PHARMACOKINETIC QUANTITATION OF NALTREXONE CONTROLLED RELEASE FROM A COPOLYMER DELIVERY SYSTEM
PHARMACOKINETIC QUANTITATION OF NALTREXONE CONTROLLED RELEASE FROM A COPOLYMER DELIVERY SYSTEM
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DOI：
10.1007/bf01058956
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发表时间：
1983-01-01
期刊：
影响因子：
--
通讯作者：
WISE, DL
中科院分区：
文献类型：
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作者：
REUNING, RH;LIAO, SHT;WISE, DL
Naltrexone release rates from a controlled release delivery system were quantitated over a time period greater than 1 mo. in the monkey. The method requires calibration of the pharmacokinetic parameters of each monkey utilizing an i.v. bolus dose and assay of unchanged naltrexone levels in plasma as a function of time after dosing. Also required are periodic plasma levels of unchanged naltrexone obtained subsequent to adminstration of the delivery system. Release rates are then calculated as well as the total amount released. Application of the methodology to a biodegradable copolymer naltrexone delivery system in 3 monkeys showed an initial release rate of 3-8% of the dose/day over the 1st 3-5 days followed by a slow, rather constant release rate of 1-3%/day from day 5 to the time of the last measurable plasma sample (36-43 days). Comparison of alternative calculation methods using both experimental and simulated plasma naltrexone data verified the accuracy of the release rate calculations. The sum of the calculated total amount of natrexone released plus the assayed amount remaining in the delivery system after reomval from the animal accounted for 91-94% of the administered dose in the 2 monkeys in which complete data were obtained.
