Detail of "2920-86-7"

Reference

Steroidal antiinflammatory agents in the horse: pharmacokinetics and action on the adrenal gland

Steroidal antiinflammatory agents in the horse: pharmacokinetics and action on the adrenal gland. Toutain, P. L.; Brandon, R. A. (Stn. Pharmacol. Toxicol., INRA, Toulouse 31300, Fr.). Vet. Pharmacol. Toxicol., Proc. Eur. Assoc. Vet. Pharmacol. Toxicol., [Congr.], 2nd, Meeting Date 1982, 353-66. Edited by: Ruckebusch, Yves; Toutain, Pierre-Louis; Koritz, Gary D. AVI: Westport, Conn. (English) 1983. CODEN: 51YHA9. DOCUMENT TYPE: Conference CA Section: 63 (Pharmaceuticals) Section cross-reference(s): 2 The pharmacokinetics and effects of steroidal anti-inflammatory agents on the adrenal gland are reviewed and data are given on dexamethasone (I) [50-02-2] and prednisolone (II) [50-24-8] in the horse. The area under the plasma concn. curve for I and I 21-isonicotinate [2265-64-7] were not different after i.v. administration. I and its sol. esters were rapidly absorbed following i.m. administration while H2O-insol. esters and slowly absorbed. Clearance times of I and its hydrosol. esters were short, while after i.m. administration of long-acting esters I persisted in urine for > 4 days. The plasma concns. of II after i.v. and i.m. administration of II succinate [2920-86-7] showed half-times of ~2 h. The elimination of II was slower than that of I. The degree of adrenal suppression was dependent on drug, its formulation, dose and duration, frequency, time and route of administration. For short-acting prepns. and for single administration, either i.v. or i.m., adrenal suppression was not always total. Repeated i.m. administration of short-acting I gave a suppressive effect on both the static and dynamic functions of the adrenal gland. Plasma cortisol levels decreased after a delay of 1-2 h after i.m. administration of long-acting II acetate [52-21-1] and reaching a low value after 12 h. Return to normal required ~20 days. The ACTH test indicated that the responsiveness of the adrenal gland was depressed equally for 3 wk.

Uptake of prodrugs by rat intestinal mucosal cells: mechanism and pharmaceutical implications

Uptake of prodrugs by rat intestinal mucosal cells: mechanism and pharmaceutical implications. Stewart, Barbra H.; Amidon, Gordon L.; Brabec, R. Kay (Med. Sch., Univ. Michigan, Ann Arbor, MI 48109, USA). J. Pharm. Sci., 75(10), 940-5 (English) 1986. CODEN: JPMSAE. ISSN: 0022-3549. DOCUMENT TYPE: Journal CA Section: 2 (Mammalian Hormones) The in vitro intestinal ring uptake of prednisolone [50-24-8], prednisolone 21-succinate [2920-86-7], and prednisolone 21-phosphate [302-25-0] was compared in rings prepd. from rat jejunum and colon. An HPLC assay was developed to det. whether the drug or intact prodrug was taken up by the tissue. In jejunum and colon, the uptake of prednisolone was limited by its soly. (0.84 mM, 37°). The freely sol. succinate and phosphate esters were well absorbed in the jejunum. The only species detected in jejunal tissue after incubation with prednisolone 21-phosphate was prednisolone, indicating hydrolysis prior to absorption. 50-24-8 and 9001-78-9 which are cas registry numbers of chemicals are mentioned. This implication was verified by light microscopy. Incubation of tissue from the jejunum with prednisolone 21-succinate resulted in uptake of a mixt. of prodrug and parent drug, with the latter form predominating. Prednisolone 21-succinate was also absorbed well in the colon, where the predominant species taken up by the tissue was the intact ester. The half-life of the succinate ester in the tissue was ~1 h postincubation, implicating enzyme mediation. Uptake of the phosphate ester by the colon was <20% of that obsd. in the jejunum, with the species absorbed still being primarily the parent alc. Light microscopy techniques confirmed that prednisolone 21-phosphate and hydrocortisone 21-phosphate are good substrates for brush border membrane alk. phosphatase [9001-78-9] in the jejunum and that lack of this enzyme in colon tissue was most likely responsible for poor uptake in the colon. .