Oral dosage form safeguarded against abuse

A technology of oral agent and dosage form, applied in the field of oral dosage form to avoid abuse

Active Publication Date: 2007-08-29
GRUNENTHAL GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, since the vast majority of delayed-release opioid release dosage forms are abused, crushing of the dosage form is still required

Method used

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  • Oral dosage form safeguarded against abuse

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0146] a) Manufacture of abuse-resistant tablets containing oxycodone

[0147] Oxycodone hydrochloride in the amounts listed in Table 1, polyethylene oxide powder and hydroxypropylmethylcellulose (Metholose 90 SH 100 000) as delayed release matrix material were mixed in a free-fall mixer. In a heating box, the tableting tool consisting of a die, an upper punch and a lower punch with a diameter of 10 mm was heated to 90°C. A 600 mg portion of the powder mixture was compression molded by means of the above-mentioned heated tool, the pressure being maintained for at least 15 seconds.

[0148] Table 1

[0149] components

per tablet

complete batch

Oxycodone Hydrochloride

80.0 mg

40.0g

Polyethylene oxide, NF, MW 7000 000

(Polyox WSR 303, Dow Chemicals)

470.0mg

235.0g

Hydroxypropyl Methyl Cellulose

100 000mPa·s (Metholose90

SH 100 000)

50.0mg

25.0g

total weight

600.0mg

...

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Abstract

The present invention relates to an abuse-proofed, oral dosage form with controlled opioid-release for once daily administration, characterised in that it comprises at least one opioid with potential for abuse (A), at least one synthetic or natural polymer (C), optionally delayed-release matrix auxiliary substances, physiologically acceptable auxiliary substances (B), optionally a wax (D) and optionally at least one delayed-release coating, component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N.

Description

technical field [0001] The present invention relates to an abuse-resistant oral dosage form for once-daily administration, controlled opioid release comprising at least one opioid of potential abuse (A), at least one synthetic or natural polymer ( C), optionally delayed-release matrix material, optionally at least one delayed-release coating, optionally physiologically acceptable auxiliary substances (B), optionally waxes (D), in each case components (C) or (D) has a breaking strength of at least 500N, preferably 750N. [0002] According to the invention, the term "opioid" refers to a compound which interacts with at least one opioid receptor. In particular, except for (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol, its physiologically acceptable salts and / or derivatives and its corresponding Other than stereoisomers and / or pharmaceutically acceptable compounds or derivatives, opioids mean those opioid compounds that exhibit abuse potential. [0003] Opioids are ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K31/135
CPCA61K9/2054A61K9/2027A61K9/0002A61K31/485A61K9/2031A61P25/04A61K9/28A61K9/2013A61K9/2095A61K9/2893A61K9/0053A61K9/2068
Inventor J·巴索罗莫斯H·库格尔曼E·阿肯奥-马里克
Owner GRUNENTHAL GMBH
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