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Pharmaceutical Formulations Comprising Nitrocatechol Derivatives And Methods Of Making Thereof

A technology for nitrocatechol and derivatives is applied in the field of pharmaceutical preparations including nitrocatechol derivatives and their preparation, and can solve the problems of poor flow characteristics, low bulk density, increased difficulty and the like

Inactive Publication Date: 2016-08-24
BIAL PORTELA & CA SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, it has also been found that compounds of formula I may exhibit very low bulk density, poor solubility and / or poor flow characteristics, which increases the difficulty of formulating and / or producing dosage forms containing the active compound

Method used

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  • Pharmaceutical Formulations Comprising Nitrocatechol Derivatives And Methods Of Making Thereof
  • Pharmaceutical Formulations Comprising Nitrocatechol Derivatives And Methods Of Making Thereof
  • Pharmaceutical Formulations Comprising Nitrocatechol Derivatives And Methods Of Making Thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Four laboratory-scale high-dose capsules were prepared as follows. First, API and dicalcium phosphate and / or microcrystalline cellulose, croscarmellose sodium and / or, povidone, and / or pregelatinized starch The amounts shown in Table 1 below were mixed in a laboratory scale high shear mixer (Stephan). The API used in these examples is 2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl )-4,6-lutidine 1-oxide. Purified water is added to each mixture, and the mixture is granulated.

[0078] The granules are then dried in a laboratory-scale fluidized bed dryer (Aeromat). The dried granules were sieved, and then the granules were mixed with the remaining ingredients described in Table 1 in a 1L drum mixer (Turbula). A manual filling machine was used to fill the capsules with the composition.

[0079] The bulk density and tapped density of the pellets and final composition were evaluated using the method described above. Passed USP 31, Volume 1, Test , Unite...

Embodiment 2

[0085] To prepare low-dose capsules, two variants of batch A formulations were prepared on a laboratory scale. Two batches of low-dose capsules were prepared using the composition shown in Table 2 below. First, API, dicalcium phosphate, microcrystalline cellulose, croscarmellose sodium, and povidone were mixed in a V-shaped mixer in the amounts shown in Table 3 below. The API used in these examples is 2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl )-4,6-lutidine 1-oxide. Purified water is added to the mixture, and the mixture is manually mixed and granulated.

[0086] The granules were then dried in a chamber dryer at 50°C for approximately 300 minutes. The dried granules are sieved. The sieved granules were then mixed with the remaining croscarmellose sodium and colloidal silica hydrate described in Table 3 in a V-shaped mixer. Then add magnesium stearate and talc and mix. A capsule filling machine is used to fill capsules with the composition.

[0087...

Embodiment 3

[0094] Three batches of pilot scale capsules with different dosages were prepared using the composition shown in Table 3 below. Batch H is a low-dose capsule, batch J is an intermediate-dose capsule, and batch L is a high-dose capsule.

[0095] First, API, dicalcium phosphate, microcrystalline cellulose, croscarmellose sodium, and povidone were mixed in a high-shear mixer granulator in the amounts shown in Table 3 below. The API used in these examples is 2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl )-4,6-lutidine 1-oxide. Purified water is added to the mixture, and the mixture is mixed in a high-shear mixer granulator.

[0096] The granules are then dried in a fluidized bed dryer. The dried granules are sieved. The sieved granules were then mixed with the remaining croscarmellose sodium and colloidal silica hydrate described in Table 3 in a V-shaped mixer. Then add magnesium stearate and talc and mix. A capsule filling machine is used to fill capsules ...

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Abstract

The present disclosure relates to compositions and pharmaceutical formulations comprising at least one active pharmaceutical ingredient chosen from nitrocatechol derivatives of formula I as defined herein and salts, esters, hydrates, solvates and derivatives thereof and methods of making said compositions and pharmaceutical formulations.

Description

[0001] This application is a divisional application of a Chinese invention patent application with an application date of March 31, 2010, an application number of 201080022653.X, and an invention title of "pharmaceutical preparations including nitrocatechol derivatives and their preparation methods". Technical field [0002] The present invention relates to compositions and pharmaceutical preparations comprising at least one active pharmaceutical ingredient selected from nitrocatechol derivatives and salts thereof. Background technique [0003] Levodopa (L-DOPA) has been used in clinical practice for decades and is used for the symptomatic treatment of various conditions including Parkinson's disease. L-DOPA can cross the blood-brain barrier and then be converted to dopamine and increase the level of dopamine. However, the conversion of L-DOPA to dopamine can also occur in peripheral tissues, which may cause side effects when L-DOPA is administered. Therefore, the co-administrati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K9/16A61K9/48A61P25/16A61P25/18A61P25/14A61P9/12A61P7/10A61P1/00
CPCA61K9/1611A61K9/1635A61K9/1652A61K9/4808A61K9/4858A61K9/4866A61K31/4439A61K31/4245A61K31/44A61K45/06A61P1/00A61P1/04A61P25/02A61P25/14A61P25/16A61P25/18A61P43/00A61P7/10A61P9/12A61K2300/00A61K9/20A61K9/4833A61K31/41
Inventor T·C·D·瓦斯康塞洛斯R·J·D·S·利马R·C·D·C·科斯塔
Owner BIAL PORTELA & CA SA
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