Details for Patent: 5,876,761
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| Title: | Sustained release formulations of water soluble peptides |
| Abstract: | The invention discloses microparticles comprising a polypeptide, preferably somatostatin or an analog or derivative thereof, more preferably octreotide, in a polymeric matrix, preferably poly(lactide-co-glycolide) glucose. The invention also discloses sustained release formulations containing said microparticles and the use of said formulations in treating acromegaly and breast cancer. |
| Inventor(s): | Bodmer; David (Klingnau, CH), Fong; Jones W. (Parsippany, NJ), Kissel; Thomas (Staufen, DE), Maulding; Hawkins V. (Mendham, NJ), Nagele; Oskar (Sissach, CH), Pearson; Jane E. (Ogdensburg, NJ) |
| Assignee: | Novartis AG (Summit, NJ) |
| Filing Date: | Jun 06, 1995 |
| Application Number: | 08/470,907 |
| Claims: | 1. A process for the production of microparticles comprising ostreotide distributed throughout, which comprises intensively mixing: a) a solution of octreotide in a weight/volume ratio of 2.5 g/10 ml in a buffer of pH 3-8 and b) a solution of a polylactide-co-glycolide in methylene chloride in a weight/volume ratio of 40 g/100 ml in such a manner that the weight/weight ratio of the drug to the polymer is 1/16 and the volume/volume ratio of the aqueous medium/organic solvent is 1/10, intensively mixing the w/o-emulsion of a) in b) together with c) an excess of a buffer of a pH 3-8, containing gelatine in a concentration of 0.5% of weight at a volume/volume mixing speed ratio of ab)/c) of 1/40, without adding any drug retaining substance to the water-in-oil emulsion or applying any intermediate viscosity increasing step, hardening the embryonic microparticles in the formed w/o/w-emulsion by evaporation of the methylene chloride and by isolating, washing and drying the generated microparticles. |
