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(2-Hydroxypropyl)-β-cyclodextrin is a widely used drug delivery vehicle to improve the stability and bioavailability.
White to slightly yellow solution (clear, colorless)
278 °C (dec.)
soluble in water.
The inclusion complex of AQ and H-beta-CD is prepared with 1:1 ratio using the coprecipitation method. An accurate weight (0.5 g) of H-beta-CD is dissolved in distilled water to become a saturated solution. However, accurate weight of (0.125 g) of AQ is dissolved in distilled water to get a saturated solution. The AQ solution is added slowly to the H-beta-CD solution up to suspension is formed. The suspension is stirred continuously for 48 hours at 303 K. The solution is kept in a refrigerator for 24 h. After 24 h, the solution become as yellow, orange- precipitate, then it is slowly changing to a clear solution. To get the solid product, the whole solution is allowed into freeze-drying, also known as lyophilization process. At the end of the process, a yellowish orange precipitate is obtained and it is called as solid complex between AQ and H-beta-CD.CUR/HPbetaCD-IC was formed according to the co-precipitation method at 1:2 molar ratio (CUR:HPbetaCD) and the final molar ratio of CUR/HPbetaCD-IC was confirmed by proton nuclear magnetic resonance (1H NMR) measurement. First of all, HPbetaCD was dissolved in aqueous solution; then CUR was added and the solution was stirred for 12 h at RT. Finally, the solution was filtrated after keeping it in refrigerator for 6 h and dried in hood for 2 days. 1H NMR spectra of CUR, HPbetaCD, and CUR/HPbetaCD-IC dissolved in DMSO-d6 were taken on Bruker DPX-400. The assignment of protons of CUR and HPbetaCD are depicted in Fig. S1. Then, the molar ratio of CUR and HPbetaCD in CUR/HPbetaCD-IC was calculated by using the integration of the chemical shifts (d) given in parts per million (ppm) calculated via Mestrenova software.Cilnidipine-HP-beta-CD inclusion complex was prepared using a LGJ-10 freeze-dryer (SongYuan Huaxing, China) as follows. Briefly, excess solid cilnidipine was added to HP-beta-CD aqueous solutions, followed by the suspension was stirred at room temperature for 24 h. The mixture was then filtered through a 0.45 mum membrane into glass vials. The resulting solution was frozen at -20C for 48 h to ensure complete solidification followed by the frozen sample was evaporated under reduced pressure (<10 Pa) to remove water for 12 h to achieve the solid products.
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