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[Biological availability of digoxin and beta-acetyldigoxin after single-dose administration (author's transl)].

The biological availability of digoxin tablets (Lanicor) and beta-acetyldigoxin tablets (Novodigal) was tested after single-dose administration. Plasma levels over 48 hours, the area under the blood-level curves and the cumulative urinary excretion over seven days served as a measure of biological availability. The area under the blood-level curve after 1.0 mg digoxin by mouth was 40.7 +/- 1.7 ng . ml-1 . h and after 1.0 mg beta-acetyldigoxin by mouth 39.1 +/- 1.4 ng . ml-1 h, compared with 56.1 +/- 1.4 after 1.0 mg digoxin intravenously. Seven days later 0.67 +/- 0.12 mg digoxin of the orally administered digoxin, 0.68 +/- 0.12 mg digoxin of the orally administered beta-acetyldigoxin and 0.81 +/- 0.08 mg of the intravenously administered digoxin were excreted in the urine. There was no significant difference in the biological availability of the two drugs (P greater than 0.05).

Acetyldigoxins

Biological availability to the rat of intrinsic and extrinsic iron with soybean protein isolates.

Evaluations were conducted to assess the biological availability of iron in three food grade isolated soybean proteins and to evanuate the influence of these proteins on iron added to the diet from a source of known high biological availability. Ferrous sulfate was used as the standard iron source in all experiments. The biological availability was measured by a 14-day hemoglobin repletion after a 4 week depletion period using multiple dose response and comparing the test samples and standard iron source by the slope ratio assay procedure. The relative iron bioavailability for three isolated soybean proteins was A = 60%; B = 64% and C = 59% with a mean value of 61%. Autoclaving isolated soybean protein B at 108.4 degrees improved iron bioavailability over the unheated samples while isolated soybean protein A was unaffected by this treatment. Iron added to the diets containing isolated soybean protein had bioavailabilities similar to that of iron present in the soybean which supports the common dietary iron pool hypothesis. The high iron content (0.18 mg/g protein) coupled with the bioavailability data make the isolated soybean proteins a good dietary iron source.

Animals

[Biological availability of diagoxin in patients with or without gastric resection (Billroth II) (author's transl)].

Biological availability of digoxin tablets was measured during maintenance therapy in ten hospitalized patients who had had a Billroth II gastric resection at least two years previously. Twelve patients on digoxin maintenance for heart failure but without gastro-intestinal disease served as controls. The mean value of daily digoxin urinary excretion over ten days in the resection group was 38.09 +/- 0.70% of the administered dose. The serum-digitalis level 12 and 24 hours after the last dose of glycoside (0.5 mg) was 1.30 +/- 0.04 ng/ml and did not significantly differ from that of the control group, nor did digoxin elimination in urine and the digoxin/creatinin excretion ratio. It is concluded that two-third gastric resection with exclusion of antigrade duodenal passage does not influence biological availability of digoxin given in tablets.

Adult

[Biological availability of digoxin from a combination drug].

In a randomized cross-over study with 14 voluntary test persons the absolute biological availability of digoxin in Card-Dusodril 1/8 and 1/4 respectively was investigated. 6 test persons received 4 drag. Card-Dusodril 1/8 (= 0.5 mg digoxin), 8 test persons 4 drag. Card-Dusodril 1/4 (= 1 mg digoxin) orally, in comparison to the corresponding group with intravenously applied digoxin as standard. Based on the cumulative digoxin excretion in the urine an absolute biological availability of Card-Dusodril 1/8 of 79%, of Card-Dusodril 1/4 of 76% could be demonstrated. With regard to an average resorption of oral digoxin preparations of approx. 70%, the present values, which correspond in direct comparison to those of acetyl digoxin, can be considered good. Maximum serum levels were achieved after 86 +/- 6.8 minutes which also indicates a quick resorption.

Administration, Oral

[Biological availability of spironolactone in two different galenic forms (author's transl)].

The biological availability of spironolactone in two different galenic preparations (Spiro-Tablinen and Aldactone-100 Caps) was investigated in a single-blind, randomised, cross-over study in six healthy probands. The serum concentration of canrenone after oral intake of spironolactone (100 mg) was investigated in the steady state as well as the renal excretion of canrenone. There were no statistically significant differences between the two preparations either in the course of the serum concentration of canrenone or in the cumulative renal excretion.

Adult

[Biologic availability and metabolic transit of amino acids modified by technological processing].

The biological availability of amino acids modified by industrial processes has been measured in trials on rats, and their metabolic transit (urinary and faecal excretions, transformation into CO2 and retention in organs) has been studied using molecules labelled with 14C. Maillard reaction products. epsilon-fructose-lysine is not utilized as lysine source. However, less than 10 p. 100 of this substance, bound to proteins, is excreted unmodified in the urine. Intestinal flora destroys most of the fraction which is not absorbed. Premelanoidins are partially absorbed and "burnt" in the organism, whereas high molecularightwe melanoïdins are totally excreted in the faeces. epsilon-(gamma-glutamyl)-lysine and epsilon-(beta-aspartyl)-lysine isopeptides. 80 to 100 p. 100 of free epsilon-(gamma-glutamyl)-lysine are utilized by the Rat. It seems to be absorbed by the intestine, and subsequently hydrolyzed by the kidney, thus releasing lysine. Utilization of this isopeptide bound to proteins has not been shown till now. Free epsilon-(beta-aspartyl)-lysine is not utilized as lysine source. Methionine sulfoxyde and methionine sulfone. Methionine sulfone is not utilized as methionine source whereas most of the free and bound methionine sulfoxide is, in part, it is "reduced" by the liver (perfused liver). Lysino-alanine. Formation of lysino-alanine reduces the availability of lysine and cystine. It is partially excreted in urines, mainly as free lysino-alanine, but also as acetylated derivatives and unknown catabolites.

Amino Acids

Relationship between the biological availability and solubility rate of reduced iron.

Solubility rate determinations were conducted on electrolytic iron and hydrogen reduced iron and carbonyl iron samples to study the correlation of biological availability and solubility. There was excellent correlation for the hydrogen reduced iron and electrolytic iron samples,. The carbonyl iron samples showed a direct relationship between solubility and bioavailability, but these data were not numerically equivalent to data from other types.

Biological Availability

[Biological availability of fluoride after combined administration with vitamin D3 in man (author's transl)].

Six adults ingested 1 mg fluoride, first as NaF in a watery solution and, secondly, in tablet form (D-Fluoretten 1000). Fluoride concentration was almost identical in the two series. After initial values within the normal range concentrations rapidly rose to a maximum (six times normal) reached on average after 30 minutes, followed by an, at first steep then more gradual, fall in concentration over eight hours. The area under the curve was similar in the two series. These results indicate that the biological availability of fluoride is not influenced by vitamin D3 in the adult and, presumably, in the small child as well.

Adult

[Rate of tetracycline dissolution from tablets and capsules and the biological availability of the antibiotic].

Relation between the rate of tetracycline dissolution from tablets and capsules and the biological acceptibility of the antibiotic in the host was studied. The antibiotic dissolution rate from the pharmaceutical forms was determined in a modernized apparatus "Rotary basket" in water, the speed of the basket rotation was 200 r.p.m. In addition the tetracycline blood levels in patients treated with the drug in the above pharmaceutical forms were estimated. It was found that the rate of the antibiotic dissolution characterized the antibiotic biological acceptibility. A test for the dissolution rate was developed. It may be used for estimation of production batches of tetracycline tablets.

Administration, Oral