曲札茋苷平衡溶解度和表观油水分配系数的测定
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昆明制药集团股份有限公司,云南昆明650100

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R283

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基金项目:云南省科技厅重点新产品开发专项资助(2012ZA002)收稿日期:2014-12-17作者简介:方芳(1979-),女,云南个旧人,高级工程师,主要从事新药研发质量标准研究工作。△通信作者:陈云建,E-mail:chyjkm@163.com


Determine the Equilibrium Solubility and Apparent Oil/Water Partition Coefficient ofPiceatannol 3’-O-β-D-glucopyranoside
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Kunming Pharmaceutical Corp, Kunming 650100, China

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    摘要:

    目的测定曲札茋苷在不同介质中的平衡溶解度,在正辛醇—水和正辛醇—缓冲液体系中的表观油水分配系数,为曲札茋苷制剂的开发研究提供基础。方法采用紫外分光光度-摇瓶法测定曲札茋苷的平衡溶解度浓及表观油水分配系数,测定波长为319nm。结果37℃时,曲札茋苷在水中的溶解度为5.77mg/mL,在0.1mol/LHCl溶液中的溶解度为4.53mg/mL,在生理盐水中的溶解度为5.21mg/mL,在其他不同pH的磷酸盐缓冲溶液中随着pH的升高逐渐升高;曲札茋苷在正辛醇—水相的表观油水分配系数Papp为3.12;当pH在2~8之间时,受pH影响无规律,表现为亲油性。结论曲札茋苷在水中的平衡溶解度及油水分配系数与介质的pH值有关,可以通过改变pH值,增加该药物新剂型的稳定性。其测定结果对进一步研究曲札茋苷的提取分离、制剂及其在生物体内的吸收、分布和代谢过程具有重要的参考价值。

    Abstract:

    Objective To determine the equilibrium solubility of Piceatannol 3’-O-β-D-glucopyranoside by UV Spectrophotometry in different media and the octanol-water and octanol in a buffer fluid system apparent oil-water partition coefficient to provide a basis for the development of design Piceatannol 3’-O-β-D-glucopyranoside preparations. Methods Measuring the equilibrium solubility of Piceatannol 3’-O-β-D-glucopyranoside in different medium. Using the shake flask method for the determination of Piceatannol 3’-O-β-D-glucopyranoside apparent oil-water partition coefficient, measuring wavelength of 319nm. Results The equilibrium solubility of Piceatannol 3’-O-β-D-glucopyranoside in water was 5. 77 mg/ml at 37 ℃, and the solubility was 4.53mg/mL in 0.1mol/L HCl, in physiogical saline was 5. 21mg/mL, in a phosphate buffer solution of different pH value, its solubility gradually increased with the increase of pH;Piceatannol 3’-O-β-D-glucopyranoside in n-octanol and water relative to the performance of oil-water partition coefficient, Papp was 3. 12;when pH is during 2 to 8, there is no significantly affected by pH influence performance hydrophilic. Conclusion The equilibrium solubility in water and oil-water partition coefficient of Piceatannol 3’-O-β-D-glucopyranoside are correlated to pH of the medium, The stability of the new formulation of the drugs can be increased by changing the pH value. Its measurement results are important to further research to Piceatannol 3’-O-β-D-glucopyranoside, formulation research and in vivo absorption, distribution and metabolic processes important reference.

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