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Neramexane MR matrix tablet

A technology of neramexane, release agent, applied in the direction of anti-inflammatory agent, pill delivery, antifungal agent, etc.

Inactive Publication Date: 2008-11-05
MERZ PHARMA GMBH & CO KGAA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The development of a modified release dosage form for neramexin is challenging due to the high solubility of the molecule in aqueous media over a wide range of pH

Method used

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  • Neramexane MR matrix tablet
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  • Neramexane MR matrix tablet

Examples

Experimental program
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Effect test

Embodiment approach

[0091] The present invention is further illustrated by the following examples, which, however, should not be construed as limiting the scope of the invention.

Embodiment 1

[0093] Example 1: Preparation of neramexin modified-release matrix tablet

[0094] Matrix tablets containing about 25 mg or 50 mg or 75 mg or 100 mg of neramexin mesylate are prepared as follows. Appropriate amount of neramexin mesylate, hydroxypropyl methylcellulose (HPMC, this example is Methocel K 100M CR), microcrystalline cellulose (MCC, this example is Avicel PH 102), magnesium stearate and gum SiO2 (SiO 2 , in this case Aerosil 200) were weighed and blended using a free-fall blender (Bohle PTM 200). Or an appropriate amount of neramexin mesylate, hydroxypropyl methylcellulose, microcrystalline cellulose, magnesium stearate and colloidal silicon dioxide is sieved before blending using a free-fall blender. The appropriate amount for each batch is calculated based on the target content of each dosage unit shown in Table 1. The optical characteristics of the powder blend showed no lack of homogeneity such as flakes, agglomerates or tendency to separate. All blends showe...

Embodiment 2

[0098] Example 2: Coating of Neramexin Modified Release Matrix Tablets

[0099] The matrix tablet prepared in Example 1 was coated with a white water-soluble coating composition Sepifilm LP 770 white using a porous or non-porous standard pan coater under controlled air. Tablets were weighed and dedusted prior to coating. The coating dispersion was then sprayed onto the tablets using a 1.0 mm nozzle. The temperature of the tablet cores during coating was between 34 and 39°C. The inlet temperature was between 59 and 64°C and the spray rate was about 40 to 53 grams / minute. Spraying was continued until the tablet weight gain was about 4%. The optical appearance of the coated tablets was excellent. Visibly free from sticking, the surface is smooth, bright and extremely uniform without any cracks or damage.

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Abstract

The invention provides novel oral modified release dosage forms of neramexane which are useful for the continuous therapy of patients suffering from diseases and conditions such as Alzheimer's dementia and neuropathic pain. The compositions have drug release profiles that are suitable for achieving steady state plasma concentrations of neramexane which have relatively small fluctuation when administered on a twice-daily or even once-daily regimen. The dosage forms may be designed as modified release matrix tablets, which are optionally coated for taste masking. The invention further provides therapeutic methods of treating conditions such as Alzheimer's dementia and neuropathic pain which involve the administration of such dosage forms.

Description

【Technical field】 [0001] The present invention relates to pharmaceutical dosage forms, in particular to modified release dosage forms suitable for oral administration. In another aspect, the present invention relates to new uses of the active compound neramexane and methods of treatment related to this use. 【Background technique】 [0002] Neramexin - also known as 1-amino-1,3,3,5,5-pentamethylcyclohexane - is a member of the orally active class of 1-aminocyclohexanes that has been found to be useful in the treatment of Various diseases, especially certain neurological diseases, including Alzheimer's disease and neuropathic pain. This compound and its derivatives are disclosed in detail in US Patent Nos. 6,034,134 and 6,071,966, the subject matter of which are incorporated herein by reference. It is believed that the therapeutic effect of neramexin is the inhibition of the excess glutamate effect on N-methyl-D-aspartate (NMDA) receptors of nerve cells, so this compound is a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/13A61K9/20A61K9/28
CPCA61K9/2866A61K31/13A61K9/2054A61P1/00A61P1/14A61P17/06A61P21/00A61P21/02A61P25/00A61P25/04A61P25/16A61P25/18A61P25/28A61P27/16A61P29/00A61P31/10A61P3/04A61P43/00A61K9/20A61K9/48
Inventor B·豪普特迈尔A·贝克尔
Owner MERZ PHARMA GMBH & CO KGAA
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