Pharmaceutical compositions of entacapone co-micronized with sugar alcohols

一种恩他卡朋、共微粉化的技术，应用在制备此类组合物领域，能够解决不可预料等问题

Inactive Publication Date: 2011-01-05
WOCKHARDT RES CENT (IN)
View PDF14 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thus, the properties of substances processed by micronization or milling, especially their solubility and bioavailability, appear to be unpredictable and conflicting results may be obtained

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 compositions of entacapone co-micronized with sugar alcohols
  • Pharmaceutical compositions of entacapone co-micronized with sugar alcohols
  • Pharmaceutical compositions of entacapone co-micronized with sugar alcohols

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment 1: See Table 1 for the composition of each batch of materials. The following formulations are representative of preferred embodiments of the invention. The preparation of Example 1 is detailed below.

[0036] Table 1: Entacapone Composition

[0037]

[0038] Procedure: Entacapone and mannitol are mixed and co-micronized by a multimill. The crospovidone, povidone and magnesium stearate were added to the co-micronized mixture, mixed with a roller compactor and granulated to produce granules of suitable size. To the granules are added the crospovidone and magnesium stearate, and the resulting mixture is compressed using suitable tools to form tablets.

[0039] Table 2: Comtan Compared with the dissolution data of the composition of the present invention prepared in Example 1. The drug release rate was determined using a USP type 2 apparatus (rpm 50) with 900 ml of phosphate buffered saline, pH 5.5 at 37°C ± 0.5°C as medium.

[0040]

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 invention relates to pharmaceutical compositions comprising entacapone or pharmaceutically acceptable salts thereof along with one or more sugar alcohols; wherein the entacapone is co-micronized with one or more sugar alcohols. The invention also relates to processes of making such compositions.

Description

technical field [0001] The present invention relates to a pharmaceutical composition comprising entacapone or a pharmaceutically acceptable salt thereof and one or more sugar alcohols, wherein entacapone and one or more sugar alcohols are co-micronized. The invention also relates to methods of preparing such compositions. Background technique [0002] Entacapone, a catechol ortho-methyltransferase (COMT) inhibitor, is a nitro-catechol-structured compound used as an adjunct to the levodopa / carbidopa dose regimen Therapy is used to treat Parkinson's disease. Chemically, entacapone is (E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethyl-2-acrylamide, The structural formula is as follows: [0003] [0004] Entacapone belongs to Class IV drugs in the biopharmaceutical classification system, causing problems of low solubility, low dissolution rate, and thus low bioavailability. [0005] US patent US4963590 provides a pharmaceutical composition comprising entacapone and a...

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): A61K31/275A61K9/14A61K47/26A61K9/16A61K9/26
CPCA61K9/1635A61K9/2018A61K9/145A61K31/275A61K9/2027A61P25/16
Inventor R·卡珀S·梅特M·塔尔沃G·K·简恩
Owner WOCKHARDT RES CENT (IN)
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap