Water-swellable polymers
First Claim
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1. A controlled release composition, comprising a cross-linked polyurethane polymer loaded with misoprostol;
- wherein the cross-linked polyurethane polymer is formed from a polyethylene glycol, a triol and a diisocyanate, and at least about 80% of the misoprostol is released when the composition is immersed in water at 37°
C. for 480 minutes.
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Abstract
A water-swellable linear polyurethane polymer is formed by reacting a polyethylene oxide (e.g. PEG 4000 to 35,000), a difunctional compound (e.g. a diamine or diol such as 1,10-decanediol) with a diisocyanate. The ratio of the three components is generally in the range 0.1-1.5 to 1 to 1.1-2.5. The polyurethane is water-swellable in the range 300 to 1700% and soluble in certain organic solvents such as dichloromethane. It can be loaded with pharmaceutically active agents, particularly of high molecular weight, to produce controlled release compositions, such as pessaries etc.
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Citations
10 Claims
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1. A controlled release composition, comprising a cross-linked polyurethane polymer loaded with misoprostol;
wherein the cross-linked polyurethane polymer is formed from a polyethylene glycol, a triol and a diisocyanate, and at least about 80% of the misoprostol is released when the composition is immersed in water at 37°
C. for 480 minutes.
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2. The composition of claim 1, wherein the cross-linked polyurethane polymer is formed from PEG8000, hexanetriol and dicyclohexylmethane-4.4-diisocyanate.
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3. The composition of claim 2, wherein the ratio of PEG8000:
- hexanetriol;
dicyclohexylmethane-4.4-diisocyanate is in the range of 0.8-1.0;
1.0-1.2;
2.3-2.8.
- hexanetriol;
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4. The composition of claim 3, wherein the ratio of PEG8000:
- hexanetriol;
dicyclohexylmethane-4.4-diisocyanate is 1.0;
1.2;
2.8.
- hexanetriol;
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5. The composition of claim 3, wherein the ratio of PEG8000:
- hexanetriol;
dicyclohexylmethane-4.4-diisocyanate is 0.8;
1.0;
2.3.
- hexanetriol;
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6. The composition of claim 1, wherein the misoprostol content is 200 μ
- g.
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7. The composition of claim 1, wherein the composition is in the form of a pessary.
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8. The composition of claim 7, wherein the composition has been dried in a vacuum oven at room temperature for at least 24 hours.
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9. The composition of claim 7, wherein the composition has a misoprostol release rate of 4.507 minute−
- 0.5.
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10. The composition of claim 1, wherein the polyurethane polymer has a swellability of about 295%.
Specification