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Blood levels and bioavailability of ascorbic acid after administration of a sustained-release formulation to humans.

Plasma and whole blood concentrations of ascorbate have been measured after administration of 1000 mg of the vitamin as standard or sustained-release capsule formulations to human subjects. A peak of mean whole blood and plasma concentrations of 8.5 mug/ml and 5.7 mug/ml respectively (corrected for predose concentrations of "endogenous" ascorbate) occurred at 12 h and 6 h respectively after administration of a sustained-release formulation. After administration of a standard formulation, the peak of mean whole blood and plasma concentrations of 9.4 mug/ml and 8.6 mug/ml respectively occurred at 4 h. In whole blood, mean concentrations of ascorbate declined with a half-life of about 34 h. The bioavailability of ascorbate from the sustained-release formulation was 149% and 180% of that from the standard formulation by calculation from whole blood and plasma concentration data respectively.

Adult↗

Dissociation of acetylsalicylic acid in blood and joint fluid.

Assay method in blood of 30 patients, who had ingested 0.6 g buffered aspirin, showed earlier appearance of acetylsalicylate (ASA) than of de-acetylated salicylate (SA); the values for ASA averaged 7.7 min, and for SA, 10.9 min. Similarly in joint fluid, ASA appeared earlier than SA; the values of ASA averaged 19.4 min, and those for SA, 21.9 min. Transport times did not differ significantly between ASA and SA in most types of synovitis. Close to maximum concentrations in blood averaged 18.9 mg/l for total salicylates (TSA), 3.3 mg/l for ASA, and 23.3 mg/l for SA, whereas maximum concentrations in joint fluid averaged 15.7 mg/l for TSA, 2.5 mg/l for ASA, and 14.5 mg/l for SA. ASA in blood initially consituted 65% of TSA and decreased to less than measurable amounts 75 min after intake. Joint fluid initially contained a somewhat smaller maximal proportion of ASA, but de-acetylation progressed more slowly than in blood; ASA decreased to undetectable levels within 140-145 min after intake.

Adult↗

[Approaches in medical treatment in glaucoma (author's transl)].

The developments concern methods of application and therapeutic agents. Regarding drug aplication Ocusert has to be mentioned: inserted in the cul de sac of the eye once a week it releases a low concentration of a substance continuously and with a constant rate. For acetazolamid (Diamox) it has been shown, that in long term treatment much lower concentrations than usual are effective. Efforts regarding new local agents reducing intraocular pressure are stimulating as well as inhibiting the sympathetic tone. The practically most important discovery so far is Clonidine, whose pressure lowering mechanism is not quite clarified yet and which, due to other problems, demands a very critical indication. Beta-receptor-blocking agents, such as Propranolol could become somewhat important, as well as for some special indications the chemical sympathectomy by 6-Hydroxydopamine. The sympatholytic agent Guanethidine proves to be very valuable in special cases. Besides the pressure reducing treatment medicamentally achieved increase of the blood supply to the optic nerve becomes more important. It becomes more and more evident that the elevation of the stroke volume--thus heart output--by cardiac therapy is important what demands collaboration with colleagues of other disciplines.

Acetazolamide↗