Modified release formulations of oxcarbazepine and derivatives thereof

A dosage form and oral preparation technology, applied in the field of oxcarbazepine preparations, can solve problems such as blood level fluctuations and side effects

Inactive Publication Date: 2005-10-19
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

One problem that may arise is fluctuations in blood levels of the compounds of the invention when administered repeatedly, which fluctuations may be associated with side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment A

[0149] Example A (Variant 1 - Faster Matrix System)

[0150] Preparation (mg)

[0151] Chip:

[0152] Compound of the present invention 600.0

[0153] Avicel PH 102 131.2

[0154] Cellulose HPM 603 16.8

[0155] Methocel 60 HG 4000 CP 45.0

[0156] Polyvinylpyrrolidone XL 30.0

[0157] Aerosil 200 3.0

[0158] Magnesium stearate 8.0

[0159] Core Weight 834.0

[0160] Coating:

[0161] Iron oxide yellow 0.84

[0162] TiO 2 1.25

[0163] PEG4000 1.67

[0164] Cellulose HPM 603 16.70

[0165] Talc 2.93

[0166] Tablet weight 857.385

[0167] a) A premix containing the compound of the invention, Avicel PH 102 and cellulose HPM 603 was prepared.

[0168] b) Granulate the premix by wet granulation using a high-shear mixer (eg Aeromatic GP65).

[0169] c) sieving the resulting granules using, for example, a Q...

Embodiment B

[0178] Example B (variation 1 - disintegrating tablet with faster encapsulated granule system)

[0179] preparation

[0180] (mg)

[0181] Chip:

[0182] Compound of the present invention 600.0

[0183] Aquacoat ECD30 90.0

[0184] Avicel PH 102 150.0

[0185] Croscarmellose Sodium (Na-CMC XL) 75.0

[0186] Aerosil 200 2.8

[0187] Magnesium stearate 4.5

[0188] Core Weight 922.3

[0189] Coating:

[0190] Iron oxide yellow 0.86

[0191] TiO 2 1.30

[0192] PEG4000 1.73

[0193] Cellulose HPM 603 17.25

[0194] Talc 3.02

[0195] Tablet Weight 946.46

[0196] a) Compounds of the invention are granulated in a 30% Aquacoat ECD30 dispersion using a high-shear mixer (eg Aeromatic GP65).

[0197] b) Sift the wet granules using a mill (eg Quadracomill).

[0198]...

Embodiment C

[0208] Example C (Variant 1 - Disintegrating tablet with encapsulated granule system)

[0209] Preparation (mg)

[0210] Chip:

[0211] Compound of the present invention 600.0

[0212] Trimethylammonium methacrylate, Eudragit RL30D 90.0

[0213] Avicel PH 102 150.0

[0214] Croscarmellose Sodium (Na-CMC XL) 75.0

[0215]Aerosil 200 2.8

[0216] Magnesium Stearate 4.5

[0217] Core Weight 922.3

[0218] Coating:

[0219] Iron oxide yellow 0.86

[0220] TiO 2 1.30

[0221] PEG4000 1.73

[0222] Cellulose HPM 603 17.25

[0223] Talc 3.02

[0224] Tablet Weight 946.46

[0225] a) Compounds of the invention are granulated in a 30% Eudragit RL30D dispersion using a high-shear mixer (eg Aeromatic GP65).

[0226] b) Sift the wet granules using eg a Quadracomill.

[0227] c) drying with a fluidized bed dryer (eg Aeroma...

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Abstract

Oral once a day dosage forms comprising oxcarbazepine are disclosed.

Description

field of invention [0001] The present invention relates to formulations of oxcarbazepine (hereinafter referred to as "compounds of the invention"). Background of the invention [0002] Oxcarbazepine (also known as OXC) is an anticonvulsant. The preparation of oxcarbazepine and pharmaceutically acceptable salts thereof is described, for example, in German Patent 2,011,087, which is hereby incorporated by reference. A commercially advantageous process for the preparation of oxcarbazepine is disclosed in European Patent No. 28 028, wherein oxcarbazepine is obtained by hydrolysis of 5-carbamoyl-10-amino-5H-dibenzo[b,f]azepine . For example, nitration of 5-cyano-5H-dibenzo[b,f]azepine, hydrolysis of the resulting nitro derivative to the 5-carbamoyl derivative, reduction of the nitro moiety and hydrolysis of the reduced product to Oxcarbazepine. This patent is hereby incorporated by reference. Oxcarbazepine is indicated as monotherapy and adjunctive therapy for the treatment ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/28A61K31/55A61P25/08
CPCA61K31/55A61K9/2054A61K9/2866A61P25/08
Inventor M-C·沃尔夫O·卡尔布J-D·邦尼S·希尔施
Owner NOVARTIS AG
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