Coprocessed microcrystalline cellulose and calcium carbonate composition and its preparation

• US 4,744,987 A
• Filed: 08/03/1987
• Issued: 05/17/1988
• Est. Priority Date: 03/08/1985
• Status: Expired due to Term

• Current Assignee: FMC Corporation
• Original Assignee: FMC Corporation
• Inventors: Wiggins, J. Donald, West, Kenneth P., Mehra, Dev K.
• Primary Examiner(s): Griffin, Ronald W.
• Application Number:
  US07/081,584
• Time in Patent Office: 288 Days
• Field of Search: 106/203, 106/204, 106/163.1, 424/500, 424/156, 514/781
• US Class Current: 424/687
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

A particulate coprocessed microcrystalline cellulose and calcium carbonate composition having the respective components present in a weight ratio of from about 75:25 to 35:65. The composition is useful as a pharmaceutical excipient.

The coprocessed composition is prepared by forming a well-dispersed aqueous slurry of microcrystalline cellulose and calcium carbonate and then drying the slurry, preferably by spray drying, to yield a particulate product.

Claims

1. A composition of matter useful as a pharmaceutical excipient comprising dried particulate agglomerates of coprocessed microcrystalline cellulose and calcium carbonate, the two components being present in a weight ratio of from about 75:

25 to 35;

65 microcrystalline cellulose;

calcium carbonate and intimately associated with each other.

2. The composition of claim 1, wherein the particulate material is spray-dried coprocessed microcrystalline cellulose and calcium carbonate.

3. The composition of claim 1 wherein the weight ratio of the two components is in the range of from about 70:

30 to 40;

60 microcrystalline cellulose;

calcium carbonate.

4. The composition of claim 1 wherein the weight ratio of the two components is in the range of from about 65:

35 to 50;

50 microcrystalline cellulose;

calcium carbonate.

5. The composition of claim 1 wherein the particle size of the coprocessed microcrystalline cellulose and calcium carbonate is substantially all less than No. 60 sieve (250 μ

m).

6. The composition of claim 1 wherein the particulate coprocessed microcrystalline cellulose and calcium carbonate has an average particle size in the range of from 20 μ

m to 150 μ

m.

7. The composition of claim 1 wherein the particulate, coprocessed microcrystalline cellulose and calcium carbonate has a moisture content of from 1-8 wt % H₂ O.

8. A process for preparing a particulate material useful as a pharmaceutical excipient, which comprises

forming a well-dispersed aqueous slurry of microcrystalline cellulose and calcium carbonate, both being present in particulate form and in amounts which produce a component ratio within the range specified below for the particulate coprocessed product, and

drying the aqueous slurry by removing water therefrom to yield a particulate coprocessed product, in which the weight ratio of microcrystalline cellulose to calcium carbonate is in the range of from about 75:

25 to 35;

65.

10. The process of claims 8 or 9 wherein the aqueous slurry is dried by spray drying.

9. A process for preparing a particulate material useful as a pharmaceutical excipient, which comprises

dispersing microcrystalline cellulose and calcium carbonate, both in particulate form, into an aqueous medium to form a well-dispersed aqueous slurry containing relative amounts of microcrystalline cellulose and calcium carbonate that provide a component ratio within the range specified below for the particulate coprocessed product, and

drying the aqueous slurry by removing water therefrom to yield a particulate coprocessed product, in which the weight ratio of microcrystalline cellulose to calcium carbonate is in the range of from about 75:

25 to 35;

65.

11. A process for preparing a particulate material useful as a pharmaceutical excipient, which comprises the steps of

dispersing particulate microcrystalline cellulose into an aqueous medium in an amount of from about 5 to 25 wt % based on the slurry weight;

introducing particulate calcium carbonate into the aqueous microcrystalline cellulose slurry in an amount which provides a component ratio within the range specified below for the particulate coprocessed product;

dispersing the slurry solid components uniformly throughout the aqueous slurry, the amounts of solids previously introduced into the slurry being sufficient to provide a total solids content of at least 10 wt % based on total slurry weight; and

spray drying the well-dispersed slurry to yield a particulate coprocessed product, in which the weight ratio of microcrystalline cellulose to calcium carbonate is in the range of from about 75;

25 to 35;

65.

12. The process of claims 8, 9 or 11 wherein the weight ratio of microcrystalline cellulose to calcium carbonate is in the range of from about 65:

35 to 50;

50.

13. The process of claims 8, 9 or 11 wherein the drying conditions are adjusted to yield a dried particulate coprocessed product having a residual moisture content of from 1-8 wt % H₂ O.

14. The process of claims 8, 9 or 11 wherein the drying conditions are adjusted to yield a dried particulate coprocessed product having particle size that is substantially all less than No. 60 Sieve (250 μ

m).

15. The process of claim 14 wherein the dried particulate coprocessed product has an average particle size in the range of from 20 μ

m to 150 μ

m.

16. The process of claims 8, 9 or 11 wherein the particulate microcrystalline cellulose is never-dried material from a microcrystalline cellulose manufacturing process.

17. The process of claims 8, 9 or 11 wherein the particulate calcium carbonate in the aqueous slurry is substantially finer than the particulate microcrystalline cellulose therein.

18. The process of claims 8, 9 or 11 wherein the particulate microcrystalline cellulose in the aqueous slurry has a particle size that is substantially all less than No. 20 Sieve (250 μ

m).

19. The process of claims 8, 9 or 11 wherein the particulate calcium carbonate is substantially all smaller than 30 μ

m.

20. The process of claims 8, 9 or 11 wherein the particulate calcium carbonate is substantially all smaller than 10 μ

m.

21. The process of claims 8, 9 or 11 wherein the average particle size of the particulate calcium carbonate is less than 5 μ

m.

22. The process of claims 8, 9 or 11 wherein the well-dispersed aqueous slurry to be dried has a solids content of at least 20 wt % solids, based on the total slurry weight.

23. The process of claim 11 wherein the spray drying operation is carried out with a drier outlet temperature in the range of from about 40°

-100°

C.

24. The process of claim 11 wherein the spray drying operation is carried out with a drier inlet temperature in the range of from about 90°

-300°

C.