Granted Patent B2

US 8,211,466 · App. 12/707,369 · Granted Jul 3, 2012

Abstract

Claims (33)

1. A mucosal bioadhesive slow release carrier formulation comprising

(I) at least one antiviral agent, wherein said antiviral agent is:

(i) valacyclovir, gancyclovir and zidovudine in an amount of 10 mg to 200 mg, or

(ii) acyclovir in an amount of 10 mg to 500 mg;

(II) 1% to 75% by weight of microcrystalline cellulose;

(III) 2% to 10% by weight of sodium lauryl sulphate;

(IV) 0.5% to 5% by weight of polyvinylpyrrolidone;

(V) 10% to 40% by weight of natural milk proteins; and

(VI) 10% to 40% by weight of hypromellose,

said mucosal bioadhesive slow release carrier formulation being obtained by a process comprising the steps of:

(a) mixing said at least one antiviral agent with said sodium lauryl sulfate and said microcrystalline cellulose, thereby producing a mixture;

(b) wetting said mixture of (a) with said polyvinylpyrrolidone;

(c) drying and calibrating said mixture of (b);

(d) granulating said mixture of (c) to form primary granules;

(e) blending said primary granules with said natural milk proteins and said hypromellose and at least one compression agent; and

(f) compressing said blended granules of (e).

2. The mucosal bioadhesive slow release carrier formulation according to claim 1 , in which said antiviral agent is acyclovir in an amount of 10 mg to 500 mg.

3. The mucosal bioadhesive slow release carrier formulation according to claim 2 in which said acyclovir is present in an amount from 10 mg to 200 mg.

4. The mucosal bioadhesive slow release carrier formulation according to claim 2 , in which said acyclovir is present in an amount from 50 mg to 100 mg.

5. The mucosal bioadhesive slow release carrier formulation according to claim 2 , which is devoid of lactose and of corn starch.

6. The mucosal bioadhesive slow release carrier formulation according to claim 1 , which further comprises a second active principle selected from: an antiviral, an antifungal, an analgesic, an anaesthetic, an antalgic, an antiemetic, a salivation agent, an antiseptic, an anti-inflammatory, an antibiotic and mixtures thereof.

7. A method of treating a viral mucosal disease, selected from orofacial herpes, herpes simplex complex 1 (HSV-1) infection, genital herpes (HSV-2) infection, and oral hairy leukoplakia comprising:

administering to a patient in need thereof a therapeutically effective amount of the mucosal bioadhesive slow release carrier formulation of claim 1 .

8. The method of claim 7 , wherein the viral mucosal disease is a buccal disease.

9. A method of treating a viral infection, wherein said virus is selected from herpes simplex complex 1 (HSV-1), genital herpes (HSV-2), varicella zoster virus (VZV), Epstein-Barr virus, human herpes virus 8, avian influenza, mumps, HIV, respiratory syncitial virus, influenza virus, parainfluenza virus and cytomegalovirus, comprising: administering to a patient in need thereof a therapeutically effective amount of the mucosal bioadhesive slow release carrier formulation of claim 1 .

10. A method for preparing a mucosal bioadhesive slow release carrier formulation according to claim 1 , the method comprising:

(a) mixing at least one antiviral agent with sodium lauryl sulphate and microcrystalline cellulose, thereby producing a mixture;

(b) wetting said mixture of (a) with polyvinylpyrrolidone;

(c) drying and calibrating said mixture of (b);

(d) granulating said mixture of (c) to form primary granules;

(e) blending said primary granules with natural milk proteins and hypromellose and at least one compression agent; and

(f) compressing said blended granules of (e).

11. The method according to claim 10 , wherein a second active principle selected from: an antiviral, an antifungal, an analgesic, an anaesthetic, an antalgic, an antiemetic, a salivation agent, an antiseptic, an anti-inflammatory, an antibiotic and mixtures thereof, is mixed with said antiviral agent, sodium lauryl sulphate, and microcrystalline cellulose in step (a).

Assignments (8)