Anand Kumar T C, David G F, Sankaranarayanan A, Puri V, Sundram K R
Proc Natl Acad Sci U S A. 1982 Jul;79(13):4185-9. doi: 10.1073/pnas.79.13.4185.
The pharmacokinetics of progesterone (dose: 10 microgram per animal) were studied in blood and cerebrospinal fluid of adult ovariectomized rhesus monkeys after the administration of the steroid as an intravenous injection, intravenous infusion (duration of infusion: 10 min), or nasal spray. The bioavailability of progesterone, in terms of area under the time--concentration curve and the maximal concentration in the two body fluids, was significantly higher when the steroid was infused or sprayed intranasally than when it was injected intravenously. The clearance of the steroid from the serum, as estimated by its elimination rate constant, elimination half-life, and total body clearance, did not differ for the three methods of administration. These findings suggest that the bioavailability of progesterone is enhanced by extending the duration over which the steroid is delivered into the hemic circulation.
对成年去卵巢恒河猴静脉注射、静脉输注(输注持续时间:10分钟)或鼻腔喷雾给予孕酮(剂量:每只动物10微克)后,研究了其在血液和脑脊液中的药代动力学。就时间 - 浓度曲线下面积和两种体液中的最大浓度而言,经鼻腔输注或喷雾给予孕酮时,其生物利用度显著高于静脉注射。通过消除速率常数、消除半衰期和全身清除率估算,三种给药方法的类固醇血清清除率无差异。这些发现表明,通过延长类固醇进入血液循环的持续时间可提高孕酮的生物利用度。