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A number of esters of hydrocortisone and related steroids have been examined for activity in the granuloma inhibition (subcutaneous cotton pellet) test, both after local application of the steroids and after systemic administration. Liver glycogen deposition activity was examined by a one-day oral test in mice, a six-day test in rats, and for duration of action after a single subcutaneous injection. Rates of absorption and activity per mg. of steroid absorbed also were determined. Wide differences in activity were found, depending upon the configuration at C-21. Part of this difference was due to diverse rates of absorption, but there were also differences in activity per mg. of steroid absorbed. It is concluded that ease of hydrolysis of the ester is also a factor in determining potency. The tertiary butyl acetate is particularly effective when locally applied, but systemic activity of this ester is relatively low because of reduced rate of absorption and decreased activity per mg. absorbed. After subcutaneous injection, the free alcohol of hydrocortisone is more rapidly absorbed and gives a more prompt response than any of its esters examined. The 9α-fluoro derivative is more gradually absorbed and gives a more sustained response than does hydrocortisone. |
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