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Process for the production of an abuse-proofed dosage form

a technology of dosage form and process, which is applied in the direction of presses, manufacturing tools, drug compositions, etc., can solve the problems of many pharmaceutical active ingredients, abuse potential, etc., and achieve the effect of preventing parenteral, nasal and/or oral abus

Inactive Publication Date: 2013-12-05
GRUNENTHAL GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0019]The use of polymers (C) having the stated minimum breaking strength in the process according to the invention, preferably in quantities such that the dosage form also exhibits such a minimum breaking strength, means that pulverisation of the dosage form is considerably more difficult using conventional means, so considerably complicating or preventing the subsequent abuse.
[0022]The dosage form obtained according to the invention is thus suitable for preventing parenteral, nasal and / or oral abuse of pharmaceutical active ingredients with potential for abuse.

Problems solved by technology

Many pharmaceutical active ingredients, in addition to having excellent activity in their appropriate application, also have potential for abuse, i.e. they can be used by an abuser to bring about effects other than those intended.

Method used

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  • Process for the production of an abuse-proofed dosage form
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  • Process for the production of an abuse-proofed dosage form

Examples

Experimental program
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Effect test

example 1

[0154]

ComponentsPer tabletComplete batchTramadol HCl100.0 mg 60.0 gPolyethylene oxide, NF, MFI221.0 mg132.6 g(190° C. at 21.6 kg / 10 min)MW7,000,000 (Polyox WSR 303,Dow Chemicals)Hydroxypropylmethylcellulose 20.0 mg 12.0 g100,000 cP (Metholose 90 SH100,000)Magnesium stearate 9.0 mg 5.4 gTotal weight350.0 mg210.0 g

[0155]Tramadol hydrochloride and polyethylene oxide powder and hydroxypropyl methylcellulose were mixed in a free-fall mixer. The magnesium stearate powder was then mixed in. The powder mixture was pressed into tablets on a Korsch EK0 eccentric press. The tabletting tool has a diameter of 10 mm and a radius of curvature of 8 mm. These tablets were further processed with the assistance of a laboratory heat sealer (Kopp laboratory sealer SPGE 20, Hot & Cold tack heat-sealed seam strength tester from Kopp). The heat sealing bars were replaced with two metal rails, into each of which had been milled a concavity having a diameter of 10 mm and a radius of 8 mm. The surface of the ...

example 2

[0158]

ComponentsPer tabletComplete batchTramadol HCl100.0 mg 60.0 gPolyethylene oxide, NF, MFI221.0 mg132.6 g(190° C. at 21.6 kg / 10 min)MW5,000,000 (Polyox WSRCoagulant, Dow Chemicals)Hydroxypropylmethylcellulose 20.0 mg 12.0 g100,000 cP (Metholose 90 SH100,000)Magnesium stearate 9.0 mg 5.4 gTotal weight350.0 mg210.0 g

[0159]As stated in Example 1, tablets with a diameter of 10 mm and a radius of curvature of 8 mm were produced.

[0160]The tablets were also further processed as in Example 1, except that the sealing bars were heated to 100° C.

[0161]The breaking strength of the tablets is determined using the above-described method. No breakage occurred when a force of 500 N was applied. The tablets could not be comminuted using a hammer, nor with the assistance of a pestle and mortar.

[0162]In vitro release of the active ingredient from the preparation was determined in a paddle stirrer apparatus with sinker in accordance with Pharm. Eur. The temperature of the release medium was 37° C. ...

example 3

[0163]

ComponentsPer tabletComplete batchTramadol HCl100.0 mg 60.0 gPolyethylene oxide, NF, MFI221.0 mg132.6 g(190° C. at 21.6 kg / 10 min)MW7,000,000, fine powder (PolyoxWSR 303 FP, Dow Chemicals)Hydroxypropylmethylcellulose 20.0 mg 12.0 g100,000 cP (Metholose 90 SH100,000)Magnesium stearate 9.0 mg 5.4 gTotal weight350.0 mg210.0 g

[0164]Tablets were produced as described in Example 1. The tablets were also further processed as explained in Example 1.

[0165]The breaking strength of the tablets was determined using the above-described method. No breakage occurred when a force of 500 N was applied. The tablets could not be comminuted using a hammer, nor with the assistance of a pestle and mortar.

[0166]In vitro release of the active ingredient from the preparation was determined in a paddle stirrer apparatus with sinker in accordance with Pharm. Eur. The temperature of the release medium was 37° C. and the rotational speed of the stirrer 75 min−1. The release medium used was an intestinal j...

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Abstract

The present invention relates to a process for the production of abuse-proofed, thermoformed dosage forms containing, apart from one or more active ingredients with potential for abuse and optionally physiologically acceptable auxiliary substances, at least one synthetic or natural polymer with a breaking strength of at least 500 N.

Description

[0001]This application is a continuation of U.S. patent application Ser. No. 12 / 140,718, now allowed, which is a division of U.S. patent application Ser. No. 11 / 471,428, filed Jun. 20, 2006, now abandoned, which is, in turn, a continuation of International Patent Application No. PCT / EP04 / 14679, filed on Dec. 23, 2004, which claims priority of German Patent Application No. 103 61 596.2, filed Dec. 24, 2003.[0002]The present invention relates to a process for the production of solid pharmaceutical dosage forms with at least reduced potential for abuse, by[0003]a) shaping a formulation mixture containing at least one active ingredient with potential for abuse and at least one synthetic or natural polymer (C), which exhibits a breaking strength of at least 500 N, into formed articles by application of force,[0004]b) optionally singulating the formed articles and optionally in each case grading them by size and,[0005]c) after or during heating at least to the softening point of the polym...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K9/20A61K31/485A61K31/515A61K31/5513B30B11/16
CPCA61K9/2095A61K31/485A61K31/515A61K31/5513B30B11/16A61K31/135A61P25/04A61P25/30A61P25/36A61P29/00A61K9/2031A61K9/2054A61K9/2072B30B11/34
Inventor ARKENAU-MARIC, ELISABETHBARTHOLOMAUS, JOHANNES
Owner GRUNENTHAL GMBH
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