Preparation of silymarin-SBE-β-CD inclusion complex / 中草药

Objective: The inclusion compound of silymarin-SBE-β-CD was prepared. Methods: Phase solubility method was used to screen the inclusion materials of cyclodextrin and determine the type of inclusion. The technological conditions of silymarin inclusion complex were optimized by orthogonal design. The solubility of inclusion was determined and its structure was characterized by means of microscope, infrared spectrum analysis and X-ray diffraction analysis. Results: Due to its higher solubilization effect on silymarin, SBE-β-CD was determined as inclusion material. The ratio of drug to cyclodextrin was coated in the mode of 1:n. The process optimized by orthogonal design was as follow: molar ratio of silymarin to SBE-β-CD of 1:8, inclusion temperature of 60 ℃, and inclusion time of 3 h. Microscope, infrared spectrum analysis and X-ray diffraction analysis showed that the inclusion compound was formed and the drug existed in the inclusion compound as amorphous. Conclusion: The inclusion compound of silymarin-SBE-β-CD has been successfully prepared, which can significantly improve the solubility of the drug, and provide experimental basis for its clinical application.

Solubilization effect of SBE-β-CD and HP-β-CD on prasugrel / 中国药学杂志

OBJECTIVE: To improve the solubility of prasugrel in aqueous solution, the solubilization effect of SBE-β-CD and HP-β-CD research on prasugrel.

Study on chiral separation of three drugs collected pharmacopoeia N-alkyl group by HPLC using chiral mobile phase additive and its mechanism / 中国药学杂志

OBJECTIVE: To performe chiral separation of three pharmaceutical racemates collected in Ch. P 2010 containing N-alkyl groups, including verapamil hydrochloride, chlorphenamine maleate, and chloroquine diphosphate by using SBE-β-CD as a mobile-phase additive in an HPLC system. METHODS: The analysis was carried out on an Alltima C18 column. The mobile phase consisted of acetonitrile and a phosphate solution added with SBE-β-CD and NaH2PO4, whose pH value was adjusted to 2.5 by phosphoric acid. The flow rate was set at 0.8 mL · min-1, and the column temperature was 25°C. The UV detection was carried out at 332, 264 and 278 nm, respectively. The effects of different factors on the separation effect were investigated, including CD types (β-CD, HP-β-CD), SBE-β-CD concentration, pH value, oven temperature, and buffer concentration. RESULTS: The established method was able to separate the three racemates and the mechanism had been discussed. CONCLUSION: Three racemates can be separated on C18 column using SBE-β-CD as a chiral mobile phase additive. This method might be applied to separate various types of biologically important enantiomers which have N-alkyl groups in the chemical structure.