Buprenorphine - Commercial Preparations

Commercial Preparations

British firm Reckitt & Colman (now Reckitt Benckiser) first marketed buprenorphine under the trade names Temgesic (sublingual/parenteral preparations) and Buprenex (parenteral). Subsequently two more formulations were released: Subutex (white colour, oval shape, bitter, no active additives) and Suboxone (white colour, hexagonal tablet, lime-flavoured, one part naloxone for every four parts buprenorphine). Subutex and Suboxone are available in 2 mg and 8 mg sublingual dosages. On October 8, 2009, Roxane Laboratories of Columbus, Ohio, United States won FDA approval for a generic preparation of Subutex and as of October 23, 2009 announced that it is ready for distribution nationwide in 2 mg and 8 mg sublingual dosages. The demand for this generic was so high that Roxane did not produce enough to meet market demand, resulting in pharmacies running out and being unable to order more. Teva Pharmaceutical Laboratories of Tel Aviv, Israel also received approval (as of 1 April 2010) for a generic formulation of Subutex sublingual tablets in 2 mg and 8 mg dosages that are currently available in limited distribution in America as of 20 June 2010.

Since 2001, buprenorphine is also available transdermally as 35, 52.5 and 70 mcg/hr transdermal patches that deliver the dose over ninety-six hours. This dosage form is marketed as Transtec in most European countries by Grunenthal (Napp Pharmaceuticals in the UK, Norpharma in Denmark) for the treatment of moderate to severe cancer pain and severe non-cancer pain not responding to non-opioids.

Other available buprenorphine formulations include a 5, 10 and 20 mcg/hr, 7-day patch, marketed as Butrans in the U.S. by Purdue Pharma (and by Napp Pharmaceuticals in the UK) indicated for the management of moderate to severe chronic pain in patients requiring a continuous, around-the-clock opioid analgesic for an extended period of time. A similar transdermal system is marketed by a collaboration between Mundipharma and Grunenthal in Australia under the name Norspan, with indications for moderate chronic pain not responding to non-opioids, dosed in 5, 10 or 20 mcg/hr patches.

In India: Addnok 0.4, 2 & 8 Mg Sublingual Tablets by Rusan Pharma Ltd., Tidigesic 0.2 mg (slow release) or 0.3 mg/mL injectable by Sun Pharmaceuticals; Bupregesic (0.3 mg/mL) by Neon Laboratories; Morgesic (0.3 mg/mL) by Samarth Pharma; Norphin (0.3 mg/mL) Unichem Laboratories.

A novel implantable formulation of buprenorphine (Probuphine), using a polymer matrix sustained-release technology, has been developed to offer treatment for opioid dependence while minimizing risks of patient noncompliance and illicit diversion.

In addition to the sublingual tablet, Suboxone is now marketed in the form of a sublingual film, available in both the 2 mg/0.5 mg and 8 mg/2 mg dosages; the film is not available in Canada or the United Kingdom (where it was discovered). The makers of Suboxone, Reckitt Benckiser, claim that the film has some advantages over the traditional tablet in that it dissolves faster and, unlike the tablet, adheres to the oral mucosa under the tongue, preventing it from being swallowed or falling out; that patients favor its taste over the tablet, stating that "more than 71% of patients scored the taste as neutral or better"; that each film strip is individually wrapped in a compact unit-dose pouch that is child-resistant and easy to carry; and that it is clinically interchangeable with the Suboxone tablet and can also be dosed once daily. Reckitt Benckiser also states that the film discourages misuse and abuse, as the paper-thin film is more difficult to crush and snort. Also, a 10-digit code is printed on each pouch, which helps facilitate medication counts and, therefore, serves to deter diversion into the illegal drug market.