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The novel depot of buprenorphine propionate has a long‐acting effect on physical dependence on morphine
Author(s) -
Liu KuoSheng,
Lin ChingNan,
Shieh JaPing,
Chu ChinChen,
Kuei ChunHsiung,
Wang JhiJoung
Publication year - 2006
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.20107
Subject(s) - buprenorphine , propionate , morphine , physical dependence , pharmacology , saline , depot , chemistry , naltrexone , medicine , anesthesia , opioid , biochemistry , receptor , archaeology , history
Buprenorphine is a promising drug for the treatment of physical dependence on opioids. The aim of the present study was to evaluate the efficacy and duration of action of a novel depot form of a buprenorphine prodrug, buprenorphine propionate, on physical dependence on morphine. Following intramuscular injection in morphine‐dependent mice, the efficacy and duration of action of buprenorphine propionate in sesame oil were evaluated. Two other dosage forms of buprenorphine were used as controls. Intramuscular injection of buprenorphine HCl (0.1 µmol/kg in saline) attenuated the severity of morphine dependence ( P <0.05) with a 9‐h duration of action. However, a further increase in dose up to 60‐fold could not further increase its duration of action. On the other hand, buprenorphine base and propionate when prepared in sesame oil produced longer durations of action than did buprenorphine HCl in saline under an equimolar basis of 6 µmol/kg ( P <0.05, for each comparison). Among dosage forms, buprenorphine propionate in sesame oil produced the longest duration of action, 11.3‐fold longer than that of buprenorphine HCl in saline and 2‐fold longer than buprenorphine base in oil. In conclusion, the novel depot of buprenorphine propionate produced a dose‐related long‐acting effect on physical dependence on morphine in mice. Drug Dev. Res. 67:462–469, 2006. © 2006 Wiley‐Liss, Inc.