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Pharmaceutical formulation and process

a technology of pharmaceutical formulation and process, applied in the field of new pharmaceutical formulation, can solve the problems of discoloration of active compound content and loss of content with time, and the inability to apply at least two different layers, and achieve the effect of simplifying the preparation of enteric coated articles

Inactive Publication Date: 2003-06-19
ASTRAZENECA AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These proton pump inhibitors are, however, susceptible to degradation / transformation in acidic reacting and neutral media.
If covered with such an enteric coating layer, the acid labile substance may rapidly decompose by direct or indirect contact with the acidic groups resulting in discoloration of the content and loss in content of the active compound with the passage of time.
The prior art techniques to apply at least two different layers on a pellet core or a tablet comprising an acid labile compound is rather complicated and there is a demand for finding new processes and formulations to simplify the manufacturing of such enteric coated articles comprising acid labile substances.

Method used

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  • Pharmaceutical formulation and process
  • Pharmaceutical formulation and process
  • Pharmaceutical formulation and process

Examples

Experimental program
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example 1

[0046] Tablets containing lansoprazole and arginine are produced according to the following procedure. Firstly, dry ingredients are thoroughly mixed and then granulated with a solution in a laboratory mixer. The dried granules are mixed with lubricants etc. in a final mixing step.

1 Concentration Dry ingredients for granulation (mmol / g dry ingredients in (for approx. 4000 tablets) the alkaline tablet core) Lansoprazole 40.4 g L-arginine (passing 120 mesh) 365.4 g 4.2 Microcrystalline cellulose 38.5 g Granulating solution Distilled water 173 g Corn starch 7.7 g

[0047] The solution is poured over the premixed powder mass during mixing. The wet granules are dried on a tray in a drying cabinet. The dried granules are milled to pass a 1.0 mm sieve. The granules are mixed with

2 Talc 3.1 g Sodium dodecyl sulphate 20.8 g Microcrystalline cellulose 19.2 g Magnesium stearate 5.0 g

[0048] in a laboratory mixer, and then compressed into tablets having a size of 7 mm .O slashed. and a weight of app...

example 2

[0052] Core material containing the magnesium salt of (-)-omeprazole and the alkaline reacting compound trometamine (=tris-buffer) is prepared by extrusion and spheronization.

[0053] The powder mass is mixed in a laboratory mixer and then water is added.

4 Concentration (mmol / g dry ingredients in the Powder mixture alkaline core material) Magnesium salt of (-)-omeprazole 400 g Microcrystalline cellulose 300 g Trometamine 1000 g 4.1 PVP-XL 100 g Mannitol pwd 195 g Hydroxypropyl methylcellulose 6 cps 5 g Water q.s.

[0054] The powder mixture is mixed with the water and the wet mass is mixed to obtain a suitable consistency of the mass.

[0055] Extrusion is performed with an extruder fitted with 1.0 mm screen. The extrudate is formed into pellets on a spheronizer and dried in a fluidized bed drier.

[0056] 200 g of the obtained pellets are spray coated with the enteric coating dispersion described below, in a Wurster equipped fluidized bed.

5 Enteric coating dispersion Water 93.9 g Polyethylene...

example 3

[0059] Core material containing omeprazole and N-methyl-D-glucamine (=meglumine) is prepared by extrusion and spheronization of the below described composition using the same procedure as in Example 2;

6 Concentration (mmol / g dry ingredients in the Powder mixture alkaline core material) Omeprazole 100.0 g Microcrystalline cellulose 50.0 g Meglumine 500.0 g 2.6 Mannitol pwd 297.0 g Sodium starch glycolate 48.0 g Sodium laurylsulphate 5.0 g Water q.s.

[0060] Obtained dried pellets / cores are spray coated with the enteric coating dispersion described below, in a Wurster equipped fluidized bed.

7 Enteric coating dispersion Water 93.9 g Polyethylene glycol 400 4.6 g Eudragit .TM. L30D-55 151.5 g

[0061] This single coating step resulted in tablets having two polymeric layers with different characteristics. The inner layer is not soluble in acetone, as the outer one, but soluble in water. The separating layer is spontaneously formed in situ during the process, as a salt between the alkaline rea...

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Abstract

A new oral pharmaceutical dosage form comprising a core material that contains a proton pump inhibitor, one or more alkaline reacting compounds and optionally pharmaceutical excipients having a water soluble separating layer and an enteric coating layer. The core material as such is alkaline reacting and the separating layer between the alkaline reacting core material and the enteric coating layer is formed in situ as a water soluble salt between the alkaline reacting compound(s) and the enteric coating polymer. The invention also describes a new efficient process for the manufacture of such a dosage form comprising two functionally different layers in one manufacturing step, and its use in medicine.

Description

FIELD OF THE INVENTION[0001] The present invention refers to new pharmaceutical formulations comprising acid labile heterocyclic compounds with gastric inhibitory effect, in the following referred to as proton pump inhibitors. The new formulations are intended for oral use. Furthermore, the present invention refers to a new method for the manufacture of such a formulation and, the use of the new formulations in medicine.BACKGROUND OF THE INVENTION The proton pump inhibitors are for example compounds of the general formula I[0002] 1[0003] wherein[0004] N in the benzimidazole moiety means that one of the carbon atoms substituted by R.sub.6-R.sub.9 optionally may be exchanged for a nitrogen atom without any substituents;[0005] R.sub.1, R.sub.2 and R.sub.3 are the same or different and selected from hydrogen, alkyl, alkoxy optionally substituted by fluorine, alkylthio, alikoxyalkoxy, dialkylamino, piperidino, morpholino, halogen, phenyl and phenylalkoxy;[0006] R.sub.4 and R.sub.5 are th...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/16A61K9/20A61K9/22A61K9/28A61K9/30A61K9/32A61K9/36A61K9/50A61K9/52A61K31/00A61K31/4184A61K31/4188A61K31/435A61K31/44A61K31/4439A61K31/444A61K45/00A61K47/00A61K47/18A61P1/04
CPCA61K9/1617A61K9/2081A61K9/2866A61K9/2886A61K9/5026A61K9/5073Y10S514/925A61K31/00A61K31/4184A61K31/4188A61K31/435A61K31/4439A61K31/444A61K9/5078A61P1/04
Inventor LUNDBERG, PER JOHANLOVGREN, KURT
Owner ASTRAZENECA AB
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