Sustained-release composition and method for producing the same

摘要

Sustained-release compositions wherein a water-soluble physiologically active peptide is substantially uniformly dispersed in a microcapsule comprised of a lactic acid polymer or a salt thereof, and the physiologically active substance is contained in an amount of 15 to 35 wt/wt % to the total microcapsules and weight-average molecular weight (Mw) of the lactic acid polymer is about 11,000 to about 27,000, which is characterized by having a high content of the physiologically active substance, and suppression of the initial excessive release within one day after the administration and a stable drug sustained-release over a long period of time, and method for producing the same.

主权项

1. A method for treating prostate cancer, prostatic hyperplasia, endometriosis, uterine fibroid, uterine fibroma, precocious puberty, dysmenorrhea, or breast cancer, or a method of contraception, comprising administering to a mammal an effective amount of a sustained-release composition in which a physiologically active substance, which is a peptide of formula: 5-oxo-Pro-His-Trp-Ser-Tyr-DLeu-Leu-Arg-Pro-NH—C2H5 or an acetate thereof, is substantially uniformly dispersed in a microcapsule comprised of a lactic acid polymer or a salt thereof, wherein the physiologically active substance is contained in an amount of 15 to 35 (weight/weight) % to the total microcapsules, weight-average molecular weight (Mw) of the lactic acid polymer is about 11,000 to about 27,000, and the sustained-release composition further contains stearic acid.