A water-swellable linear polymer is made by reacting together a polyethylene oxide of number average molecular weight less than 4,000, an aliphatic diol, and a difunctional diisocyanate. Controlled release composition comprises the polymer together with an active agent. The polymer is able to take u
A water-swellable linear polymer is made by reacting together a polyethylene oxide of number average molecular weight less than 4,000, an aliphatic diol, and a difunctional diisocyanate. Controlled release composition comprises the polymer together with an active agent. The polymer is able to take up pharmaceutically active agents of molecular weight 200 to 20,000.
대표청구항▼
1. A controlled-release composition, comprising: a water-swellable linear polymer together with an active agent, the water-swellable linear polymer obtained by reacting together:(a) a polyethylene oxide of number average molecular weight less than or equal to 4000 g/mol;(b) a C8 to C15 aliphatic dio
1. A controlled-release composition, comprising: a water-swellable linear polymer together with an active agent, the water-swellable linear polymer obtained by reacting together:(a) a polyethylene oxide of number average molecular weight less than or equal to 4000 g/mol;(b) a C8 to C15 aliphatic diol; and(c) a difunctional isocyanate,wherein the ratio of components (a) to (b) to (c) is in the range of 0.01-0.1 to 1 to 1.01-1.1 in terms of equivalent weights, the amount of the polyethylene oxide is less than 50 wt % of the polymer, the polymer has a water swelling percentage of 20-100%, and the composition is in a solid dosage form. 2. The composition of claim 1, wherein the polyethylene oxide is a diol of molecular weight 200 to 4000 g/mol. 3. The composition of claim 1, wherein the aliphatic diol is 1,10-decanediol or 1,12-dodecanediol. 4. The composition of claim 1, wherein the difunctional isocyanate is dicyclohexylmethane-4.4-diisocyanate, diphenylmethane-4,4-diisocyanate, or 1,6-hexamethylene diisocyanate. 5. The composition of claim 1, wherein the amount of the aliphatic diol exceeds 20 wt % of the polymer. 6. The composition of claim 1, wherein the amount of the difunctional isocyanate is 20-50 wt % of the polymer. 7. The composition of claim 1, wherein the dosage form is a suppository, vaginal ring or pessary, a bucchal insert, or a transdennal patch. 8. The composition of claim 1, wherein the dosage form is an implant. 9. The composition of claim 1, wherein the active agent is a pharmaceutically active agent of molecular weight in the range 200 to 20,000 g/mol. 10. The composition of claim 1, wherein: (a) is a polyethylene glycol having a molecular weight of 4000 g/mol;(b) is 1,10-decanediol; and(c) is dicyclohexylmethane-4,4-diisocyanate. 11. The composition of claim 1, wherein the amount of the polyethylene oxide is less than 30 wt % of the polymer. 12. A method of producing the composition of claim 1, comprising melting and drying the polyethylene oxide together with the aliphatic diol at a temperature of 85° C. to 100° C. under vacuum; and then adding the difunctional isocyanate.
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