Abstract: The present invention relates to a process for commercial production of octreotide using solution peptide chemistry and inexpensive amino acid derivatives. Thus the hexapeptide (Boc) D-Phe-Cys(Acm)-Phe-D-Trp-Lys(Boc)-Thr-OMe is synthesized by condensation of two tripeptide fragments, saponified and condensed with Cys(Acm)-Thr-OL to give the linear octapeptide alcohol. The linear peptide alcohol is treated with iodine, after removal of Boc groups, to give the cyclic peptide octreotide. The linear octapeptide alcohol can alternately be made by condensation of the protected hexapeptide acid with the dipeptide Cys(Acm)-Thr-OMe, followed by reduction with sodium borohydride.

Abstract: The present invention relates to a process for commercial production of octreotide using solution peptide chemistry and inexpensive amino acid derivatives. Thus the hexapeptide (Boc) D-Phe-Cys(Acm)-Phe-D-Trp-Lys(Boc)-Thr-OMe is synthesized by condensation of two tripeptide fragments, saponified and condensed with Cys(Acm)-Thr-OL to give the linear octapeptide alcohol. The linear peptide alcohol is treated with iodine, after removal of Boc groups, to give the cyclic peptide octreotide. The linear octapeptide alcohol can alternately be made by condensation of the protected hexapeptide acid with the dipeptide Cys(Acm)-Thr-OMe, followed by reduction with sodium borohydride.

Abstract: A ready-to use, stable, gelled polymer droplet-in-oil dispersion is described which helps in in-situ formation of a multitude of small solid, semisolid, or gelled microcarriers. The dispersion is placed into a body in a semisolid form and cures to form the delivery system in-situ. The process for making such a dispersion comprises the steps of (i) dissolving a polymer in a biocompatible solvent at an elevated temperature to form a polymer solution, (ii) preparing a second oil phase solution of a biocompatible oil and a biocompatible emulsifier at an elevated temperature, (iii) mixing the polymer solution with the oil phase solution at an elevated temperature and subsequently cooling to refrigeration temperature. Placing the gelled dispersion within a body produces the microcarrier delivery system in-situ.