Jump to main content
Jump to site search
PLANNED MAINTENANCE Close the message box

Scheduled maintenance work on Wednesday 22nd May 2019 from 11:00 AM to 1:00 PM (GMT).

During this time our website performance may be temporarily affected. We apologise for any inconvenience this might cause and thank you for your patience.



Crystal habit modification and polymorphic stability assessment of a long-acting β2-adrenergic agonist

Author affiliations

Abstract

Properties such as particle orientation, flowability, packing, compaction, syringeability, suspension stability and dissolution are the most influenced by changes in the crystal habit and polymorphic form of a drug substance. The crystal habit of a drug substance (long-acting β2-adrenergic agonist (LABA)), as well as its purity and polymorphic stability, was studied after performing slurry tests with 1,2-dimethoxyethane : heptane solution at 50 °C. In these slurry tests, the product was kept suspended and undissolved, with agitation, for polymorphic conversion evaluation. Since no significant modifications were observed in the crystal shape and dimensions at 50 °C, a new slurry test was performed at a temperature above the melting point of the starting material (80 °C). In the latter test, it was possible to obtain crystals with increased dimensions by 480% compared with the starting material. Additionally, the desired polymorphic form (form I) was obtained as well as an acceptable purity of approximately 99%. These are promising results, not only for downstream purposes, but also concerning the bioavailability of the drug substance. This work shows that working at a temperature higher than the melting point of the compound seems to modify the crystal habit of the product.

Graphical abstract: Crystal habit modification and polymorphic stability assessment of a long-acting β2-adrenergic agonist

Back to tab navigation

Publication details

The article was received on 04 Mar 2019, accepted on 07 May 2019 and first published on 08 May 2019


Article type: Paper
DOI: 10.1039/C9CE00309F
CrystEngComm, 2019, Advance Article

  •   Request permissions

    Crystal habit modification and polymorphic stability assessment of a long-acting β2-adrenergic agonist

    A. Tulcidas, N. M. T. Lourenço, R. Antunes, B. Santos, S. Pawlowski and F. Rocha, CrystEngComm, 2019, Advance Article , DOI: 10.1039/C9CE00309F

Search articles by author

Spotlight

Advertisements