Buprenorphine

Buprenorphine is a semisynthetic mixed opiate agonist-antagonist.The parenteral formulation is used for the relief of moderate to severe pain. Sublingual administration of tablets is used for the treatment of opioid dependence. Buprenorphine is prescribed for opioid dependence.

Buprenorphine’s innovator is Mundipharma and is marketed world-wide by the band name Transtec (Grünentall) and Buprenorphine Hydrochloride is known by the brand name Subutex (Reckitt Benckiser).

Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. Opiate agonist are believed to exert their effects by stimulating specific opiate receptors, designated as mu, kappa, and delta, which have been reclassified by an International Union of Pharmacology subcommittee as OP1 (delta), OP2 (kappa), and OP3 (mu). Mu-receptors are considered the classic morphine-receptor type, as stimulation at this receptor produces supraspinal analgesia, respiratory depression, euphoria, and physical dependence. Actions at kappa-receptors are believed to produce alterations in the perception of pain and the emotional response to pain. Buprenorphine increases mu-receptor activity and blocks kappa-receptor activity. Buprenorphine has less intrinsic activity at mu-receptors than full agonists. Blockade of the effects of full mu-receptor agonists occurs after acute administration of buprenorphine. Buprenorphine slowly dissociates from the mu-receptor, which likely accounts for its longer duration of action than morphine, the unpredictability of its reversal by opioid antagonists, and its low level of manifested physical dependence.

Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor. Naloxone is an antagonist at the mu-opioid receptor.

General data on Buprenorphine Active Pharmaceutical Ingredient

Buprenorphine

CAS Registry: 52485-79-7
ATC: N02AE01
Molecular Formula: C29H41NO4
Molecular Weight: 467.6
Pharmacopoeias: In Eur.

Buprenorphine HCl

CAS Registry: 53152-21-9
ATC: N07BC01
Molecular Formula: C29H41NO4, HCl
Molecular Weight: 504.1
Pharmacopoeias: In Chin., Eur., and US.

TAPI's Buprenorphine Pharmaceutical Ingredient

TAPI's Buprenorphine Active Pharmaceutical Ingredient is produced in IVAX Pharmaceuticals s.r.o. in Opava-Komarov, Czech Republic.

Buprenorphine is produced by TAPI by Organic synthetic synthesis and considered to be medium volume Active Pharmaceutical Ingredient.

Pharmacopeias

Ph. Eur. 5.5: Buprenorphine is a white or almost white crystalline powder.  Buprenorphine is very slightly soluble in water; freely soluble in acetone; slightly soluble in cyclohexane; soluble in methyl alcohol. It dissolves in dilute solutions of acids.

Ph. Eur. 5.5: Buprenorphine Hydrochloride is a white or almost white crystalline powder. Buprenorphine Hydrochloride is sparingly soluble in water; soluble in alcohol; practically insoluble in cyclohexane; freely soluble in methyl alcohol.

USP 29: Buprenorphine Hydrochloride has a pH of a 1% solution in water is between 4.0 and 6.0.

Legal Note

Product exploitation, including development, sales and offer for sale are performed where permissible by patent law. This presentation is not and should not constitute an offer for sale in territories where it is not permitted by law. In USA Products  that  Currently on Patent are available for R&D Use in Accordance with 35 USC §271 (e) (1).

*TAPI stands for Teva's Active Pharmaceutical Ingredients