喜树碱微粉的制备工艺_溶出及生物利用度特征研究_李永.pdfVIP

3016 Chinese Traditional and Herbal Drugs 47 17 2016 9 1 2 2* 1. 116034 2. 150040 camptothecin camptothecin micronized powder -80 0.4%-82 1 mg/mL737 000 r/min 11 min 165.65.3nm 1.36 4.09 2.10 GC ICH R283.6 A 0253 - 2670(2016)17 - 3016 - 07 DOI: 10.7501/j.issn.0253-2670.2016.17.010 Preparation, dissolution, and bioavailability characteristics of camptothecin micronized powder 1 2 2 LI Yong , ZHAO Xiu-hua , ZHANG Yin 1. National Engineering Research Center of Seafood, Dalian Polytechnic University, Dalian 116034, China 2. Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, Harbin 150040, China Abstract: Objective Camptothecin (CPT) as a kind of poorly soluble drug was conducted micronization research. Methods CPT micronized powder was prepared by emulsification method using emulsification machine and high pressure homogenizer. Moreover, single factor method was utilized to optimize. Dissolution and oral bioavailability study on CPT micronized powder prepared under the best emulsification conditions was conducted. Results The best preparation conditions were as follows: The dosage of Tween-80 as the surfactant was 0.4%; The concentration of CPT in chloroform-methanol (82) mixed solution was 1 mg/mL; The volume ratio of water-organic phase was 73; The homogenate speed was 7 000 r/min for 11 min. The particle size of CPT micronized powder prepared under the optimized conditions was (165.6 ± 5.3) nm. The scanning electron microscopy (SEM) results showed that CPT micronized powder presented regular strip shape and uniform particle size. The dissolution study indicated that the solubility and dissolution rate of CPT micronized powder was increased by 1.36 and 4.09 times compared wit