Crush resistant delayed-release dosage forms

a technology of delayed release and dosage form, which is applied in the field of dosage form, can solve the problems of difficult comminution of dosage form with such apparatus, affecting the safety of patients, and general unsuitability of pharmaceutical substances for “immediate release” formulations

Inactive Publication Date: 2006-08-31
GRUNENTHAL GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0023] As a consequence of the resistance to crushing, delayed release is maintained

Problems solved by technology

Such pharmaceutical substances are therefore generally unsuitable for “immediate release” formulations, in particular if it is desired to administer said formulations only two or three times daily.
However, older patients in particular frequently have difficulties in taking solid dosage forms, such as tablets, gelatine capsules, etc.
However, the comminution of dosage forms with such apparatuses is problematic if the dosage forms are delayed-release formulations.
Depending on the physiological activity of the substance, this may cause considerable side-effects however, and in extreme cases may even lead to the death of the patient.
Delayed-release formulations may also cause problems for small children.
For instance, children frequently cannot distinguish solid dosage forms from sweets.
If children find such dosage forms, for example because their parents have carelessly left them lying around in the home, there is a risk that the children may think that the dosage forms are sweets and put them in their mouths and chew them.
If said dosage fo

Method used

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  • Crush resistant delayed-release dosage forms
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  • Crush resistant delayed-release dosage forms

Examples

Experimental program
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Effect test

process embodiment 1

[0169] In this embodiment, the dosage form according to the invention is preferably produced without using an extruder by preferably mixing components (A), (C), optionally (B) and the optionally present component (D) and, optionally after granulation, shaping the resultant mixture by application of force to yield the dosage form with preceding and / or simultaneous exposure to heat.

[0170] This heating and application of force for the production of the dosage form proceeds without using an extruder.

[0171] Components (A), (C), optionally (B) and optionally (D) are mixed in a mixer known to the person skilled in the art. The mixer may, for example, be a roll mixer, shaking mixer, shear mixer or compulsory mixer.

[0172] The resultant mixture is preferably directly shaped into the dosage form according to the invention by application of force with preceding and / or simultaneous exposure to heat. The mixture may, for example, be formed into tablets by direct tabletting. In direct tablettin...

process embodiment 2

[0178] In this process variant, the dosage form according to the invention is produced by thermoforming with the assistance of an extruder, without there being any observable consequent discoloration of the extrudate.

[0179] In order to investigate the extent of discoloration due to this thermoforming, the color of the mixture of starting components of which the dosage form consists is first determined without addition of a color-imparting component, such as for example a coloring pigment or an intrinsically coloured component (for example α-tocopherol). This composition is then thermoformed according to the invention, wherein all process steps, including cooling of the extrudate, are performed under an inert gas atmosphere. By way of comparison, the same composition is produced by the same process, but without an inert gas atmosphere. The color of the dosage form produced according to the invention from the starting composition and of the dosage form produced by way of comparison i...

process embodiment 3

[0201] In this process variant for the production of the dosage form according to the invention energy is applied to a mixture of the components by means of ultrasonication.

[0202] First of all a homogeneous mixture of at least component (A) and component (C) (=binder) is produced. Further auxiliary substances, such as for example fillers, plasticisers, slip agents or dyes, may also be incorporated into this mixture. A low molecular weight polyethylene glycol is preferably used as plasticiser.

[0203] Mixing may be performed with the assistance of conventional mixers. Examples of suitable mixers are roll mixers, which are also known as tumbler, drum or rotary mixers, container mixers, barrel mixers (drum hoop mixers or tumbling mixers) or shaking mixers, shear mixers, compulsory mixers, plough bar mixers, planetary kneader-mixers, Z kneaders, sigma kneaders, fluid mixers or high-intensity mixers.

[0204] Selection of the suitable mixer is determined inter alia by the flowability and c...

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Abstract

The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substances (A) from the dosage form is at least partially delayed.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application claims priority from German Patent Application No. 10 2005 005 446.3, filed on Feb. 4, 2005 and U.S. patent application Ser. No. 10 / 718,112 filed on Nov. 20, 2003.BACKGROUND OF THE INVENTION [0002] The present invention relates to a dosage form for administering a physiologically active substance (A), wherein the dosage form is mechanically stabilised, such that it cannot be comminuted by conventional methods, such as pounding, crushing, grinding in a mortar etc., or at least comminuted only with very great difficulty. The substance (A) is released from the dosage form according to the invention under physiological conditions with an at least partially delayed release profile. [0003] Numerous physiologically active substances, such as nutritional supplements, pharmaceutical substances etc., are provided as delayed-release formulations, i.e., in contrast to conventional formulations (for example “immediate release” formu...

Claims

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Application Information

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IPC IPC(8): A61K9/26B29C48/21B29C48/40B29C48/44
CPCA61K9/2031B29K2105/0035B29C35/0261B29C45/0001A61J3/005A61K31/55A61K9/4808A61K31/4418A61K31/277A61K31/135A61K9/2013A61K31/554A61K9/2072A61K31/485B29C48/0011B29C48/21B29C48/022B29C48/0022B29C48/146B29C2793/009A61K31/4422B29B7/002B29B9/12A61J3/10B29C43/24B29C48/44B29C48/40A61P1/00A61P13/00A61P17/00A61P19/00A61P25/04A61P25/30A61P27/00A61P37/00A61P5/00A61P7/00A61P9/00A61K9/20A61K9/48A61K47/30A61K9/0053A61K9/2095A61K9/205A61K9/2054A61K9/2893B29B9/02B29C43/02B29K2105/251B29K2995/0056B29L2031/772A61J3/06A61K9/2009A61K9/2068A61K9/2086B29K2105/0044B29L2031/753
Inventor ASHWORTH, JUDYARKENAU MARIC, ELISABETHBARTHOLOMAUS, JOHANNES
Owner GRUNENTHAL GMBH
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