A DOUBLE-PEAK PHENOMENON IN THE PHARMACOKINETICS OF ACEBUTOLOL ENANTIOMERS AFTER ORAL ADMINISTRATION: DISCONTINUOUS ABSORPTION OF ACEBUTOLOL

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ABOLFAZL MOSTAFAVI S.; FOSTER R.T.

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Journal: DARU Journal of Pharmaceutical Sciences Year:2002 | Volume:10 | Issue:4 Page(s): 141-147

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Information Journal Paper

Title

A DOUBLE-PEAK PHENOMENON IN THE PHARMACOKINETICS OF ACEBUTOLOL ENANTIOMERS AFTER ORAL ADMINISTRATION: DISCONTINUOUS ABSORPTION OF ACEBUTOLOL

Author(s)

ABOLFAZL MOSTAFAVI S. | FOSTER R.T. | Issue Writer Certificate

Keywords

ACEBUTOLOL

PHARMACOKINETICS

ENANTIOMER

SITE DEPENDENT

DOUBLE PEAKS

Abstract

ACEBUTOLOL (AC) is a chiral l3-adrenergicblocking drug, which is used primarily in the treatment of hypertension. After oral administration of a racemic mixture of the drug a secondary peak is observed in plasma concentration-time profiles of both R and S-enantiomers of AC. In the present study the PHARMACOKINETICS of AC ENANTIOMERs in rats after intraduodenal (ID) and intraileal (11) administration was investigated to inspect the generation of DOUBLE PEAKS due to window absorption. Another possibility for the formation of double peak due to bile depletion in the gut lumen was investigated in male Sprague-Dawley rats. In a bile duct cannulated rat, the blood concentration-time profiles contained two peaks. The bioavailability after oral administration for R- and S-enantiomers of AC were 36% and 34% which increased to 47% and 46% following 11administration respectively. These values increased to 69% and 68% after ID administration. While following 11administration of the racemate, the double peak disappeared, it retained after ID administration. These results suggest that the double peak phenomenon observed after oral administration of AC is due to SITE DEPENDENT absorption of the drug.

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APA: Copy

ABOLFAZL MOSTAFAVI, S., & FOSTER, R.T.. (2002). A DOUBLE-PEAK PHENOMENON IN THE PHARMACOKINETICS OF ACEBUTOLOL ENANTIOMERS AFTER ORAL ADMINISTRATION: DISCONTINUOUS ABSORPTION OF ACEBUTOLOL. DARU JOURNAL OF PHARMACEUTICAL SCIENCE, 10(4), 141-147. SID. https://sid.ir/paper/275268/en

Vancouver: Copy

ABOLFAZL MOSTAFAVI S., FOSTER R.T.. A DOUBLE-PEAK PHENOMENON IN THE PHARMACOKINETICS OF ACEBUTOLOL ENANTIOMERS AFTER ORAL ADMINISTRATION: DISCONTINUOUS ABSORPTION OF ACEBUTOLOL. DARU JOURNAL OF PHARMACEUTICAL SCIENCE[Internet]. 2002;10(4):141-147. Available from: https://sid.ir/paper/275268/en

IEEE: Copy

S. ABOLFAZL MOSTAFAVI, and R.T. FOSTER, “A DOUBLE-PEAK PHENOMENON IN THE PHARMACOKINETICS OF ACEBUTOLOL ENANTIOMERS AFTER ORAL ADMINISTRATION: DISCONTINUOUS ABSORPTION OF ACEBUTOLOL,” DARU JOURNAL OF PHARMACEUTICAL SCIENCE, vol. 10, no. 4, pp. 141–147, 2002, [Online]. Available: https://sid.ir/paper/275268/en

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