Chiang C N, Hollister L E, Gillespie H K, Foltz R L
Drug Alcohol Depend. 1985 Sep;16(1):1-8. doi: 10.1016/0376-8716(85)90076-6.
A clinical evaluation of the naltrexone bead, a biodegradable sustained-release dosage form of 3.0 mg in weight containing 70% naltrexone in a copolymer of lactic and glycolic acids, was carried out in 4 healthy normal males. Subjects were given an intravenous dose of 10 mg naltrexone and approx. 1 week later a 63-mg dose of naltrexone by subcutaneous administration of the beads. Challenge doses of 15 mg morphine were given to each subject during the study for the assessment of narcotic blockade effects of naltrexone. For a 2-4-week period after bead administration, relatively constant plasma levels were maintained at 0.30-0.46 ng/ml for naltrexone and were 0.64-1.07 ng/ml for naltrexol. Urine levels for unchanged and conjugated naltrexone were 79-215 ng/ml and for naltrexol were 315-500 ng/ml. From kinetic analysis, an average of 2.4-2.7% of implanted dose was absorbed each day from the administration of the beads. Opiate effects of morphine challenges were mitigated during the 2-4-week period after administration of naltrexone beads.
对纳曲酮微球进行了临床评估，该微球是一种可生物降解的缓释剂型，重量为3.0毫克，由乳酸和乙醇酸共聚物制成，含70%纳曲酮。对4名健康正常男性进行了研究。受试者先静脉注射10毫克纳曲酮，大约1周后通过皮下植入微球给予63毫克纳曲酮剂量。在研究期间，给每位受试者注射15毫克吗啡激发剂量，以评估纳曲酮的麻醉阻滞效果。在植入微球后的2至4周内，纳曲酮的血浆水平相对稳定，维持在0.30 - 0.46纳克/毫升，纳曲醇的血浆水平为0.64 - 1.07纳克/毫升。未变化和结合型纳曲酮的尿液水平为79 - 215纳克/毫升，纳曲醇的尿液水平为315 - 500纳克/毫升。通过动力学分析，每天从微球给药中吸收的植入剂量平均为2.4% - 2.7%。在给予纳曲酮微球后的2至4周内，吗啡激发试验的阿片类效应得到缓解。
