Unlock instant, AI-driven research and patent intelligence for your innovation.

Pharmaceutical preparation and preparation method thereof

A tablet and compound technology, applied in the field of pharmaceutical preparations and its preparation, can solve problems such as channel gating defects, no drugs available, and reduced transport of anions across epithelial cells

Active Publication Date: 2018-05-25
VERTEX PHARMA INC
View PDF34 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition to impaired trafficking, mutations lead to defective channel gating
Reduced number of channels in the membrane and defective gating together result in reduced transport of anions across epithelial cells, resulting in defective ion and fluid transport
This indicates a significant unmet need for effective treatment of the causes of cystic fibrosis through symptomatic treatment
Additionally, a common challenge with FDA-approved drugs is that there are sometimes no drugs available for patients in need
Thus, there is a clear unmet need for the presently disclosed formulation of Compound 1 and the process for its preparation in a continuous and controlled manner

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 preparation and preparation method thereof
  • Pharmaceutical preparation and preparation method thereof
  • Pharmaceutical preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

example

[0401] XRPD (X-ray powder diffraction)

[0402] X-ray diffraction (XRD) data for Compound 1, Compound 1 Form I, Compound 1 Form II, or Compound 1 HCl Salt Form A were collected on a Bruker D8 DISCOVER powder diffractometer with a HI-STAR 2-dimensional detector and a flat graphite monochromator. A Cu sealed tube with Kα radiation was used at 40 kV, 35 mA. Samples were placed on silicon wafers with zero background at 25°C. For each sample, with 2 different θ 2 Angle Two data frames were collected at 120 seconds: 8° and 26°. Data were integrated using GADDS software and DIFFRACT plus EVA software merged. The reported uncertainty of the peak positions is ±0.2 degrees.

[0403] Jet Milling Description

[0404] Unmicronized Compound 1, Compound 1 Form I, Compound 1 Form II, or Compound 1 HCl Salt Form A was screened to remove lumps before it was placed in the jet mill hopper. All sieves are disposable, wipe clean before use. Using compressed nitrogen to control the feed ...

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

PropertyMeasurementUnit
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

A pharmaceutical composition is disclosed, the pharmaceutical composition comprising Compound 1, (3-(6-(l-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a disintegrant, a surfactant, a binder, and a lubricant, the composition being suitable for oral administration to a patient in need thereof totreat a CFTR mediated disease such as Cystic Fibrosis. Processes of preparing pharmaceutical compositions comprising Compound 1 are also disclosed.

Description

[0001] This application is the application number 201380014510.8, the application date is January 25, 2013, and the invention name is "3-(6-(1-(2,2-difluorobenzo[D][1,3]dioxa Cyclopenten-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid preparation "patent application divisional application. technical field [0002] The present invention relates to a compound comprising 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methanol Pyridin-2-yl)benzoic acid (Compound 1), methods for making such compositions, and methods for administering pharmaceutical compositions comprising the same. Background technique [0003] CFTR is a cAMP / ATP-mediated anion channel expressed in a variety of cell types, including absorptive and secretory epithelia, where it regulates transmembrane anion flux and the activity of other ion channels and proteins. In epithelial cells, proper functioning of CFTR is critical for maintaining the transport of electrolytes t...

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): A61K9/36A61K9/16A61K9/20A61K31/443A61K31/47A61K45/06A61J3/10A61K31/4709A61P43/00
CPCA61K9/1623A61K9/1652A61K9/2054A61K9/2077A61K9/2866A61K31/47A61K31/4709A61K31/443A61K45/06A61P1/10A61P1/16A61P1/18A61P11/00A61P11/02A61P11/06A61P15/10A61P19/08A61P19/10A61P21/02A61P21/04A61P25/00A61P25/08A61P25/14A61P25/16A61P25/28A61P27/02A61P3/00A61P35/00A61P3/06A61P43/00A61P5/14A61P5/18A61P7/00A61P7/10A61P9/04A61P3/10A61K2300/00A61J3/10A61K9/0053A61K9/16A61K9/20A61K9/2013A61K9/2027A61K9/2095A61K47/10A61K47/12A61K47/32A61K47/38A61K2121/00A61K9/28
Inventor M·J·沃维基斯
Owner VERTEX PHARMA INC