Kinetic study of ultrasonic antisolvent crystallization of sirolimus
Kinetic study of ultrasonic antisolvent crystallization of sirolimus
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DOI：
10.1002/crat.200900717
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发表时间：
2010-03-01
影响因子：
1.5
通讯作者：
Murthy, Z. V. P.
中科院分区：
文献类型：
--
作者：
Gandhi, P. J.;Murthy, Z. V. P.
西罗莫司是由吸水链霉菌衍生而来的，通常用于器官移植。采用传质控制超声抗溶剂法测定西罗莫司的沉淀动力学。采用超声波法测定了温度对西罗莫司溶于甲醇和抗溶剂水的粒径、回收率、临界核半径、传质系数等的影响。研究采用经典成核理论，该理论也适用于沉淀过程。在45℃、50℃、60℃和70℃下进行了实验，西罗莫司的回收率分别为90.74、91.5、92.64和93.61%，以每毫升溶剂溶解8毫克，再加入12毫升的高效液相色谱法，回收率分别为90.74、91.5、92.64和93.61%。在此温度下观察到的晶体最终平均直径分别为1371、1287、1063和863 nm。结果表明，该体系为传质控制体系，其质量扩散系数分别为3.97×10~(-9)、4.00×10~(-9)、3.01×10~(-9)和1.92×10~(-9)m~(-9)/S。2010年威利-VCH Verlag GmbH&Co.KGaA，Weinheim
Sirolimus, generally used in organ transplantation, is derived from bacterium Streptomyces hygroscopicus. Mass transfer controlled ultrasonic antisolvent method was used for determining the precipitation kinetics of sirolimus. The effect of temperature was determined on the particles size, percentage recovery, critical radius of nucleus, mass transfer coefficient, etc. for sirolimus dissolved in methanol and antisolvent water using ultrasonic treatment. The study was done using classical nucleation theory, which can also be applied to precipitation processes. Experiments were carried out at various temperatures; viz: 45, 50, 60 and 70 degrees C and the percentage recoveries of sirolimus were found to be 90.74, 91.5, 92.64 and 93.61%, respectively, for initial amount of 8 mg dissolved in 1 mL of solvent and further introduced into 12 mL of HPLC water. The final average diameters of crystals observed for the temperatures were 1371, 1287, 1063 and 863 nm, respectively. The systems were found to be mass transfer controlling and that the mass diffusivities were found to be about 3.97x10(-9), 4.00x10(-9), 3.01x10(-9) and 1.92x10(-9) m(2)/s, respectively. 0 2010 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim