Effect of food coadministration on 5-aminosalicylic acid oral suspension bioavailability

Yu, Dale K.; Elvin, Alfred T.; Morrill, Bruce; Eichmeier, Larry S.; Lanman, Robert C.; Lanman, M. B.; Giesing, Dennis H.

doi:10.1038/clpt.1990.113

Cited by 33 publications

(16 citation statements)

References 0 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Absorption of 5-ASA took place rapidly (t max Յ 0.5 h), showing the t max is shorter than the reported values of 1 h. 22 Plasma concentration of N-acetyl-5-ASA was higher than that of 5-ASA and elimination was nearly complete in 7 h (Fig. 3).…”

Section: Plasma Concentration Profiles After Oral Administration Of 5mentioning

confidence: 54%

Synthesis and In Vitro/In Vivo Evaluation of 5‐Aminosalicyl‐Glycine as a Colon‐Specific Prodrug of 5‐Aminosalicylic Acid

Jung

Lee

Kim

2000

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Section: Plasma Concentration Profiles After Oral Administration Of 5mentioning

confidence: 54%

Synthesis and In Vitro/In Vivo Evaluation of 5‐Aminosalicyl‐Glycine as a Colon‐Specific Prodrug of 5‐Aminosalicylic Acid

Jung

Lee

Kim

2000

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

“…Without sulfapyridine, the adverse reaction profile following 5-ASA treatment is supposed to be more acceptable. We previously described the pharmacokinetics of 5-ASA suspension [8]. This study demonstrated the need to develop a modified release oral formulation to provide adequate drug to the small and large intestines.…”

mentioning

confidence: 96%

Pharmacokinetics of 5-aminosalicylic acid from controlled-release capsules in man

Yu¹,

Morrill²,

Eichmeier³

et al. 1995

Eur J Clin Pharmacol

View full text Add to dashboard Cite

One gram single dose of Pentasa controlled-release capsules was administered to 24 healthy volunteers under fasting condition. Mean plasma 5-aminosalicylic acid (5-ASA) and acetyl 5-ASA concentrations peaked at 0.53 microgram.ml-1 and 1.33 micrograms.ml-1 from 3 to 4 hours following dosing, respectively. The half-lives of both compounds could not be determined as absorption of 5-ASA was continuous throughout the gastrointestinal tract. An average of 29.4% (CV: 27%) of the dose was excreted in the urine primarily as acetyl 5-ASA. Up to 91.1% of the dose was released from the capsules. Forty percent of the dose (CV: 40%) was eliminated in the feces, with 8.9% of the dose remained as formulation bounded 5-ASA, indicating that controlled-release capsules continue to release drug throughout the GI tract. 5-ASA contributed 46.7% of the salicylates eliminated in the feces and acetyl 5-ASA accounted for the balance. Controlled-release capsules produced three times more total salicylates and 10 times more total and free 5-ASA in the feces than did 5-ASA suspension. Thus, while lower systemic levels of salicylates were absorbed, greater therapeutic quantities of 5-ASA were available in the bowel.

show abstract

“…Mixing of drug and feed may, however, result in interactions affecting the bioavailability of the drug and thereby the possibilities of achieving therapeutically active concentrations at the site of the infection (Palmer et al 1983;Kniffen et al 1989). Furthermore, it can be assumed that the influence of feed present in the gastrointestinal tract on the absorption of orally administered drugs will not be the same for different drugs (Yu et al 1990;Baggot 1992;Sutter et al 1993). Previous studies with sulphadiazine and trimethoprim (Nielsen & Gyrd-Hansen 1994a) have shown that the bioavailability of these two compounds after oral administration to fasted pigs was 89% and 90%, respectively, versus 85% and 92% in the group of fed pigs.…”

mentioning

confidence: 99%

Bioavailability of Enrofloxacin after Oral Administration to Fed and Fasted Pigs

Nielsen

Gyrd‐Hansen

1997

Pharmacology & Toxicology

View full text Add to dashboard Cite

The disposition of enrofloxacin was measured after intravenous and oral administration to pigs. Eight clinically healthy pigs weighing 25 to 40 kg received a dose of 5 mg/kg intravenously and 10 mg/kg orally in both a fasted and a fed condition in a three-way cross-over design. Enrofloxacin was present in plasma for up to 72 hr after both intravenous and oral administration to fasted as well as fed pigs. The steady state volume of distribution was determined to 3.950.5 Vkg body weight which indicates that enrofloxacin was widely distributed in the body. The bioavailability was determined to 83213% in fed and to 101?32% in fasted pigs. Based on the bioavailability and the resulting plasma concentrations it is concluded that a therapeutically active concentration for the most common porcine microbial pathogens are maintained for at least 24 hr after oral administration of 10 mg/kg body weight to fasted as well as to fed pigs. Ciprofloxacin which is an active metabolite of enrofloxacin was observed in plasma samples from all treated pigs, but the concentration never exceeded 0.1 pg/ml. During the first 24 hr after the administration of enrofloxacin the concentration of the metabolite made up less than 10% of the corresponding concentration of the parent compound.Bacterial infections, especially in the respiratory and alimentary tract, are very common in pigs and most often have to be treated on a flock basis. Such treatment may include large numbers of pigs, and consequently, the most practical way of dosing the animals is by oral administration of an appropriate antimicrobial agent. Oral administration of drugs to pigs may be done either by mixing the drug with feed, or by dissolving it in the drinking water. In general, the former is preferred because it may be commercially available as medicated feed; not all drugs are watersoluble, and the feed may hide any unpleasant taste of the drug. Mixing of drug and feed may, however, result in interactions affecting the bioavailability of the drug and thereby the possibilities of achieving therapeutically active concentrations at the site of the infection (Palmer et al. 1983;Kniffen et al. 1989). Furthermore, it can be assumed that the influence of feed present in the gastrointestinal tract on the absorption of orally administered drugs will not be the same for different drugs (Yu et al. 1990;Baggot 1992;Sutter et al. 1993). Previous studies with sulphadiazine and trimethoprim (Nielsen & Gyrd-Hansen 1994a) have shown that the bioavailability of these two compounds after oral administration to fasted pigs was 89% and 90%, respectively, versus 85% and 92% in the group of fed pigs. Thus the bioavailability was not significantly influenced by the presence of feed in the gastrointestinal tract. For penicillin V the oral bioavailability was only 19% in fasted and 17% in (Nielsen & Gyrd-Hansen 1994b). In spite of the low bioavailability it was possible to obtain therapeutically active concentrations up to 6 hr after administration of 50 mg/kg body weight to fasted as...

show abstract

Effect of food coadministration on 5-aminosalicylic acid oral suspension bioavailability

Cited by 33 publications

References 0 publications

Synthesis and In Vitro/In Vivo Evaluation of 5‐Aminosalicyl‐Glycine as a Colon‐Specific Prodrug of 5‐Aminosalicylic Acid

Synthesis and In Vitro/In Vivo Evaluation of 5‐Aminosalicyl‐Glycine as a Colon‐Specific Prodrug of 5‐Aminosalicylic Acid

Pharmacokinetics of 5-aminosalicylic acid from controlled-release capsules in man

Bioavailability of Enrofloxacin after Oral Administration to Fed and Fasted Pigs

Contact Info

Product

Resources

About