A Facile Two‐Column Chromatographic Process for Efficient Purification of Paclitaxel from Crude Extract

Abstract

A facile, preparative low‐pressure chromatographic process was developed for purification of paclitaxel from crude extract of Taxus spp. The process consisted of normal‐phase and a reversed‐phase chromatography without utilization of any liquid–liquid partition step. The normal‐phase chromatography was designed to separate paclitaxel from a majority of unwanted compounds to obtain an initial purification. Silica gel and Al₂O₃ were compared as packing materials for this step. The result demonstrated that basic Al₂O₃ was better than silica gel to give a higher throughput. A further advantage of the Al₂O₃ was its ability of removing 10‐deacetyl‐7‐epi‐paclitaxel, a compound difficult to be separated from the paclitaxel in subsequent purification. The chromatographic fraction of Al₂O₃ was purified by a subsequent reversed‐phase column chromatography, employing a novel uniform porous microsphere, named PST, as the packing material. Combination of the two steps of column chromatography and one step of crystallization was able to purify paclitaxel, from 0.46% to more than 98% with the total recovery of 71%. This integrated chromatographic procedure was reproducible, efficient, and simple to use.

Keywords:

• Crude extract of Taxus spp.
• paclitaxel
• 10‐deacetyl‐7‐epi‐paclitaxel
• preparative low‐pressure chromatography
• purification

Acknowledgment

This work was supported by the National Natural Science Foundation of China under Contract No. 20125616 and 20136020.