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Details for Patent: 4,894,238

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Details for Patent: 4,894,238

Title: Controlled release compositions
Abstract:A controlled release composition comprising an active substance other than a prostaglandin and a polymeric carrier therefor comprising residues having a ratio of number average molecular weight to functionality greater than 1000 which comprises polyethylene oxide and are cross-linked through urethane groups.
Inventor(s): Embry; Mostyn P. (Woodstock, GB3), Graham; Neil B. (Bearsden, GB6)
Assignee: National Research Development Corporation (London, GB2)
Filing Date:Jun 14, 1988
Application Number:07/208,849
Claims:1. A controlled release composition comprising an active substance other than a prostaglandin, and a polymeric carrier therefore 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 is a crystalline hydrogel in the dry form and exhibits syneresis in the wet form.

2. The controlled release composition according to claim 1, wherein the polyethylene oxide has a ratio of number average molecular weight to functionality greater than 2,000.

3. The composition according to claim 1, wherein the polyethylene oxide is the reaction product of a mixture comprising:

(i) an aliphatic or aromatic compound which is di-, tri- or tetrasubstituted by at least one of hydroxyl, carboxyl, amino or mercapto groups with (ii) ethylene oxide.

4. The composition according to claim 3, wherein:

(i) comprises a di- or tri- hydroxyl-substituted aliphatic compound.

5. The composition according to claim 1, 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.

6. The composition according to claim 1, 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.

7. The composition according to claim 1, 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.

8. The composition according to claim 1, 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.

9. The composition according to claim 1, wherein the polymeric carrier comprises up to 20% by weight of an additional polyalkylene oxide.

10. The composition according to claim 1, 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.

11. The composition according to claim 1, wherein the polymeric carrier comprises up to 30% of its weight of a water-extractable fraction.

12. The composition according to claim 11, wherein the amount of water-extractable fraction has been reduced to no more than 5% of the polymeric carrier.

13. The composition according to claim 1, wherein the drug is a hypnotic, sedative, tranquilliser, anti-pyretic, anti-inflammatory agent, anti-histamine, anti-tussive, agent for the treatment of malignant neoplastia, topical or dermatological agent, diuretic agent, anti-depressant, anti-fungal agent, steriod or analgesic.

14. The composition according to claim 1, in the shape of a cylinder, film or slab.

15. The composition according to claim 14, wherein the cylinder is hollow or the film or slab has at least one hole or hollow therein to modify the release properties.

16. The composition according to claim 1, wherein the active substance comprises a fungicide, algaecide, herbicide, nematocide or insecticide.

17. The composition according to claim 1, wherein the active substance is lithium.

18. The composition according to claim 1, wherein the active substance comprises a polymerization inhibitor.
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