Fate of 14C-3-methylamino-1,2,3,4-tetrahydrocarbazole hydrochloride in rats and dogs.

The fate of 14C-3-methylamino-1,2,3,4-tetrahydrocarbazole hydrochloride, a potential psychotherapeutic agent, was studied in rats and dogs. Rats were given a single oral or intraperitoneal dose while dogs received the drug either orally or intravenously. Radioactivity in plasma samples and excreta was determined by liquid scintillation counting. In addition, 14C-levels in various rat tissues were estimated. The drug appeared to be well absorbed in both species. 14C-levels were highest in liver and lung and lowest in plasma. Excretion was primarily urinary and was more complete within the first 96 hr in the rat than in the dog, which suggested a longer 14C-half-life in the dog. No evidence was seen that the drug was demethylated.

Improved colorimetric determination of aspirin and salicylic acid concentrations in human plasma.

An improvement in a previously described method for the determination of plasma salicylic acid and aspirin levels in humans is described. The procedure was simplified by employing only one plasma sample for both salicylates. More accurate estimation of salicylates, particularly aspirin, was achieved by using two different calibration curves. Salicylic acid was estimated by reaction with an aqueous solution of the Folin-Ciocalteu phenol reagent. Absorbance of the blue-colored complex, which formed on addition of sodium hydroxide, was measured at 670 nm. The influence of alkalinity in the formation of the colored complex is discussed. The average recovery of aspirin added to plasma was 94.61%; it was 214.72% by the previous method.

Evaluation of the safety of cantastim in normal humans.

CANTASTIM, a good immunomodulatory agent obtained from a highly pathogenic strain of Pseudomonas aeruginosa was inoculated during 12 weeks in 21 healthy individuals aged 18-45 years. The subjects were clinically and laboratory investigated for body weight, antibodies against DNA, collage, cardiolipin, number of blood cells, blood and urine enzymes etc. After this intensive therapy, all the studied parameters were found in normal range of values. The results are a proof that this immunomodulator is not antigenic and has not side effects.

Rates of release of subcutaneously injected antigens in the rat. Comparison of an aqueous preparation with two alum-precipated preparations.

Release of antigen E-125 I from the site of subcutaneous injection in male rats was delayed significantly when either of two alum-precipitated preparations containing 1.0-1.2 mg of Al/ml was administered rather than an aqueous preparation. The rates of 125I excretion were similarly influenced being statistically slower through the first week after single doses of the alum-precipitated preparations. The results of these studies strongly support the view that alum-precipitated vaccines offer more protection from system reactions than aqueous vaccines.

Absorption, distribution, and excretion of 8-methoxypsoralen in HRA/Skh mice.

The tissue distribution and excretion of [3H]8-methoxypsoralen (8-MOP), a well-accepted therapeutic agent for the treatment of psoriasis, was studied in hairless HRA/Skh female mice. Mice were given single oral doses of 6 mg of [3H]8-MOP or 5-[14C]8-MOP/kg in corn oil. Radiochemical analyses of tissues and excreta were accomplished by liquid scintillation counting. The 8-MOP appeared to be rapidly absorbed through the gastrointestinal tract, where the tritium levels were highest, followed by skin, blood, and liver; levels were lowest in fat (adipose tissue). In female HRA/Skh mice which had not been irradiated with UVA (320-400 nm), 84% of the carbon-14 and 58% of the tritium were recovered in the urine and feces within 24 hours of oral administration of 5-[14C]8-MOP or [3H]8-MOP, respectively. Animals that were exposed to UVA and received [3H]8-MOP excreted approximately 12% less tritium in the urine and feces compared with the animals which received no UVA.