Readily available konjac glucomannan as a sustained release excipient

• US 5,486,364 A
• Filed: 08/15/1994
• Issued: 01/23/1996
• Est. Priority Date: 12/30/1992
• Status: Expired due to Fees

• Current Assignee: FMC Corporation
• Original Assignee: FMC Corporation
• Inventors: King, Victor L., Erkoboni, David F., Wheatley, Thomas A.
• Primary Examiner(s): Webman, Edward J.
• Application Number:
  US08/290,457
• Time in Patent Office: 526 Days
• Field of Search: 424/488, 424/409, 424/464, 424/465, 424/499, 424/195.1, 424/78.17, 424/78.38, 514/960, 514/961, 514/777, 514/54, 426/72, 426/73, 426/658, 536/114, 536/127, 536/128
• US Class Current: 424/488
• CPC Class Codes: A61K 9/205 Polysaccharides, e.g. alginate, gums; Cyclodextrin

Abstract

A solid dosage form, such as a pharmaceutical tablet, containing a rapidly hydratable konjac glucomannan sustained release excipient such as clarified konjac, cryogenically ground konjac and plasticized konjac. The method of making the tablets by compressing excipient and pharmaceutically active ingredient as dry powders.

Claims

1. A solid dosage form, comprising an active ingredient and a sustained release excipient which excipient is at least 7 weight percent of a readily available konjac glucomannan based on the weight of the solid dosage form, wherein the dosage form contains no gas producing disintegrant.

2. The solid dosage form of claim 1, wherein:

the amount of readily available konjac glucomannan sustained release agent is 7 to 50 wt%, and

the readily available konjac glucomannan and the active were compounded dry without having been previously conditioned by wetting of hydrating.

3. The solid dosage form of claim 2, further including xanthan gum, wherein the weight ratio of readily available konjac glucomannan to xanthan gum is within the range of from 15:

1 to 5;

1 and the sustained release time within the range of 3 to 12 hours at a pH within the range of 1 to 7.4.

4. The solid dosage form of claim 2, further including xanthan gum, wherein the weight ratio or readily available konjac glucomannan to xanthan gum is within the range of 12:

1 to 6;

1.

5. The solid dosage form of claim 1, wherein:

the amount of readily available konjac glucomannan sustained release agent is 10 to 40 wt%; and

the readily available konjac glucomannan and the active were compounded dry without having been previously conditioned by wetting or hydrating.

6. The solid dosage form of claim 5, further including xanthan gum, and wherein the weight ratio of readily available konjac glucomannan to xanthan gum is within the range of 20:

1 to 1;

1 and exhibits a sustained time release at a pH of approximately I to 7.4.

7. The solid dosage form of claim 5 further including xanthan gum, wherein:

the readily available konjac is a rapidly hydratable konjac

the ratio of rapidly hydratable konjac sustained release excipient to xanthan gum is within the range of from 12;

1 to 6;

1, and

the sustained release time is within the range of from 3 to 10 hours.

8. The solid dosage form of claim 5, wherein the readily available konjac is selected from the group consisting of clarified konjac, cryogenically ground konjac, and plasticized konjac.

9. The solid dosage form of claim 1, further including xanthan gum, and

wherein:

the weight ratio of readily available konjac glucomannan to xanthan gum is within the range of 20;

1 to 1;

1; and

the readily available konjac glucomannan, xanthan gum and the active were compounded dry without having been previously conditioned by wetting or hydrating.

10. The solid dosage form of claim 9, wherein the readily available konjac glucomannan is selected from the group consisting of clarified konjac, cryogenically ground konjac, and plasticized konjac.

11. The solid dosage form of claim 9, wherein the solid dosage form has a sustained release time within the range 3 to 12 hours at a pH within the range of 1 to 7.4.

12. The solid dosage form of claim 1, wherein the readily available konjac glucomannan is selected from the group consisting of clarified konjac, cryogenically ground konjac, and plasticized konjac.

13. Solid dosage forms as in any of claims 1 to 8 in the form of a tablet.

14. Solid dosage forms as in any of claims 1 to 8, wherein the active ingredient is a pharmaceutically active ingredient and wherein the solid dosage form is a tablet.

15. A method for making a pharmaceutical tablet comprising the steps of forming a mixture of a dry pharmaceutically active ingredient with a sustained release excipient of at least 7 weight percent of a dry, readily available konjac glucomannan, and compressing the dry mixture at a pressure sufficient to form a table with a hardness of at least 6 kg, wherein no gas producing disintegrant is included in the tablet.

16. The method of claim 15, wherein the readily available konjac glucomannan excipient is within the range of from 7 to 50 wt %.

17. The method of claim 16, wherein compressing the dry mixture is by direct compression which occurs at a pressure sufficient to form a tablet with a hardness within the range of 8 to 14.

18. The method of claim 17, further including admixing xanthan gum with the readily available konjac glucomannan in a ratio within the range of 20:

1 to 1;

20 prior to the direct compression step.

19. The method of claim 18, wherein the ratio of readily available konjac glucomannan to xanthan gum is within the range of 6:

1 to 12;

1.

20. The pharmaceutical formulation of claim 19, wherein the readily available konjac glucomannan is selected from the group consisting of clarified konjac, cryogenically ground konjac, and plasticized konjac.

21. The pharmaceutical formulation of claim 17, wherein the readily available konjac glucomannan is selected from the group consisting of clarified konjac, cryogenically ground konjac, and plasticized konjac.

22. A sustained release excipient consisting essentially of readily available konjac glucomannan.

23. A solid dosage form, comprising an active ingredient and a sustained release excipient which excipient consists essentially of at least 7 weight percent of a readily available konjac glucomannan based on the weight of the solid dosage form, wherein the dosage form contains no gas producing disintegrant.

24. A method for making a pharmaceutical tablet comprising the steps of forming a mixture of a dry pharmaceutically active ingredient with a sustained release excipient consisting essentially of at least 7 weight percent of a dry, readily available konjac glucomannan, and compressing the dry mixture at a pressure sufficient to form a table with a hardness of at least 6 kg, wherein no gas producing disintegrant is included in the tablet.