You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 28, 2024

Claims for Patent: 5,128,143


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 5,128,143
Title: Sustained release excipient and tablet formulation
Abstract:A slow release pharmaceutical excipient of an inert diluent and a hydrodrophilic material including xanthan gum and a galactomannan gum capable of cross-linking the xanthan gum in the presence of aqueous solutions.
Inventor(s): Baichwal; Anand R. (Poughkeepsie, NY), Staniforth; John N. (Bath, GB2)
Assignee: Edward Mendell Co., Inc. (Patterson, NY)
Application Number:07/491,189
Patent Claims: 1. A controlled release pharmaceutical excipient for use in oral solid dosage forms, comprising

from about 20 to about 60 percent by weight of a hydrophilic material comprising xanthan gum and a galactomannan gum capable of cross-linking said xanthan gum in the presence of aqueous solutions, the ratio of said xanthan gum to said galactomannan gum being from about 3:1 to about 1:3, and

from about 40 to about 80 percent by weight of an inert 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 hydrophilic material being from about 4:1 to about 0.67:1.

2. A controlled-release tablet for absorption of an active medicament in the gastrointestinal tract, comprising

a controlled-released excipient comprising a hydrophilic gum matrix comprising a xanthan gum and a galactomannan gum capable of cross-linking said xanthan gum when exposed to gastric fluid, the ratio of said xanthan gum to said galactomannan gum being from about 3:1 to doubt 1:3, and an inert diluent, the ratio of said inert diluent to said hydrophilic gum matrix being from about 4:1 to about 0.67:1, and an effective amount of a medicament to render a therapeutic effect, the ratio of said medicament to said hydrophilic gum matrix being from about 1:3 to about 1:10.

3. The excipient of claim 1, wherein said galactomannan comprises locust bean gum.

4. The excipient of claim 1, wherein said inert pharmaceutical filler comprises lactose, dextrose, sucrose, fructose, microcrystalline cellulose, xylitol, sorbitol or mixtures thereof.

5. The excipient of claim 1 to which an effective amount of a therapeutically active medicament is added.

6. The excipient of claim 1, wherein an effective amount of a therapeutically active medicament is added via dry granulation, yet granulation or a combination of dry and wet granulation and the resultant granulation is compressed to form solid tablets.

7. The excipient of claim 3, wherein said hydrophilic material further comprises one or more of tragacanth, acacia, karaya, alginates, agar, pectin, guar, hydroxypropyl guar, carrageenan, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, methylcellulose, carboxymethyl cellulose, polyvinyl pyrollidone, and mixtures of any of the foregoing.

8. The excipient of claim 3, wherein said hydrophilic material further comprises propylene glycol alginate.

9. The excipient of claim 3, wherein said hydrophilic material further comprises a hydrocolloid, said hydrocolloid comprising up to about 50% by weight of said hydrophilic material.

10. The excipient of claim 1, wherein an effective amount of a therapeutically active medicament is added and the resulting mixture is encapsulated.

11. The excipient of to claim 1, wherein an effective amount of a therapeutically active ingredient is added and the resulting mixture provides a zero order controlled release when provided as a solid dosage form.

12. The excipient of claim 3, wherein said ratio of xanthan gum to locust bean gum is about 1:1.

13. A slow release pharmaceutical excipient, for use in solid oral dosage forms comprising

a hydrophilic gum matrix comprising xanthan gum and locust bean gum in a ratio of about 3:1 to about 1:3; and

an inert diluent, the ratio of said inert diluent to said hydrophilic gum matrix being from about 2.3:1 to about 1:1.

14. The tablet of claim 2, wherein said galactomannan gum is locust bean gum.

15. The tablet of claim 2, wherein said medicament is added to said excipient via dry granulation, wet granulation or a combination of dry and wet granulation.

16. A controlled release tablet for oral administration comprising

(I) from about 20 to about 60 percent by weight of a hydrophilic material comprising from about 10 to about 90 percent of a heteropolysaccharide and from about 90 to about 10 percent of a cross-linking agent capable of cross-linking said heteropolysaccharide; and

(II) up to about 80 percent of an inert pharmaceutical filler selected from the group consisting of a monosaccharide, a disaccharide, a polyhydric alcohol, and mixtures thereof, the ratio of said inert pharmaceutical filler to said hydrophilic material being from about 4:1 to about 0.67:1; and

(III) an effective amount of a therapeutically active medicament to render a therapeutic effect.

17. The tablet of claim 16, wherein said heteropolysaccharide comprises xanthan gum and said cross-linking agent comprises a galactomannan.

18. The tablet of claim 17, wherein at least 3.5 hours ar required for 50 percent of said therapeutically active medicament to be released when said tablet is exposed to gastric fluid.

19. The tablet of claim 17, wherein said tablet provides a zero order controlled release of said therapeutically active medicament when said tablet is exposed to gastric fluid.

20. The tablet of claim 17, wherein said galactomannan comprises locust bean gum, and the ratio of xanthan gum to locust bean gum is about 1:1.

21. The tablet of claim 17, wherein said inert pharmaceutical filler comprises lactose, dextrose, sucrose, fructose, xylitol, sorbitol or mixtures thereof.

22. The tablet of claim 17, wherein said hydrophilic material further comprises a polysaccharide gum selected from the group consisting of tragacanth, acacia, karaya, alginates, agar, pectin, carrageenan, hydroxypropylmethyl cellulose, hydroxypropyl cellulose, methylcellulose, carboxymethyl cellulose, polyvinyl pyrollidone, and mixtures of any of the foregoing.

23. The tablet of claim 22, wherein said hydrophillic material further comprises propylene glycol alginate.

24. The tablet of claim 22, wherein said hydrophilic material further comprises a hydrocolloid.

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.