Rectal Absorption of Omeprazole from Suppository in Humans

Choi, Misook; Chung, Suk‐Jae; Shim, Chang‐Koo

doi:10.1021/js950375w

Cited by 21 publications

(25 citation statements)

References 9 publications

(7 reference statements)

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“…, 1996). In humans, no significant differences in the AUC of omeprazole were noted following oral and rectal administration suggesting that the bioavailability is similar between oral and rectal routes (Choi et al. , 1996).…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of intrarectal omeprazole in alpacas

Marmulak

Stanley

Kass

et al. 2010

Vet Pharm & Therapeutics

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The purpose of this study was to evaluate the pharmacokinetics of omeprazole in three different vehicles when administered rectally to six alpacas. Alpacas were given single doses of omeprazole (4 mg/kg) in a double-blinded, randomized cross-over design with a 1 week washout period. Omeprazole formulations consisted of (1) Treatment A: omeprazole paste mixed in surgical lubricant (2) Treatment B: omeprazole capsule contents in 8.4% sodium bicarbonate and (3) Treatment C: omeprazole capsule contents in surgical lubricant and 8.4% sodium bicarbonate solution. Plasma samples were drawn at 0, 5, 10, 15, 30, 45, 60, 90, 120, 180, 300 and 480 min. Omeprazole plasma concentrations were determined by high-pressure liquid chromatography-mass spectrometry. Pharmacokinetic results demonstrated median peak plasma concentrations (C(max)) of 7.35 (3.2-15.2), 7.30 (1.7-10.9) and 8.65 (1.8-19.3) ng/mL and median area under the concentration curve (AUC((0-180))) of 747 (237-1681) min x ng/mL, 552.9 (39-1063) min x ng/mL, and 972 (107-1841) min x ng/mL for treatments A, B and C, respectively. The median half-lives were similar between groups: 38, 50, and 53 min. As a result of the low measured omeprazole plasma concentrations, it is assumed that rectal absorption of omeprazole is poor in alpacas and not an effective route of administration.

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of intrarectal omeprazole in alpacas

Marmulak

Stanley

Kass

et al. 2010

Vet Pharm & Therapeutics

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“…The 4-h time period used in this study was reported to be an enough time of exposure for examining the effect of the drugs/complexes on gastric and rectal tissues. [25][26][27] The specimens embedded in paraffin using an embedding center and cut into slices. Then, the slices were stained with hematoxylin-eosin and observed under a light microscope (Leitz Laborlux 12 Pols; Ernst Leitz GmbH, Wetzlar, Germany).…”

Section: Histopathological Studymentioning

confidence: 99%

Preparation and investigation of acetyl salicylic acid-caffeine complex for rectal administration

Fouad¹,

El-Badry²,

Alanazi³

et al. 2010

Pharmaceutical Development and Technology

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An acetyl salicylic acid-caffeine complex was prepared and evaluated for the potential use in rectal administration. The results revealed the formation of a complex between acetyl salicylic acid and caffeine in a 1:1 molar ratio by a charge transfer mechanism. The effects of acetyl salicylic acid and complex on the rectal tissues showed destruction in the mucosal epithelium in case of acetyl salicylic acid; however, no change in the rectal tissues was noticed upon the administration of the complex. The effect of suppository bases on the release of the complex was studied using Witepsol H15 as fatty base and polyethylene glycols (PEG) 1000 and 4000 as a water soluble suppository base. The release profiles of acetyl salicylic acid and the complex were faster from PEG than from that of Witepsol H15. The percent release for the complex and acetyl salicylic acid from PEG base were 45.8, and 34.9%, respectively. However, it was 8.7 and 7.8%, respectively, from Witepsol H15 fatty base. The release kinetic was found to follow the non-Fickian diffusion model for complex from the suppository bases. It was concluded that acetyl salicylic acid caffeine complex can be used safely for rectal administration.

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“…[4][5][6] Due to its low bioavailability, short biological half life [7] and hepatic first pass metabolism, various oral formulation of OMZ such as enteric-coated granules [8,9] and tablets [10,11] have been developed with a subsequent 40% increase in oral bioavailability [12] of OMZ but have a wide individual variation of plasma concentration in human. [8][9][10][11] To overcome this problem, alternative dosage forms such as rectal suppository [13] and buccal adhesive tablets [14] were also developed. But all the dosage form of OMZ gives only systemic effect.…”

Section: Introductionmentioning

confidence: 99%

Antacids incorporation in immediate release tablets failed to improve the stability of omeprazole in acidic media

Chavda

Chaudhary

Patel

2011

J Pharm Negative Results

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Background:The stability of omeprazole (OMZ) decreases in acidic medium. In this investigation, attempts have been made to develop oral tablet containing antacids/buffers to increase the pH of dissolution media for certain time. Materials and Methods: Tablet formulations were prepared by the direct compression technique. For the selection of superdisintegrant, Croscarmellose sodium, used initially was replaced with other superdisintegrants. The prepared tablets were evaluated for hardness, weight variation, thickness, friability, drug content, disintegration time and in vitro drug release studies. During the in vitro drug release studies, the pH of dissolution media was measured. Results and Discussion: All batches showed very short disintegration time, within 0.5-2 min except F1 and S5. Batch F7 was able to provide the immediate drug release. The study showed that the incorporation of antacid improved the pH of dissolution media, but failed to maintain it. Even though the high quantities of antacids were incorporated; the stability of drug in media was not improved. Other superdisintegrants did not show any significant changes in drug release or disintegration time. Bath F7 was stable for the period of 6 months at 40 o C / 75 %RH. Conclusions: Incorporation of higher quantities of antacids failed to retain the stability of OMZ in acidic media.

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Rectal Absorption of Omeprazole from Suppository in Humans

Cited by 21 publications

References 9 publications

Pharmacokinetics of intrarectal omeprazole in alpacas

Pharmacokinetics of intrarectal omeprazole in alpacas

Preparation and investigation of acetyl salicylic acid-caffeine complex for rectal administration

Antacids incorporation in immediate release tablets failed to improve the stability of omeprazole in acidic media

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