PHARMACEUTICAL COMPOSITION CONTAINING NALBUPHINE HYDROCHLORIDE, USE THEREOF TO TREAT MODERATE TO SEVERE PAIN AND METHOD FOR PRODUCING SAID PHARMACEUTICAL COMPOSITION

摘要

This invention relates to the field of medicine and the chemical/pharmaceutical industry, and more particularly to the creation, production and use of a drug for the treatment (relief) of moderate to severe pain in different branches of medicine, particularly oncology. The aim of the invention is to create novel pharmaceutical compositions in the form of rectal suppositories containing nalbuphine or a salt thereof on various suppository bases, which are intended for treating (relieving) episodes of moderate to severe pain and have an effective and prolonged analgesic effect without having a laxative effect, as well as to provide methods for producing such compositions. In order to achieve this aim, it is proposed to use a nalbuphine salt in the form of suppositories on a hydrophilic emulsion base to treat moderate to severe pain. The pharmaceutical composition in suppository form for treating moderate to severe pain contains nalbuphine hydrochloride as active principle and a suppository base. As the suppository base, the composition contains a hydrophilic emulsion base that includes binders, a poloxamer, a filler, an emulsifier, propylene glycol and polyethylene oxide-400 as a solvent. The binders contained in the composition are preferably polyethylene oxide 4000 and polyethylene oxide 1500, and the poloxamer is poloxamer 188. The filler contained in the composition is preferably solid fat. Further, the emulsifier contained in the composition is preferably a complex emulsifier in the form of a blend of a type 1 emulsifier and a type 2 emulsifier. In particular embodiment the type 1 emulsifier contained in the composition is macrogol 20 cetostearyl ether, and the type 2 emulsifier is cetostearyl alcohol with mass ratio thereof from 0.5:5.5 to 2.0:4.0. Proposed is a method for producing a pharmaceutical composition, according to which nalbuphine hydrochloride is dissolved in propylene glycol, the solution is mixed with a melted suppository base and homogenized; the liquid suppository mass is dosed into blister pockets and cooled.