米诺膦酸的多晶型及热稳定性研究
Study on polymorphism and thermostability of minodronic acid
分类号:
出版年·卷·期(页码):2012,32 (10):0-0
DOI:
10.16155/j.0254-1793.2017.01.01
-----摘要:-------------------------------------------------------------------------------------------
目的: 建立米诺膦酸的多晶型及热稳定性的研究方法。 方法: 通过热重分析和X射线衍射及其原位高温装置对米诺膦酸的多晶型及在加热过程中的晶型稳定性进行检测与分析。 结果: 米诺膦酸存在一水、半水和无水结晶结构,一水米诺膦酸在加热过程中晶型会发生改变,分步失去结晶水后转变为无水米诺膦酸。 结论: 该方法操作简单,重复性好,能够为寻找药物新晶型提供方法。
-----英文摘要:---------------------------------------------------------------------------------------
Objective: To establish a method for study of polymorphism and themostability of minodronic acid. Methods: The thermostability of minodronic acid was evaluated by thermogravimetric analyzer(TGA),and crystal structure was analyzed by X-ray diffraction(XRD) with in-situ high temperature accessories. Results: The minodronic acid showed different crystal forms of monohydrate,hemihydrate and anhydrate.Minodronic acid monohydrate would lose their crystal water during the heating process,and its crstal would change into anhydrate crystal. Conclusion: The method is simple and reproducible,which can be used to study the new drug crystal structures.
-----参考文献:---------------------------------------------------------------------------------------
1 ZHAO Li-jia(赵丽嘉),WANG Li-hua(王利华),HU Ya-ping(胡雅萍),et al.Minodronic acid hydrate(米诺膦酸水合物).Drug Eval Res (药物评价研究),2010,33(6):479
2 Takeuchi M,Sakamoto S,Kawamuki K.Studies on novel bone resorption inhibitors.Ⅱ.Synthesis and pharmacological activities of fused aza-heteroarylbisphosphonate derivaties.Chem Pharm Bull,1998,46(11):1703
3 PI Shi-qing(皮士卿),ZHAO Guo-qing(赵国庆),SHEN Run-pu(沈润溥),et al.Synthesis of disodium minodronate(米诺膦酸二钠的合成).Chin J Pharm(中国医药工业杂志),2004,35(4),193
4 Masako I,Teruki S,Masao F.Effect of minodronic acid hydrate on hip geometry in Japanese women with postmenopausal osteoporosis.Bone Miner Metab,2010,28(3):334
5 Hiroshi M,Makoto T,Ryoji K,etal.Minodronic acid(ONO-5920/YM529)prevents decrease in bone mineral density and bone strength,and improves bone microarchitecture in ovariectomized cynomolgus monkeys.Bone Miner Metab,2008,43(5):840
6 Shuichiro K,Yukinori N,Seiji T,et al.Minodronic acid,a third-generation bisphosphonate,antagonizes purinergic P2X(2/3) receptor function and exerts an analgesic effect in pain models.Eur J Pharmacol,2008,589(1-3):98
7 Katsutoshi N,Shigeharu Y,Takashi S.Failure of stability prediction for minodronic acid injectable by accelerated stability testing.Int J Pharm,2002,241(1):65
8 Katsutoshi N,Shigeharu Y,Masataka K,et al.A new stressed test to predict the foreign matter formation of minodronic acid in solution.Int j Pharm,2003,251(1-2):99
9 Katsutoshi N,Tomonari T,Katsumi S,et al.Stabilization of minodronic acid in aqueous solution for pareneral formulation.Int J Pharm,2002,222(1):91
10 Yasuo I,Makoto T,Ibaraki,et al.Crystal of monohydrate of heterocyclic bis(phosphonic acid) derivative.US:005480875,1996-1-2
11 ZHAO Yan-nan(赵亚男),CHEN Xiao-qing(陈小青),ZHU Kan(朱侃),et al.Thermostability and crystal structure of anticancer drug dasatinib(抗癌药达沙替尼的热稳定性与晶型研究).Acta Pharm Sin(药学学报),2011,46(9):1104
12 LI Gang(李钢),XU Qun-wei(徐群为),MO Xiang-yin(莫祥银),et al.Study on stability of nateglinide polymorphism(不同晶型那格列奈的稳定性研究).Acta Chem Sin(化学学报),2003,61(2):291
13 LI Gang(李钢),ZHOU Xiao-feng(周晓峰),CHENG Yong-ke(程永科),et al.Study on composition and thermal character of mineral traditional Chinese medicine chalcanthite(矿物药胆矾的物相与热性能分析).Chin J Pham Anal(药物分析杂志),2008,28(12):2103
欢迎阅读《药物分析杂志》!您是该文第 3033位读者!