gamma-Cyclodextrine → Salbutamol

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Salbutamol caprate and gamma-cyclodextrin were complexed by the kneading method. Salbutamol caprate (2.409 g) and gamma-cyclodextrin (7.591 g) were blended together. Water (12 mL) was added and the mixture ground together in a mortar with a pestle to form a uniform paste. Grinding was continued for 30 minutes. The paste was then dried in a vacuum oven (40° C.; 0 bar) for 48 hours. The solid mass was broken up, passed through a 60 mesh screen and returned to the vacuum oven (40° C.; 0 bar) for 12 hours in order to ensure uniform drying of the complex. Analysis by HPLC for salbutamol base content, and Karl Fischer for moisture content gave the following results: % salbutamol base was 12.83%, and the moisture content was 7.92%. The complex was characterised by DSC, FT-IR and XRD. The solubility in aqueous solution was 3.2 mg/mL, and the pH of a saturated aqueous solution was 7.00.

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