United States Patent (19) 11 Patent Number: 5,981,489 Stevenson Et Al
USOO5981489A United States Patent (19) 11 Patent Number: 5,981,489 Stevenson et al. (45) Date of Patent: Nov. 9, 1999 54) NON-AQUEOUS PROTIC PEPTIDE Okada, et al., “Preparation of Three-Month Depot Injectable FORMULATIONS MicroSpheres of Leuprorelin Acetate Using Biodegradable Polymers”, Pharmaceutical Research, 11/8, pp. 1143–1147 75 Inventors: Cynthia L. Stevenson, Mountain View; (1994). Sally A. Tao, San Jose; Steven J. Okada, et al., “New Degradation Product of Prestrelski, Mountain View; James B. Des-Gly'-NH-LH-RH-Ethylamide (Fertirelin) in Aque Eckenhoff, deceased, late of Los Altos, ous Solution”, J. of Pharmaceutical Sciences, 80/2, pp. by Bonnie J. Eckenhoff, executrix; 167–170 (1991). Jeremy C. Wright, Los Altos; John J. Oyler, et al., “Characterization of the Solution Degradation Leonard, Jr., Cupertino, all of Calif. Products of Histrelin, a Gonadotropin Releasing Hormone (LH/RH) Agonist”, J. of Pharmaceutical Sciences, 80/3, pp. 73 Assignee: Alza Corporation, Palo Alto, Calif. 271-275 (1991). Powell, et al., “Peptide Liquid Crystals: Inverse Correlation 21 Appl. No.: 08/874,680 of Kinetic Formation and Thermodynamic Stability in Aque ous Solution”, Pharmaceutical Research, 11/9, pp. 22 Filed: Jun. 13, 1997 1352–1354 (1994). Related U.S. Application Data Powell, et al., “Parenteral Peptide Formulations: Chemical and Physical Properties of Native Luteinizing Hormone-R- 60 Provisional application No. 60/022,129, Jul. 3, 1996. eleasing Hormone (LHRH) and Hydrophobic Analogues in 51 Int. Cl. ........................... A61K38/00; CO7K5/00; Aqueous Solution”, Pharmaceutical Research, 8/10, pp. CO7K 7/00 1258–1263 (1991). 52 U.S. Cl. ............................. 514/15; 530/313; 530/328 Powers, et al., “Solution Behavior of Leuprolide Acetate, an 58 Field of Search .......................
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