Exacerbation of tinea corporis during treatment with 1% clotrimazole/0.05% betamethasone diproprionate (Lotrisone)
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Five electrokinetic chromatography systems were compared concerning retention behavior and lipophilicity. Comparison was based on capacity (retention) factors of some steroidal drugs, and on log P(OW) values derived by the aid of reference substances. In all systems the aqueous buffer consisted of phosphate (20 mM, pH 7.5). Two systems had micelles, three systems microdroplets as negatively charged pseudostationary phases. The micelles were formed by sodium dodecyl sulfate (SDS) and sodium cholate, respectively. One microemulsion consisted (as usual) from octane as oil, butanol as cosurfactant and SDS as charged tenside. Two microemulsions were made from biosurfactants (phosphatidylcholine, isopropylmyristate) to better simulate biopartitioning of the drugs. Even for noncharged analytes a change in migration sequence and thus in log P(OW) was observed for the systems consisting of the biosurfactants, compared to the others. For the former systems, log P(OW) derived from the capacity factors agree for all analytes with those obtained from calculation by computer software based on the structure of the drugs, and with experimental data directly obtained from octanol/water partitioning.
A case is presented illustrating the complicating effects of antepartum steroids on a pregnant diabetic woman. The possible rapid deterioration of the diabetic state and the temporary suppression of estriol production are discussed.
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The effect of a liposomal preparation of beta-methasone dipropionate (0.039%, BDP) has been compared to that of a commercial propylene glycol-gel containing 0.064% BDP in a double-blind, randomized, paired trial lasting 14 d in 10 patients with atopic eczema and 10 patients with psoriasis vulgaris. In eczema, the liposome preparation tended to reduce erythema and scaling more than the conventional gel, the difference in the latter parameter being significant on Day 7. There was greater improvement of psoriasis on the side treated with the reference gel. Hence, liposome encapsulation of BDP may increase the antiinflammatory action but not the antiproliferative effect. Since inhibition of mitotic activity is linked to the atrophogenicity of topical corticosteroids, the results suggest that liposome encapsulation may improve the benefit-risk ratio in eczema.
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Bethamethasone was administered to pregnant rhesus monkeys of 134 to 150 days' gestation. At operative delivery, umbilical venous plasma cortisol concentrations were significantly lower in the treated group than in the control group, indicating that the agent crossed the placenta. In the treated group, accelerated differentiation was present in several fetal organs including lung, liver, kidney, and adrenal gland. Brain histologic changes suggestive of neuronal injury were found in some instances. There were no differences in the weights of these fetal organs except for liver. It was markedly increased in steroid-treated fetuses and this was accompanied by a fourfold rise in total hepatic glycogen content. These observations suggest that in the subhuman fetal primate, the differentiation of fetal organs in addition to lung is enhanced by short-term corticosteroid treatment while growth is not affected.