{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,4]],"date-time":"2026-10-04T18:18:50Z","timestamp":1791137930276,"version":"4.1.0"},"reference-count":54,"publisher":"Wiley","issue":"3","license":[{"start":{"date-parts":[[2006,2,27]],"date-time":"2006-02-27T00:00:00Z","timestamp":1140998400000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/onlinelibrary.wiley.com\/termsAndConditions#vor"}],"content-domain":{"domain":["onlinelibrary.wiley.com"],"crossmark-restriction":true},"short-container-title":["Addiction"],"published-print":{"date-parts":[[2006,3]]},"abstract":"<jats:title>ABSTRACT<\/jats:title><jats:p><jats:bold>Aim\u2003<\/jats:bold> Buprenorphine is an effective medication for treatment of opioid dependence. An injectable depot formulation of buprenorphine has been developed using biodegradable polymer microcapsule technology. This formulation may offer effective treatment of opioid dependence and enhance treatment delivery while minimizing risks of patient non\u2010adherence or illicit diversion of the medication. This report provides a characterization of the biodelivery of this injectable depot in humans and of the relationship of drug blood levels to pharmacodynamic indices.\u200a<\/jats:p><jats:p><jats:bold>Method and participants\u2003<\/jats:bold> The data are from two studies in which 11 opioid\u2010dependent volunteers each received a single depot injection containing 58\u2003mg of buprenorphine, and include previously unreported detailed plasma concentration data over a 6\u2010week time\u2010course following depot administration and examination of their relationship to pharmacodynamic indices.<\/jats:p><jats:p><jats:bold>Findings\u2003<\/jats:bold> Mean plasma buprenorphine increased gradually following depot administration, peaked at 2\u20133\u2003days with a mean concentration of 1.25\u2003ng\/ml and then decreased gradually, approaching undetectable levels (&lt;\u20030.10\u2003ng\/mL) by 6 weeks. There was substantial between\u2010subject consistency in several aspects of buprenorphine biodelivery, including time to first detectable blood level (4\u2003hours), peak blood level (2\u2003days) and undetectable blood level (6\u20136.5\u2003weeks). In contrast, there was marked between\u2010subject variability in the magnitude of peak buprenorphine concentrations, ranging from 0.17 to 3.47\u2003ng\/ml. Extent of opioid blockade was tested by weekly opioid challenges with 3\u2003mg subcutaneous hydromorphone; subjective response and pupillary constriction were related inversely to both buprenorphine and norbuprenorphine plasma concentrations (<jats:italic>r<\/jats:italic>\u2003=\u20030.84\u20130.95).<\/jats:p><jats:p><jats:bold>Conclusion\u2003<\/jats:bold> The data document that this depot formulation provides effective buprenorphine delivery for several weeks and that effects persist even at fairly low buprenorphine plasma concentrations. Suggestions are offered for further research needed to develop this formulation for clinical use as a detoxification and\/or maintenance pharmacotherapy for opioid dependence.<\/jats:p>","DOI":"10.1111\/j.1360-0443.2006.01348.x","type":"journal-article","created":{"date-parts":[[2006,2,27]],"date-time":"2006-02-27T08:36:48Z","timestamp":1141029408000},"page":"420-432","update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":42,"title":["An injection depot formulation of buprenorphine: extended biodelivery and effects"],"prefix":"10.1111","volume":"101","author":[{"given":"Stacey C.","family":"Sigmon","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"David E.","family":"Moody","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Elie S.","family":"Nuwayser","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"George E.","family":"Bigelow","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"311","published-online":{"date-parts":[[2006,2,27]]},"reference":[{"key":"e_1_2_6_2_1","unstructured":"Aceto M. 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