目的 制備長(zhǎng)春瑞濱磷脂復(fù)合物，提高藥物的脂溶性，以期進(jìn)一步制備長(zhǎng)春瑞濱微粒載藥系統(tǒng)。方法 采用溶劑揮發(fā)法制備長(zhǎng)春瑞濱磷脂復(fù)合物，以復(fù)合率為評(píng)價(jià)指標(biāo)進(jìn)行單因素優(yōu)化試驗(yàn)。采用差示掃描量熱法、X射線衍射法、紫外分光光度法對(duì)復(fù)合物進(jìn)行鑒別，并考察復(fù)合物的體外溶解性質(zhì)變化。結(jié)果 優(yōu)化條件下制備的磷脂復(fù)合物復(fù)合率為89.3%～93.7%；差示掃描量熱法、X射線衍射法、紫外分光光度法驗(yàn)證了復(fù)合物的形成；形成磷脂復(fù)合物后，長(zhǎng)春瑞濱的脂溶性顯著提高。結(jié)論 制備的長(zhǎng)春瑞濱磷脂復(fù)合物能顯著增加藥物的脂溶性，為進(jìn)一步制備長(zhǎng)春瑞濱微粒載藥系統(tǒng)奠定基礎(chǔ)。

Objective To prepare vinorelbine-phospholipid complex (VPC) for enhancing the liposolubility of vinorelbine. Methods The complex was prepared using solvent evaporation method. The preparation technology was optimized by single factor design, using the combining ratio as the assessment index. Differential scanning calorimetry (DSC), X-ray diffraction (XRD) spectrum, and UV spectrophotometry were carried out to investigate its characterization. The in vitro solubility change of the complex was also determined. Results The combining ratio of the complex prepared under the optimized conditions was between 89.3% and 93.7%; UV spectrum, DSC and XRD spectra confirmed the formation of the complex. After phospholipid complex being made, the liposolubility of vinorelbine was remarkably enhanced. Conclusions Prepared vinorelbine-phospholipid complex could effectively enhance the liposolubility of vinorelbine and provide the reference for preparation of vinorelbine microsomal drug-loaded system.

國(guó)家重點(diǎn)基礎(chǔ)研究發(fā)展計(jì)劃（973計(jì)劃）課題（2010CB735602，2012CB724002）；國(guó)家重大新藥創(chuàng)制科技重大專(zhuān)項(xiàng)——國(guó)家生物醫(yī)藥國(guó)際創(chuàng)新園（天津）創(chuàng)新藥物孵化基地建設(shè)（2010ZX09401）