Details for Patent: 8,067,030

Title:	Controlled release composition and method of producing the same
Abstract:	A controlled release composition containing a physiologically active substance in high content, suppressing the initial excess release, and achieving a stable release speed over a long period of time is provided. A controlled release composition comprising (1) a physiologically active substance or salt thereof in an amount of about 14% (w/w) to about 24% (w/w) based on the total composition weight, (2) hydroxynaphthoic acid selected from the group consisting of 3-hydroxy-2-naphthoic acid and 1-hydroxy-2-naphthoic acid or salt thereof, and (3) a lactic acid polymer or salt thereof having a weight-average molecular weight of 15000 to 50000 in which the content of polymers having molecular weights of 5000 or less is about 5% by weight or less, wherein the molar ratio of said hydroxynaphthoic acid or salt thereof to said physiologically active substance or salt thereof is from 3:4 to 4:3.
Inventor(s):	Yamamoto; Kazumichi (Kyoto, JP), Yamada; Akiko (Kyoto, JP), Hata; Yoshio (Hokkaido, JP)
Assignee:	Takeda Pharmaceutical Company Limited (Osaka, JP)
Filing Date:	Jul 29, 2008
Application Number:	12/181,472
Claims:	1. A method of treating prostatic cancer, prostatic hyperplasia, endometriosis, uterine myoma, uterine fibroma, precocious puberty, dysmenorrhea or breast cancer or a method of contraception, comprising administrating administering to a mammal in need thereof an effective amount of a controlled release composition comprising a LH-RH derivative or salt thereof wherein the LH-RH derivative is a peptide of the formula: 5-oxo-Pro-His-Trp-Ser-Tyr-Y-Leu-Arg-Pro-Z [wherein, Y represents DLeu, DAla, DTrp, DSer(tBu), D2Nal or DHis(ImBzl), and Z represents NH--C.sub.2H.sub.5 or Gly-NH.sub.2] or a salt thereof, and a lactic acid polymer or salt thereof having a weight-average molecular weight of 15,000 to 50,000, in which a content of polymers having molecular weights of 5,000 or less is about 5% by weight or less; wherein the controlled release composition does not contain hydroxynaphthoic acid or salt thereof. 2. A method of treating recurrence of breast cancer after an operation for premenopausal breast cancer, comprising administering to a mammal in need thereof an effective amount of a controlled release composition comprising a LH-RH derivative or salt thereof, and a lactic acid polymer or salt thereof wherein the LH-RH derivative is a peptide of the formula: 5-oxo-Pro-His-Trp-Ser-Tyr-Y-Leu-Arg-Pro-Z [wherein, Y represents DLeu, DAla, DTrp, DSer(tBu), D2Nal or DHis(ImBzl), and Z represents NH--C.sub.2H.sub.5 or Gly-NH.sub.2] or a salt thereof having a weight-average molecular weight of 15,000 to 50,000 in which the content of polymers having molecular weights of 5000 or less is about 5% by weight or less; wherein the controlled release composition does not contain hydroxynaphthoic acid or salt thereof. 3. The method according to claim 1, wherein the content of polymers having molecular weights of 3,000 or less in the lactic acid polymer is about 1.5% by weight or less. 4. The method according to claim 2, wherein the content of polymers having molecular weights of 3,000 or less in the lactic acid polymer is about 1.5% by weight or less. 5. The method according to claim 1, wherein the content of polymers having molecular weights of 1,000 or less in the lactic acid polymer is about 0.1% by weight or less. 6. The method according to claim 2, wherein the content of polymers having molecular weights of 1,000 or less in the lactic acid polymer is about 0.1% by weight or less. 7. The method according to claim 1, wherein the lactic acid polymer has a weight-average molecular weight of 15,000 to 40,000. 8. The method according to claim 2, wherein the lactic acid polymer has a weight-average molecular weight of 15,000 to 40,000. 9. The method according to claim 1, wherein the lactic acid polymer has a weight-average molecular weight of 17,000 to 26,000. 10. The method according to claim 2, wherein the lactic acid polymer has a weight-average molecular weight of 17,000 to 26,000. 11. The method according to claim 1, wherein the LH-RH derivative or salt thereof is contained in an amount of 3% (w/w) to 24% (w/w) in the controlled release composition. 12. The method according to claim 2, wherein the LH-RH derivative or salt thereof is contained in an amount of 3% (w/w) to 24% (w/w) in the controlled release composition. 13. The method according to claim 1, wherein the controlled release composition is for injection. 14. The method according to claim 2, wherein the controlled release composition is for injection.