琚祥,陈葵,朱家文

• 1:华东理工大学化学工程研究所

摘要(Abstract)：

使用平衡法测定了288.15～323.15 K时Ⅱ晶型利福平在正丁醇-丙酮和水-丙酮混合溶剂中的溶解度。实验结果表明Ⅱ晶型利福平在两种混合溶剂中的溶解度均随着温度升高而增大;在正丁醇-丙酮混合溶剂中,溶解度随着正丁醇的摩尔分数增加先增大后减小,在摩尔比0.350附近溶解度最大;在水-丙酮体系中,溶解度随着水的摩尔分数增加而增大。使用Apelblat方程、理想状态方程和(CNIBS)/Redlich-Kister方程关联溶解度数据,Apelblat方程关联结果优于理想状态方程,平均相对偏差小于5%。使用修正的van't Hoff方程计算了两种体系的溶解焓、溶解熵和吉布斯自由能。溶解度数据及拟合方程为利福平研究和工业生产提供了基础数据。

关键词(KeyWords)： 利福平;溶解度;混合溶剂;模型

Abstract:

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基金项目(Foundation):

作者(Author): 琚祥,陈葵,朱家文

参考文献(References)：

• [1]HENWOOD S Q,DE VILLIERS M M,LIEBENBERG W,et al.Solubility and dissolution properties of generic rifampicin raw materials[J].Drug Development and Industrial Pharmacy,2000,26(4):403-408.
• [2]黄慧玲.给药途径及剂型因素对两种晶型利福平药动学的影响[D].天津:天津大学,2014.HUANG H L.Effects of delivery route and dosage form on the pharmacokinetics of two crystal forms of rifampicin[D].Tianjin:Tianjin University,2014.
• [3]兰静,胡昌勤.制剂中利福平晶型的确定[J].中国抗生素杂志,2003,28(6):347-350.LAN J,HU C Q.Determination of rifampicin crystalline forms in preparation[J].Chinese Journal of Antibiotics,2003,28(6):347-350.
• [4]杨培明.甲哌力复霉素Ⅰ型结晶的研制[J].抗生素,1979(1):20-30.YANG P M.Development of rifampicin form I crystallization[J].Chinese Journal of Antibiotics,1979(1):20-30.
• [5]甲哌力复霉素生产工艺改革[J].中国抗生素杂志,1978(2):11-17.Reform of rifampicin production process[J].Chinese Journal of Antibiotics,1978(2):11-17.
• [6]JING D,GU Y,XIA H.Solid-state and solution-mediated polymorphic transformation of rifampicin[J].Chemical Engineering&Technology,2018(6):1-9.
• [7]AGRAWAL S,ASHOKRAJ Y,BHARATAM P V,et al.Solid-state characterization of rifampicin samples and its biopharmaceutic relevance[J].European Journal of Pharmaceutical Sciences,2004,22(2/3):127-144.
• [8]FANG W J,CHEN K,JI L J,et al.Solubility and thermodynamic properties of N-acetylglucosamine in mono-solvents and binary solvents at different temperatures[J].Physics and Chemistry of Liquids,2019,57(5):587-599.
• [9]于玉振,张晓慧,李鹏坤,等.普瑞巴林晶型I在纯溶剂及丙酮-水混合溶剂中的溶解度测定与关联[J].高校化学工程学报,2017,31(1):7-12.YU Y Z,ZHANG X H,LI P K,et al.Measurement and correlation of Pregabalin form I solubility in pure solvents and acetone-water mixtures[J].Journal of Chemical Engineering of Chinese Universities,2017,31(1):7-12.
• [10]支娟娟,徐家阔,刘琼,等.喜树碱在二甲亚砜和甲醇(或乙醇)混合溶剂中溶解度的测定和关联[J].高校化学工程学报,2016,30(5):999-1006.ZHI J J,XU J K,LIU Q,et al.Measurement and correlation of Camptothecine solubility in dimethylsulfoxide-methanol/ethanol mixed solvents[J].Journal of Chemical Engineering of Chinese Universities,2016,30(5):999-1006.
• [11]周彩荣,石晓华,冯伟,等.新戊二醇在溶剂中溶解度的测定及关联[J].高校化学工程学报,2010,24(3):365-369.ZHOU C R,SHI X H,FENG W,et al.Measurement and correlation of solubilities of neopentyl glycol in solvents[J].Journal of Chemical Engineering of Chinese Universities,2010,24(3):365-369.
• [12]PINHO S P,MACEDO,EUGéNIA A.Solubility of NaCl,NaBr,and KCl in water,methanol,ethanol,and their mixed solvents[J].Journal of Chemical&Engineering Data,2005,50(1):29-32.
• [13]佟瑶.乙水杨胺-糖精的共结晶过程及其多晶型转化机理研究[D].天津:天津大学,2017.TONG Y.Study on cocrystallization process and polymorphic transformation mechanism of ethenzamide-saccharin cocrystal[D].Tianjin:Tianjin University,2017.
• [14]APELBLAT A,MANZUROLA E.Solubilities of o-acetylsalicylic,4-aminosalicylic,3,5-dinihdsalicylic,p-toluicacid and magnesium-DLaspartate in water from T=(278 to 348)K[J].The Journal Chemical Thermodynamics,1999,31(10):85-91.
• [15]韩世钧.化工相平衡[M].北京:中国石化出版社,1991.HAN S J.Chemical phase equilibrium[M].Beijing:China Petrochemical Press,1991.
• [16]杨久利,沙作良,杨立斌,等.甘氨酸在丙酮-水混合溶剂中溶解度的测定与关联[J].高校化学工程学报,2015,29(2):471-475.YANG J L,SHA Z L,YANG L B,et al.Measurement and correlation of glycine solubility in acetone-water mixture[J].Journal of Chemical Engineering of Chinese Universities,2015,29(2):471-475.
• [17]NAM K,HA E S,KIM J S,et al.Solubility of oxcarbazepine in eight solvents within the temperature range T=(288.15~308.15)K[J].The Journal of Chemical Thermodynamics,2017,104:45-49.