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Author:(Qi-Shen LIAN)

1.Optimization of Purification and Isolation of Punicalagin from Pomegranate Peel

Shu LIU ; Wanli SHEN ; Guan LIAN ; Wen CHEN ; Rong QI

China Pharmacist 2017;20(1):14-19

Objective: To establish the methods for extraction and isolation of punicalagin from pomegranate peel, and further study the purification and quantification of punicalagin. Methods: Using an ultrasonic-assisted extraction method, punicalagin in pomegranate peel was extracted at room temperature by 50% ethanol with 20-fold volume of raw material. The content of punicalagin in the crude extract was determined by HPLC. To optimize the purification process of punicalagin, static adsorption and desorption experi-ments were employed to study five kinds of macroporous adsorbent resins (D101, A8-8, NKA-9, HPD-100 and HPD-500) for the one with the highest purification efficacy of punicalagin. In addition, the technical parameters of the macroporous adsorbent resin were opti-mized to obtain punicalagin with higher purity. Punicalagin was further separated and purified by using a reverse phase MCI GEL CHP20P column. Results:HPD500 resin showed the best ability to absorb and separate punicalagin in among five kinds of macro-porous adsorbent resins. The best technical parameters were as follows:the mass concentration of sample solution was 15 mg·ml-1 , the loading amount was 2BV, the pH was 2 and the eluting solvent was 8BV of 30% ethanol. With the best process as described a-bove, the content of punicalagin extracted from pomegranate peel increased from 10. 3% to 30. 7%. The obtained punicalagin could be further purified to 61. 3% from 30% in ethanol eluate by the reverse phase MCI GEL CHP20P column. Conclusion:HPD500 resin is the most effective in the purification of punicalagin from pomegranate peel, and the content of punicalagin can be dramatically increased after the purification by a reverse phase MCI GEL CHP20P column. The optimized process shows good reproducibility and stability.

BACKGROUND:In recent years, the use of prednisolone has good achievements in functional recovery after peripheral nerve injury, but its short half-life, instable plasma concentrations and greater adverse reactions limit its clinical application. OBJECTIVE:To prepare prednisolone implantable films and to explore the sustained-release property of prednisolone implantable films. METHODS:Novel reverse micellar emulsion-solvent evaporation method was used to prepare nanoparticles which contains prednisolone, and we investigated the properties of prednisolone-loaded nanoparticles, including morphological form, diameter, drug loading, encapsulation efficiency, in vitro release properties. Then, composite film was prepared with the nanoparticles above and col agen, chitosan, soybean phosphatidylcholine. The properties of composite films, such as morphological form, the interaction among film materials, in vitro releasing curve, were investigated. RESULTS AND CONCLUSION:The prednisolone-loaded nanoparticles displayed favorable microstructure such as smooth surface, consistent diameters. The mean diameter of the nanoparticle was 500 nm and the max encapsulation efficiency of the nanoparticle was more than 90%. The nanoparticle displayed obvious sustained-release effect in vitro, but it exhibited a certain burst release phenomenon. We found that the nanoparticles were uniformly distributed inside and on the surface of the composite film;and the in vitro release rate of the film was slower and more stable than the nanoparticles. The composite film displayed favorable sustained-release effect with no burst release. From what we have il ustrated above, we can safely come to a conclusion that the prednisolone-loaded film possesses good sustained-release effects.