Tablets comprising a poorly compressible active agent and tocopherol polyethyleneglycol succinate (tpgs)

A technology of polyethylene glycol succinate and polyethylene glycol, which is applied in the direction of powder transportation and bulk transportation, and can solve problems such as shortening shelf life, stratification, and excessive pressure

Inactive Publication Date: 2007-09-26
EASTMAN CHEM CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Also, for substances such as water-soluble vitamins such as vitamin C and B vitamins, adding water to form a granular mixture will shorten the shelf life of the substance or reduce the potency of the substance
[0009] Another problem associated with poorly compressible substances is the need for excessively high pressures to obtain the standard hardness of the tablet
However, too high a pressure can cause capping (that is, the top of the tablet breaks) or delamination (where the layers of the tablet break apart)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Following Method 1, a granular material was prepared containing ascorbic acid (840.03 g), TPGS (120.00 g), MCC (230.60 g) and fumed silica (9.63 g). The mixture flows freely into the tablet press from the hopper. To make a 600 mg tablet requires 3900 lbs of compression force and 20 lbs of pushing force. Twenty tablets were randomly selected for the friability test (Vanderkamp, ​​model 10809). The friability is calculated as follows:

[0078] Friability (%)=(weight of 20 tablets before test−weight of 20 tablets after test) / (weight of 20 tablets before test)×100%.

[0079] The results are listed in Table 2 below.

[0080] 20 pieces

[0081] 100 tablets were randomly selected for tablet hardness and thickness testing. The average hardness and thickness of these tablets were determined to be 84 Newtons (N) and 2.34 mm, respectively. The tablets hardened over time, ranging from 84N for a fresh tablet, 98N after one hour, and 106N after one day.

Embodiment 2

[0083] Following Method 2, a granular material was prepared containing ascorbic acid (300.23g), TPGS (60.12g), MCC (230.43g) and fumed silica (9.62g). The mixture flows freely into the tablet press from the hopper. To make a 600 mg tablet requires 3400 lbs of compression force and 70 lbs of pushing force. The friability results are listed in Table 3 below.

[0084] 20 pieces

[0085] It was determined that the average hardness and thickness of 20 pieces were 106N and 2.50mm, respectively. The tablets hardened over time, with a hardness of 106N for a fresh tablet, 117N after one hour, and 117N after six hours.

Embodiment 3

[0087] Follow the steps of Method 1 to prepare the ingredients for tableting. During the production process, the point at which no flow and process problems are observed is called the working point. The operating points are listed in Table 4 below.

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PUM

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Abstract

A solid composition suitable for forming into a tablet includes a pharmaceutically active substance in an amount sufficient to provide a therapeutic effect when administered; from about 0.2 to about 15 weight %, based on the total weight of the composition, of a water-soluble preparation of a fat-soluble vitamin; and from about 10 to 80 weight %, based on the total weight of the composition, of an excipient. Another aspect of the present invention is method for making the solid composition.

Description

field of invention [0001] The present invention relates to the oral administration of pharmaceutically active substances and, more particularly, the present invention relates to the preparation of poorly compressible tablets of pharmaceutically active substances. Background of the invention [0002] Various substances, such as pharmaceutically active substances, intended for oral administration are usually formulated in solid dosage forms. The term "solid dosage form" as used herein means a presentation particularly suitable for oral or rectal administration, which has any desired form, such as tablets, coated tablets, lozenges, pills, granules and the like. The term "tablet" is well understood not only by those skilled in the art, but also by the general public at large. In general, the term "tablet" includes not only tablets per se, but similar discrete bodies, possibly also other shapes, sometimes referred to as "caplets" (e.g. caplets), lozenges and Different names suc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16
CPCA61K9/146
Inventor 袁静华N·M·克利普斯吴宏为
Owner EASTMAN CHEM CO
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