Crystalline form of sofpironium bromide and preparation method thereof
AssigneeBotanix SB, Inc.
InventorsKazuyoshi Marubayashi, Masahito Watanabe, Herbert R. Brinkman
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Abstract
A cocrystal containing the 1′R-diastereomer and the 1'S-diastereomer of sofpironium bromide at a ratio of 1:3 (Form CO), a crystal mixture (for example, Form B) containing Form CO and a crystalline form of the 1′R-diastereomer (Form MN), and a method for preparing sofpironium bromide, which is suitable for manufacture of the crystal mixture are provided. Form CO and a crystalline form of sofpironium bromide containing Form CO (for example, Form B) have superior stability without hygroscopic property, and accordingly they can be preferably used as a raw material of medicaments.
Claims5
A stable co-crystal Form CO of sofpironium bromide, said co-crystal Form CO comprising in a 1:3 ratio:
- a) a compound shown as formula I-a
- and
- b) a compound shown as formula I-b
- wherein the purity of co-crystal Form CO is not less than 98% w/w based on the content of the compound (I), represented by the formula (I)
- wherein said co-crystal Form CO is physicochemically stable and non-hygroscopic, exhibits a single sharp endothermic peak value of 150° C. using Differential Scanning Calorimetry thermal analysis method as described in Japanese Pharmacopoeia (17th Edition), and is characterized as showing peaks at 5.9±0.2, 7.6±0.2, 11.0±0.2, and 22.2±0.2 degrees as diffraction angles 2θ in a powder X-ray diffraction spectrum.
Dependencies are inferred from the claim text.