| 摘要 |
A buprenorphine formulation comprises a suspension of 5-20 wt% of buprenorphine in water, wherein the buprenorphie is in particulate form with an average particle size of less than 200µ, preferably less than 20µ. The formulation may further comprise a water soluble polymer selected from the group consisting of polyethylene glycol (PEG), carboxymethyl cellulose (CMC), polyvinyl pyrrolidone (PVP), polyvinyl acetate (PVA) and dextran, preferably PEG. The composition may also comprise: a non-ionic surfactant selected from the group including Tween 20(RTM), Tween 80(RTM), poloxamers and phospholipids; pharmaceutically acceptable salts or sugars to adjust the tonicity of the formulation and/or preservatives, preferably selected from the group consisting of methylparaben, propylparaben and benzyl alcohol. A formulation comprising a buprenophine free base suspension in PEG3350, Tween 80(RTM) and sodium chloride aqueous solution is exemplified. The composition is preferably useful in treatment of opioid dependence or pain relief. Also outlined are methods for formulating the composition. |
