Silicia for the inhinition of a protease

A technology of silica and protease, which is applied to medical preparations containing active ingredients, digestive system, pharmaceutical formulas, etc., can solve problems such as silica protease inhibition that is not mentioned

Inactive Publication Date: 2011-04-06
INEOS HEALTHCARE LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no teaching in these documents concerning the ability of silica to act as an active gastrointestinal substance
[0021] Although various series of substances have been shown to have an inhibitory effect on the proteolytic activity of pepsin, the suitability of silica for protease inhibition is not mentioned in the prior art

Method used

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  • Silicia for the inhinition of a protease
  • Silicia for the inhinition of a protease
  • Silicia for the inhinition of a protease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0058] Thus, according to one embodiment, the protease of the invention is an aspartic protease.

[0059] In a preferred embodiment, the protease according to the invention is pepsin.

[0060] In a preferred embodiment, the protease according to the invention is mammalian pepsin.

[0061] In a preferred embodiment, the protease according to the invention is selected from the group consisting of human pepsin, porcine pepsin, horse pepsin, mouse pepsin, sheep pepsin, dog pepsin, sheep pepsin and bovine pepsin.

[0062] In a preferred embodiment, the protease of the invention is human gastric pepsin.

[0063] In a preferred embodiment, the protease of the invention is human gastric pepsin. Preferably, the protease according to the invention is a sub-type of human pepsin. Even more preferably, the protease according to the invention is selected from pepsin 1, 3a, 3b, 3c and pepsin.

[0064] In an alternative embodiment, the protease is a serine protease, preferably trypsin. I...

Embodiment

[0110] The present invention will be described in further detail by way of example only with reference to the accompanying drawings, in which

[0111] figure 1 Shown as attached.

[0112] substance

[0113] The silica materials used in this study were obtained from Precision Colloids LLC, Cartersville USA and INEOS Silicas, Warrington UK. Other reagents used were obtained from standard laboratory suppliers.

[0114] Silica material supplied in liquid or sol form is diluted once in deionized water to the desired concentration and shaken well. A volume (as specified below for each test method) is withdrawn from this stock solution to provide the desired final concentration in the test solution (ie, the test solution containing pepsin and / or substrate).

[0115] Disperse the silica material in powder form in deionized water and dilute as needed, shake well. A volume (as specified below for each test method) is withdrawn from this stock solution to provide the desired fina...

preparation Embodiment 18 and 19

[0119] Preparation Examples 18 and 19 - Colloidal Milled Silica:

[0120] The equipment used to colloidally grind Gasil HP270 to the required particle size is as follows:

[0121] ●Eiger Torrance Micro Mill 250

[0122] ●182ml zirconia beads

[0123] The mill was assembled using 182 ml of zirconia beads according to the mill manufacturer's instructions.

[0124] A Gasil HP270 slurry (120 g, 100 ml deionized water) was prepared with 12% w / v solids content and stirred with an overhead paddle stirrer for 10 minutes. The slurry was introduced into the mill and ground for 60 minutes at 4000 rpm. Aliquots were taken every 10 minutes for particle size distribution (PSD) analysis via Malvern Mastersizer to assess milling progress.

[0125] The Malvern Mastersizer method parameters are as follows:

[0126] ●Pump, stirrer and ultrasound set to 50%

[0127] ●2.5 minutes dispersion time

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Abstract

There is provided a silica for use to inhibit a protease. In particular there is provided a silicia for treatment or prevention of a disease or condition associated with adverse protease activity or adverse proteolytic degradation within the gastrointestinal tract.

Description

field of invention [0001] The present invention relates to silicas for use as protease inhibitors, silica suspensions comprising said silicas, pharmaceutical compositions comprising said silicas and silica suspensions and their use. Background of the invention [0002] Aspartic proteases are a class of proteolytic enzymes active between pH 1.5-5.5. They are characterized by two aspartate groups in the active site of the enzyme, which function as general acid-base catalysts and are critical for peptide bond cleavage. One of the first aspartic proteases to be characterized was the pepsin of the human stomach, which includes several sub-types, namely pepsin 1, 3a, 3b, 3c and pepsin. [0003] Pepsins are synthesized in the gastric mucosa as inactive precursors called zymogens and upon stimulation of gastric chief cells are released into the gastric lumen where they are activated by hydrochloric acid in the gastric juice. The primary function of pepsin is to degrade dietary pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/00A61P1/04
CPCA61K33/00A61P1/00A61P1/04A61P43/00
Inventor A·J·托弗特P·W·迪特马尔J·C·理查德森V·司徒盖拉
Owner INEOS HEALTHCARE LTD
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