Excipient effects on gastrointestinal transit and drug absorption in beagle dogs

Schulze, Julia D. R.; Peters, Erin E.; Vickers, Ann; Staton, John; Coffin, Mark D.; Parsons, Gary E.; Basit, Abdul W.

doi:10.1016/j.ijpharm.2005.05.004

Cited by 45 publications

(19 citation statements)

References 28 publications

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“…PEG 400 is osmotically active and will "hold" fluid in the lumen of the intestine, leading to an increase in bulk fluid volume, which in turn stimulates peristalsis and hence transit. No such effects on transit have been noted with other commonly used solubility enhancing excipients such as propylene glycol, vitamin E-TPGS, Labrasol and Capmul MCM in man or dog (5,6).…”

Section: Introductionmentioning

confidence: 97%

Polyethylene Glycol 400 Enhances the Bioavailability of a BCS Class III Drug (Ranitidine) in Male Subjects but Not Females

2008

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All doses of PEG 400 enhanced the bioavailability of ranitidine in male subjects but not females, with the most pronounced effect in males noted with the 0.75 g dose of PEG 400 (63% increase in bioavailability compared to control, p < 0.05). These findings have significant implications for the use of PEG 400 in drug development and also highlight the importance of gender studies in pharmacokinetics.

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Section: Introductionmentioning

confidence: 97%

Polyethylene Glycol 400 Enhances the Bioavailability of a BCS Class III Drug (Ranitidine) in Male Subjects but Not Females

2008

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“…Recent studies showed that the absorption of rifampicin in the jejunum and the ileum was restricted by a P-gp-mediated efflux mechanism (Mariappan and Singh, 2004). Therefore, intestinal absorption of rifam- (Schulze et al, 2005).…”

Section: Introductionmentioning

confidence: 99%

Effects of Pluronic F68 and Labrasol on the intestinal absorption and pharmacokinetics of rifampicin in rats

Wei

Zhou

et al. 2011

Arch. Pharm. Res.

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The aim of this study was to investigate the effects of Pluronic F68 and Labrasol on the intestinal absorption and pharmacokinetics of rifampicin. Intestinal permeability of rifampicin with or without excipients was evaluated by an in situ single-pass perfusion method. A high-performance liquid chromatographic method was applied to study the pharmacokinetics of rifampicin with or without excipients. Labrasol or Pluronic F68 (0.1% and 0.05%, v/v), co-perfused with rifampicin (60 μg/mL), significantly increased in situ permeability. Similarly, verapamil (a typical P-gp inhibitor) also increased in situ permeability, but to a lesser extent. In vivo, the oral administration of rifampicin with or without Pluronic F68, Labrasol or verapamil resulted in statistically significant effect on t(1/2) (4.83 to 7.75, 6.42 and 7.46 h) and total body clearance (0.46 to 0.26, 0.28, 0.24 L/h/kg). In addition, Pluronic F68, Labrasol and verapamil produced minor changes in AUC(0-t), which improved 1.55-, 1.54-, and 1.73-fold in comparison to control group, respectively. These results showed that Labrasol and Pluronic F68 might inhibit the function of P-gp in the intestine, thereby increasing intestinal absorption and changing the pharmacokinetic parameters of rifampicin. Therefore, excipient selection is an important factor to consider in rational formulation design.

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“…Gamma scintigraphy is a long established technique for non-invasive monitoring of dosages in vivo (20), and its use in the dog has been previously reported for gastrointestinal formulation studies (21)(22)(23). The use of pharmacoscintigraphy to evaluate the clearance of a buprenorphine sublingual spray dose was therefore investigated, with the intention of obtaining information, which could aid in interpretation of pharmacokinetic data obtained from such sublingual studies.…”

Section: Introductionmentioning

confidence: 99%

Evaluation of the Clearance of a Sublingual Buprenorphine Spray in the Beagle Dog Using Gamma Scintigraphy

et al. 2007

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Excipient effects on gastrointestinal transit and drug absorption in beagle dogs

Cited by 45 publications

References 28 publications

Polyethylene Glycol 400 Enhances the Bioavailability of a BCS Class III Drug (Ranitidine) in Male Subjects but Not Females

Polyethylene Glycol 400 Enhances the Bioavailability of a BCS Class III Drug (Ranitidine) in Male Subjects but Not Females

Effects of Pluronic F68 and Labrasol on the intestinal absorption and pharmacokinetics of rifampicin in rats

Evaluation of the Clearance of a Sublingual Buprenorphine Spray in the Beagle Dog Using Gamma Scintigraphy

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