Oxcarbazepine pharmaceutical formulation and its method of preparation, wherein oxcarbazepine has a broad and multi-modal particle size distribution

A kind of oxcarbazepine particle, the technology of oxcarbazepine, it is applied in the preparation containing oxcarbazepine and preparation of this pharmaceutical preparation, the field of pharmaceutical preparation containing carbamazepine

Inactive Publication Date: 2008-12-31
TEVA PHARMA IND LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These factors become more problematic for pharmaceutical compositions containing oxcarbazepine due to the relatively large recommended daily dose of 1200 mg / day

Method used

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  • Oxcarbazepine pharmaceutical formulation and its method of preparation, wherein oxcarbazepine has a broad and multi-modal particle size distribution
  • Oxcarbazepine pharmaceutical formulation and its method of preparation, wherein oxcarbazepine has a broad and multi-modal particle size distribution
  • Oxcarbazepine pharmaceutical formulation and its method of preparation, wherein oxcarbazepine has a broad and multi-modal particle size distribution

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0110] Example 1: Preparation of a 10:90 ratio multimodal oxcarbazepine formulation

[0111] In the first step 1, a starting dispersion formulation is prepared from large oxcarbazepine. 1200 g of large oxcarbazepine raw material (RM) [d(0.9)=248.5] was dispersed in 4800 g of purified aqueous solution of 240 g of hypromellose (Pharmacoat 603). Add the Pharmacoat to the water and mix until you get a clear mixture. Subsequently, large oxcarbazepine was added to the Pharmacoat water mixture and dispersed with a rotor-stator mixer (Brogtec) for about 30 min. Measure the particle size distribution of large oxcarbazepine by laser diffraction (S type Malvern laser diffraction granulometer (Malvern Mastersizer)), the results are as follows:

[0112] Oxcarbazepine

d(0.1)

d(0.5)

d(0.9)

big oxcarbazepine

25.1

86.1

308.1

[0113] In the second step 2, the particle size of large oxcarbazepine was reduced by high pressure homoge...

Embodiment 2

[0125] Example 2: Preparation of a 1:5 ratio multimodal oxcarbazepine formulation

[0126] Initial four steps are with embodiment 1. In the final step 5 of preparing the granule mixture and tablets, the sprayed granules and the granules of step 4 were mixed together in a ratio of 16.6:83.3, respectively. In preparing the 600 mg dose, a mixture of the two granules is prepared, wherein the nebulized granules contain 500 mg of active material and the mixed granules contain 100 mg of active material. Therefore, the final formulation including a lubricant as an additional excipient is as follows:

[0127] Formulation of Example 2 (Batch #4)

[0128] The granule mixture was then compressed into tablets and subjected to dissolution testing. The observed dissolution rates were similar to Dissolution rates of bioequivalent formulations, such as figure 1 shown in . The particle size of oxcarbazepine used in this example was estimated to be: d(0.5) was 0.7 microns, wit...

Embodiment 3

[0129] Example 3: Using a combination of sprayed granules and mixed granules, a 55:45 ratio was prepared multimodal oxcarbazepine formulation

[0130] Initial three steps are with embodiment 1. Oxcarbazepine granules [d(0.5)=30.5] were prepared by wet granulation in step 4. The preparation of large oxcarbazepine granules is as follows:

[0131]

[0132]

[0133] Measure the particle size distribution of the large oxcarbazepine RM used for granulation by laser diffraction (S type Malvern laser diffraction particle size analyzer (MalvernMastersizer)), the results are as follows:

[0134] Oxcarbazepine

[0135] The final step 5 involves the preparation of the granule mixture and tablets. The sprayed granules of step 3 and the mixed granules of step 4 were mixed together separately in a ratio of 45:55. In preparing the 600 mg dose, a mixture of the two granules is prepared, wherein the sprayed granules contain 270 mg of active material and the mixed granules...

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Abstract

The present invention provides a pharmaceutical composition comprising oxcarbazepine .and at least one pharmaceutical excipient, wherein the oxcarbazepine in the composition has a broad particle size distribution. The broad particle size distribution of oxcarbazepine in the pharmaceutical composition is preferably a multi-modal oxcarbazepine particle size distribution, preferably with an enhanced oxcarbazepine dissolution rate.

Description

[0001] related application [0002] This application claims the benefit of US Provisional Patent Application No. (pending), filed January 31, 2006, the contents of which are incorporated herein by reference. field of invention [0003] The present invention relates to pharmaceutical preparations. In more detail, the present invention relates to oxcarbazepine-containing formulations and processes for the preparation of such pharmaceutical formulations. Given the strong similarities between oxcarbazepine and carbamazepine, including their similar low solubility, the invention is equally applicable to pharmaceutical formulations containing carbamazepine. Background of the invention [0004] Oxcarbazepine (10-oxo-10,11-dihydro-5H-dibenzo[b,f]azepine -5-formamide) has the general formula: [0005] [0006] Has valuable therapeutic properties and is used as a central nervous system sedative. current trade name Marketed for the treatment of epilepsy. according to Acco...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/26A61K31/55A61K9/16
CPCA61K9/145A61K9/1652A61K9/2018A61K9/2077A61K9/5084A61K31/55A61P25/08A61P25/16
Inventor S·布劳I·扎利特G·科拉特卡C·A·阿扎里亚
Owner TEVA PHARMA IND LTD
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