Organic compounds

• US 20020098238A1
• Filed: 01/22/2002
• Published: 07/25/2002
• Est. Priority Date: 08/01/1990
• Status: Abandoned Application

• Current Assignee: Walter Prikoszovich
• Original Assignee: Walter Prikoszovich
• Inventors: Prikoszovich, Walter
• Application Number:
  US10/054,490
• Publication Number:
  US 20020098238A1
• Time in Patent Office: Days
• US Class Current: 424/486
• CPC Class Codes: A61K 9/1647 Polyesters, e.g. poly(lactide-co-glycolide)
• CPC Class Codes: C08G 63/08 Lactones or lactides
• CPC Class Codes: C08G 63/90 Purification; Drying

Abstract

A polylactide in a purified state, which meets the requirements of

the color strengths of reference solutions B₂-B₉ of the brown colour test of the European Pharmacopoeia, 2nd Edition (1980) part I, Section V, 6.2 and

containing one or more metals in cationic form, the metal ion(s) having a concentration of at most 10 ppm.

The polylactide is especially suitable for use as microparticles or implants, and contains preferably a hydrophilic drug, like octreotide or a lipophilic drug like bromocriptine.

Claims

1. A polylactide in a purified state, which meets the requirements of

the colour strengths of reference solutions B₂-B₉ of the brown colour test of the European Pharmacopoeia, 2nd Edition (1980) part I, Section V, 6.2 and

containing one or more metals in cationic form, the metal ion(s) having a concentration of at most 10 ppm.

2. A polylactide according to claim 1, having the colour strength of reference solutions B₄-B₉.

3. A polylactide according to claim 2, having the colour strength of reference solution B₉.

4. A polylactide according to claim 1, in which the metal ion is Sn⁺⁺.

5. A polylactide according to claim 4, having a Sn⁺⁺ concentration of at most 1.5 ppm.

6. A polylactide according to claims 4, in which the Sn⁺⁺ accompanying salt anion is ethyl hexanoate.

7. A polylactide according to claim 6, having an ethyl hexanoate concentration of at most 0.5% by weight of the polylactide.

8. A polylactide according to claim 1, having a

9. A polylactide according to claim 1, containing additionally glycolide units.

10. A polylactide according to claim 9, having lactide/glycolide molar ratio'"'"'s of 100-25/0-75.

11. A polylactide according to claim 10, having molar rations of 75-25/25-75.

12. A polylactide according to claim 11, having molar ratio'"'"'s of 60-40/40-60.

13. A polylactide according to claim 1, being an ester of a polyol containing at least 3 hydroxyl groups.

14. A polylactide according to claim 13, being an ester of a sugar or of a sugar alcohol.

15. A polylactide according to claim 13, being a glucose ester.

16. A polylactide according to claims 1, being a linear polylactid-glycolide.

17. A polylactide according to claims 13 having a mean molecular weight M_w of from 10000 to 200000.

18. A polylactide according to claim 13, having a polydispersity Mw/Mn of from 1.7 to 3.0.

19. A polylactide according to claim 16, having a mean molecular weight M_w of from 25,000 to 100,000.

20. A polylactide according to claim 16, having a polydispersity Mw/Mn of from 1.2 to 2.0

21. A polylactide according to claim 1, obtained by contacting a solution of the impure polylactide with a matrix having on its surface acidic groups.

22. A method for obtaining the polylactide according to claim 1, by contacting a solution of the impure polylactide with a matrix having on its surface carboxylic groups and isolating the purified polylactide from the eluate.

23. A method for obtaining the polylactide according to claim 1, by contacting a solution of the impure polylactide with active charcoal and isolating the purified polylactide from the eluate.

24. A method according to claim 23, in which the isolation includes a further purification step, which is ultrafiltration.

25. A method according to claim 23 in which the impure polylactide is dissolved in acetone.

26. A pharmaceutical composition containing a polylactide according to claim 1 as a matrix for a drug compound.

27. A pharmaceutical composition according to claim 26, comprising bromocriptine as the drug compound.

28. A pharmaceutical composition according to claim 26, comprising a peptide as the drug compound.

29. A pharmaceutical composition according to claim 28, comprising a somatostatin as the drug compound.

30. A pharmaceutical composition according to claim 29, comprising octreotide or an acid addition salt or a derivative therof.

31. Process for the preparation of the pharmaceutical composition of claim 26, which comprises working up the polylactide of claim 1 with the drug compound to form an implantate or a microparticle.