ANALGETIC AND ANTAGONIST FOR PERORAL DOSAGE

摘要

PURPOSE: To obtain an analgesic and narcotic-antagonistic drug contg. a specified morphine deriv. in the form of its H-oxide deriv., not reducing its analgesic affect and antagonistic effect on narcotics even in the case of oral administration and having improved bioavailability even by oral administration. CONSTITUTION: This drug consists of the N-oxide deriv. (A) of nalbuphine, pentazocine, butorphanol, buprenorphine, levorphanol or levorphan and a carrier (B). The component A is obtd., e.g. by treating nalbuphine represented by the formula, that is, (-)-17-(cyclobutylmethyl)-4,5-epoxymorphinane-3,6a-14-triol with m-chloroperbenzoic acid as an oxidizing agent in a solvent such as methylene chloride at room temp. The component A is administered by daily dosage of 0.1-20 mg/kg. It is preferable that the component A is dividedly administered in 2-4 portions in a day or is administered in the form of a continuous releasing agent.