专利号:US-10882811-B2 优先权日:2016-12-23 标题 :Synthesis of lysine acetylsalicylate glycine particles 发明人:NOCKER KARLHEINZ; ZUHSE RALF; OSTROVSKYI DMYTRO 权利人:ASPIAIR GMBH 摘要:The invention relates to a method for the production of acetylsalicylic acid lysinate, optionally lysine acetylsalicylate.glycine, comprising the following steps: a) providing a solution of acetylsalicylic acid in ethanol; b) providing an aqueous solution of lysine; c) combining the solutions of step a) and b) to form a mixture; d) optionally stirring the mixture; e) adding acetone to the mixture; f) incubating the mixture, to allow the formation of a acetylsalicylic acid lysinate product; g) isolating the acetylsalicylic acid lysinate product; wherein acetylsalicylic acid is used in excess compared to lysine and wherein no seed crystals are added to the mixture; and optionally the following further steps: h) providing a recrystallized glycine; wherein the glycine has been recrystallized with the following steps: h1) dissolving glycine in water; h2) adding acetone to the glycine solution; h3) stirring the mixture until a precipitate is obtained; i) combining the recrystallized glycine of step h) with the acetylsalicylic acid lysinate product of step g) to obtain lysine acetylsalicylate.glycine (LASAG) particles.
专利号:US-2025073250-A1 优先权日:2022-01-05 标题:Improved synthesis of lysine acetylsalicylate - Glycine particles 发明人:NOCKER KARLHEINZ; ZUHSE RALF; VON SCHRADER THOMAS; BRAUNE CHRISTIAN 权利人:ASPIAIR GMBH 摘要:The invention provides an improved method for preparing lysine acetylsalicylateâ‹…glycine (LASAG) that allows for high yields without the need for an addition of seed crystal, as well as yielding controlled, small particle sizes (median particles size preferably <40 μm) and high stability of the LASAG. Advantageously, the method can be performed at room temperature without negatively impacting yield or particle properties. The invention also provides the LASAG obtained from said method, and its uses as a medicine.
参考标题: Improved Synthesis Of Lysine Acetylsalicylate . Glycine Particles Synthèse Améliorée De Particules D'Acétylsalicylate De Lysine . Glycine 摘要:The Invention Relates To A Method For The Production Of Acetylsalicylic Acid Lysinate, Optionally Lysine Acetylsalicylate . Glycine, Comprising The Following Steps: A) Providing A Solution Of Acetylsalicylic Acid In Ethanol; B) Providing An Aqueous Solution Of Lysine; C) Combining The Solutions Of Step A) And B) To Form A Mixture; D) Optionally Stirring The Mixture; E) Adding Acetone To The Mixture; F) Incubating The Mixture, To Allow The Formation Of A Acetylsalicylic Acid Lysinate Product; G) Isolating The Acetylsalicylic Acid Lysinate Product; Wherein Acetylsalicylic Acid Is Used In Excess Compared To Lysine And Wherein No Seed Crystals Are Added To The Mixture; And Optionally The Following Further Steps: H) Providing A Recrystallized Glycine; Wherein The Glycine Has Been Recrystallized With The Following Steps: H1) Dissolving Glycine In Water; H2) Adding Acetone To The Glycine Solution; H3) Stirring The Mixture Until A Precipitate Is Obtained; I) Combining The Recrystallized Glycine Of Step H) With The Acetylsalicylic Acid Lysinate Product Of Step G) To Obtain Lysine Acetylsalicylate . Glycine (Lasag) Particles.
合成参考文献
参考文献:10.1007/s10973-012-2550-9 摘要:Wesolowski M, Erecinska J. Pattern recognition methods in the study of thermal decomposition of α-amino acids. Journal of Thermal Analysis and Calorimetry. 2012 Jul 03;109(2):585–93. doi: 10.1007/s10973-012-2550-9.