期刊文献+

考布他丁A4前药溶解度及油水分布系数的测定 被引量:1

Determination of the solubility and partition coefficient of combretastatin A4 prodrug
下载PDF
导出
摘要 目的:测定考布他丁A4前药(CA4P)的溶解度和油水分布系数。方法:用平衡法测定溶解度,摇瓶法测定油水分布系数,HPLC法测定样品含量。结果:CA4P在25oC下,在纯化水、甲醇中的溶解度分别为349.82、3.5 mg/ml。CA4P的油水分布系数P接近于0。结论:CA4P亲脂性弱,口服不易吸收。 Object: To determine the solubility and partition coefficient of eombretastatin A4 prodrug (CA4P). Methods: Solubilities in water and in methanol were determined by the equilibrium method, and the partition coefficient in n-caprylic alcohol/water system was measured by shaking flask method with HPLC. Results: At 25℃, the solubility of CA4P in water was 349.8 mg/ml, in methanol was 23.5 mg/ml. The partition coefficient of CA4P was zero. Conclusion: CA4P was not absorbed in the intestinal tract.
出处 《天津药学》 2006年第1期3-4,共2页 Tianjin Pharmacy
关键词 考布他丁A4前药 溶解度 油水分布系数 combretastatin A4 produg, solubility, partition coefficient
  • 相关文献

参考文献3

二级参考文献5

共引文献26

同被引文献39

  • 1贾青竹,马沛生,王昶,王强,马少娜.2,4-二氯苯酚在水中溶解度的测定及关联[J].化学工程,2006,34(8):44-47. 被引量:10
  • 2Lipinski CA, Lombardo F, Dominy BW, et al. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Del Rev, 1997, 23(1 -3) :3.
  • 3Baka E,Nov'ak KT. Study on standardization of shake -flask solubility determination Method. Eur J Pharm Scis,2007,32 ( 1 ) :S23.
  • 4Baka E, Comer JEA, Nov'ak KT. Study of equilibrium solubility measurement by saturationshake - flask method using hydrochlorothiazide as model compound. J Pharm Biomedl Anals, 2008,46:335.
  • 5Avdeef A, Bendels S, Tsinman O,et al. Solubility - excipient classification gradient maps. Pharm Ras ,2007,24:530.
  • 6Glomme A, Marz J, Dressman JB. Comparison of a miniaturized Shake - Flask solubility method with automated potentiometric acid/ base titrations and calculated solubilities. J Pharm Sci, 2005,94 (1) ,1.
  • 7Dinter C, Schuetz A, Blume T,et al. Automated solubility determination using a customized robotic system and a turbidity probe. J Assoc Lab Aut,2005,10 (6) :408 - 411.
  • 8Cherng JPJ, Gonzalez - Zugasti J, Kane NR, et al. Integration of an opto - mechanical mass sensor with a powder - dispensing device for microgram sensitivity. J Association Lab Automation, 2004,9 ( 4 ) : 228.
  • 9Alsenz J, Meisyer E, Haenel E, et al. Development of a partially automated solubility screening (PASS) assay for early drug development. J Pharm Sci,2007,96 ( 7 ) : 1748.
  • 10Bhattachar SN, Deschenes LA, Wesley JA. Solubility it's not just for physical chemists. Drug Discovy Today,2006,11 ( 21 - 22 ) : 1012.

引证文献1

二级引证文献48

相关作者

内容加载中请稍等...

相关机构

内容加载中请稍等...

相关主题

内容加载中请稍等...

浏览历史

内容加载中请稍等...
;
使用帮助 返回顶部