Process for preparing microparticles using drug-polymer covalent conjugates

摘要

A process for preparing controlled release microsphere comprises: (a) adding drug into the polymer soln.; (b) reacting it in the presence of chemical catalyst to form the drug-polymer covalent complex (I); (c) suspending the obtd. (I) in the organic solvent to obtain the emulsified soln.; (d) hardening the (I) by heating at 80-170 deg.C or reacting the emusified soln. chemically; (e) replacing the surface of (I) with polr radical and centrifuging to obtain the precipitate; (f) washing the precipitate and freeze-drying to obtain the final product. The polymer is protein (e.g. serum albumin), sythetic polypeptide (e.g. poly-L-glutamic acid) or polysaccaride (e.g. dextran). The obtd. microsphere is useful as medicine, food additive etc.