.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 5,017,382

« Back to Dashboard

Details for Patent: 5,017,382

Title: Controlled release compositions (II)
Abstract:A process for the preparation of a controlled release composition comprising a prostaglandin and a polymeric carrier therefor comprising residues having a ratio of number average molecular weight to functionality greater than 1,000 which comprise polyethylene oxide and are cross-linked through urethane groups.
Inventor(s): Embrey; Mostyn P. (Oxford, GB2), Graham; Neil B. (Dunbartonshire, GB6)
Assignee: National Research Development Corporation (London, GB2)
Filing Date:Jan 23, 1990
Application Number:07/469,045
Claims:1. A process for the preparation of a controlled release composition, which composition comprises a prostaglandin and a polymeric carrier therefor, said polymeric carrier comprising residues having a ratio of number average molecular weight to functionality greater than 1,000 which comprise polyethylene oxide and are cross-linked through urethane groups, said process comprising:

(i) contacting said polymeric carrier with a solution of a prostaglandin and permitting said polymeric carrier to swell therein; and

(ii) removing the swollen polymeric carrier from said solution thereby obtaining a controlled release composition comprising the prostaglandin.

2. The process of claim 1, wherein, subsequent to removal from said solution, said swollen polymeric carrier is dried.

3. The process of claim 1, wherein the swelling of said polymeric carrier is from 200 to 700 parts by volume per hundred of the initial dry volume.

4. The process of claim 1, wherein said swelling is effected at a temperature of from -20.degree. C. to +20.degree. C.

5. The process of claim 1, wherein said controlled release composition comprises a prostaglandin and a polymeric carrier therefor comprising residues which are cross-linked through urethane groups, or analogues thereof, and which comprise polyethylene oxide having a ratio of number average molecular weight to functionality greater than 1,500, the degree of cross-linking being such that there is at least one cross-linking point per ten residues comprising the said polyethylene oxide but such that the proportion of the said polyethylene oxide is greater than 50% by weight of the polymeric carrier which, when prostaglandin-free, is a hydrogel, in the dry form at 20.degree. C. contains crystalline regions, and exhibits syneresis in the wet form.

6. The process of claim 1, wherein said controlled release composition comprises a prostaglandin and a polymeric carrier therefor comprising residues which are cross-linked through urethane groups, or analogues thereof, and which comprise polyethylene oxide having a ratio of number average molecular weight to functionality greater than 1,500, the degree of cross-linking being such that there is at least one cross-linking point per ten residues comprising the said polyethylene oxide but such that the proportion of the said polyethylene oxide is greater than 50% by weight of the polymeric carrier which, in the presence of said prostaglandin, is a hydrogel, in the dry form at 20.degree. C. contains crystalline regions, and exhibits syneresis in the wet form.

7. The process of claim 5, said controlled release composition further comprising an additional drug other than a prostaglandin.

8. The process of claim 6, said controlled-release composition further comprising an additional drug other than a prostaglandin.

9. The process of claim 5, wherein the polyethylene oxide has a ratio of number average molecular weight to functionality greater than 2,000.

10. The process of claim 5, wherein the polyethylene oxide is the reaction product of a mixture comprising (i) an aliphatic or aromatic compound which is di-, tri- or tetra-substituted by at least one hydroxyl, carboxyl, amino or mercapto group with (ii) ethylene oxide.

11. The process of claim 10, wherein component (i) comprises a di- or tri- hydroxyl-substituted aliphatic compound.

12. The process of claim 5, wherein the degree of cross-linking of the polymeric carrier is such that there is at least one cross-linking point per five residues comprising the said polyethylene oxide.

13. The process of claim 5, wherein the degree of cross-linking of the polymeric carrier is such that there is at least one cross-linking point per residue comprising the said polyethylene oxide.

14. The process of claim 5, wherein the degree of cross-linking of the polymeric carrier is such that the proportion of the said polyethylene oxide is greater than 70% by weight of the polymeric carrier.

15. The process of claim 5, wherein the degree of cross-linking of the polymeric carrier is such that the proportion of the said polyethylene oxide is greater than 80% by weight of the polymeric carrier.

16. The process of claim 5, wherein the polymeric carrier comprises up to 20% by weight of an additional polyalkylene oxide.

17. The process of claim 5, wherein the polymeric carrier comprises up to 20% by weight of an additional polyethylene oxide having a ratio of number average molecular weight to functionality not greater than 1000.

18. The process of claim 5, wherein the polymeric carrier comprising up to 30% of its weight of a water-extractable fraction.

19. The process of claim 5, wherein the amount of water-extractable fraction has been reduced to no more than 5% of the polymeric carrier.

20. The process of claim 5, wherein the prostaglandin is naturally-occurring prostaglandin of the E and F.sub..alpha. groups.

21. The process of claim 20, wherein the prostaglandin is PGE.sub.2 or PGF.sub.2.alpha..

22. The process of claim 5, wherein the prostaglandin is a synthetic analogue.

23. The process of claim 22, wherein the prostaglandin is 15-methyl-PGF.sub.2.alpha., 16,16-dimethyl-PGE.sub.2, 16,16-dimethyl-PGE.sub.2 parabenzaldehyde semicarbazone ester, 16-phenoxy-17,18,19,20-tetranor-PGE.sub.2, 16,16-dimethyl-trans-.DELTA..sup.2 -PGE, and its methyl ester or 16-(3-trifluoromethylphenoxy)-17,18,19,20-tetranor-PGF-.sub.2.alpha..

24. The process of claim 5, wherein said composition is in the shape of a cylinder, film or slab.

25. The process of claim 24, wherein the cylinder is hollow or the film or slab has at least one hole or hollow therein to modify the release properties.

26. The process of claim 5, said composition for use as an abortifacient.

27. The process of claim 5, said composition for use in the induction of labor.

28. The process of claim 5, said composition for use as a contraceptive.

29. The process of claim 5, said composition for use in the treatment of schizophrenia.

30. The process of claim 5, said composition for use in the treatment of cervical incompetence in livestock.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc