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Formulation comprising glycopyrrolate, method and apparatus

a glycopyrrolate and formulation technology, applied in the field of antimuscarinic agents, can solve the problems of significant physical instability and acute stability of glycopyrrola

Inactive Publication Date: 2020-05-21
VECTURA LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention reduces the amount of drug needed for treatment by improving the consistent and predictable administration of glycopyrrolate through a fine particle fraction (FPF) and fine particle dose (FPO) that is more consistent compared to current formulations. The invention also allows for smaller doses to be administered while still achieving the same therapeutic effect. The glycopyrrolate and magnesium stearate are pre-mixed to create a roughly homogeneous blend before being co-jet milled together. The micronising process reduces the particle size of glycopyrrolate to a size suitable for inhalation, with most particles falling within the range of 0.1-10 μm in diameter. The co-jet milling process creates inter-particulate spaces between the particles, which facilitate the permeation of the conditioning atmosphere during the conditioning step. The presence of the coating can be confirmed using energy-dispersive X-ray spectroscopy (EDX) and a Next Generation Impactor (NGI). This invention provides a more efficient and consistent method of administering glycopyrrolate for the treatment of airway diseases.

Problems solved by technology

Glycopyrrolate has been found to have an acute problem with respect to its stability, especially immediately following a conventional micronisation process.
The presence of non-crystalline or amorphous regions in glycopyrrolate material can lead to significant physical instability.

Method used

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  • Formulation comprising glycopyrrolate, method and apparatus
  • Formulation comprising glycopyrrolate, method and apparatus
  • Formulation comprising glycopyrrolate, method and apparatus

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examples

[0225]Selected embodiments of the present invention will now be explained with reference to the examples. It will be apparent to those skilled in the art from this disclosure that the following descriptions of the embodiments are for illustration only and not for the purpose of limiting the invention as defined by the appended claims and their equivalents.

[0226]The examples below illustrate how micronised drug particles may be conditioned, in order to reduce the surface non-crystalline material present.

[0227]Control Formulation 0 (Glycopyrrolate only)

[0228]The particle size distribution for unmicronised glycopyrrolate was determined by MALVERN MASTERSIZER® analysis (MALVERN MASTERSIZER® 3000, using the Aero S dry dispersion method at 4 Bar) and found to be D10=11.3 μm, D50=98.0 μm, D90=281 μm (see FIG. 1).

[0229]A 25 g sample from the same batch of unmicronised glycopyrrolate was added to the powder inlet of an AS-50 spiral jet mill (Inlet pressure=5 Bar, Grinding Pressure=3 Bar, Ave...

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Abstract

A method is disclosed for making a pharmaceutical composition for pulmonary administration comprising co-jet milling glycopyrrolate and magnesium stearate, wherein the co-jet milled glycopyrrolate and magnesium stearate is then subjected to a conditioning step which includes exposure of the co-jet milled glycopyrrolate and magnesium stearate to humidity. A composition made by this method is also disclosed.

Description

INTRODUCTION[0001]The present invention relates to inhalable pharmaceutical compositions comprising the antimuscarinic agent glycopyrrolate. In particular, the present invention relates to dry powder compositions which exhibit excellent physical stability and aerosol performance over time, and provides an improved process for preparing inhalable dry powder formulations of glycopyrrolate.BACKGROUND[0002]Glycopyrrolate is an antimuscarinic agent which is useful in the treatment of conditions such as chronic obstructive pulmonary disease (COPD), asthma, cystic fibrosis (CF) and related airway diseases. Glycopyrrolate is also useful as a heart rate lowering agent when administered by inhalation to patients, in particular patients with conditions such as chronic obstructive pulmonary disease (COPD), asthma, cystic fibrosis (CF) and related airway diseases. It is known to provide glycopyrrolate formulations in the form of dry powder formulations, for administration using dry powder inhale...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/40A61K31/138A61K9/51A61K9/50A61K9/00A61K31/573A61K31/4704A61K31/137A61K31/167A61K45/06A61K9/16A61K9/14
CPCA61K45/06A61K31/573A61K9/5192A61K31/167A61K9/0075A61K9/1688A61K9/145A61K31/137A61K9/5015A61K31/40A61K31/138A61K31/4704A61P11/00A61P11/04A61P11/06A61P43/00A61P9/00A61K2300/00
Inventor MANFORD, FERGUS
Owner VECTURA LTD
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