Dosage form containing pantoprazole as active ingredient

a technology of active ingredients and dosage forms, applied in the field of pharmaceutical technology, can solve the problems of affecting the effect of adsorption, and requiring a complex process to produce the peroral administration form of acid-labile active compounds,

Inactive Publication Date: 2006-10-26
NYCOMED GMBH
View PDF9 Cites 20 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the substances suitable for enteric coatings are those having free carboxyl groups, the problem results that the enteric coating is partly dissolved or even dissolved from inside because of the alkaline medium in the interior and the free carboxyl groups promote the decomposit

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Dosage form containing pantoprazole as active ingredient
  • Dosage form containing pantoprazole as active ingredient

Examples

Experimental program
Comparison scheme
Effect test

examples

A. Synthesis of Magnesium bis[5-[difluoromethoxy]-2-[[3,4-dimethoxy-2-pyridinyl]-methyl]sulfinyl]1H-benzimidazolide]dihydrate

[0069] 3.85 kg (8.9 mol) of pantoprazole Na sesquihydrate [sodium [5[-difluoromethoxy]-2-[[3,4-dimethoxy-2-pyridinyl]methyl]sulfinyl]-1H-benzimidazolide]sesquihydrate] are dissolved at 20-25° C. in 38.5 l of purified water in a stirring vessel. A solution of 1.0 kg (4.90 mol) of magnesium dichloride hexahydrate in 8 l of purified water is added with stirring at 20-30° C. in the course of 3 to 4 h. After stirring for a further 18 h, the precipitated solid is centrifuged, washed with 23 l of purified water, stirred at 20-30° C. for 1 to 2 h in 35 l of purified water, centrifuged again and washed again with 30-50 l of purified water. The solid product is dried at 50° C. in vacuo (30-50 mbar) until a residual water content of <4.8% is achieved. The product is then ground.

[0070] The title compound is obtained as a white to beige powder, which is employed directly...

example b.1

Pellets Made by Wurster Coating (Nonpareilles):

[0074] I. Active Pellets:

a.) Sucrose starter pellets (0.425-0.5 mm)500.0gb.) Sodium carbonate30.0gc.) Pantoprazole-Mg dihydrate300.0gd.) Polyvinylpyrrolidone K 2535.0g

a. is sprayed with an aqueous dispersion of b., c. and d. in a fluidised bed process (Wurster equipment) or other suitable equipments (e.g. coating pan).

[0075] II. Intermediate Layer (Subcoating):

e.) Hydroxypropylmethylcellulose120.0gf.) Titanium dioxide2.0gg.) LB Iron oxide yellow0.2gh.) Propylene glycol24.0g

e. is dissolved in water (A). f. and g. are suspended in water using a high shear mixer (B). A and B are combined and after addition of h. the resulting suspension is sieved through a suitable sieve. The suspension is sprayed onto 500 g of the active pellets obtained under I using a fluidised bed process (Wurster) or other suitable processes (e.g. coating pan).

[0076] III. Coating with a Layer which is Resistant to Gastric Juice (Enteric Coating):

i.) Eudragit...

example b.2

Pellets Made by Wurster Coating (Nonpareilles):

[0078] I. Active Pellets:

a.) Cellulose pellets (0.6-0.7 mm)1000.0gb.) Sodium carbonate75.0gc.) Pantoprazole-Mg dihydrate650.0gd.) Polyvinylpyrrolidone K 2580.0g

a. is sprayed with an aqueous dispersion of b., c. and d. in a fluidised bed process (Wurster equipment) or other suitable equipments (e.g. coating pan).

[0079] II. Intermediate Layer (Subcoating):

e.) Hydroxypropylmethylcellulose250.0gf.) Titanium dioxide5.0gg.) LB Iron oxide yellow0.45g

e. is dissolved in water (A). f. and g. are suspended in water using a high shear mixer (B). A and B are combined and the resulting suspension is sieved through a suitable sieve. The suspension is sprayed onto 1000 g of the active pellets obtained under I using a fluidised bed process (Wurster) or other suitable processes (e.g. coating pan).

[0080] III. Coating with a Layer which is Resistant to Gastric Juice (Enteric Coating):

h.) Eudragit ® L 30 D365.0gi.) Triethyl citrate15.0g

h. is suspe...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
Massaaaaaaaaaa
Massaaaaaaaaaa
Massaaaaaaaaaa
Login to view more

Abstract

Dosage forms for the oral administration of the magnesium salt of pantoprazole are described.

Description

TECHNICAL FIELD [0001] The present invention relates to the field of pharmaceutical technology and describes a dosage form for oral administration of the magnesium salt of pantoprazole. The invention additionally relates to proces-ses for producing the dosage form. PRIOR ART [0002] It is generally known to coat peroral administration forms, e.g. tablets or pellets which contain an acid-labile active compound, with an enteric coating which, after passage through the stomach, rapidly dissolves in the alkaline medium of the intestine. Examples of such acid-labile active compounds are acid-labile proton pump inhibitors (H+ / K+ ATPase inhibitors), in particular pyridin-2-ylmethylsulfinyl-1H-benzimidazoles, such as are disclosed, for example, in EP-A-0 005 129, EP-A-0 166 287, EP-A-0 174 726 and EP-A-0 268 956. On account of their H+ / K+ ATPase-inhibiting action, these are of importance in the therapy of diseases, which are due to increased gastric acid secretion. Examples of active compoun...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K31/4439A61K9/20A61K9/26A61K9/28A61K9/32A61K9/50A61K31/44
CPCA61K9/2081A61K9/2886A61K31/4439A61K31/44A61K9/5078A61P1/00A61P1/04A61K9/20A61K9/16A61K9/2086
Inventor ANSTETT, ISABEL
Owner NYCOMED GMBH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap