Evaluation of a transdermal buprenorphine formulation in opioid detoxification.
Evaluation of a transdermal buprenorphine formulation in opioid detoxification.
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评估透皮丁丙诺啡制剂在阿片类药物解毒中的作用。
DOI：
10.1111/j.1360-0443.2007.01944.x
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发表时间：
2007
期刊：
影响因子：
--
通讯作者：
Bigelow,GeorgeE
中科院分区：
文献类型：
--
作者：
Lanier,RyanK;Umbricht,Annie;Harrison,JosephA;Nuwayser,ElieS;Bigelow,GeorgeE
目的 丁丙诺啡以舌下制剂形式上市，用于治疗阿片类药物依赖。已经开发出一种透皮制剂，可以延长阿片类药物戒断的缓解，减少所需的就诊次数并提高依从性，同时减少转移和滥用的可能性。本研究评估了这种透皮丁丙诺啡制剂（即丁丙诺啡贴剂）的安全性和生物递送（血液水平），及其在抑制阿片类药物戒断综合征方面的明显功效。设计开放标签、首次人体试验。设置住宅研究设施。参与者九名身体依赖阿片类药物的使用者完成了为期 10 天的阿片类药物解毒研究。干预每位志愿者都接受了一个剩余的贴剂应用放置3天。在临床前评估中，该制剂在 3 天内平均输送 1.9 毫克/天的丁丙诺啡。测量措施收集了阿片类药物戒断和阿片类激动剂效应的生理、行为、主观和观察者评级。结果总体而言，该贴剂似乎安全且耐受性良好。使用贴剂后没有出现严重的不良事件，也没有出现阿片类药物中毒。氧饱和度、心率、血压、皮肤温度和瞳孔直径均保持在正常范围内。贴片后 48 小时，丁丙诺啡血液浓度达到峰值，浓度为 0.60 ng/ml。在使用贴剂 3 天后，志愿者自我报告的戒断症状的存在及其严重程度减少了约 50%。去除贴剂后，戒断症状略有增加。阿片类药物救援药物的使用在贴剂使用后 6 小时内消除，并在贴剂去除后略有增加。结论 贴剂使用过程中丁丙诺啡的显着生物递送和阿片类药物戒断综合征的抑制以及贴剂去除后其重新出现表明临床上有用的药效活性。透皮丁丙诺啡可能是一种有用的阿片类药物解毒治疗，可减少依从性问题，并以不太可能被转用于非法用途的配方提供丁丙诺啡。
AimsBuprenorphine is marketed in a sublingual formulation for treatment of opioid dependence. A transdermal formulation has been developed that may provide extended relief from opioid withdrawal, reduce required clinic visits and improve adherence, while having less potential for diversion and abuse. This study evaluated the safety and biodelivery (blood levels) of this transdermal buprenorphine formulation (i.e. buprenorphine patch), and its apparent efficacy in suppressing the opioid withdrawal syndrome.DesignOpen‐label, first‐in‐humans trial.SettingA residential research facility.ParticipantsNine physically dependent opioid‐users completed the 10‐day opioid detoxification study.InterventionEach volunteer received a single patch application that remained in place for 3 days. The formulation has shown an average delivery of 1.9 mg/day of buprenorphine over 3 days in pre‐clinical evaluation.MeasuresPhysiological, behavioral, subjective and observer ratings of opioid withdrawal and opioid agonist effects were collected.FindingsOverall, the patch appeared safe and well tolerated. There were no serious adverse events, and no opioid intoxication following patch application. Oxygen saturation, heart rate, blood pressure, skin temperature and pupil diameter remained well within normal ranges. Buprenorphine blood levels peaked 48 hours after patch application at a concentration of 0.60 ng/ml. Volunteers' self‐reports of the presence and severity of withdrawal symptoms were reduced by approximately 50% on the 3 days of patch application. Withdrawal symptoms increased marginally upon patch removal. Administration of opioid rescue medication was eliminated within 6 hours of patch application, and increased slightly upon patch removal.ConclusionsThe significant biodelivery of buprenorphine and the suppression of the opioid withdrawal syndrome during patch application and its reappearance after patch removal indicate clinically useful pharmacodynamic activity. Transdermal buprenorphine may be a useful opioid detoxification treatment that reduces compliance concerns, and delivers buprenorphine in a formulation less likely to be diverted to illicit use.
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丁丙诺啡的身体依赖性潜力：拮抗剂诱发人类戒断。
DOI：
--
发表时间：
1996
期刊：
The Journal of pharmacology and experimental therapeutics.
影响因子：
--
作者：
Eissenberg,T;Greenwald,MK;Johnson,RE;Liebson,IA;Bigelow,GE;Stitzer,ML
通讯作者：
Stitzer,ML
影响因子：
2.2
作者：
Lai, Siang Hui;Yao, Yi Ju;Lob, Danny Siaw Teck
通讯作者：
Lob, Danny Siaw Teck
影响因子：
2.9
作者：
Moody, DE;Slawson, MH;Foltz, RL
通讯作者：
Foltz, RL
影响因子：
39.2
作者：
Himmelsbach, CK
通讯作者：
Himmelsbach, CK
影响因子：
6
作者：
Jenkinson, RA;Clark, NC;Dobbin, M
通讯作者：
Dobbin, M