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Details for Patent: 5,554,387

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Details for Patent: 5,554,387

Title: Sustained release heterodisperse hydrogel systems for insoluble drugs
Abstract:A sustained release pharmaceutical formulation includes a sustained release excipient including a gelling agent, an inert pharmaceutical diluent, an optional cationic cross-linking agent, and a medicament having moderate to poor solubility is disclosed. In certain embodiments, the sustained release excipient is granulated with a solution or suspension of a hydrophobic polymer in an amount effective to slow the hydration of the gelling agent when the formulation is exposed to an environmental fluid. In another embodiment, the tablet is coated with a hydrophobic polymer.
Inventor(s): Baichwal; Anand R. (Wappingers Falls, NY)
Assignee: Edward Mendell Co., Ltd. (Patterson, NY)
Filing Date:May 22, 1995
Application Number:08/447,236
Claims:1. A sustained release excipient, comprising:

a gelling agent comprising a heteropolysaccharide gum and a homopolysaccharide gum which crosslinks with said heteropolysaccharide gum when exposed to a fluid in an environment of use, the ratio of said heteropolysaccharide gum to said homopolysaccharide gum being from about 1:3 to about 3:1;

an inert pharmaceutical diluent selected from the group consisting of a monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert diluent to said gelling agent being from about 1:8 to about 8:1; and

a pharmaceutically acceptable cationic cross-linking agent capable of crosslinking with said gelling agent when exposed to an environmental fluid.

2. The sustained release excipient of claim 1, wherein said heteropolysaccharide gum comprises xanthan gum and said homopolysaccharide gum comprises locust bean gum.

3. The sustained release excipient of claim 1, wherein said cationic crosslinking agent comprises from about 1 to about 20 percent of said sustained release excipient, by weight.

4. The sustained release excipient of claim 1, wherein said gelling agent, said inert diluent, and said cationic cross-linking agent are granulated with a hydrophobic material selected from the group consisting of an alkylcellulose, a copolymer of acrylic and methacrylic acid esters, waxes, shellac, zein, hydrogenated vegetable oils, and mixtures of any of the foregoing, said hydrophobic material being included in an amount effective to slow the hydration of said gelling agent when exposed to an environmental fluid.

5. The sustained release excipient of claim 4, wherein said hydrophobic material is ethylcellulose.

6. A sustained release excipient comprising:

a sustained release excipient comprising from about 10 to about 99 percent by weight gelling agent, from about 0 to about 89 percent by weight of an inert pharmaceutically acceptable diluent selected from the group consisting of a monosaccharide, a di-saccharide, a polyhydric alcohol, and mixtures thereof, and from about 1 to about 20 by weight of a pharmaceutically acceptable cationic crosslinking agent capable of cross-linking with said gelling agent when exposed to an environmental fluid to increase the gel strength.

7. The sustained release excipient of claim 6, which comprises from about 10 to about 75 percent gelling agent, from about 2 to about 15 percent cationic crosslinking agent, and from about 30 to about 75 percent inert diluent.

8. The sustained release excipient of claim 6, which comprises from about 30 to about 75 percent gelling agent, from about 5 to about 10 percent cationic crosslinking agent, and from about 15 to about 65 percent inert diluent.

9. The sustained release excipient of claim 6, wherein said gelling agent comprises a heteropolysaccharide gum and a homopolysaccharide gum which crosslinks with said heteropolysaccharide gum when exposed to an environmental fluid, the ratio of said heteropolysaccharide gum to said homopolysaccharide gum being from about 3:1 to about 1:3.

10. The sustained release excipient of claim 9, wherein said heteropolysaccharide gum is xanthan gum and said homopolysaccharide gum is locust bean gum.

11. A sustained release excipient, comprising:

a gelling agent;

an inert pharmaceutical diluent selected from the group consisting of monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert diluent to said gelling agent being from about 1:8 to about 8:1;

said gelling agent and said inert pharmaceutical diluent being granulated with a hydrophobic material selected from the group consisting of an alkylcellulose, a hydrophobic cellulosic material, a copolymer of acrylic and methacrylic acid esters, shellac, waxes, zein and mixtures of any of the foregoing, prior to the incorporation of said medicament, said hydrophobic polymer being included in an amount effective to slow the hydration of said gelling agent when exposed to an environmental fluid.

12. The sustained release excipient of claim 11, wherein said gelling agent comprises xanthan gum and locust bean gum in a ratio from about 1:3 to about 3:1.

13. The sustained release excipient of claim 11, wherein said hydrophobic polymer is included in an amount from about 1 to about 20 percent, by weight.

14. The sustained release excipient of claim 11, wherein said hydrophobic polymer is included in an amount form about 1 to about 10 percent, by weight.

15. The sustained release excipient of claim 1 wherein said cationic crosslinking agent is selected from the group consisting of an alkali metal sulfate, an alkali metal chloride, an alkali metal borate, an alkali metal bromide, an alkali metal citrate, an alkali metal acetate, an alkali metal lactate, an alkaline earth metal sulfate, an alkaline earth metal chloride, an alkaline earth metal borate, an alkaline earth metal bromide, an alkaline earth metal citrate, an alkaline earth metal acetate, an alkaline earth metal lactate, and mixtures thereof.

16. The sustained release excipient of claim 1 wherein said cationic crosslinking agent comprises calcium sulfate.

17. The sustained release excipient of claim 6 wherein said cationic crosslinking agent is selected from the group consisting of an alkali metal sulfate, an alkali metal chloride, an alkali metal borate, an alkali metal bromide, an alkali metal citrate, an alkali metal acetate, an alkali metal lactate, an alkaline earth metal sulfate, an alkaline earth metal chloride, an alkaline earth metal borate, an alkaline earth metal bromide, an alkaline earth metal citrate, an alkaline earth metal acetate, an alkaline earth metal lactate, and mixtures thereof.

18. The sustained release excipient of claim 6 wherein said cationic crosslinking agent comprises calcium sulfate.
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