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Last Updated: March 28, 2024

Details for Patent: 8,815,801


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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 13, 2012
Application Number:13/548,463
Claims:1. A medicine which comprises a controlled release composition comprising a physiologically active substance or salt thereof, and 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 controlled release composition does not contain hydroxynaphthoic acid or a salt thereof.

2. The medicine according to claim 1, wherein the controlled release composition comprises (1) a physiologically active substance or salt thereof in an amount of about 3% (w/w) to about 24% (w/w) based on the total composition weight, and (2) 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.

3. The medicine according to claim 1, wherein the lactic acid polymer has a content of polymers having molecular weights of 3000 or less is about 1.5% by weight or less.

4. The medicine according to claim 1, wherein the lactic acid polymer has a content of polymers having molecular weights of 1000 or less is about 0.1% by weight or less.

5. The medicine according to claim 1, wherein the lactic acid polymer has a weight-average molecular weight of 15000 to 40000.

6. The medicine according to claim 1, wherein the lactic acid polymer has a weight-average molecular weight of 17000 to 26000.

7. The medicine according to claim 1, wherein the physiologically active substance is a physiologically active peptide.

8. The medicine according to claim 7, wherein the physiologically active substance is a LH-RH derivative.

9. The medicine according to claim 8, 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.

10. The medicine according to claim 8, 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.

11. The medicine according to claim 1, wherein the controlled release composition is used for injection.

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