Supercharge Your Innovation With Domain-Expert AI Agents!

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 low bulk density, poor solubility, increased difficulty and the like

Active Publication Date: 2012-05-09
BIAL PORTELA & CA SA
View PDF7 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 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 comprising the active compound

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

[0076] Four laboratory-scale high-dose capsules were prepared by first mixing the API with dicalcium phosphate and / or microcrystalline cellulose, croscarmellose sodium and / or, povidone, and / or pregelatinized starch in 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 was added to each mixture, and the mixture was granulated.

[0077] The granules were then dried in a laboratory scale fluid bed dryer (Aeromat). The dried granules were sieved and mixed with the remaining ingredients described in Table 1 in a 1 L tumble mixer (Turbula). Capsules are filled with this composition using a manual filling machine.

[0078] The bulk and tap densities of the granules and final compositions were evaluated using the methods described above. Flowability was also evaluated by testing the flow rate throu...

Embodiment 2

[0084] For the preparation of low-dose capsules, two variants of the batch A formulation were prepared on 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 was added to the mixture and the mixture was manually mixed and granulated.

[0085] The granules were then dried in a cabinet dryer at 50°C for approximately 300 minutes. The dried granules are sieved. The sieved granules were then mixed with the rest of the croscarmellose sodium and colloidal silicon dioxide hydrate described in Table 3 in a V-blender. Magnesium stearate and talc are then added and mixed. Capsules are filled with this composition using ...

Embodiment 3

[0093] Three batches of pilot scale capsules with different doses were prepared using the composition shown in Table 3 below. Lot H is the low dose capsules, Lot J is the middle dose capsules and Lot L is the high dose capsules.

[0094] 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 was added to the mixture and the mixture was mixed in a high shear mixer granulator.

[0095] The granules are then dried in a fluid bed drier. The dried granules are sieved. The sieved granules were then mixed with the rest of the croscarmellose sodium and colloidal silicon dioxide hydrate described in Table 3 in a V-blender. Magnesium stearate and talc are then added and mixed. Capsules are filled with this composition ...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

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

technical field [0001] 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 [0002] Levodopa (L-DOPA) has been used in clinical practice for decades for the symptomatic treatment of a variety of conditions, including Parkinson's disease. L-DOPA is able to cross the blood-brain barrier and then be converted to dopamine and increase dopamine levels. However, the conversion of L-DOPA to dopamine can also occur in peripheral tissues, potentially causing side effects when L-DOPA is administered. Accordingly, co-administration of peripheral amino acid decarboxylase (AADC) inhibitors such as carbidopa or benserazide, which prevent conversion to dopamine in peripheral tissues, has become standard clinical practice. [0003] This has led to an interest in developing inhibitors of the enzyme catechol-O-methyltransferase (C...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K31/4245A61K31/44
CPCA61K9/4808A61K9/1652A61K45/06A61K9/1611A61K31/4245A61K31/44A61K9/1635A61K31/4439A61K9/4858A61K9/4866A61P1/00A61P1/04A61P25/02A61P25/14A61P25/16A61P25/18A61P43/00A61P7/10A61P9/12A61K2300/00A61K9/20A61K9/4833A61K31/41
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
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com