Tomlinson R V, Spires H R, Bowen J L
J Dairy Sci. 1985 Aug;68(8):2072-7. doi: 10.3168/jds.S0022-0302(85)81069-9.
Pharmacokinetic characteristics of the prostaglandin F2 alpha analog, fenprostalene, were studied in five lactating Holstein cows. Blood samples, milk, urine, and feces were collected for up to 7 d following a single subcutaneous injection of 1 mg of 13,14-hydrogen-3-fenprostalene in polyethylene glycol-400. The maximum concentration of tritium in plasma, observed 4 h after injection, equated to .17 ngeq/ml fenprostalene and declined with a fractional disappearance rate of .051 X h-1 to less than .04 ngeq/ml by 48 h. Likewise, milk contained .53 ngeq/ml fenprostalene at 4 h and the concentration declined with a fractional disappearance rate of .069 X h-1 to less than .03 ngeq/ml by 48 h. Milk was a very minor route of elimination of fenprostalene with only .46% of the injected dose recovered over a 7-d sampling. Recovery of tritium in urine accounted for 55% of the total dose and recovery in feces accounted for an additional 43%. Residues from fenprostalene at 7 d after injection were less than .1 ppb in all edible tissues. Differences in the molecular structure, formulation, and route of injection of fenprostalene resulted in a slower rate of absorption and elimination of this analog than previously reported for other prostaglandin products. Nonetheless, the percentage of the injected dose of fenprostalene secreted in milk was not increased appreciably, and no persistent tissue residues of fenprostalene were observed.
在五头泌乳期的荷斯坦奶牛身上研究了前列腺素F2α类似物氯前列烯醇的药代动力学特征。在单次皮下注射1毫克溶于聚乙二醇-400的13,14-氢-3-氯前列烯醇后，采集血样、牛奶、尿液和粪便长达7天。注射后4小时观察到血浆中氚的最大浓度相当于0.17纳克当量/毫升氯前列烯醇，随后以0.051×小时-1的分数消除率下降，到48小时时降至低于0.04纳克当量/毫升。同样，牛奶在4小时时含有0.53纳克当量/毫升氯前列烯醇，浓度以0.069×小时-1的分数消除率下降，到48小时时降至低于0.03纳克当量/毫升。牛奶是氯前列烯醇非常次要的消除途径，在7天的采样期间仅回收了0.46%的注射剂量。尿液中氚的回收占总剂量的55%，粪便中的回收占另外的43%。注射后7天，氯前列烯醇在所有可食用组织中的残留量均低于0.1 ppb。氯前列烯醇在分子结构、制剂和注射途径方面的差异导致该类似物的吸收和消除速率比先前报道的其他前列腺素产品慢。尽管如此，氯前列烯醇分泌到牛奶中的注射剂量百分比没有明显增加，并且未观察到氯前列烯醇在组织中的持续残留。
