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Process for the production of an abuse-proofed dosage form

a technology of dosage form and production process, which is applied in the direction of biocide, heterocyclic compound active ingredients, drug compositions, etc., can solve the problems of inability to actually perform safe administration and the inability to extract active ingredients from there, etc., and achieve the effect of intense negative effect and no negative

Inactive Publication Date: 2008-12-18
GRUNENTHAL GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0020]By using polymers having the stated minimum breaking strength (measured as stated in the application), preferably in quantities such that the dosage form also exhibits such a minimum breaking strength of at least 500 N, preferably of at least 1000 N, it is possible to prevent pulverisation of the dosage form with conventional means and thus considerably to complicate or to prevent any subsequent abuse.
[0117]Should, contrary to expectations, the abuser succeed in comminuting such a dosage form produced according to the invention, which comprises components (c) and / or (e) and / or (d) and / or (f) in subunits (Y), for the purpose of abusing the active ingredient and obtain a powder which is extracted with a suitable extracting agent, not only the active ingredient but also the particular component (c) and / or (e) and / or (f) and / or (d) will be obtained in a form in which it cannot readily be separated from the active ingredient, such that when the dosage form which has been tampered with is administered, in particular by oral and / or parenteral administration, it will exert its effect on taking and / or in the body combined with an additional negative effect on the abuser corresponding to component (c) and / or (d) and / or (f) or, when the attempt is made to extract the active ingredient, the coloration' will act as a deterrent and so prevent abuse of-the dosage form.

Problems solved by technology

If comminution is inadequate, parenteral, in particular intravenous, administration cannot actually be performed safely or extraction of the active ingredient therefrom takes too long for the abuser or there is no “kick” when orally abused as release is not instantaneous.

Method used

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

Examples

Experimental program
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Effect test

example 1

[0159]

Per tabletComplete batchTramadol HCl100.0mg1495.0gPolyethylene oxide,167.8mg2508.6gMW 7 000 000(Polyox WSR 303 from Dow)Hydroxypropylmethylcellulose33.5mg500.8g(Hypromellose 100 000 mPa)Butyihydroxytoluene (BHT)0.2mg3.0gTotal mass300.5mg4507.4g

[0160]The stated quantity of BHT was dissolved in ethanol (96%), such that a 7.7% (mass / mass) ethanolic solution was obtained. This was mixed initially with 150 g of polyethylene oxide in a high speed mixer for 30 minutes and then the remaining quantity of polyethylene oxide was added and stirring continued for a further 30 minutes. The composition was dried for 12 h at 40° C.

[0161]All the further components were added and mixed for 15 min in a free-fall mixer. The powder mixture was divided between moulds, each having a diameter of 13 mm and a depth of 6 mm. Using a syringe with cannula, the mixture was suspended in each case in 0.5 ml of 96% ethanol and then in each case combined with 0.5 ml of distilled water After 24 hours swelling t...

example 2

[0165]

Powder mixtureComplete batchPer tabletTramadol HCl100.1g100mgPolyethylene oxide300.0g299.7mgMW 5000 000(Polyox WSR Coagulant,from Dow),Hydroxypropylmethylcellulose50.05g50.0mg(Hypromellose 100 000 mPa)Butylhydroxytoluene (BHT)0.25g0.25mgFoam0.250g0.25mgHydroxypropylmethylcellulose(Hypromellose 100 000 mPa)Dist. water49.8g

[0166]The powder mixture was first produced as stated in Example 1.

[0167]The foam was produced by dissolving the stated quantity of Hypromellose in distilled water. A foam was then produced using a high performance homogeniser (IKA Ultraturrax 25 Basic) by stirring initially for 2 minutes at level 1, then for 2 minutes with a mixer / granulator at level 2 and finally for 3 minutes at level 3. The powder mixture was slowly added to the foam with constant stirring in a mixer (Kenwood Major Classic 25 Basic).

[0168]The granulated mixture was then dried for 24 hours—at 40° C. and, after being passed through a screen (from Frewitt, model GLA-A-ORV) with 1 mm orifices,...

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Abstract

The present invention relates to a process for the production of an abuse-proofed dosage form 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 (C) with a breaking strength of at least 500 N, wherein the formulation mixture is combined with a solvent for the polymer (C) at least in quantities such that the formulation mixture is at least uniformly moistened, the at least moistened composition is optionally divided into sub-portions, dried and shaped to yield the dosage form.

Description

[0001]The present invention relates to a process for the production of an abuse-proofed solid dosage form, in which there is added to a formulation mixture containing, one or more active ingredients with potential for abuse (A) and optionally physiologically acceptable auxiliary substances (B) and at least one synthetic or natural polymer (C), which exhibits a breaking strength of at least 500 N,[0002]a) a solvent for the polymer (C) at least in quantities such that the formulation mixture is uniformly moistened,[0003]b) the composition which has been at least moistened in this manner is optionally divided into sub-portions,[0004]c) the portion(s) are dried and[0005]d) shaped to yield the dosage formBACKGROUND OF THE INVENTION[0006]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.[0007]Opiates, for exampl...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/485A61P25/04
CPCA61K9/1694A61K31/135A61K9/2054A61K9/2027A61K31/485A61P25/04A61K9/2095A61K9/2031A61K31/05A61K9/2013
Inventor ARKENAU-MARIC, ELISABETHBARTHOLOMAUS, JOHANNES
Owner GRUNENTHAL GMBH
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