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Rapid CommunicationShort Communication

Pharmacokinetics of Aminolevulinic Acid after Oral and Intravenous Administration in Dogs

James Meyer, Marvin C. Meyer and Allyn L. Golub
Drug Metabolism and Disposition April 1999, 27 (4) 432-435;
James Meyer
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Marvin C. Meyer
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Allyn L. Golub
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Abstract

The purpose of these studies was to examine the pharmacokinetics, oral bioavailability, and systemic side effects of aminolevulinic acid (ALA) in beagle dogs after oral and i.v. administration. Oral and i.v. doses of ALA (128 mg of ALA hydrochloride, equivalent to 100 mg of ALA) were administered to four animals using a crossover design. Animals were allowed a 2-week washout period between doses. Plasma ALA concentrations were determined using precolumn fluorescent derivatization and reversed-phase HPLC. Plasma concentrations after i.v. administration declined rapidly with a terminal half-life of 19.5 ± 2.5 min (mean ± S.D.). Total body clearance and volume of distribution at steady state averaged 6.79 ± 1.77 ml/min/kg and 259 ± 128 ml/kg, respectively. Peak plasma concentrations of ALA after oral administration ranged from 1.27 to 9.42 μg/ml. Oral bioavailability in these animals averaged 41.2 ± 14.8% (range, 23.5–58.5%). These studies demonstrate that oral administration may provide a convenient and efficient route of delivery of ALA for photodynamic therapy in patients.

Footnotes

  • Send reprint requests to: James T. Dalton, Ph.D., Department of Pharmaceutical Sciences, University of Tennessee, Memphis, 874 Union Avenue, Crowe Building, Room 5, Memphis, TN 38163. E-mail: jdalton{at}utmem1.utmem.edu

  • These studies were supported by a grant from DUSA Pharmaceuticals, Inc. (Valhalla, NY).

  • Abbreviations used are::
    PDT
    photodynamic therapy
    ALA
    aminolevulinic acid
    PpIX
    protoporphyrin IX
    Tmax
    time to reach maximum plasma concentration
    Vdss
    volume of distribution at steady state
    CL
    total plasma clearance
    AUC
    area under the plasma concentration-time curve
    • Received September 8, 1998.
    • Accepted December 18, 1998.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 27 (4)
Drug Metabolism and Disposition
Vol. 27, Issue 4
1 Apr 1999
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Rapid CommunicationShort Communication

Pharmacokinetics of Aminolevulinic Acid after Oral and Intravenous Administration in Dogs

James Meyer, Marvin C. Meyer and Allyn L. Golub
Drug Metabolism and Disposition April 1, 1999, 27 (4) 432-435;

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Rapid CommunicationShort Communication

Pharmacokinetics of Aminolevulinic Acid after Oral and Intravenous Administration in Dogs

James Meyer, Marvin C. Meyer and Allyn L. Golub
Drug Metabolism and Disposition April 1, 1999, 27 (4) 432-435;
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