Synthesis and druggability study of triptolide stearate
10.3969/j.issn.1006-0111.2017.02.011
- VernacularTitle:雷公藤甲素-硬脂酸酯的合成及其制剂成药性研究
- Author:
Zhiqin FU
1
;
Youfa XU
;
Bingchen CHEN
;
Dan CHENG
;
Juanjuan MA
;
Jianming CHEN
Author Information
1. 福建中医药大学药学院
- Keywords:
triptolide stearate;
prodrug;
liposome;
emulsion;
druggability
- From:
Journal of Pharmaceutical Practice
2017;35(2):141-145
- CountryChina
- Language:Chinese
-
Abstract:
Objective To synthesize a lipophilic prodrug of triptolide (TP) and improve its druggability .Methods Trip-tolidestearate (TP-SA)was synthesized via the DMAP-catalyzed DCC method and identified by MS ,1H-NMR and 13C-NMR. The shake-flask method was used to study the oil/water partition coefficient .The preparations of TP and TP-SA liposomes and emulsions were compared .Their encapsulation efficiency and stability were investigated .Results TP-SA was synthesized suc-cessfully .Its log P in octanol/water system was 2 .33 .It was difficult to prepare TP liposome or emulsion .By contrast ,TP-SA liposome and emulsion can be prepared successfully with the same formulation process .The particle size of TP-SA lipo-somes were about 90 nm and TP-SA emulsions were about 110 nm .The encapsulation efficiency was above 95% .Their stabili-ty were studied at 4℃ and 25℃ .The preparation parameters ,such as particle size and encapsulation efficiency ,had no signif-icant change in a week .Conclusion Triptolide stearate enhanced drug lipophilicity .Its druggability was improved significant-ly .These data can be used for the TP related drug design and development .
