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The Application Of HP-Beta-CD In Natural Drug Preparation---Alkaloids

HP-β-CD & Alkaloids

Alkaloids are natural nitrogenous organic compounds.9 - nitro - camptothecin is topoisomerase Ⅰ inhibitors, pharmacological studies have shown that its antitumor activity higher than that of camptothecin, but its solubility in water is lower than 5 ug/mL (25 ℃) limits the clinical application, under the condition of physiological 9 - there is activity of camptothecin lactone ring and inactive hydroxy acid salt, the transformation between the thus enhance its stability and solubility is a research hotspot in recent years.Jiang et al. prepared 9-nitro-camptothecin hp-a-cd clathrates and evaluated them in vivo.In the research of 6 kinds of CD in HP - beta - CD solubilization, the largest is similar to 2.5 times the beta CD, at the same time, the HP - beta - CD inclusion compound of 9 - nitro - camptothecin lactone ring hydrolysis speed is far less than the free state of 9 - nitro - camptothecin.Rat plasma pharmacokinetic studies have shown that static note 9 - nitro - camptothecin clathrate AUC0 - up for (538.05 + 107.29) (ng h.)/mL is much higher than the free condition (538.39 + 127.32) (ng · h)/mL (P < 0.05), so after the inclusion has higher bioavailability.


Colchicine induces tumor cell apoptosis by destroying the alpha and beta subunits of the microtubule dimer.Because the structure contains a strong base, ionization leads to low bioavailability under physiological PH conditions.Chau-han et al. increased the solubility of colchicine in water by 1.75 times by preparation of colchicine HP- beta-cd inclusion.The dissolution curve showed that the dissolution of colchicine was increased under the physiological condition (PH7.4), and the inclusion form also prevented the ionization of colchicine.The study showed that the absolute bioavailability of colchicine was 1.82 times.H-NMR and ROESY confirm that the NHCOCH3 part of colchicine has entered the cavity of hp-beta -CD.

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