Composition and pharmaceutical dosage form for colonic drug delivery using polysaccharides

A composition and drug technology, applied in the directions of drug combination, sugar-coated pills, drug delivery, etc., can solve the problems of colon enzymes cannot easily reach polysaccharides, cannot display colon-specific drug delivery, slow drug release, etc.

Inactive Publication Date: 2001-08-29
SAMYANG BIOPHARMLS CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, the application of hydrophobic film-forming materials also brings some undesired consequences: the composition disintegrates slowly in the colon due to the hydrophobic nature of the mixed polymers, which delays the disintegration caused by colonic enzymes
It may also...

Method used

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  • Composition and pharmaceutical dosage form for colonic drug delivery using polysaccharides
  • Composition and pharmaceutical dosage form for colonic drug delivery using polysaccharides
  • Composition and pharmaceutical dosage form for colonic drug delivery using polysaccharides

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Embodiment 1

[0055] EXAMPLES Example 1: Preparation of a film made from the composition

[0056] Pectin and guar gum (4:1 w / w) were mixed and dissolved in distilled water to a final concentration of 2% (w / v). Dilute aliquots with Na 2 CO 3 The pH of the mixture was adjusted to 4, 5, 6, 7, 8, and 10. Each was cast on a polytetrafluoroethylene plate to form a film with a thickness of 150 µm.

[0057] Some other samples were also prepared in which locust bean gum was substituted for guar gum and the pH of the samples was adjusted to 4 and 8. The film is cast and dried. The thickness of these dried films was 150 μm.

[0058] Some other samples were also prepared in which pectin was dissolved in distilled water with Na 2 CO 3 Adjust pH to 4 and 8. The samples were cast and dried. The thickness of these dried films was also 150 μm.

[0059] Finally, guar gum and locust bean gum were used at pH 7 and 14 to prepare films as described above. The thickness of these dried films was also 15...

Embodiment 2

[0063] Table 2

[0064] The results show that the prepared membranes prepared at pH around 7 or above have better tonic properties compared to the prepared membranes prepared at pH below 7. Embodiment 3: with this composition tablet coating

Embodiment 3

[0064] The results show that the prepared membranes prepared at pH around 7 or above have better tonic properties compared to the prepared membranes prepared at pH below 7. Embodiment 3: with this composition tablet coating

[0065] Tablets containing 100 mg of ibuprofen as a model drug were coated with the composition prepared according to the method of Example 1. The weight ratio of pectin to guar gum was 4:1, and the pH was adjusted to 8. Coat with Hi-Coater (HCT-MINI, Freund Ind., Japan), coating amount is 8mg / cm 2 ,15mg / cm 2 ,26mg / cm 2 , and 35mg / cm 2 .

[0066] Another tablet containing 100 mg of ibuprofen as a model drug was coated with the composition prepared according to the method of Example 1, wherein locust bean gum was used instead of guar gum. The weight ratio of pectin to locust bean gum was 4:1, and the pH was adjusted to 8. Coat with Hi-Coater (HCT-MINI, Freund Ind., Japan), coating amount is 15mg / cm 2 .

[0067] Control preparations containing 100 m...

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Abstract

A colonic drug delivery composition contains a first polysaccharide and a second polysaccharide wherein both polysaccharides are degradable by colonic enzymes and are mixed at a environmental pH of about 7 or above. A colon selective pharmaceutical composition and dosage form for oral delivery of a drug, nutrient, diagnostic reagent, or mixture thereof includes the drug, nutrient, diagnostic reagent, or mixture thereof in contact with the polysaccharide composition. A method of preparing such a colonic drug delivery composition and the colon selective pharmaceutical composition and dosage form are also disclosed.

Description

field of invention [0001] The present invention relates to compositions and oral pharmaceutical dosage forms for selective delivery to the colon. More specifically, the present invention relates to compositions and oral pharmaceutical dosage forms that release biologically active ingredients in the colon while avoiding or reducing release in the upper part of the gastrointestinal tract, such as the stomach and small intestine. Background of the invention [0002] Many pharmaceutical products based on oral delivery have been successfully developed and marketed, but many others are difficult to administer orally, are incompatible with the physical and / or chemical environment of the upper GI tract, and / or are ingested in the upper GI tract rare. Due to the lack of digestive enzymes, the colon is considered a suitable absorption site for many drugs. However, colonic drug delivery is difficult to achieve because oral formulations pass through the stomach and small intestine whe...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K9/22A61K9/28A61K9/36A61K9/48A61K9/50A61K9/51A61K9/62A61K31/138A61K31/192A61K31/196A61K31/4164A61K31/435A61K31/445A61K31/454A61K31/506A61K31/519A61K31/573A61K31/70A61K38/00A61K38/095A61K38/22A61K38/23A61K38/27A61K38/28A61P1/00C08L5/06
CPCA61K9/4891C08L5/06Y10S514/96Y10S514/962A61K9/4816A61K9/5036A61K9/286A61K9/5078A61P1/00C08L2666/02A61K31/70
Inventor 李承瑞林昶伯裴哲民李守贞朴仁西门健朴嬉南
Owner SAMYANG BIOPHARMLS CORP
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