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Dry granulation binders, products, and use thereof

A technology of adhesives and granules, applied in the field of microcrystalline cellulose-based adhesives, which can solve problems such as lack of compactness

Inactive Publication Date: 2009-09-09
FMC CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after the first compaction step, MCC granules may not be sufficiently compact for the second compaction, tableting step

Method used

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  • Dry granulation binders, products, and use thereof
  • Dry granulation binders, products, and use thereof
  • Dry granulation binders, products, and use thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0047] The preparation and properties of co-processed microcrystalline cellulose:sugar alcohol compositions are described in co-filed U.S. Patent Application FMC Attorney No. 60560-USA, "Co-processed microcrystalline cellulose and sugar alcohols as excipients for tablet ingredients." (Co-processed Microcrystalline Cellulose and Sugar Alcohol as an Excipient for Tablet Formulations)", which application is hereby incorporated by reference.

[0048] co-processing

[0049] A method of preparing a co-processed composition involves forming a well-dispersed aqueous slurry of MCC and a sugar alcohol such as mannitol. The relative amounts of the two components in the slurry are adjusted to achieve the desired specific weight ratio of the coprocessed product after final drying. The aqueous slurry is then dried by removing the water to form a coprocessed product. Preferably, the slurry is dried using spray drying techniques known in the art. But other drying techniques such as flash d...

Embodiment 1

[0077] This example shows that the highest secondary compression tensile strength of the coprocessed MCC / sugar alcohol blend is greater than that of a physical blend of the same composition and nature.

[0078] A co-processed 75:25 MCC / mannitol mixture was prepared by adding mannitol to the MCC wet cake and spray drying the slurry. The co-treated 75:25 MCC / mannitol mixture and the 75:25 non-co-processed MCC / mannitol physical mixture were each tested according to the general procedure described. The results for the co-processed mixture are shown in Figure 4 . The test results on the physical mixture are shown in Figure 5 .

[0079] The co-processed MCC:mannitol had a maximum primary compressive tensile strength of 9.5 MPa. The maximum secondary compression tensile strength is 6.5MPa. However, the physical mixture of MCC and mannitol has a maximum primary compaction tensile strength of 9.0 MPa and a maximum secondary compaction tensile strength of 5.0 MPa.

Embodiment 2

[0081] Co-processed MCC:CMC by 4% 7HF grade sodium carboxymethylcellulose (eg, 4 grams of CMC per 100 grams of MCC) is prepared by a method that does not impose high shear conditions on the MCC. A 15% slurry was prepared by dispersing the MCC wet cake in deionized water. The slurry was heated to 60°C and the pH of the slurry was adjusted to 8 with ammonia. Add enough calcium chloride to the slurry to achieve a concentration of 0.01 mol / L, then use The mixer was stirred for 5 minutes. Add pulverized CMC in this mixture, stir and disperse CMC well at the same time, then this batch material is spray-dried under processing condition, obtains and PH-101 comparable particle size.

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Abstract

The invention discloses a method for the preparation of microcrystalline cellulose containing tablets by roller compaction followed by tabletting. A tablet formulation is converted to a dry granulate by roller compaction, and the dry granulate lubricated dry granulate and compacted to a tablet. The tablet formulation comprises at least one active, an microcrystalline cellulose containing material, and, optionally other pharmaceutically acceptable excipients. The microcrystalline cellulose containing material has a maximum primary compaction tensile strength of at least 9 MPa or at least 9.5 MPa and a secondary compaction tensile strength of at least 5 MPa, at least 5.5 MPa, or at least 6 MPa.

Description

[0001] Cross References to Related Applications [0002] This application claims U.S. Provisional Application Serial No. 60 / 855,106, filed October 27, 2006, U.S. Provisional Application Serial No. 60 / 928,166, filed May 8, 2007, and U.S. Provisional Application Serial No. 60 / 928,166, filed October 27, 2006 Priority to Serial No. 60 / 855,066, the contents of the above provisional application are hereby incorporated by reference. field of invention [0003] The present invention relates to dry granulation binders having high recompactability for the preparation of solid dosage forms by multiple compaction. In particular, the present invention relates to microcrystalline cellulose-based binders which ensure good granulation quality, sufficient recompactability of the granules to obtain tablets of the required tensile strength. Background of the invention [0004] Individual doses of pharmaceutical compositions suitable for oral administration are conveniently administered in sol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16
Inventor G·汤伦斯B·莱克勒克B·卡林P·J·里雷M·A·加西亚
Owner FMC CORP