Crystalline form of tiotropium bromide with lactose
US9765082B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Aug 23, 2016 |
| Grant date | Sep 19, 2017 |
| Priority date | — |
| Expiry date | Aug 23, 2036 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07B2200/13
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A cocrystal of tiotropium bromide and lactose monohydrate is herein disclosed. In the cocrystal the components tiotropium bromide and lactose are preferably present in an almost stoichiometric ratio. Said cocrystal has a single endothermic event at about 191-193° C. determined by DSC. A process for the preparation of the cocrystal is also disclosed. Preferably, the cocrystal has a particle size distribution of D90<10 μm. The cocrystal is also disclosed for use as medicament, in particular for the treatment of a respiratory complaint, such as chronic obstructive pulmonary disease (COPD), bronchitis, emphysema and asthma. A pharmaceutical composition comprising the cocrystal as active ingredient is also disclosed, in particular for administration by inhalation. In the latter case, said cocrystal has a mean particle size of 0.5 to 10 μm, preferably 1 to 6 μm, more preferably 1.5 to 5 μm.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.