The present invention relates to a process for the preparation of a salt of O-desmethylvenlafaxine comprising a) dissolving or suspending O-desmethylvenlafaxine in the form of its base in a liquid medium selected from the group of solvents and suspending agents,- b) contacting O-desmethylvenlafaxine with a pharmaceutically acceptable acid to form a pharmaceutically acceptable salt of O-desmethylvenlafaxine wherein the pharmaceutically acceptable acid is selected from the group consisting of HCl,HBr, H2SO4, H3PO4, acetic acid, adipic acid, galactaric acid, D-gluconic acid, glutamic acid, glutaric acid, glycolic acid, hippuric acid, lactic acid,oxalic acid, methanesulphonic acid, ethanesulphonic acid, p- toluenesulphonic acid, camphorsulphonic acid, benzenesulphonic acid, malonic acid, L-ascorbic acid, naphtalene-2-sulfonic acid and benzoic acid; and c) separating the pharmaceutically acceptable salt of 0- desmethylvenlaf axine from the liquid medium to recover the salt, and to pharmaceutical formulations containing these salts.

The present invention relates to a process for the preparation of a salt of O-desmethylvenlafaxine comprising a) dissolving or suspending O-desmethylvenlafaxine in the form of its base in a liquid medium selected from the group of solvents and suspending agents; b) contacting O-desmethylvenlafaxine with a pharmaceutically acceptable acid to form a pharmaceutically acceptable salt of O-desmethylvenlafaxine wherein the pharma-ceutically acceptable acid is selected from the group consisting of maleic acid, citric acid, tartaric acid and L-aspartic acid, optionally filtering the solution; and c) separating the pharmaceutically acceptable saltof 0- desmethylvenlaf axine from the liquid medium to recover the salt, and to pharmaceutical formulations containing these salts.

Cisteinske proteaze so encimi, ki sodelujejo v stevilnih fizioloskih procesih,njihovo nepravilno delovanje pa je povezano z doloèenimi bolezenskimiprocesi. Katepsina X in B sta edini karboksipeptidazi v tej druzini. Vloga katepsina B v organizmu je ze dobro raziskana, kar pa ne velja za katepsin X. Njegova prisotnost v celicah imunskega sistema kaze na vlogo pri imunskem odgovoru, vendar mehanizem delovanja se ni poznan. Z uporabo MTS testa smo doloèili vpliv katepsina B in katepsina X na proliferacijo in adhezijo promonocitnih U937 celic. Pri poskusih smo uporabili nespecifiène sintezne inhibitorje cisteinskih proteaz in pa nevtralizacijska monoklonska protitelesa proti katepsinu B oz. X. Vpliv na proliferacijo celic ni bil opazen pri nobenem od uporabljenih inhibitorjev. Drugaène rezultate pa smo dobili pri doloèanju vpliva cisteinskih proteaz na adhezijo U937 celic diferenciranih s 4Ž-forbol 12- miristat 13-acetatom. Delez adheriranih celic se je moèno zmanjsal z visanjem koncentracij inhibitorjev E-64 (splosni inhibitor cisteinskih proteaz), CA-074 in CA-074-Me (inhibitorja katepsina B in X) ter protiteles proti katepsinu X, nobenega uèinka pa nismo opazili pri nevtralizacijskih protitelesih proti katepsinu B. Kokosji cistatin, ki je moèan inhibitor katepsina B, manj pa katepsina X, je le delno zmanjsal adhezijo diferenciranih U937 celic. Nasi rezultati kazejo, da inhibitorji katepsina X, ne pa katepsina B, zavrejo adhezijo diferenciranih U937 celic, kar kaze na pomembno vlogo tega encima pri regulaciji imunskega odziva.