involve the passage of drug molecules through the tight junctions of cells as well as possible involvement of the lymphatic system (8). The roles of calcium and magnesium, as well as ionic strength, have been discussed (3,14).The enhanced absorption for the cephamycin antibiotics cefmatozole and cefoxitin (13,14; Fix et al. in preparation) is particularly interesting because at present both agents are given by intravenous (i.v.) or intramuscular (i.m.) injection. A well-absorbed rectal formulation would be an advantage, particularly as a means of reducing muscle damage caused by repeated injections (14). This paper describes the evaluation of cefoxitin suppositories containing absorptionenhancing adjuvants in humans. rectally to humans by microenema and suppositories at concentrations up to 20% or as 0.5-g doses in suppositories (5,15,16). Brij 35 surfactants previously have been administered rectally to humans at low concentrations without adverse reactions (1). Higher concentrations of nonionic surfactants are known to cause his...

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“…Assuming linearity of cefoxitin elimination kinetics in the dose range used (Schrogie et al, 1978), cefoxitin bioavailability was calculated as AUCrect/AUCi.v., the subscripts rect and i.v. indicating rectal and i.v.…”

Section: Discussionmentioning

confidence: 99%

Rate‐controlled rectal absorption enhancement of cefoxitin by co‐ administration of sodium salicylate or sodium octanoate in healthy volunteers.

Hoogdalem

Wackwitz

Boer

et al. 1989

Brit J Clinical Pharma

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1 The effects of sodium octanoate and sodium salicylate on the rectal absorption of cefoxitin were investigated in healthy volunteers. Drug solutions were given either as a bolus or as a zero-order infusion. 2 On rectal infusion sodium octanoate and sodium salicylate both enhanced mean cefoxitin bioavailability (± s.d.) from 5.0 ± 1.2% to 9.1 ± 1.3% and 9.2 ± 1.5%, respectively. After rectal bolus delivery octanoate increased the mean cefoxitin bioavailability from 7 ± 3% to 17 ± 3%, whereas bolus salicylate did not produce a statistically significant effect. All formulations were well tolerated by the volunteers. 3 It is concluded that both octanoate and salicylate are capable of enhancing rectal cefoxitin absorption in man; rate of delivery seems to be an important factor.

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Bioavailability and pharmacokinetics of cefoxitin sodium

Cited by 48 publications

References 0 publications

Cefoxitin: intravenous pharmacokinetics and intramuscular bioavailability in kwashiorkor.

Cefoxitin: intravenous pharmacokinetics and intramuscular bioavailability in kwashiorkor.

Use of adjuvants for enhancement of rectal absorption of cefoxitin in humans

Rate‐controlled rectal absorption enhancement of cefoxitin by co‐ administration of sodium salicylate or sodium octanoate in healthy volunteers.

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