[Isomerisation and Bioavailability of Beta- and Alpha-acetyldigoxin (author's Transl)]

Overview

Journal Klin Wochenschr

Specialty General Medicine

Date 1977 Jul 1

PMID 895002

Authors

N Rietbrock

H F Vohringer

J Kuhlmann

K Maertin

Affiliations

Soon will be listed here.

Abstract

Bioavailability of acetylated derivatives of digoxin tablets have been studied in healthy subjects after a single oral and intravenous dose as well as during maintenance therapy. alpha-acetyldigoxin shows a lower bioavailability than beta-acetyldigoxin even if the alpha-acetylated derivative is incorporated in a matrix of aerosil (SiO2). Moreover, beta-acetyldigoxin can be transferred to alpha-acetyldigoxin in alkaline solutions. This isomerisation leads to a decrease of the bioavailability of such fixed preparations which contain beta-acetyldigoxin and the hygroscopic salts of potassium-magnesium-aspartate. A prevention of the isomerisation is attained by isolating beta-acetyldigoxin from potassium-magnesium-aspartate. The bioavailability of a such new formulation is comparable to that of beta-acetyldigoxin alone. The experiments show the bioavailability of acetylated derivatives of digoxin to be influenced by the physico-chemical properties of a drug and its preparation.

References

Rietbrock N . [Therapeutic equivalence and inequivalence of chemically identical substances using cardiac glycosides for an example (author's transpl)]. Arzneimittelforschung. 1976; 26(1A):135-46. View

Kuhlmann J, Abshagen U, Rietbrock N . Cleavage of glycosidic bonds of digoxin and derivatives as function of pH and time. Naunyn Schmiedebergs Arch Pharmacol. 1973; 276(2):149-56. DOI: 10.1007/BF00501187. View

Rietbrock N, Abshagen U . [Metabolism and pharmacokinetics of lanatosides in man]. Dtsch Med Wochenschr. 1973; 98(3):117-22. DOI: 10.1055/s-0028-1106760. View

Mallis G, Schmidt D, Lindenbaum J . Superior bioavailability of digoxin solution in capsules. Clin Pharmacol Ther. 1975; 18(6):761-8. DOI: 10.1002/cpt1975186761. View

Larbig D, Kochsiek K . [Determination of serum-digoxin concentrations by radioimmunoassay]. Klin Wochenschr. 1971; 49(18):1031-2. DOI: 10.1007/BF01487735. View

Flasch H . [Bioavailability of beta-acetyldigoxin and digoxin (author's transl)]. Klin Wochenschr. 1975; 53(18):873-7. DOI: 10.1007/BF01466961. View

Shaw T, CARLESS J, Howard M, Raymond K . Particle size and absorption of digoxin. Lancet. 1973; 2(7822):209-10. DOI: 10.1016/s0140-6736(73)93049-3. View

Ochs H, BODEM G, DENGLER H . [Bioavailability of digoxin in fixed combinations (author's transl)]. Klin Wochenschr. 1974; 52(13):637-9. DOI: 10.1007/BF01468799. View

Jounela A, Pentikainen P, Sothmann A . Effect of particle size on the bioavailability of digoxin. Eur J Clin Pharmacol. 1975; 8(5):365-70. DOI: 10.1007/BF00562664. View

10.

Maertin K, Rietbrock N . [Radioimmunological estimation of digoxin in urine (author's transl)]. Klin Wochenschr. 1977; 55(9):429-38. DOI: 10.1007/BF01488580. View

11.

Jounela A, Sothmann A . Bioavailability of digoxin. Lancet. 1973; 1(7796):202-3. DOI: 10.1016/s0140-6736(73)90032-9. View

12.

Kaiser F, Schaumann W . [Metabolism of helveticoside and helveticosol derivatives]. Naunyn Schmiedebergs Arch Exp Pathol Pharmakol. 1969; 262(1):87-96. View

13.

Rietbrock N, Kuhlmann J . Isomerisation of beta-acetyldigoxin in a buffered alkaline solution. Naunyn Schmiedebergs Arch Pharmacol. 1973; 279(4):413-6. DOI: 10.1007/BF00500806. View